References
- Amidon GL, Lennernäs H, Shah VP, et al. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res [Internet]. 1995 [cited 2019 Jan 19];12:413–420. Available from: http://www.ncbi.nlm.nih.gov/pubmed/7617530.
- Martinez MN, Amidon GL A mechanistic approach to understanding the factors affecting drug absorption: A review of fundamentals. J Clin Pharmacol. 2002;42:620–643. doi:10.1177/00970002042006005
- Pereira De Sousa I, Bernkop-Schnürch A Pre-systemic metabolism of orally administered drugs and strategies to overcome it. J Control Release. 2014; 192 301–309 doi:10.1016/j.jconrel.2014.08.004
- Lozoya-Agullo I, Zur M, Beig A, et al. Segmental-dependent permeability throughout the small intestine following oral drug administration: Single-pass vs. Doluisio approach to in-situ rat perfusion. Int J Pharm [Internet]. 2016 [cited 2019 Oct 22];515:201–208. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27667756.
- Alejandro RP, Isabel LA, Miguel OA, et al. Comparison of segmental-dependent permeability in human and in situ perfusion model in rat. Eur J Pharm Sci [Internet]. 2017 [cited 2019 Jul 28];107:191–196. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28687530.
- Chaudhari SP, Patil PS Pharmaceutical Excipients: A review. Int J Adv Pharm Biol Chem [Internet]. 2012 [cited 2019 Nov 20];1:21–34. Available from: www.ijapbc.com.
- Dahlgren D, Sjöblom M, Lennernäs H Intestinal absorption-modifying excipients: A current update on preclinical in vivo evaluations. Eur J Pharm Biopharm. 2019;142:411–420. doi:10.1016/j.ejpb.2019.07.013
- Loftsson T Excipient pharmacokinetics and profiling. Int J Pharm. 2015;480:48–54. doi:10.1016/j.ijpharm.2015.01.022
- Zarmpi P, Flanagan T, Meehan E, et al. Biopharmaceutical aspects and implications of excipient variability in drug product performance. Eur J Pharm Biopharm [Internet]. 2017 [cited 2019 Jan 30];111:1–15. Available from: https://www.sciencedirect.com/science/article/abs/pii/S0939641116305604.
- Kubbinga M, Moghani L, Langguth P Novel insights into excipient effects on the biopharmaceutics of APIs from different BCS classes: Lactose in solid oral dosage forms. Eur J Pharm Sci. 2014;61:27–31. doi:10.1016/j.ejps.2014.03.008
- Gerber W, Hamman JH, Steyn JD Excipient-drug pharmacokinetic interactions: effect of disintegrants on efflux across excised pig intestinal tissues. J Food Drug Anal. 2018;26:S115–S124. doi:10.1016/j.jfda.2018.01.007
- Flanagan T Potential for pharmaceutical excipients to impact absorption: a mechanistic review for BCS Class 1 and 3 drugs. Eur J Pharm Biopharm [Internet]. 2019 [cited 2020 Mar 21];141:130–138. Available from: doi:10.1016/j.ejpb.2019.05.020.
- Dash RP, Srinivas NR, Babu RJ Use of sorbitol as pharmaceutical excipient in the present day formulations–issues and challenges for drug absorption and bioavailability. Drug Dev Ind Pharm. 2019;45:1421–1429. doi:10.1080/03639045.2019.1640722
- AAA -A-A, Nielsen RB, Steffansen B, et al. Nonionic surfactants modulate the transport activity of ATP-binding cassette (ABC) transporters and solute carriers (SLC): relevance to oral drug absorption. Int J Pharm. 2019; Jul 20;566:410-433.
- Schittny A, Huwyler J, Puchkov M Mechanisms of increased bioavailability through amorphous solid dispersions: a review. Drug Deliv. 2020; 27 110–127 doi:10.1080/10717544.2019.1704940
- Pentafragka C, Symillides M, McAllister M, et al. The impact of food intake on the luminal environment and performance of oral drug products with a view to in vitro and in silico simulations: a PEARRL review. J Pharm Pharmacol. 2019; 71 557–580 doi:10.1111/jphp.12999
- O’Shea JP, Holm R, O’Driscoll CM, et al. Food for thought: formulating away the food effect – a PEARRL review [Internet]. J Pharm Pharmacol. Blackwell Publishing Ltd; 2019 [ cited 2020 Jun 21]; 71: p. 510–535. Available from: https://pubmed.ncbi.nlm.nih.gov/29956330/.
- Ditzinger F, Price DJ, Ilie AR, et al. Lipophilicity and hydrophobicity considerations in bio-enabling oral formulations approaches – a PEARRL review. J Pharm Pharmacol. 2019; 71:464–482. doi:10.1111/jphp.12984
- García-Arieta A Interactions between active pharmaceutical ingredients and excipients affecting bioavailability: Impact on bioequivalence. Eur J Pharm Sci. 2014;18:89–97. doi:10.1016/j.ejps.2014.09.004
- Bransford P, Cook J, Gupta M, et al. ICH M9 Guideline in Development on Biopharmaceutics Classification System-Based Biowaivers: An Industrial Perspective from the IQ Consortium. Mol Pharm. 2020; doi:10.1021/acs.molpharmaceut.9b01062
- Vertzoni M, Augustijns P, Grimm M, et al. Impact of regional differences along the gastrointestinal tract of healthy adults on oral drug absorption: An UNGAP review. Eur J Pharm Sci. 2019;134:153–175. doi:10.1016/j.ejps.2019.04.013
- Kostewicz ES, Aarons L, Bergstrand M, et al. PBPK models for the prediction of in vivo performance of oral dosage forms. Eur J Pharm Sci [Internet]. 2014;57:300–321. Available from: 10.1016/j.ejps.2013.08.024.
- Bermejo M, Kuminek G, Al-Gousous J, et al. Exploring bioequivalence of dexketoprofen trometamol drug products with the gastrointestinal simulator (GIS) and precipitation pathways analyses. Pharmaceutics [Internet]. 2019 [cited 2019 Aug 9];11:122. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30884755.
- Taniguchi C, Kawabata Y, Wada K, et al. Microenvironmental pH-modification to improve dissolution behavior and oral absorption for drugs with pH-dependent solubility. Expert Opin Drug Deliv [Internet]. 2014 [cited 2020 Mar 21];11:505–516. Available from: http://www.ncbi.nlm.nih.gov/pubmed/24472170.
- Chen M-L, Sadrieh N, Yu L Impact of osmotically active excipients on bioavailability and bioequivalence of BCS Class III Drugs. AAPS J [Internet]. 2013;15:1043–1050. Available from: http://link.springer.com/10.1208/s12248-013-9509-z.
- JMM D-S, Ruiz-Picazo A, Gonzalez-Alvarez M, et al. Impact on intestinal permeability of pediatric hyperosmolar formulations after dilution: studies with rat perfusion method. Int J Pharm. [Internet]. 2019 [cited 2019 Jan 15];557:154–161. Available from: https://linkinghub.elsevier.com/retrieve/pii/S0378517318309657.
- Van Den Abeele J, Brouwers J, Tack J, et al. Exploring the link between gastric motility and intragastric drug distribution in man. Eur J Pharm Biopharm [Internet]. 2017 [cited 2020 Mar 21];112:75–84. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27865990.
- Kelly K, O’Mahony B, Lindsay B, et al. Comparison of the rates of disintegration, gastric emptying, and drug absorption following administration of a new and a conventional paracetamol formulation, using gamma scintigraphy. Pharm Res [Internet]. 2003 [cited 2019 Jan 21];20:1668–1673. Available from: http://www.ncbi.nlm.nih.gov/pubmed/14620524.
- Koch KM, Parr AF, Tomlinson JJ, et al. Effect of Sodium Acid Pyrophosphate on Ranitidine Bioavailability and Gastrointestinal Transit Time. Pharm Res An Off J Am Assoc Pharm Sci. 1993;10:1027–1030.
- Klein S, Garbacz G, Pišlar M, et al. The role of individual gastric emptying of pellets in the prediction of diclofenac in vivo dissolution. J Control Release [Internet]. 2013 [cited 2020 Mar 21];166:286–293. Available from: http://www.ncbi.nlm.nih.gov/pubmed/23306025.
- Chen M-L, Straughn AB, Sadrieh N, et al. A Modern View of Excipient Effects on Bioequivalence: Case Study of Sorbitol. Pharm Res [Internet]. 2006 [cited 2019 Jan 21];24:73–80. Available from: http://link.springer.com/10.1007/s11095-006-9120-4.
- Layer P, Chan AT, Go VL, et al. Human pancreatic secretion during phase II antral motility of the interdigestive cycle. Am J Physiol [Internet]. 1988 [cited 2020 Mar 21];254:G249–53. Available from: http://www.ncbi.nlm.nih.gov/pubmed/3348376.
- Abrantes CG, Duarte D, Reis CP An Overview of Pharmaceutical Excipients: Safe or Not Safe? J Pharm Sci 2016;105:2019–2026. doi:10.1016/j.xphs.2016.03.019
- CFR FDA - Code of Federal Regulations Title 21 [Internet]. [ cited 2019 Nov 20]. Available from: https://www.accessdata.fda.gov/scripts/cdrh/cfdocs/cfcfr/cfrsearch.cfm.
- FDA. CDER/FDA. Inactive Ingredient Search for Approved Drug Products [Internet]. [ cited 2019 Nov 20]. Available from: https://www.accessdata.fda.gov/scripts/cder/iig/index.Cfm.
- Panakanti R, Narang AS Impact of Excipient Interactions on Drug Bioavailability from Solid Dosage Forms. 2012 [ cited 2019 Jan 21];29:2639–2659. Available from: http://link.springer.com/10.1007/978-3-319-20206-8_10.
- Deng Y, Misselwitz B, Dai N, et al. Lactose intolerance in adults: biological mechanism and dietary management. Nutrients. 2015;7:8020–8035. doi:10.3390/nu7095380
- Saluja V, Sekhon BS The regulation of pharmaceutical excipients. J Excipients Food Chem. [Internet]. 2014 [cited 2019 Nov 20];4:95–106. Available from: https://ojs.abo.fi/ojs/index.php/jefc/article/view/213.
- Rowe RC, Sheskey PJ, Owen SC, et al. Handbook of pharmaceutical excipients [Internet]. London and Washington: Pharmaceutical Press; 2006 [ cited 2019 Jan 30]. Available from: https://www.ncbi.nlm.nih.gov/nlmcatalog/101258346.
- Definition of Pharmaceutical Excipients - pharma excipients [Internet]. [ cited 2020 Apr 18]. Available from: https://www.pharmaexcipients.com/pharmaceutical-excipients-some-definition/.
- Vasconcelos T, Marques S, Sarmento B The biopharmaceutical classification system of excipients. Ther Deliv. 2017;8:65–78.doi:10.4155/tde-2016-0067
- Zhang W, Li Y, Zou P, et al. The effects of pharmaceutical excipients on gastrointestinal tract metabolic enzymes and transporters—an update. AAPS J. 2016;18:830–843. doi:10.1208/s12248-016-9928-8
- Ramirez E, Laosa O, Guerra P, et al. Acceptability and characteristics of 124 human bioequivalence studies with active substances classified according to the biopharmaceutic classification system. Br J Clin Pharmacol [Internet]. 2010 [cited 2019 Sep 25];70:694–702. Available from: 10.1111/j.1365-2125.2010.03757.x.
- Colón-Useche S, González-Álvarez I, Mangas-Sanjuan V, et al. Investigating the discriminatory power of BCS-biowaiver in vitro methodology to detect bioavailability differences between immediate release products containing a class i drug. Mol Pharm. 2015;12:3167–3174. doi:10.1021/acs.molpharmaceut.5b00076
- Ren X, Mao X, Si L, et al. Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm [Internet]. 2008 [cited 2020 Mar 25];70:279–288. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18499414.
- Engel A, Oswald S, Siegmund W, et al. Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm [Internet]. 2012 [cited 2019 Nov 22];9:2577–2581. Available from: http://www.ncbi.nlm.nih.gov/pubmed/22808947.
- Otter M, Oswald S, Siegmund W, et al. Effects of frequently used pharmaceutical excipients on the organic cation transporters 1–3 and peptide transporters 1/2 stably expressed in MDCKII cells. Eur J Pharm Biopharm [Internet]. 2017 [cited 2020 Mar 25];112:187–195. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27903454.
- Cornaire G, Woodley J, Hermann P, et al. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int J Pharm. 2004;278:119–131. doi:10.1016/j.ijpharm.2004.03.001
- Akers MJ, Lach JL, Fischer LJ Alterations in absorption of dicumarol by various excipient materials. J Pharm Sci [Internet]. 1973 [cited 2019 Nov 22];62:391–395. Available from: http://www.ncbi.nlm.nih.gov/pubmed/4120637.
- Legen I, Kračun M, Salobir M, et al. The evaluation of some pharmaceutically acceptable excipients as permeation enhancers for amoxicillin. Int J Pharm. 2006;308:84–89. doi:10.1016/j.ijpharm.2005.10.036
- Oda M, Saitoh H, Kobayashi M, et al. β-Cyclodextrin as a suitable solubilizing agent for in situ absorption study of poorly water-soluble drugs. Int J Pharm. 2004;280:95–102. doi:10.1016/j.ijpharm.2004.05.003
- Jones DS, Dressman JB, Loftsson T, et al. Pharmacokinetics of cyclodextrins and drugs after oral and parenteral administration of drug/cyclodextrin complexes. J Pharm Pharmacol. 2016;68:544–555.
- Hugger ED, Audus KL, Borchardt RT Effects of poly (ethylene glycol) on Efflux transporter activity in Caco-2 cell monolayers. J Pharm Sci. 2002;91:1980–1990.
- Hugger ED, Novak BL, Burton PS, et al. A comparison of commonly used polyethoxylated pharmaceutical excipients on their ability to inhibit P-glycoprotein activity in vitro. J Pharm Sci 2002;91:1991–2002. doi:10.1002/jps.10176
- Yamagata T, Kusuhara H, Morishita M, et al. Effect of excipients on breast cancer resistance protein substrate uptake activity. J Control Release [Internet]. 2007 [cited 2019 Nov 22];124:1–5. Available from: http://www.ncbi.nlm.nih.gov/pubmed/17900739.
- Hanke U, May K, Rozehnal V, et al. Commonly used nonionic surfactants interact differently with the human efflux transporters ABCB1 (p-glycoprotein) and ABCC2 (MRP2). Eur J Pharm Biopharm. [Internet]. 2010;76:260–268. Available from: 10.1016/j.ejpb.2010.06.008.
- Wagner D, Spahn-Langguth H, Hanafy A, et al. Intestinal drug efflux: formulation and food effects. Adv Drug Deliv Rev 2001;50 Suppl 1:S13-31.
- Parr A, Hidalgo IJ, Bode C, et al. The effect of excipients on the permeability of BCS Class III compounds and implications for biowaivers. Pharm Res. [Internet]. 2016;33:167–176. Available from: 10.1007/s11095-015-1773-4.
- Cuomo J, Appendino G, Dern AS, et al. Comparative absorption of a standardized curcuminoid mixture and its lecithin formulation. J Nat Prod. 2011;74:664–669. doi:10.1021/np1007262
- Nakano M Effects of interaction with surfactants, adsorbents, and other substances on the permeation of chlorpromazine through a dimethyl polysiloxane membrane. J Pharm Sci. [Internet]. 1971 [cited 2019 Nov 22];60:571–575. Available from: http://www.ncbi.nlm.nih.gov/pubmed/5128367.
- Richards RM, Xing JZ, Mackay KM Excipient interaction with cetylpyridinium chloride activity in tablet based lozenges. Pharm Res. [Internet]. 1996 [cited 2019 Nov 22];13:1258–1264. Available from: http://www.ncbi.nlm.nih.gov/pubmed/8865323.
- Vaithianathan S, Haidar SH, Zhang X, et al. Effect of common excipients on the oral drug absorption of biopharmaceutics classification system Class 3 drugs Cimetidine and Acyclovir. J Pharm Sci. [Internet]. 2016 [cited 2019 Nov 27];105:996–1005. Available from: 10.1002/jps.24643&token=WzEzNTA1MTcsIjEwLjEwMDIvanBzLjI0NjQzIl0.vba0HotMhjhrTY8aJr8so-gbvWw.
- Chowdary KPR, Suresh Babu KVV Dissolution, bioavailability and ulcerogenic studies on solid dispersions of indomethacin in water soluble cellulose polymers. Drug Dev Ind Pharm. 1994;20:799–813. doi:10.3109/03639049409038332
- Krylova OO, Pohl P Ionophoric activity of pluronic block copolymers. Biochemistry. 2004;43:3696–3703. doi:10.1021/bi035768l
- Shen Q, Wang L, Huang Y, et al. Oriented aggregation and novel phase transformation of vaterite controlled by the synergistic effect of calcium dodecyl sulfate and n-pentanol. J Phys Chem B [Internet]. 2006 [cited 2019 Nov 22];110:23148–23153. Available from: http://www.ncbi.nlm.nih.gov/pubmed/17107157.
- Singh P, Guillory JK, Sokoloski TD, et al. Effect of inert tablet ingredients on drug absorption. I. Effect of polyethylene glycol 4000 on the intestinal absorption of four barbiturates. J Pharm Sci [Internet]. 1966 [cited 2019 Nov 22];55:63–68. Available from: http://www.ncbi.nlm.nih.gov/pubmed/5918653.
- Li GF, Tan YF, Guo D, et al. [Effect of Tween-80 on the permeability of rhodamine 123, a P-gp substrate across rat intestinal membranes in vitro]. Nan Fang Yi Ke Da Xue Xue Bao [Internet]. 2008;28:579–581. Available from: http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=18495595.
- Li M, Si L, Pan H, et al. Excipients enhance intestinal absorption of ganciclovir by P-gp inhibition: assessed in vitro by everted gut sac and in situ by improved intestinal perfusion. Int J Pharm. [Internet]. 2011;403:37–45. Available from: 10.1016/j.ijpharm.2010.10.017.
- Cornaire G, Woodley JF, Saivin S, et al. Effect of polyoxyl 35 castor oil and Polysorbate 80 on the intestinal absorption of digoxin in vitro. Arzneimittel-Forschung/Drug Res. 2000;50:576–579.
- Thi H, Tran T, Ha P, et al. New findings on melatonin absorption and alterations by pharmaceutical excipients using the Ussing chamber technique with mounted rat gastrointestinal segments. Int J Pharm. 2009;378:9–16.
- Chang T, Benet LZ, Hebert MF The effect of water-soluble vitamin E on cyclosporine pharmacokinetics in healthy volunteers. Clin Pharmacol Ther. 1996;59:297–303. doi:10.1016/S0009-9236(96)80007-5
- Jobin G, Cortot A, Godbillon J, et al. Investigation of drug absorption from the gastrointestinal tract of man. I. Metoprolol in the stomach, duodenum and jejunum. Br J Clin Pharmacol [Internet]. 1985 [cited 2020 Mar 21];19 Suppl 2:97S–105S. Available from: http://www.ncbi.nlm.nih.gov/pubmed/4005135.
- Vidon N, Palma R, Godbillon J, et al. Gastric and intestinal absorption of oxprenolol in humans. J Clin Pharmacol [Internet]. 1986 [cited 2020 Mar 21];26:611–615. Available from: http://www.ncbi.nlm.nih.gov/pubmed/3793952.
- González Álvarez I, MÁ CP, Bermejo Sanz M Del V Metodologías Biofarmacéuticas en el Desarrollo de Medicamentos. Universidad Miguel Hernández, editor. Spain: Universidad Miguel Hernández; 2015.
- Garrigues TM, Pérez-Varona AT, Climent E, et al. Gastric absorption of acidic xenobiotics in the rat: Biophysical interpretation of an apparently atypical behaviour. Int J Pharm. 1990;64:127–138. doi:10.1016/0378-5173(90)90261-2
- Bermejo M, Ruíz-García A, Sánchez-Castaño G, et al. Gastric absorption in the presence of Sodium Taurocholate: interpretation of its ulcerogenic effect. Poster present. AAPS Annu. Meet. New Orleans, USA, [Internet]. 1999 [cited 2020 Mar 21]; Available from: https://www.uv.es/~mbermejo/Neworleans5.pdf.
- Govindarajan R, Landis M, Hancock B, et al. Surface acidity and solid-state compatibility of excipients with an acid-sensitive API: case study of atorvastatin calcium. AAPS PharmSciTech [Internet]. 2015 [cited 2019 Nov 20];16:354–363. Available from: http://www.ncbi.nlm.nih.gov/pubmed/25319055.
- Pudipeddi M, Zannou EA, Vasanthavada M, et al. Measurement of surface pH of pharmaceutical solids: A critical evaluation of indicator dye-sorption method and its comparison with slurry pH method. J Pharm Sci. 2008;97:1831–1842. doi:10.1002/jps.21052
- Abhijeet K, Namita D Studies on solubility enhancement of poorly soluble NSAID using dual approach of micro-environmental pH modulation and melt granulation. Curr Drug Deliv [Internet]. 2017 [cited 2020 Mar 22];14:1201–1212. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28578642.
- Dong L, Mai Y, Liu Q, et al. Mechanism and improved dissolution of glycyrrhetinic acid solid dispersion by alkalizers. Pharmaceutics [Internet]. 2020 [cited 2020 Mar 22];12. Available from: http://www.ncbi.nlm.nih.gov/pubmed/31968604. 82
- Hou HH, Jia W, Liu L, et al. Effect of microenvironmental pH modulation on the dissolution rate and oral absorption of the salt of a weak acid - case study of GDC-0810. Pharm Res [Internet]. 2018 [cited 2020 Mar 22];35:37. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29380076.
- Vo AQ, Feng X, Zhang J, et al. Dual mechanism of microenvironmental pH modulation and foam melt extrusion to enhance performance of HPMCAS based amorphous solid dispersion. Int J Pharm [Internet]. 2018 [cited 2020 Mar 22];550:216–228. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30142354.
- Badawy SIF, Hussain MA Microenvironmental pH modulation in solid dosage forms. J Pharm Sci [Internet]. 2007 [cited 2019 Sep 27];96:948–959. Available from: http://www.ncbi.nlm.nih.gov/pubmed/17455349.
- Buckley ST, Bækdal TA, Vegge A, et al. Transcellular stomach absorption of a derivatized glucagon-like peptide-1 receptor agonist. Sci Transl Med [Internet]. 2018 [cited 2019 Nov 20];10. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30429357. eaar7047
- Cooke AR Control of gastric emptying and motility. Gastroenterol [Internet]. 1975 [cited 2020 Mar 22];68:804–816. Available from: http://www.ncbi.nlm.nih.gov/pubmed/1123145.
- Goyal RK, Guo Y, Mashimo H Advances in the physiology of gastric emptying. Neurogastroenterol Motil [Internet]. 2019 [cited 2020 Mar 22];31:e13546. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30740834.
- Deloose E, Janssen P, Depoortere I, et al. The migrating motor complex: control mechanisms and its role in health and disease. Nat Rev Gastroenterol Hepatol [Internet]. 2012 [cited 2020 Mar 22];9:271–285. Available from: http://www.ncbi.nlm.nih.gov/pubmed/22450306.
- Mudie DM, Murray K, Hoad CL, et al. Quantification of gastrointestinal liquid volumes and distribution following a 240 mL dose of water in the fasted state. Mol Pharm. 2014;11:3039–3047. doi:10.1021/mp500210c
- Liere EJV, Sleeth CK The emptying time of the normal human stomach as influenced by acid and alkali with a review of the literature. Am J Dig Dis. 1940;7:118–123. doi:10.1007/BF02997180
- Kato R, Takanaka A, Onoda K, et al. Effect of syrup on the absorption of drugs from gastrointestinal tract. Jpn J Pharmacol [Internet]. 1969 [cited 2019 Jan 21];19:331–342. Available from: http://www.ncbi.nlm.nih.gov/pubmed/5307466.
- Pestel S, Martin H-J, Maier G-M, et al. Effect of commonly used vehicles on gastrointestinal, renal, and liver function in rats. J Pharmacol Toxicol Methods [Internet]. 2006 [cited 2019 Jan 21];54:200–214. Available from: http://www.ncbi.nlm.nih.gov/pubmed/16567111.
- Grattan T, Hickman R, Darby-Dowman A, et al. A five way crossover human volunteer study to compare the pharmacokinetics of paracetamol following oral administration of two commercially available paracetamol tablets and three development tablets containing paracetamol in combination with sodium bicarbonate or calcium carbonate. Eur J Pharm Biopharm 2000;49:225–229. doi:10.1016/s0939-6411(00)00081-3
- Hunt JN, Pathak JD The osmotic effects of some simple molecules and ions on gastric emptying. J Physiol [Internet]. 1960 [cited 2020 Mar 22];154:254–269. Available from: http://www.ncbi.nlm.nih.gov/pubmed/16992067.
- Markl D, Zeitler JAA Review of disintegration mechanisms and measurement techniques. Pharm Res [Internet]. 2017 [cited 2019 Jan 30];34:890–917. Available from: http://link.springer.com/10.1007/s11095-017-2129-z.
- Banker GS, Fox SH The theory and practice of industrial pharmacy. J Pharm Sci [Internet]. 1970 [cited 2019 Jan 22];59. Available from: https://books.google.de/books/about/The_Theory_and_Practice_of_Industrial_Ph.html?id=p_VsAAAAMAAJ&redir_esc=y. 1531
- Corveleyn S, Remon JP Formulation and production of rapidly disintegrating tablets by lyophilisation using hydrochlorothiazide as a model drug. Int J Pharm [Internet]. 1997 [cited 2019 Nov 20];152:215–225. Available from: https://biblio.ugent.be/publication/184182.
- Desai PM, Liew CV, Heng PWS Review of disintegrants and the disintegration phenomena. J Pharm Sci [Internet]. 2016 [cited 2019 Jan 30];105:2545–2555. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27506604.
- Dey P, Maiti S Orodispersible tablets: a new trend in drug delivery. J Nat Sci Biol Med 2010;1:2–5. doi:10.4103/0976-9668.71663
- Sheshala R, Khan N, Chitneni M, et al. Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants. Arch Pharm Res 2011;34:1945–1956. doi:10.1007/s12272-011-1115-y
- Habib W, Khankari R, Hontz J Fast-dissolve drug delivery systems. Crit Rev Ther Drug Carrier Syst [Internet]. 2000 [cited 2019 Nov 20];17:61–72. Available from: http://www.ncbi.nlm.nih.gov/pubmed/10755211.
- Yang S, Fu Y, Jeong SH, et al. Application of poly(acrylic acid) superporous hydrogel microparticles as a super-disintegrant in fast-disintegrating tablets. J Pharm Pharmacol [Internet]. 2004 [cited 2019 Nov 20];56:429–436. Available from: http://www.ncbi.nlm.nih.gov/pubmed/15099437.
- Ozeki T, Yasuzawa Y, Katsuyama H, et al. Design of rapidly disintegrating oral tablets using acid-treated yeast cell wall: a technical note. AAPS PharmSciTech [Internet]. 2003 [cited 2019 Nov 20];4:E70. Available from: http://www.ncbi.nlm.nih.gov/pubmed/15198565.
- Lozoya-Agullo I, González-Álvarez I, Merino-Sanjuán M, et al. Preclinical models for colonic absorption, application to controlled release formulation development. Eur J Pharm Biopharm. 2018;130:247–259. doi:10.1016/j.ejpb.2018.07.008
- Zhao N, Augsburger LL Functionality comparison of 3 classes of superdisintegrants in promoting aspirin tablet disintegration and dissolution. AAPS PharmSciTech. 2005;6:E634–E640. doi:10.1208/pt060479
- Nickerson B, Kong A, Gerst P, et al. Correlation of dissolution and disintegration results for an immediate-release tablet. J Pharm Biomed Anal [Internet]. 2018 [cited 2020 Mar 22];150:333–340. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29287259.
- Gupta A, Hunt RL, Shah RB, et al. Disintegration of highly soluble immediate release tablets: a surrogate for dissolution. AAPS PharmSciTech [Internet]. 2009 [cited 2020 Mar 22];10:495–499. Available from: http://www.ncbi.nlm.nih.gov/pubmed/19387843.
- Koner JS, Rajabi-Siahboomi AR, Missaghi S, et al. Conceptualisation, development, fabrication and in vivo validation of a novel disintegration tester for orally disintegrating tablets. Sci Rep [Internet]. 2019 [cited 2020 Mar 22];9:12467. Available from: http://www.ncbi.nlm.nih.gov/pubmed/31462654.
- Radwan A, Wagner M, Amidon GL, et al. Bio-predictive tablet disintegration: effect of water diffusivity, fluid flow, food composition and test conditions. Eur J Pharm Sci [Internet]. 2014 [cited 2019 Sep 27];57:273–279. Available from: http://www.ncbi.nlm.nih.gov/pubmed/24036239.
- Radwan A, Amidon GL, Langguth P Mechanistic investigation of food effect on disintegration and dissolution of BCS class III compound solid formulations: the importance of viscosity. Biopharm Drug Dispos [Internet]. 2012 [cited 2019 Nov 26];33:403–416. Available from: http://www.ncbi.nlm.nih.gov/pubmed/22782559.
- Zaheer K, Langguth P Formulation strategy towards minimizing viscosity mediated negative food effect on disintegration and dissolution of immediate release tablets. Drug Dev Ind Pharm [Internet]. 2018 [cited 2019 Sep 27];44:444–451. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29098885.
- Zaheer K, Langguth P Designing robust immediate release tablet formulations avoiding food effects for BCS class 3 drugs. Eur J Pharm Biopharm [Internet]. 2019 [cited 2019 Sep 27];139:177–185. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30902732.
- Zarmpi P, Flanagan T, Meehan E, et al. Biopharmaceutical understanding of excipient variability on drug apparent solubility based on drug physicochemical properties. Case study: superdisintegrants. AAPS J [Internet]. 2020 [cited 2020 Mar 22];22:46. Available from: http://www.ncbi.nlm.nih.gov/pubmed/32048079.
- Yuen KH The transit of dosage forms through the small intestine. Int J Pharm [Internet]. 2010 [cited 2019 Jan 21];395:9–16. Available from: http://www.ncbi.nlm.nih.gov/pubmed/20478371.
- Adkin D, Davis S, Sparrow R, et al. The effects of pharmaceutical excipients on small intestinal transit. Br J Clin Pharmacol [Internet]. 1995 [cited 2019 Jan 21];39:381–387. Available from: 10.1111/j.1365-2125.1995.tb04466.x.
- Adkin DA, Davis SS, Sparrow RA, et al. The effect of different concentrations of Mannitol in solution on small intestinal transit: implications for drug absorption. Pharm Res [Internet]. 1995 [cited 2019 Jan 21];12:393–396. Available from: http://link.springer.com/10.1023/A:1016256619309.
- Basit AW, Podczeck F, Newton JM, et al. Influence of polyethylene glycol 400 on the gastrointestinal absorption of Ranitidine. Pharm Res. [Internet]. 2002 [cited 2019 Jan 21];19:1368–1374. Available from: http://link.springer.com/10.1023/A:1020315228237.
- Basit AW, Newton JM, Short MD, et al. The effect of polyethylene glycol 400 on gastrointestinal transit: implications for the formulation of poorly-water soluble drugs. Pharm Res [Internet]. 2001 [cited 2019 Jan 21];18:1146–1150. Available from: http://link.springer.com/10.1023/A:1010927026837.
- Schulze JDRR, Waddington WA, Ell PJ, et al. Concentration-dependent effects of polyethylene glycol 400 on gastrointestinal transit and drug absorption. Pharm Res [Internet]. 2003 [cited 2019 Jan 21];20:1984–1988. Available from: http://link.springer.com/10.1023/B:PHAM.0000008046.64409.bd.
- Ashiru DAI, Patel R, Basit AW Polyethylene glycol 400 enhances the bioavailability of a BCS class III drug (ranitidine) in male subjects but not females. Pharm Res. 2008;25:2327–2333. doi:10.1007/s11095-008-9635-y
- Mai Y, Dou L, Madla CM, et al. Sex-dependence in the effect of pharmaceutical excipients: polyoxyethylated solubilising excipients increase oral drug bioavailability in male but not female Rats. Pharm [Internet]. 2019 [cited 2020 Mar 22];11:228. Available from: https://www.mdpi.com/1999-4923/11/5/228.
- García Pérez WM Metodología en el desarrollo de software. Univ Nac la Amaz Peru. [Internet]. 2015;567. Available from: https://editorial.edu.umh.es/2015/05/24/metodologias-biofarmaceuticas-en-el-desarrollo-de-medicamentos/.
- Fernandez-Teruel C, Mangas-Sanjuan V, Gonzalez-Alvarez I, et al. Mathematical modeling of oral absorption and bioavailability of a fluoroquinolone after its precipitation in the gastrointestinal tract. Xenobiotica. 2013;43:745–754. doi:10.3109/00498254.2012.759667
- Tsume Y, Mudie DM, Langguth P, et al. The biopharmaceutics classification system: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC. Eur J Pharm Sci. [Internet]. 2014 [cited 2019 Jan 19];57:152–163. Available from: http://www.ncbi.nlm.nih.gov/pubmed/24486482.
- Stegemann S, Leveiller F, Franchi D, et al. When poor solubility becomes an issue: from early stage to proof of concept. Eur J Pharm Sci [Internet]. 2007 [cited 2019 Jan 23];31:249–261. Available from: http://www.ncbi.nlm.nih.gov/pubmed/17616376.
- Lipinski CA Drug-like properties and the causes of poor solubility and poor permeability. J Pharmacol Toxicol Methods [Internet]. 2000 [cited 2019 Jan 23];44:235–249. Available from: http://www.ncbi.nlm.nih.gov/pubmed/11274893.
- Rodríguez‐hornedo N, Murphy D Significance of controlling crystallization mechanisms and kinetics in pharmaceutical systems. J Pharm Sci. [Internet]. 1999 [cited 2019 Jan 23];88:651–660. Available from: https://www.sciencedirect.com/science/article/pii/S002235491550837X.
- Box K, Comer J, Gravestock T, et al. New ideas about the solubility of drugs. Chem Biodivers [Internet]. 2009 [cited 2019 Jan 23];6:1767–1788. Available from: http://www.ncbi.nlm.nih.gov/pubmed/19937815.
- Yamashita T, Kokubo T, Zhao C, et al. Antiprecipitant screening system for basic model compounds using bio-relevant media. J Assoc Lab Autom [Internet]. 2010 [cited 2019 Jan 23];15:306–312. Available from: http://journals.sagepub.com/doi/10.1016/j.jala.2009.12.001.
- Yamashita K, Nakate T, Okimoto K, et al. Establishment of new preparation method for solid dispersion formulation of tacrolimus. Int J Pharm [Internet]. 2003 [cited 2019 Jan 24];267:79–91. Available from: http://www.ncbi.nlm.nih.gov/pubmed/14602386.
- Gao P, Rush BD, Pfund WP, et al. Development of a supersaturable SEDDS (S‐SEDDS) formulation of paclitaxel with improved oral bioavailability. J Pharm Sci [Internet]. 2003 [cited 2019 Jan 24];92:2386–2398. Available from: https://www.sciencedirect.com/science/article/pii/S0022354916313752.
- Bi M, Kyad A, Kiang Y-H, et al. Enhancing and sustaining AMG 009 dissolution from a matrix tablet via microenvironmental pH modulation and supersaturation. AAPS PharmSciTech [Internet]. 2011 [cited 2019 Jan 24];12:1157–1162. Available from: http://link.springer.com/10.1208/s12249-011-9679-x.
- Gao P, Guyton ME, Huang T, et al. Enhanced oral bioavailability of a poorly water soluble drug PNU‐91325 by supersaturatable formulations. Drug Dev Ind Pharm [Internet]. 2004 [cited 2019 Jan 24];30:221–229. Available from: http://www.tandfonline.com/doi/full/10.1081/DDC-120028718.
- Li S, Pollock-Dove C, Dong LC, et al. Enhanced bioavailability of a poorly water-soluble weakly basic compound using a combination approach of solubilization agents and precipitation inhibitors: a case study. Mol Pharm [Internet]. 2012 [cited 2019 Jan 23];9:1100–1108. Available from: http://pubs.acs.org/doi/10.1021/mp200352q. • Recommendation for the utility of excipients when precipitation of poorly soluble drugs wants to be avoided.
- Savla R, Browne J, Plassat V, et al. Review and analysis of FDA approved drugs using lipid-based formulations. Drug Dev Ind Pharm [Internet]. 2017 [cited 2020 Mar 22];43:1743–1758. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28673096.
- Pouton CW Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci. 2006;29:278–287. doi:10.1016/j.ejps.2006.04.016
- Pouton CW, Porter CJH Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv Drug Deliv Rev [Internet]. 2008 [cited 2020 Mar 22];60:625–637. Available from: http://www.ncbi.nlm.nih.gov/pubmed/18068260.
- Banerjee S, Pillai J Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs. Expert Opin Drug Metab Toxicol [Internet]. 2019 [cited 2020 Mar 22];15:499–515. Available from: http://www.ncbi.nlm.nih.gov/pubmed/31104522.
- Talegaonkar S, Bhattacharyya A Potential of lipid nanoparticles (SLNs and NLCs) in enhancing oral bioavailability of drugs with poor intestinal permeability. AAPS PharmSciTech [Internet]. 2019 [cited 2020 Mar 22];20:121. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30805893.
- Kalepu S, Manthina M, Padavala V Oral lipid-based drug delivery systems – an overview. Acta Pharm Sin B 2013;3:361–372. doi:10.1016/j.apsb.2013.10.001
- Williams HD, Ford L, Igonin A, et al. Unlocking the full potential of lipid-based formulations using lipophilic salt/ionic liquid forms. Adv Drug Deliv Rev 2019;142:75–90. doi:10.1016/j.addr.2019.05.008
- Dumont C, Bourgeois S, Fessi H, et al. Lipid-based nanosuspensions for oral delivery of peptides, a critical review. Int J Pharm [Internet]. 2018 [cited 2020 Mar 22];541:117–135. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29476783.
- Carrière F Impact of gastrointestinal lipolysis on oral lipid-based formulations and bioavailability of lipophilic drugs. Biochimie [Internet]. 2016 [cited 2020 Mar 22];125:297–305. Available from: http://www.ncbi.nlm.nih.gov/pubmed/26607242.
- Feeney OM, Crum MF, McEvoy CL, et al. 50years of oral lipid-based formulations: provenance, progress and future perspectives. Adv Drug Deliv Rev [Internet]. 2016 [cited 2020 Mar 22];101:167–194. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27089810.
- Swarnakar NK, Venkatesan N, Critical BG In vitro characterization methods of lipid-based formulations for oral delivery: a comprehensive review. AAPS PharmSciTech [Internet]. 2018 [cited 2020 Mar 22];20:16. Available from: http://www.ncbi.nlm.nih.gov/pubmed/30569266.
- Beig A, Fine-Shamir N, Lindley D, et al. Advantageous solubility-permeability interplay when using amorphous solid dispersion (ASD) formulation for the BCS Class IV P-gp substrate Rifaximin: simultaneous increase of both the solubility and the permeability. AAPS J. [Internet]. 2017 [cited 2020 Mar 22];19:806–813. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28204967.
- Beig A, Agbaria R, Dahan A The use of captisol (SBE7-β-CD) in oral solubility-enabling formulations: Comparison to HPβCD and the solubility-permeability interplay. Eur J Pharm Sci. [Internet]. 2015 [cited 2020 Mar 22];77:73–78. Available from: http://www.ncbi.nlm.nih.gov/pubmed/26006306.
- Dahan A, Beig A, Lindley D, et al. The solubility-permeability interplay and oral drug formulation design: two heads are better than one. Adv Drug Deliv Rev. [Internet]. 2016 [cited 2020 Mar 22];101:99–107. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27129443.
- Fine-Shamir N, Methacrylate-Copolymer Eudragit DA EPO as a solubility-enabling excipient for anionic drugs: investigation of drug solubility, intestinal permeability, and their interplay. Mol Pharm. [Internet]. 2019 [cited 2020 Mar 22];16:2884–2891. Available from: http://www.ncbi.nlm.nih.gov/pubmed/31120762.
- Porat D, Dahan A Active intestinal drug absorption and the solubility-permeability interplay. Int J Pharm. 2018;537:84–93. doi:10.1016/j.ijpharm.2017.10.058
- Sun L, Liu X, Xiang R, et al. Structure-based prediction of human intestinal membrane permeability for rapid in silico BCS classification. Biopharm Drug Dispos [Internet]. 2013 [cited 2019 Jan 18];34:321–335. Available from: http://www.ncbi.nlm.nih.gov/pubmed/23716273.
- Twarog C, Fattah S, Heade J, et al. Intestinal Permeation Enhancers for Oral Delivery of Macromolecules: A Comparison between Salcaprozate Sodium (SNAC) and Sodium Caprate (C10). Pharmaceutics. 2019;11:78. doi:10.3390/pharmaceutics11020078
- Stepensky D, Friedman M, Srour W, et al. Preclinical evaluation of pharmacokinetic-pharmacodynamic rationale for oral CR metformin formulation. J Control Release [Internet]. 2001 [cited 2019 Nov 20];71:107–115. Available from: http://www.ncbi.nlm.nih.gov/pubmed/11245912.
- Samiei N, Mangas-Sanjuan V, González-Álvarez I, et al. Ion-pair strategy for enabling amifostine oral absorption: Rat in situ and in vivo experiments. Eur J Pharm Sci 2013;49:499–504. doi:10.1016/j.ejps.2013.04.025
- Lozoya-Agullo I, González-Álvarez I, González-Álvarez M, et al. Development of an ion-pair to improve the colon permeability of a low permeability drug: Atenolol. Eur J Pharm Sci. [Internet]. 2016 [cited 2019 Nov 20];93:334–340. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27552904.
- Goole J, Lindley DJ, Roth W, et al. The effects of excipients on transporter mediated absorption. Int J Pharm. [Internet]. 2010 [cited 2019 Jan 21];393:17–31. Available from: https://www.sciencedirect.com/science/article/pii/S0378517310002917.
- Garrigues TM, Ferez-Varona AT, Bermejo MV, et al. Absorption-partition relationships for true homologous series of xenobiotics as a possible approach to study mechanisms of surfactants in absorption. IV. Phenylacetic acid derivatives and anionic surfactants. Int J Pharm. 1992;79:135–140. doi:10.1016/0378-5173(92)90104-A
- Carmona-Ibáñez G, Del Val Bermejo-Sanz M, Rius-Alarcó F, et al. Experimental studies on the influence of surfactants on intestinal absorption of drugs. Cefadroxil as model drug and sodium taurocholate as natural model surfactant: studies in rat colon and in rat duodenum. Arzneimittelforschung. [Internet]. 1999 [cited 2019 Dec 2];49:44–50. Available from: http://www.ncbi.nlm.nih.gov/pubmed/10028379.
- Fabra-Campos S, J V R, Gomez-Meseguer V, et al. Biophysical absorption models for phenyl-alkyl acids in the absence and in the presence of surfactants. Studies in the rat small intestine. Eur J Drug Metab Pharmacokinet [Internet]. 1991 [cited 2020 Jan 3];Spec No 3:32–42. Available from: http://www.ncbi.nlm.nih.gov/pubmed/1820901.
- Rege BD, Kao JPY, Polli JE Effects of nonionic surfactants on membrane transporters in Caco-2 cell monolayers. Eur J Pharm Sci. 2002;16:237–246. doi:10.1016/S0928-0987(02)00055-6
- Martin GP, Marriott C, Kellaway IW Direct effect of bile salts and phospholipids on the physical properties of mucus. Gut [Internet]. 1978 [cited 2019 Jan 21];19:103–107. Available from: http://www.ncbi.nlm.nih.gov/pubmed/631625.
- Tomita M, Hayashi M, Horie T, et al. Enhancement of colonic drug absorption by the transcellular permeation route. Pharm Res [Internet]. 1988 [cited 2019 Jan 21];05:786–789. Available from: http://link.springer.com/10.1023/A:1015992819290.
- Rege BD, Yu LX, Hussain AS, et al. Effect of common excipients on Caco-2 transport of low-permeability drugs. J Pharm Sci [Internet]. 2001 [cited 2019 Jan 21];90:1776–1786. Available from: http://linkinghub.elsevier.com/retrieve/pii/S0022354916308668.
- Kang ML, Il IG. Drug delivery systems for intra-articular treatment of osteoarthritis. Expert Opin Drug Deliv 2014;11:269–282. doi:10.1517/17425247.2014.867325
- Takizawa Y, Kishimoto H, Nakagawa M, et al. Effects of pharmaceutical excipients on membrane permeability in rat small intestine. Int J Pharm [Internet]. 2013 [cited 2019 Jan 21];453:363–370. Available from: 10.1016/j.ijpharm.2013.05.055.
- Peppas NA, Kavimandan NJ Nanoscale analysis of protein and peptide absorption: Insulin absorption using complexation and pH-sensitive hydrogels as delivery vehicles. Eur J Pharm Sci [Internet]. 2006 [cited 2019 Jan 21];29:183–197. Available from: https://www.sciencedirect.com/science/article/pii/S0928098706001175.
- Larocque G, Arnold AA, É C, et al. Effect of sodium bicarbonate as a pharmaceutical formulation excipient on the interaction of fluvastatin with membrane phospholipids. Eur Biophys J [Internet]. 2010 [cited 2019 Jan 21];39:1637–1647. Available from: http://link.springer.com/10.1007/s00249-010-0622-y.
- Bermejo M, Mangas-Sanjuan V, Gonzalez-Alvarez I, et al. Enhancing oral absorption of β-Lapachone: progress till date. Eur J Drug Metab Pharmacokinet. [Internet]. 2017 [cited 2020 Mar 25];42:1–10. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27538882.
- Li X, Uehara S, Sawangrat K, et al. Improvement of intestinal absorption of curcumin by cyclodextrins and the mechanisms underlying absorption enhancement. Int J Pharm [Internet]. 2018 [cited 2020 Mar 25];535:340–349. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29157961.
- Purpura M, Lowery RP, Wilson JM, et al. Analysis of different innovative formulations of curcumin for improved relative oral bioavailability in human subjects. Eur J Nutr [Internet]. 2018 [cited 2020 Mar 25];57:929–938. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28204880.
- Zhang H, Huang X, Zhang Y, et al. Efficacy, safety and mechanism of HP-β-CD-PEI polymers as absorption enhancers on the intestinal absorption of poorly absorbable drugs in rats. Drug Dev Ind Pharm [Internet]. 2017 [cited 2020 Mar 25];43:474–482. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27892724.
- Wang D, Chen G, Ren L Preparation and characterization of the Sulfobutylether-β-Cyclodextrin inclusion complex of amiodarone hydrochloride with enhanced oral bioavailability in fasted state. AAPS PharmSciTech [Internet]. 2017 [cited 2020 Mar 25];18:1526–1535. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27757923.
- Maher S, Brayden D, Casettari L, et al. Application of Permeation Enhancers in Oral Delivery of Macromolecules: An Update. Pharmaceutics [Internet]. 2019 [cited 2019 Oct 17];11:41. Available from: http://www.mdpi.com/1999-4923/11/1/41.
- Zhang H, Yao M, Morrison RA, et al. Commonly used surfactant, Tween 80, improves absorption of P-glycoprotein substrate, digoxin, in rats. Arch Pharm Res. [Internet]. 2003 [cited 2019 Jan 21];26:768–772. Available from: http://link.springer.com/10.1007/BF02976689.
- Lo YL Relationships between the hydrophilic-lipophilic balance values of pharmaceutical excipients and their multidrug resistance modulating effect in Caco-2 cells and rat intestines. J Control Release. 2003;90:37–48. doi:10.1016/S0168-3659(03)00163-9
- Shen Q, Lin Y, Handa T, et al. Modulation of intestinal P-glycoprotein function by polyethylene glycols and their derivatives by in vitro transport and in situ absorption studies. Int J Pharm. [Internet]. 2006 [cited 2019 Jan 21];313:49–56. Available from: https://www.sciencedirect.com/science/article/pii/S0378517306000652.
- Brouwers J, Tack J, Lammert F, et al. Intraluminal drug and formulation behavior and integration in in vitro permeability estimation: a case study with amprenavir. J Pharm Sci. [Internet]. 2006 [cited 2019 Nov 20];95:372–383. Available from: http://www.ncbi.nlm.nih.gov/pubmed/16374852.
- Collnot EM, Baldes C, Schaefer UF, et al. Vitamin e TPGS P-glycoprotein inhibition mechanism: Influence on conformational flexibility, intracellular ATP levels, and role of time and site of access. Mol Pharm. 2010;7:642–651. doi:10.1021/mp900191s
- Batrakova EV, Li S, Li Y, et al. Effect of Pluronic P85 on ATPase activity of drug efflux transporters. Pharm Res. [Internet]. 2004 [cited 2019 Jan 21];21:2226–2233. Available from: http://link.springer.com/10.1007/s11095-004-7675-5.
- Sawangrat K, Yamashita S, Tanaka A, et al. Modulation of intestinal transport and absorption of topotecan, a BCRP substrate, by various pharmaceutical excipients and their inhibitory mechanisms of BCRP transporter. J Pharm Sci 2019; 108 1315–1325 doi:10.1016/j.xphs.2018.10.043
- Yamagata T, Kusuhara H, Morishita M, et al. Improvement of the oral drug absorption of topotecan through the inhibition of intestinal xenobiotic efflux transporter, breast cancer resistance protein, by excipients. Drug Metab Dispos [Internet]. 2007 [cited 2019 Nov 22];35:1142–1148. Available from: http://dmd.aspetjournals.org/cgi/content/abstract/dmd.106.014217v1%5Cnpapers2://publication/doi/10.1124/dmd.106.014217.
- Nielsen CU, Abdulhussein AA, Colak D, et al. Polysorbate 20 increases oral absorption of digoxin in wild-type Sprague Dawley rats, but not in mdr1a(-/-) Sprague Dawley rats. Int J Pharm. [Internet]. 2016 [cited 2019 Sep 27];513:78–87. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27601334.
- Arima H, Yunomae K, Morikawa T, et al. Contribution of cholesterol and phospholipids to inhibitory effect of dimethyl-beta-cyclodextrin on efflux function of P-glycoprotein and multidrug resistance-associated protein 2 in vinblastine-resistant Caco-2 cell monolayers. Pharm Res [Internet]. 2004 [cited 2019 Nov 20];21:625–634. Available from: http://www.ncbi.nlm.nih.gov/pubmed/15139519.
- Arima H, Yunomae K, Hirayama F, et al. Contribution of P-glycoprotein to the enhancing effects of dimethyl-β-cyclodextrin on oral bioavailability of Tacrolimus. J Pharmacol Exp Ther 2001;297(2):547-555.
- Ferté J Analysis of the tangled relationships between P-glycoprotein-mediated multidrug resistance and the lipid phase of the cell membrane. Eur J Biochem. [Internet]. 2000 [cited 2019 Jan 21];267:277–294. Available from: 10.1046/j.1432-1327.2000.01046.x.
- Bromberg L, Alakhov V Effects of polyether-modified poly(acrylic acid) microgels on doxorubicin transport in human intestinal epithelial Caco-2 cell layers. J Control Release [Internet]. 2003 [cited 2019 Jan 21];88:11–22. Available from: https://www.sciencedirect.com/science/article/pii/S0168365902004194.
- Suzuki M, Komura H, Yoshikawa T, et al. Characterization of gastrointestinal absorption of digoxin involving influx and efflux transporter in rats: Application of mdr1a knockout (-/-) rats into absorption study of multiple transporter substrate. Xenobiotica [Internet]. 2014 [cited 2019 Sep 27];44:1039–1045. Available from: http://www.ncbi.nlm.nih.gov/pubmed/24839994.
- Caldeira TG, Ruiz-Picazo A, Lozoya-Agullo I, et al. Determination of intestinal permeability using in situ perfusion model in rats: Challenges and advantages to BCS classification applied to digoxin. Int J Pharm [Internet]. 2018;551:148–157. Available from: https://linkinghub.elsevier.com/retrieve/pii/S0378517318306732.
- Tayrouz Y, Ding R, Burhenne J, et al. Pharmacokinetic and pharmaceutic interaction between digoxin and Cremophor RH40. Clin Pharmacol Ther. [Internet]. 2003 [cited 2019 Jan 21];73:397–405. Available from: 10.1016/S0009-9236(03)00059-6.
- Maher S, Mrsny RJ, Brayden DJ Intestinal permeation enhancers for oral peptide delivery. Adv Drug Deliv Rev. [Internet]. 2016 [cited 2019 Nov 25];106:277–319. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27320643.
- McCartney F, Gleeson JP, Brayden DJ Safety concerns over the use of intestinal permeation enhancers: a mini-review. Tissue Barriers [Internet]. 2016 [cited 2019 Nov 25];4:e1176822. Available from: http://www.ncbi.nlm.nih.gov/pubmed/27358756.
- Fox CB, Kim J, Le LV, et al. Micro/nanofabricated platforms for oral drug delivery. J Control Release [Internet]. 2015 [cited 2019 Nov 25];219:431–444. Available from: http://www.ncbi.nlm.nih.gov/pubmed/26244713.
- Maher S, Wang X, Bzik V, et al. Evaluation of intestinal absorption and mucosal toxicity using two promoters. II. Rat instillation and perfusion studies. Eur J Pharm Sci. 2009;38:301–311. doi:10.1016/j.ejps.2009.07.011
- Sharma P, Varma MVS, Chawla HPS, et al. Absorption enhancement, mechanistic and toxicity studies of medium chain fatty acids, cyclodextrins and bile salts as peroral absorption enhancers. Farmaco. 2005;60:884–893. doi:10.1016/j.farmac.2005.08.008
- Lucarini S, Fagioli L, Cavanagh R, et al. Synthesis, structure–activity relationships and in vitro toxicity profile of lactose-based fatty acid monoesters as possible drug permeability enhancers. Pharmaceutics. 2018;10(3):81.
- Uchiyama T, Sugiyama T, Quan Y-S, et al. Enhanced Permeability of Insulin across the Rat Intestinal Membrane by Various Absorption Enhancers: Their Intestinal Mucosal Toxicity and Absorption-enhancing Mechanism of n-Lauryl-β-D-maltopyranoside. J Pharm Pharmacol. 1999;51:1241–1250. doi:10.1211/0022357991776976
- Moroz E, Matoori S, Leroux JC Oral delivery of macromolecular drugs: where we are after almost 100 years of attempts. Adv Drug Deliv Rev. 2016;101:108–121. doi:10.1016/j.addr.2016.01.010
- Dahlgren D, Roos C, Lundqvist A, et al. Time-dependent effects on small intestinal transport by absorption-modifying excipients. Eur J Pharm Biopharm 2018;132:19–28. doi:10.1016/j.ejpb.2018.09.001
- Dahlgren D, Roos C, Lundqvist A, et al. Effect of absorption-modifying excipients, hypotonicity, and enteric neural activity in an in vivo model for small intestinal transport. Int J Pharm. 2018;549:239–248. doi:10.1016/j.ijpharm.2018.07.057
- Dahlgren D, Roos C, Johansson P, et al. The effects of three absorption-modifying critical excipients on the in vivo intestinal absorption of six model compounds in rats and dogs. Int J Pharm. 2018;547:158–168. doi:10.1016/j.ijpharm.2018.05.029
- Kolte BP, Tele KV, Mundhe VS, et al. Colon targeted drug delivery system – a novel perspective. Asian J Biomed Pharm Sci [Internet]. 2012;2(14):21–28. [cited 2019 Nov 20]. Available from: https://www.alliedacademies.org/abstract/colon-targeted-drug-delivery-system–a-novel-perspective-4832.html.
- Chourasia MK, Jain SK Pharmaceutical approaches to colon targeted drug delivery systems. J Pharm Pharm Sci. 2003;6:33–66.
- Patel MM Cutting-edge technologies in colon-targeted drug delivery systems. Expert Opin Drug Deliv. [Internet]. 2011 [cited 2019 Nov 20];8:1247–1258. Available from: http://www.ncbi.nlm.nih.gov/pubmed/21933030.
- Muraoka M, Hu Z, Shimokawa T, et al. Evaluation of intestinal pressure-controlled colon delivery capsule containing caffeine as a model drug in human volunteers. J Control Release [Internet]. 1998 [cited 2019 Nov 20];52:119–129. Available from: http://www.ncbi.nlm.nih.gov/pubmed/9685942.
- Singh K, Walia MK, Agarwal G, et al. Osmotic pump drug delivery system: a noval approach. J Drug Delivery Ther. 2013;3(5).
- Gupta RN, Gupta R, Basniwal PK, et al. Osmotically controlled oral drug delivery systems: a review. Int J Pharm Sci. [Internet]. 2009 [cited 2019 Nov 20];1:269–275. Available from: https://www.researchgate.net/publication/270823132_Osmotically_Controlled_Oral_Drug_Delivery_Systems_A_Novel_Approach.
- Singh KI, Singh J, Sharma D, et al. Colon specific drug delivery system: review on novel approaches. Int J Pharm Sci Res. [Internet]. 2012 [cited 2019 Nov 20];3:637–647. Available from: http://ijpsr.com/bft-article/colon-specific-drug-delivery-system-review-on-novel-approaches/.
- Lozoya-Agullo I, Araújo F, González-Álvarez I, et al. PLGA nanoparticles are effective to control the colonic release and absorption on ibuprofen. Eur J Pharm Sci [Internet]. 2018 [cited 2019 Nov 20];115:119–125. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29248559.
- Lozoya-Agullo I, Planelles M, Merino-Sanjuán M, et al. Ion-pair approach coupled with nanoparticle formation to increase bioavailability of a low permeability charged drug. Int J Pharm 2019;557:36–42. doi:10.1016/j.ijpharm.2018.12.038
- González-Alvarez M, Coll C, Gonzalez-Alvarez I, et al. Gated mesoporous silica nanocarriers for a “Two-Step” targeted system to colonic tissue. Mol Pharm. [Internet]. 2017 [cited 2019 Nov 20];14:4442–4453. Available from: http://www.ncbi.nlm.nih.gov/pubmed/29064714.
- Campiñez MD, Benito E, Romero-Azogil L, et al. Development and characterization of new functionalized polyurethanes for sustained and site-specific drug release in the gastrointestinal tract. Eur J Pharm Sci. [Internet]. 2017 [cited 2019 Nov 20];100:285–295. Available from: http://www.ncbi.nlm.nih.gov/pubmed/28108361.
- Alshahrani SM, Alshetaili AS, Alalaiwe A, et al. Anticancer efficacy of self-nanoemulsifying drug delivery system of Sunitinib Malate. AAPS PharmSciTech. 2018;19:123–133. doi:10.1208/s12249-017-0826-x
- Kolter K, Guth F Development of new excipients. Pharm Excipients Prop Funct Appl Res Ind [Internet]. Hoboken, NJ, USA: John Wiley & Sons, Inc.; 2016 [ cited 2019 Nov 20]. p. 269–301. Available from: 10.1002/9781118992432.ch7.
- Kortejärvi H, Malkki J, Shawahna R, et al. Pharmacokinetic simulations to explore dissolution criteria of BCS i and III biowaivers with and without MDR-1 efflux transporter. Eur J Pharm Sci. 2014; 61 18–26 doi:10.1016/j.ejps.2014.02.004
- Kambayashi A, Kiyota T, Fujiwara M, et al. PBPK modeling coupled with biorelevant dissolution to forecast the oral performance of amorphous solid dispersion formulations. Eur J Pharm Sci. 2019; 135 83–90 doi:10.1016/j.ejps.2019.05.013
- Kesisoglou F, Mitra A Application of Absorption Modeling in Rational Design of Drug Product Under Quality-by-Design Paradigm. AAPS J. 2015; 17 1224–1236 doi:10.1208/s12248-015-9781-1 .
- Chow ECY, Talattof A, Tsakalozou E, et al. Using physiologically based Pharmacokinetic (PBPK) modeling to evaluate the impact of pharmaceutical excipients on oral drug absorption: sensitivity analyses. AAPS J. 2016; 18 1500–1511 doi:10.1208/s12248-016-9964-4