Bibliography
- VENKATESH S, UPPER RA: Role of the development scientist in compound lead selection and optimization. J. Pharm. Sci. (2000) 89(2):145–154
- VAN DE WATERBEEMD H, SMITH DA, BEAUMONT K, WALKER DK: Property-based design: optimization of drug absorption and pharmacokinetics. J. Med. Chem. (2001) 44(9):1313–1333
- •Interesting review and discussion of lead optimisation parameters
- AJAY: Predicting drug-likeness: why and how? Curr. Top. Med. Chem. (2002) 2(12):1273–1286
- KERNS EH, DI L: Multivariate pharmaceutical profiling for drug discovery. Curr. Top. Med. Chem. (2002) 2(1):87–98
- ALANINE A, NETTEKOVEN M, ROBERTS E, THOMAS AW: Lead generation: enhancing the success of drug discovery by investing in the hit to lead process. Comb. Chem. High Throughput Screen. (2003) 6(1):51–66
- GARDNER CR, WALSH CT, ALMARSSON 0: Drugs as materials: valuing physical form in drug discovery. Nat. Rev. Drug Discov. (2004) 3(11):926–934
- •Informative review of formulation design strategies and trends
- LOMBARDINO JG, LOWE JA 3rd: The role of the medicinal chemist in drug discovery-then and now. Nat. Rev. Drug Discov. (2004) 3(10):853–862
- •Informative review of medicinal chemistry strategies and trends
- SAKAEDA T, OKAMURA N, NAGATA S et al.: Molecular and pharmacokinetic properties of 222 commercially available oral drugs in humans. Biol. Pharm. Bull. (2001) 24(8):935–940
- WENLOCK MC, AUSTIN RP, BARTON P, DAVIS AM, LEESON PD: A comparison of physiochemical property profiles of development and marketed oral drugs. J. Med. Chem. (2003) 46(7):1250–1256
- •Interesting review of trends in physiochemical properties that favour successful clinical development to market
- VIETH M, SIEGEL MG, HIGGS RE et al.: Characteristic physical properties and structural fragments of marketed oral drugs. J. Med. Chem. (2004) 47(1):224–232
- •Analysis of factors that determine oral bioavailability of marketed drugs
- LEESON PD, DAVIS AM: Time-related differences in the physical property profiles of oral drugs. J. Med. Chem. (2004) 47(25):6338–6348
- LIPINSKI CA, LOMBARDO F, DOMINY BW, FEENEY PJ: Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deli v. Rev. (1997) 23(1–3):3–25
- ANDREWS CW, BENNETT L, YU LX: Predicting human oral bioavailability of a compound: development of a novel quantitative structure-bioavailability relationship. Pharm. Res. (2000) 17(0:639–644
- VEBER DF, JOHNSON SR, CHENG HY SMITH BR, WARD KW, KOPPLE KD: Molecular properties that influence the oral bioavailability of drug candidates. J. Med. Chem. (2002) 45(12):2615–2623
- BERGSTROM CA, STRAFFORD M, LAZOROVA L, AVDEEF A, LUTHMAN K, ARTURSSON P: Absorption classification of oral drugs based on molecular surface properties. J. Med. Chem. (2003) 46(4):558–570
- HUM, AMIDON GL: Passive and carrier-mediated intestinal absorption components of captopril. j Pharm. Sci. (1988) 77(12):1007–1011
- BAT PF, SUBRAIVIANIAN P, MOSBERG HI, AMIDON GL: Structural requirements for the intestinal mucosal-cell peptide transporter: the need for N-terminal alpha-amino group. Pharm. Res. (1991) 8(5):593–599
- OH DM, SINKO PJ, AMIDON GL: Characterization of the oral absorption of some beta-lactams: effect of the alpha-amino side chain group. J. Pharm. (1993) 82(9):897–900
- DANTZIG AH, DUCKWORTH DC, TABAS LB: Transport mechanisms responsible for the absorption of loracarbef, cefixime, and cefuroxime axetil into human intestinal Caco-2 cells. Biochim. Biophys. Acta (1994) 1191(1):7–13
- DANTZIG AH, HOSKINS JA, TABAS LB et al.: Association of intestinal peptide transport with a protein related to the cadherin superfamily. Science (1994) 264(5157):430–433
- HUM, ZHENG L, CHEN J et al.: Mechanisms of transport of quinapril in Caco-2 cell monolayers: comparison with cephalexin. Pharm. Res. (1995) 12(8):1120–1125
- SCHINKEL AH: Pharmacological insights from P-glycoprotein knockout mice. Int. J. Clin. Pharmacol Ther. (1998) 36(1):9–13
- KULLAK-UBLICK Gk, BECKER MB: Regulation of drug and bile salt transporters in liver and intestine. Drug Metab. Rev. (2003) 35(4):305–317
- YATES CR, CHANG C, KEARBEY JD et al.: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm. Res. (2003) 20(11):1794–1803
- SCHINKEL AH, JONKER JW: Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview. Adv. Drug Deli v. Rev. (2003) 55(1):3–29
- CHAN LM, LOWES S, HIRST BH: The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability. Eur. Pharm. Sci. (2004) 21(1):25–51
- BARTHE L, WOODLEY J, HOUIN G: Gastrointestinal absorption of drugs: methods and studies. Fundam. Clin. Pharmacol (1999) 13(2):154–168
- HIDALGO IJ: Assessing the absorption of new pharmaceuticals. Curr. Top. Med. Chem. (2001) 1(5):385–401
- BOHETS H, ANNAERT P, MANNENS G et al.: Strategies for absorption screening in drug discovery and development. Curr. Top. Med. Chem. (2001) 1(5):367–383
- AGORAM B, WOLTOSZ WS, BOLGER MB: Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv. Drug Deliv. Rev. (2001) 50\(Suppl. 1):541–567
- STENBERG P, BERGSTROM CA, LUTHMAN K, ARTURSSON P: Theoretical predictions of drug absorption in drug discovery and development. Clin. Pharmacokinet. (2002) 41(11):877–899
- Drug Bioavailability. Estimation of Solubility Permeability Absorption and Bioavailability. H van de Waterbeemd, H Lennernas, P Artursson (Eds), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, Germany (2004)
- •Comprehensive review of factors influencing oral bioavailability and emerging estimation methods
- ETTMAYER P, AMIDON GL, CLEMENT B, TESTA B: Lessons learned from marketed and investigational prodrugs. J. Med. Chem. (2004) 47(10):2393–2404
- •Comprehensive review of prodrug approaches
- DJALDETTI R, GILADI N, HASSIN-BAER S, SHABTAI H, MELAMED E: Pharmacokinetics of etilevodopa compared to levodopa in patients with Parkinson's disease: an open-label, randomized, crossover study. Clin. Neuropharmacol (2003) 26(6):322–326
- DANTA M, DUSHEIKO G: Adefovir dipivoxil: review of a novel acyclic nucleoside analogue. Int. J. Clin. Pract. (2004) 58(9):877–886
- HADZIYANNIS SJ, PAPATHEODORIDIS GV: Adefovir dipivoxil in the treatment of chronic hepatitis B virus infection. Expert Rev. Anti Infect. Ther. (2004) 2(4):475–483
- TESTA B: Prodrug research: futile or fertile? Biochem. Pharmacol. (2004) 68(11):2097–2106
- MILANO G, FERRERO JM, FRANCOIS E: Comparative pharmacology of oral fluoropyrimidines: a focus on pharmacokinetics, pharmacodynamics and pharmacomodulation. Br. J. Cancer (2004) 91(4):613–617
- HAYDEN FG, JENNINGS L, ROBSON R et al.: Oral oseltamivir in human experimental influenza B infection. Antiviral Ther. (2000) 5(3):205–213
- YOSHIKAWA M, NISHIYAMA S, TAKAITI 0: Metabolism of dopamine prodrug, docarpamine. Hypertens. Res. (1995) 18\(Suppl. 1):S211–S213
- VAN GELDER J, DEFERME S, NAESENS L et al.: Intestinal absorption enhancement of the ester prodrug tenofovir disoproxil fitmarate through modulation of the biochemical barrier by defined ester mixtures. Drug Metab. Dispos. (2002) 30(8):924–930
- CHAPMAN T, MCGAVIN J, NOBLE S: Tenofovir disoproxil fitmarate. Drugs (2003) 63(15):1597–1608
- KEARNEY BP, FLAHERTY JF, SHAH J: Tenofovir disoproxil fumarate: clinical pharmacology and pharmacokinetics. Clin. Pharmacokinet. (2004) 43(9):595–612
- VIAL HJ, WEIN S, FARENC C et al.: Prodrugs of bisthiazolium salts are orally potent antimalarials. Proc. Nail. Acad. Sci. USA (2004) 101 (43):15458–15463
- VICKERS S, DUNCAN CA, CHEN IW, ROSEGAY A, DUGGAN DE: Metabolic disposition studies on simvastatin, a cholesterol-lowering prodrug. Drug Metab. Dispos. (1990) 18(2):138–145
- MAURO VF: Clinical pharmacokinetics and practical applications of simvastatin. Clin. Pharmacokinet. (1993) 24(3):195–202
- ISHIGAMI M, HONDA T, TAKASAKI W et al.: A comparison of the effects of 3-hydroxy-3-methylglutaryl-coenzyme a (HMG-CoA) reductase inhibitors on the CYP3A4-dependent oxidation of mexazolam in vitro. Drug Metab. Dispos. (2001) 29(3):282–288
- SWAAN PW, TUKKER JJ: Molecular determinants of recognition for the intestinal peptide carrier. J. Pharm. Sci. (1997) 86(5):596–602
- DORING F, WILL J, AMASHEH S, CLAUSS W, AHLBRECHT H, DANIEL H: Minimal molecular determinants of substrates for recognition by the intestinal peptide transporter. J. Biol. Chem. (1998) 273(30:23211–23218
- THEIS S, HARTRODT B, KOTTRA G, NEUBERT K, DANIEL H: Defining minimal structural features in substrates of the H(*)/peptide cotransporter PEPT2 using novel amino acid and dipeptide derivatives. Mol. Pharmacol (2002) 61(1):214–221
- BRAS AP, SITAR DS, AOKI FY: Comparative bioavailability of acyclovir from oral valacyclovir and acyclovir in patients treated for recurrent genital herpes simplex virus infection. Can. j Clin. Pharmacol (2001) 8(4):207–211
- FRIEDRICHSEN GM, CHEN W, BEGTRUP M, LEE CP, SMITH PL, BORCHARDT RT: Synthesis of analogs of 1-valacyclovir and determination of their substrate activity for the oligopeptide transporter in Caco-2 cells. Eur. Pharm. Sci. (2002) 16(1-2):1–13
- RAZONABLE RR, PAYA CV: Valganciclovir for the prevention and treatment of cytomegalovirus disease in immunocompromised hosts. Expert Rev. Anti Infect. Ther. (2004) 2(1):27–41
- UMAPATHY NS, GANAPATHY V, GANAPATHY ME: Transport of amino acid esters and the amino-acid-based prodrug valganciclovir by the amino acid transporter ATB(0,+). Pharm. Res. (2004) 21(7):1303–1310
- HATANAKA T, HARAMURA M, FEI YJ et al.: Transport of amino acid-based prodrugs by the Na*- and Cl() -coupled amino acid transporter ATB0,+ and expression of the transporter in tissues amenable for drug delivery. J. Pharmacol. Exp. Ther. (2004) 308(3):1138–1147
- JAIN R, MAJUMDAR S, NASHED Y, PAL D, MITRA AK: Circumventing P-glycoprotein-mediated cellular efflux of quinidine by prodrug derivatization. Mol Pharm. (2004) 1(4):290–299
- SWAAN PW, HILLGREN KM, SZOKA FC Jr, OIE S: Enhanced transepithelial transport of peptides by conjugation to cholic acid. Bioconjug. Chem. (1997) 8(4):520–525
- KAGEDAHL M, SWAAN PW, REDEMANN CT et al.: Use of the intestinal bile acid transporter for the uptake of cholic acid conjugates with HIV-1 protease inhibitory activity. Pharm. Res. (1997) 14(2):176–180
- MACIAS RI, EL-MIR MY, MONTE MJ, SERRANO MA, GARCIA MJ, MARIN JJ: Cholephilic characteristics of a new cytostatic complex of cisplatin with glycocholate (Bamet-R2). J. Control. Release (1999) 57(2):161–169
- DOMINGUEZ MF, MACIAS RI, IZCO-BASURKO I et al.: Low in vivo toxicity of a novel cisplatin-ursodeoxycholic derivative (Bamet-UD2) with enhanced cytostatic activity versus liver tumors. Pharmacol Exp. Ther. ( 2001) 297(3):1106–1112
- KRAMER W, WESS G, ENHSEN A et al.: Bile acid derived HMG-CoA reductase inhibitors. Biochim. Biophys. Acta (1994) 1227(3):137–154
- WESS G, KRAMER W, HAN XB et al.: Synthesis and biological activity of bile acid-derived HMG-CoA reductase inhibitors. The role of 21-methyl in recognition of HMG-CoA reductase and the ileal bile acid transport system. J. Med. Chem. (1994) 37(20):3240–3246
- CUNDY KC, ANNAMALAI T, BU L et al.:XP13512 R+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: II. Improved oral bioavailability, dose proportionality, and colonic absorption compared with gabapentin in rats and monkeys. J. Pharmacol. Exp. Ther. (2004) 311(1):324–333
- CUNDY KC, BRANCH R, CHERNOV-ROGAN T et al.:XP13512 R+/-)-1-([(alpha-isobutanoyloxyethoxy)carbonyl] aminomethyl)-1-cyclohexane acetic acid], a novel gabapentin prodrug: I. Design, synthesis, enzymatic conversion to gabapentin, and transport by intestinal solute transporters. J. Pharmacol. Exp. Ther. (2004) 311(1):315–323
- MIZUMA T, OHTA K, HAYASHI M, AWAZU S: Intestinal active absorption of sugar-conjugated compounds by glucose transport system: implication of improvement of poorly absorbable drugs. Biochem. Pharmacol. (1992) 43(9):2037–2039
- MIZUMA T, NAGAMINE Y, DOBASHI A, AWAZU S: Factors that cause the beta-anomeric preference of Nei glucose cotransporter for intestinal transport of monosaccharide conjugates. Biochim. Biophys. Acta (1998) 1381(3):340–346
- MIZUMA T, AWAZU S: Intestinal metabolism and transport of alpha-disaccharide conjugates: the role of disaccharidase in the Na/glucose cotransporter-mediated transport. Res. Commun. MoL PathoL Pharmacol. (1998) 100(1):43–52
- OHNISHI T, HIGASHI S, MIZUMA T, AWAZU S: Transport mechanisms of a glycoside, p-nitrophenyl-beta-d-glucopyranoside, across rat small intestinal brush-border membranes. Biochim. Biophys. Acta (1998) 1370(2):192–198
- MIZUMA T, SAKAI N, HAGI K, AWAZU S: Transport and recognition of aminopeptidase-resistant cellobiose-coupled tyrosylglycylglycine by intestinal Nei glucose cotransporter (SGLT1): recognition of sugar conjugates by SGLT1 is much less restricted than transport. Biol. Pharm. Bull. (1999) 22(8):876–879
- MIZUMAT MASUBUCHI S, AWAZU S: Intestinal absorption of acyclovir beta-glucoside: comparative study with acyclovir, guanosine, and kinetin beta-glucoside. Pharm. Res. (1999) 16(1):69–73
- MIZUMA T, HAGI K, AWAZU S: Intestinal transport of beta-thioglycosides by Na/glucose cotransporter. j Pharm. Pharmacol. (2000) 52(3):303–310
- KOBAYASHI D, NOZAWA T, IMAI K, NEZU J, TSUJI A, TAMAI I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J. Pharmacol. Exp. Ther. (2003) 306(2):703–708
- ZHANG EY, KNIPP GT, EKINS S, SWAAN PW: Structural biology and function of solute transporters: implications for identifying and designing substrates. Drug Metab. Rev. (2002) 34(4):709–750
- ZHANG EY, PHELPS MA, CHENG C, EKINS S, SWAAN PW: Modeling of active transport systems. Adv. Drug Deliv. Rev. (2002) 54(3):329–354
- BRODIN B, NIELSEN CU, STEFFANSEN B, FROKJAER S: Transport of peptidomimetic drugs by the intestinal Di/tri-peptide transporter, PepTl. Pharmacol. lbxicoL (2002) 90(6):285–296
- CHU XY, SANCHEZ-CASTANO GP, HIGAKI K, OH DM, HSU CP, AMIDON GL: Correlation between epithelial cell permeability of cephalexin and expression of intestinal oligopeptide transporter. J. Pharmacol. Exp. Ther. (2001) 299(2):575–582
- NIELSEN CU, BRODIN B: Di/tri-peptide transporters as drug delivery targets: regulation of transport under physiological and patho-physiological conditions. Curr. Drug Targets (2003) 4(5):373–388
- YUASA H, AMIDON GL, FLEISHER D: Peptide carrier-mediated transport in intestinal brush border membrane vesicles of rats and rabbits: cephradine uptake and inhibition. Pharm. Res. (1993) 10(3):400–404
- BALIMANE P, SINKO P: Effect of ionization on the variable uptake of valacyclovir via the human intestinal peptide transporter (hPepT1) in CHO cells. Biopharm. Drug Dispos. (2000) 21(5):165–174
- NOZAWA T, TOYOBUKU H, KOBAYASHI D, KURUMA K, TSUJI A, TAMAI I: Enhanced intestinal absorption of drugs by activation of peptide transporter PEPT1 using proton-releasing polymer. Pharm. Sci. (2003) 92(11):2208–2216
- OKAMURA M, TERADA T, KATSURAT, SAITO H, INUI K: Inhibitory effect of zinc on PEPT1-mediated transport of glycylsarcosine and beta-lactam antibiotics in human intestinal cell line Caco-2. Pharm. Res. (2003) 20(9):1389–1393
- BERLIOZ F, MAORET JJ, PARIS H, LABURTHE M, FARINOTTI R, ROZE C: Alpha(2)-adrenergic receptors stimulate oligopeptide transport in a human intestinal cell line. J. Pharmacol. Exp. Ther. (2000) 294(2):466–472
- WATANABE K, JINRIKI T, SATO J: Effects of progesterone and norethisterone on cephalexin uptake in the human intestinal cell line Caco-2. Biol. Pharm. Bull. (2004) 27(4):559–563
- KUSUHARA H, SUGIYAMA Y: Role of transporters in the tissue-selective distribution and elimination of drugs: transporters in the liver, small intestine, brain and kidney. J. Control. Release (2002) 78(1-3):43–54
- WERDENBERG D, JOSHI R, WOLFFRAM S, MERKLE HP, LANGGUTH P: Presystemic metabolism and intestinal absorption of antipsoriatic fitmaric acid esters. Biopharm. Drug Dispos. (2003) 24(6):259–273
- TALENS-VISCONTI R, GARRIGUES TM, CANTON E, FREIXAS J, MARTIN-VILLODRE A. PLA-DELFINA JM: Activity-bioavailability balance in oral drug development for a selected group of 6-fluoroquinolones. Pharm. Sci. (2002) 91(11):2452–2464
- CLARK RD, WOLOHAN PR: Molecular design and bioavailability. Curr. Top. Med. Chem. (2003) 3(11):1269–1288
- HURYN DM, KONRADI AW, ASHWELL S et al.: The identification and optimization of orally efficacious, small molecule VLA-4 antagonists. Curr. Top. Med. Chem. (2004) 4(14):1473–1484
- MEUNIER V, BOURRIE M, BERGER Y, FABRE G: The human intestinal epithelial cell line Caco-2; pharmacological and pharmacokinetic applications. Cell BioL ToxicoL (1995) 11(3–4):187-194.
- KANSY M, SENNER F, GUBERNATOR K: Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J. Med. Chem. (1998) 41(7):1007–1010
- NORRIS DA, LEESMAN GD, SINKO PJ, GRASS GM: Development of predictive pharmacokinetic simulation models for drug discovery. J. ControL Release (2000) 65(1-2):55–62
- ROBERTS SA: High-throughput screening approaches for investigating drug metabolism and pharmacokinetics. Xenobiotica (2001) 31(8-9):557–589
- CALD WELL GW, RITCHIE DM, MASUCCI JA, HAGEMAN W, YAN Z: The new pre-preclinical paradigm: compound optimization in early and late phase drug discovery. Curr. Top. Med. Chem. (2001) 1(5):353–366
- KARIV I, ROURICK RA, KASSEL DB, CHUNG TD: Improvement of "hit-to-lead" optimization by integration of in vitro HTS experimental models for early determination of pharmacokinetic properties. Comb. Chem. High Throughput Screen. (2002) 5(6):459–472
- SELICK HE, BERESFORD AP TARBIT MH: The emerging importance of predictive ADME simulation in drug discovery. Drug Discov. Today (2002) 7(2):109–116
- EGAN WJ, LAURI G: Prediction of intestinal permeability. Adv. Drug Deliv. Rev. (2002) 54(3):273–289
- TAVELIN S, TAIPALENSUU J, HALLBOOK F, VELLONEN KS, MOORE V, ARTURSSON P: An improved cell culture model based on 2/4/ Al cell monolayers for studies of intestinal drug transport: characterization of transport routes. Pharm. Res. (2003) 20(3):373–381
- SUN D, YU LX, HUSSAIN Mk WALL DA, SMITH RL, AMIDON GL: In vitro testing of drug absorption for drug 'developability assessment: forming an interface between in vitro preclinical data and clinical outcome. Curr. Opin. Drug Discov. Dev. (2004) 7(1):75–85
- MANOURY PM, BINET JL, ROUSSEAU J, LEFEVRE-BORG F, CAVERO IG: Synthesis of a series of compounds related to betaxolol, a new betal-adrenoceptor antagonist with a pharmacological and pharmacokinetic profile optimized for the treatment of chronic cardiovascular diseases. J. Med. Chem. (1987) 30(6):1003–1011
- FLOYD DM, KIMBALL SD, KRAPCHO J et al.: Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones. J. Med. Chem. (1992) 35(4):756–772
- STJERNLOF P, ELEBRING T, NILSSON J et al.: 6,7,8,9-Tetrahydro-N,N-di-n-propy1-3H-benzindo1-8-amines. Derivatives as potent and orally activeserotonin 5-HT1A receptor agonists. J. Med. Chem. (1994) 37(20):3263–3273
- CAPDEVILLE R, BUCHDUNGER E, ZIMMERMANN J, MATTER A: Glivec (5TI571, imatinib), a rationally developed, targeted anticancer drug. Nat. Rev. Drug Discov. (2002) 1(7):493–502
- STEARNS RA, MILLER RR, TANG W et al.: The pharmacokinetics of a thiazole benzenesulfonamide betao-adrenergic receptor agonist and its analogs in rats, dogs, and monkeys: improving oral bioavailability. Drug Metab. Dispos. (2002) 30(7):771–777
- PRUITT JR, PINTO DJ, GALEMMO RA JR et al.: Discovery of 1-(2-aminomethylpheny1)-3-trifluoromethyl-N- [3-fluoro-24-(aminosulfonyl) [1, 1(t-bipheny1)1-4-yll -1H-pyrazole-5-carboxyam ide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1). J. Med. Chem. (2003) 46(25):5298–5315
- LAM PY, CLARK CG, LI R et al.: Structure-based design of novel guanidine/ benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants. J. Med. Chem. (2003) 46(21):4405–4418
- BIRNER k Pharmacology of oral chemotherapy agents. Clin. J. Oncol Nurs. (2003) 7(6 Suppl.):11–19
- COPPER RD: The carbacephems: a new beta-lactam antibiotic class. Am. J. Med. (1992) 92(6A):25–65
- KUME M, KUBOTA T, KIMURA Y, NAKASHIMIZU H, MOTOKAWA K: Orally active cephalosporins. III. Synthesis and structure-activity relationships of new 3-heterocyclicthiomethylthio-7 beta-[(Z)-2-(2-aminothiazol-4-y1)-2-hydroxyiminoacetamido1-3-cephem-4 - carboxylic acids. J. Antibiot. (1993) 46(2):316–330
- SNYDER NJ, TABAS LB, BERRY DM, DUCKWORTH DC, SPRY DO, DANTZIG AH: Structure-activity relationship of carbacephalosporins and cephalosporins: antibacterial activity and interaction with the intestinal proton-dependent dipeptide transport carrier of Caco-2 cells. Antimicrob. Agents Chemother. (1997) 41(8):1649–1657
- RAEISSI SD, LI J, HIDALGO IJ: The role of an alpha-amino group on FP -dependent transepithelial transport of cephalosporins in Caco-2 cells. J. Pharm. Pharmacol (1999) 51(1):35–40
- YAMAMOTO H, TERASAWA T, NAKAMURA A et al.: Orally active cephalosporins. Part 2: synthesis, structure-activity relationships and oral absorption of cephalosporins having a C-3 pyridyl side chain. Bioorg. Med. Chem. (2000) 8(5):1159–1170
- YAMAMOTO H, EIKYU Y, OKUDA S et al.: Orally active cephalosporins. Part 4: synthesis, structure--activity relationships and oral absorption of novel 3-(4-pyrazolylmethylthio)cephalosporins with various C-7 side chains. Bioorg. Med. Chem. (2002) 10(5):1535–1545
- CHANG C, SWAAN PW, NGO LY, LUM PY, PATIL SD, UNADKAT JD: Molecular requirements of the human nucleoside transporters hCNT1, hCNT2, and hENT1. Mol Pharmacol (2004) 65(3):558–570
- SOLDNER A, CHRISTIANS U, SUSANTO M, WACHER VJ, SILVERMAN JA, BENET LZ: Grapefruit juice activates P-glycoprotein-mediated drug transport. Pharm. Res. (1999) 16(4):478–485
- BENET LZ, CUMMINS CL: The drug efflux-metabolism alliance: biochemical aspects. Adv. Drug Deliv. Rev. (2001) 50\(Suppl. 1):53–S11
- PATEL J, MITRA AK: Strategies to overcome simultaneous P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of drugs. Pharmacogenomics (2001) 2(4):401–415
- WAGNER D, SPAHN-LANGGUTH H, HANAFY A, KOGGEL A, LANGGUTH P: Intestinal drug efflux: formulation and food effects. Adv. Drug Deliv. Rev. (2001) 50\(Suppl. 1):513–531
- SPAHN-LANGGUTH H, LANGGUTH P: Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur. j Pharm. Sci. (2001) 12(4):361–367
- PATRAVALE VB, DATE AA, KULKARNI RM: Nanosuspensions: a promising drug delivery strategy. J. Pharm. Pharmacol (2004) 56(7):827–840
- WASAN KM: Formulation and physiological and biopharmaceutical issues in the development of oral lipid-based drug delivery systems. Drug Dev. Ind. Pharm. (2001) 27(4):267–276
- GURSOY RN, BENITA S: Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed. Pharmacother. (2004) 58(3):173–182
- KAYSER O, OLBRICH C, YARDLEY V, KIDERLEN AF, CROFT SL: Formulation of amphotericin B as nanosuspension for oral administration. Int. J. Pharm. (2003) 254(1):73–75
- RABINOW BE: Nanosuspensions in drug delivery. Nat. Rev. Drug Discov. (2004) 3(9):785–796
- •Comprehensive review of applications of nanosuspensions to oral drug delivery
- RAO GC, KUMAR MS, MATHIVANAN N, RAO ME: Nanosuspensions as the most promising approach in nanoparticulate drug delivery systems. Pharmazie (2004) 59(1)5–9
- WU Y, LOPER A, LANDIS E et al.: The role of biopharmaceutics in the development of a clinical nanoparticle formulation of MK-0869: a Beagle dog model predicts improved bioavailability and diminished food effect on absorption in human. Int. J. Pharm. (2004) 285(1-2):135–146
- CHOWDARY KB KAMALAKARA RG: Controlled release of nifedipine from mucoadhesive tablets of its inclusion complexes with beta-cyclodextrin. Pharmazie (2003) 58(10):721–724
- WESTERBERG G, WIKLUND L: Beta-cyclodextrin reduces bioavailability of orally administered [(3)FI]benzolalpyrene in the rat. J. Pharm. Sci. (2004) 94(1):114–119
- MERISKO-LIVERSIDGE E, LIVERSIDGE GG, COOPER ER: Nanosizing: a formulation approach for poorly-water-soluble compounds. Eur. Pharm. Sci. (2003) 18(2):113–120
- CHAUBAL MV: Application of drug delivery technologies in lead candidate selection and optimization. Drug Discov. Today (2004) 9(14):603–609
- MORISSETTE SL, ALMARSSON O, PETERSON ML et al.: High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids. Adv. Drug Deliv. Rev. (2004) 56(3):275–300
- TFELT-HANSEN P, PAALZOW L, IBRAHEEM JJ: Bioavailability of sublingual ergotamine. Br. J. Clin. Pharmacol (1982) 13(2):239–240
- TAKESHIMA T, NISHIKAWA S, TAKAHASHI K: Sublingual administration of flunarizine for acute migraine: will flunarizine take the place of ergotamine? Headache (1988) 28(9):602–606
- RENOUF L: Sublingual ergotamine in the treatment of migraine. Med. J. Aust. (1990) 153(2):120
- SEAGER H: Drug-delivery products and the Zydis fast-dissolving dosage form. Pharm. Pharmacol (1998) 50(4):375–382
- FARRAR JT, CLEARY J, RAUCK R, BUSCH M, NORDBROCK E: Oral transmucosal fentanyl citrate: randomized, double-blinded, placebo-controlled trial for treatment of breakthrough pain in cancer patients. J. Natl. Cancer Inst. (1998) 90(8):611–616
- SHEPHARD SE, LANGGUTH P, PANIZZON RG: Pharmacokinetic behaviour of sublingually administered 8-methoxypsoralen for PUVA therapy. Photodermatol Photoimmunol Photomed. (2001) 17(1):11–21
- LEHOCZKY O, UDVARY J, PULAY T: Freeze dried ondansetron: first observations with the fast dissolving oral antiemetic Zofran Zydis for the prophylaxis of the cisplatin-induced emesis in gynecological cancer patients. Neop/asma (2002) 49(2):126–128
- CLARKE A. JOHNSON ES, MALLARD N et al.: A new low-dose formulation of selegiline: clinical efficacy, patient preference and selectivity for MAO-B inhibition. J. Neural Transm. (2003) 110(11):1257–1271
- KINON BJ, HILL AL, LIU H, KOLLACK-WALKER S: Olanzapine orally disintegrating tablets in the treatment of acutely ill non-compliant patients with schizophrenia. Int. J. Neuropsychopharmacol. (2003) 6(2):97–102
- CARPAY J, SCHOENEN J, AHMAD F, KINRADE F, BOSWELL D: Efficacy and tolerability of sumatriptan tablets in a fast-disintegrating, rapid-release formulation for the acute treatment of migraine: results of a multicenter, randomized, placebo-controlled study. Clin. Ther. (2004) 26(2):214–223
- WATERS CH, SETHI KD, HAUSER RA, MOLHO E, BERTONI JM: Zydis selegiline reduces off time in Parkinson's disease patients with motor fluctuations: a 3-month, randomized, placebo-controlled study. Mov. Disord. (2004) 19(4):426–432
- ARTURSSON P, LINDMARK T, DAVIS SS, ILLUM L: Effect of chitosan on the permeability of monolayers of intestinal epithelial cells (Caco-2). Pharm. Res. (1994) 11(9):1358–1361
- LINDMARK T, NIKKILA T, ARTURSSON P: Mechanisms of absorption enhancement by medium chain fatty acids in intestinal epithelial Caco-2 cell monolayers. J. Pharmacol Exp. Then (1995) 275(2):958–964
- TOMITA M, HAYASHI M, AWAZU S: Absorption-enhancing mechanism of EDTA, caprate, and decanoylcarnitine in Caco-2 cells. J. Pharm. Sci. (1996) 85(6):608–611
- LINDMARK T, SCHIPPER N, LAZOROVA L, DE BOER AG, ARTURSSON P: Absorption enhancement in intestinal epithelial Caco-2 monolayers by sodium caprate: assessment of molecular weight dependence and demonstration of transport routes./ Drug Target. (1998) 5(3):215–223
- LINDMARK T, KIMURA Y, ARTURSSON P: Absorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells. J. Pharmacol Exp. Ther. (1998) 284(1):362–369
- LIU DZ, LECLUYSE EL, THAKKER DR: Dodecylphosphocholine-mediated enhancement of paracellular permeability and cytotoxicity in Caco-2 cell monolayers. Pharm. Sci. (1999) 88(11):1161–1168
- MINE Y, ZHANG JW: Surfactants enhance the tight-junction permeability of food allergens in human intestinal epithelial Caco-2 cells. Int. Arch. Allergy Immunol. (2003) 130(2):135–142
- ROSS BP, DECRUZ SE, LYNCH TB, DAVIS-GOFF K, TOTH I: Design, synthesis, and evaluation of a liposaccharide drug delivery agent: application to the gastrointestinal absorption of gentamicin. J. Med. Chem. (2004) 47(5):1251–1258
- LEONE-BAY A, LEIPOLD H, SARUBBI D, VARIANO B, RIVERA T, BAUGHMAN RA: Oral delivery of sodium cromolyn: preliminary studies in vivo and in vitro. Pharm. Res. (1996) 13(2):222–226
- DING X, RATH P, ANGELO R et al.: Oral absorption enhancement of cromolyn sodium through non-covalent complexation. Pharm. Res. (2004) 21(12):2196–2206
- SOOD A. Design of controlled release delivery systems using a modified pharmacokinetic approach: a case study for drugs having a short elimination half-life and a narrow therapeutic index. Int. J. Pharm. (2003) 261(1-2):27–41
- PRISANT LM, ELLIOTT WJ: Drug delivery systems for treatment of systemic hypertension. Clin. Pharmacokinet. (2003) 42(10:931–940
- KUBO W, KONNO Y, MIYAZAKI S, ATT WOOD D: In situ gelling pectin formulations for oral sustained delivery of paracetamol. Drug Dev. Ind. Pharm. (2004) 30(0:593–599
- KUBO W, MIYAZAKI S, DAIRAKU M, TOGASHI M, MIKAMI R, ATT WOOD D: Oral sustained delivery of ambroxol from in situ-gelling pectin formulations. Int. j Pharm. (2004) 271(1-2):233–240
- VERMA RK, KRISHNA DM, GARG S: Formulation aspects in the development of osmotically controlled oral drug delivery systems. J. Control. Release (2002) 79(1-3):7–27
- GUPTA KC, RAW KUMAR MN: pH dependent hydrolysis and drug release behavior of chitosan/poly(ethylene glycol) polymer network microspheres. J. Mater. Sci. Mater. Med. (2001) 12(9):753–759
- BERNKOP-SCHNURCH A. REICH-ROHRWIG E, MARSCHUTZ M, SCHUHBAUER H, KRATZEL M: Development of a sustained release dosage form for alpha-lipoic acid. II. Evaluation in human volunteers. Drug Dev. Ind. Pharm. (2004) 30(1):35–42
- SINGH BN, KIM KH: Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J. Control. Release (2000) 63(3):235–259
- HOU SY, COWLES VE, BERNER B: Gastric retentive dosage forms: a review. Crit. Rev. Ther. Drug Carrier Syst. (2003) 20(6):459–497
- •Recent review of gastroretentive dosage forms
- KLAUSNER EA, LAVY E, BARTA M, CSEREPES E, FRIEDMAN M, HOFFMAN A: Novel gastroretentive dosage forms: evaluation of gastroretentivity and its effect on levodopa absorption in humans. Pharm. Res. (2003) 20(9):1466–1473
- UMAMAHESHWARI RB, JAIN S, JAIN NK: A new approach in gastroretentive drug delivery system using cholestyramine. Drug Deliv. (2003) 10(3):151–160
- STREUBEL A. SIEPMANN J, BODMEIER R: Multiple unit gastroretentive drug delivery systems: a new preparation method for low density microparticles. J. Microencapsul. (2003) 20(3):329–347
- KLAUSNER EA, LAVY E, STEPENSKY D et al.: Furosemide pharmacokinetics and pharmacodynamics following gastroretentive dosage form administration to healthy volunteers. J. Clin. Pharmacol. (2003) 43(7):711–720
- KLAUSNER EA, LAVY E, FRIEDMAN M, HOFFMAN A: Expandable gastroretentive dosage forms. J. Control. Release (2003) 90(2):143–162
- ELKHESHEN S, YASSIN AE, ALKHALED F: Per-oral extended-release bioadhesive tablet formulation of verapamil HC1. Boll. Chim. Farm. (2003) 142(5):226–231
- HOFFMAN A, STEPENSKY D, LAVY E, EYAL S, KLAUSNER E, FRIEDMAN M:
- TALUKDER R, FASSIHI R: Gastroretentive delivery systems: hollow beads. Drug Dev. Ind. Pharm. (2004)
- LIPKA E, CRISON J, AMIDON GL: Transmembrane transport of peptide type compounds: prospects for oral delivery. J. Control. Release (1996) 39(2–3):121-129.
- FIX JA: Oral controlled release technology for peptides: status and future prospects. Pharm. Res. (1996) 13(12):1760–1764
- GOMEZ-ORELLANA I, PATON DR: Adavances in the oral delivery of proteins
- GOMEZ-ORELLANA I, PATON DR: Advances in the oral delivery of proteins
- SOOD A, PANCHAGNULA R: Peroral route: an opportunity for protein and peptide drug delivery. Chem. Rev. (2001) 101(11):3275–3303
- •Comprehensive review of approaches for oral delivery of proteins and peptides
- SHAH RB, AHSAN F, KHAN MA: Oral delivery of proteins: progress and prognostication. Crit. Rev. Ther. Drug Carrier Syst. (2002) 19(2):135–169
- LEE HJ: Protein drug oral delivery: the recent progress. Arch. Pharm. Res. (2002) 25(5):572–584
- GOLDBERG M, GOMEZ-ORELLANA I: Challenges for the oral delivery of macromolecules. Nat. Rev. Drug Discov. (2003) 2(4):289–295
- LIU J, PERVIN A, GALLO CM, DESAI UR, VAN GORP CL, LINHARDT RJ: New approaches for the preparation of hydrophobic heparin derivatives. J. Pharm. Sci. (1994) 83(7):1034–1039
- ASADA H, DOUEN T, WAKI M et al.: Absorption characteristics of chemically modified-insulin derivatives with various fatty acids in the small and large intestine. Pharm. Sci. (1995) 84(6):682–687
- LEE Y, NAM JH, SHIN HC, BYUN Y: Conjugation of low-molecular-weight heparin and deoxycholic acid for the development of a new oral anticoagulant agent. Circulation (2001) 104(25):3116–3120
- RUSSELL-JONES GJ, WEST WOOD SW, HABBERFIELD AD: Vitamin B12 mediated oral delivery systems for granulocyte-colony stimulating factor and erythropoietin. Bioconjug. Chem. (1995) 6(4):459–465
- RUSSELL-JONES GJ, WEST WOOD SW, FARN WORTH PG, FINDLAY JK, BURGER HG: Synthesis of LHRH antagonists suitable for oral administration via the vitamin B12 uptake system. Bioconjug. Chem. (1995) 6(1):34–42
- SWAAN PW: Recent advances in intestinal macromolecular drug delivery via receptor-mediated transport pathways. Pharm. Res. (1998) 15(0:826–834
- RUSSELL-JONES GJ: Use of vitamin B12 conjugates to deliver protein drugs by the oral route. Crit. Rev. Ther. Drug Carrier Syst. (1998) 15(6):557–586
- ZIV E, LIOR O, KIDRON M: Absorption of protein via the intestinal wall. A quantitative model. Biochem. PharmacoL (1987) 36(7):1035–1039
- ZIV E, KIDRON M, RAZ I et al.: Oral administration of insulin in solid form to nondiabetic and diabetic dogs. J. Pharm. Sci. (1994) 83(6):792-794. gastroretentive drug delivery system using cholestyramine. Drug Deliv. (2003) 10(3):151–160
- SUZUKI A, MORISHITA M, KAJITA M et al.: Enhanced colonic and rectal absorption of insulin using a multiple emulsion containing eicosapentaenoic acid and docosahexaenoic acid. J. Pharm. Sci. (1998) 87(10):1196–1202
- ONUKI Y, MORISHITA M, TAKAYAMA K et al.: In vivo effects of highly purified docosahexaenoic acid on rectal insulin absorption. Int. j Pharm. (2000) 198(2):147–156
- THANOU M, VERHOEF JC, JUNGINGER HE: Oral drug absorption enhancement by chitosan and its derivatives. Adv. Drug Deliv. Rev. (2001) 52(2):117–126
- EAIMTRAKARN S, RAMA PRASAD YV, OHNO T et al.: Absorption enhancing effect of labrasol on the intestinal absorption of insulin in rats. J. Drug Target. (2002) 10(3):255–260
- MALKOV D, ANGELO R, WANG HZ, FLANDERS E, TANG H, GOMEZ-ORELLANA I: Oral delivery of insulin with the Eligen® technology: mechanistic studies. Curs: Drug Deliv. (2005) 2(2):191–197
- MILSTEIN SJ, LEIPOLD H, SARUBBI D et al.: Partially unfolded proteins efficiently penetrate cell membranes--implications for oral drug delivery. J. Control. Release (1998) 53(1-3):259–267
- STOLL BR, LEIPOLD HR, MILSTEIN S, EDWARDS DA: A mechanistic analysis of carrier-mediated oral delivery of protein therapeutics. J. Control. Release (2000) 64(1-3):217–228
- MALKOV D, WANG HZ, DINH S, GOMEZ-ORELLANA I: Pathway of oral absorption of heparin with sodium N48-(2-hydroxybenzoyDamino] caprylate. Pharm. Res. (2002) 19(8):1180–1184
- WEBSTER DE, GAHAN ME, STRUGNELL RA, WESSELINGH SL: Advances in oral vaccine delivery options. Am. J. Drug Deliv. (2003) 1(4):227–240
- SHAKWEH M, PONCHEL G, FATTAL E: Particulate uptake by Peyer's patches: a pathway for drug and vaccine delivery. Expert Opin. Drug Deliv. (2004) 1(1):141–163
- WOODLEY JF: Enzymatic barriers for GI peptide and protein delivery. Crit. Rev. Ther. Drug Carrier Syst. (1994) 11(2–3):61-95.
- BERNKOP-SCHNURCH A: The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins. J. Control. Release (1998) 52(1-2):1–16
- FORAKER AB, WALCZAK RJ, COHEN MH, BOIARSKI TA, GROVE CF, SWAAN PW: Microfabricated porous silicon particles enhance paracellular delivery of insulin across intestinal Caco-2 cell monolayers. Pharm. Res. (2003) 20(1):110–116
- LIU H, TANG R, PAN WS, ZHANG Potential utility of various protease inhibitors for improving the intestinal absorption of insulin in rats. J. Pharm. Pharmacol. (2003) 55(11):1523–1529
- LEHR CM: Bioaclhesion technologies for the delivery of peptide and protein drugs to the gastrointestinal tract. Crit. Rev. Ther. Drug Carrier Syst. (1994) 11(2–3):119-160.
- WOODLEY J: Bioaclhesion: new possibilities for drug administration? Clin. Pharmacokinet. (2001) 40(2):77–84
- BERNKOP-SCHNURCH A, HOFFNER MH, KAFEDJIISKI K: Thiomers for oral delivery of hydrophilic macromolecular drugs. Expert Opin. Drug Deliv. (2004) 1(1):87–98
- WHITEHEAD K, SHEN Z, MITRAGOTRI S: Oral delivery of macromolecules using intestinal patches: applications for insulin delivery. J. Control. Release (2004) 98(1):37–45
- CLEMENT S, STILL JG, KOSUTIC G, MCALLISTER RG: Oral insulin product hexyl-insulin monoconjugate 2 (HIM2) in type 1 diabetes mellitus: the glucose stabilization effects of HIM2. Diabetes Technol Ther. (2002) 4(4):459–466
- KIPNES M, DANDONA P, TRIPATHY D, STILL JG, KOSUTIC G: Control of postprandial plasma glucose by an oral insulin product (HIM2) in patients with type 2 diabetes. Diabetes Care (2003) 26(2):421–426
- WAJCBERG E, MIYAZAKI Y, TRIPLITT C, CERSOSIMO E, DEFRONZO RA: Dose-response effect of a single administration of oral hexyl-insulin monoconjugate 2 in healthy nondiabetic subjects. Diabetes Care (2004) 27(12):2868–2873
- CLEMENT S, DANDONA P, STILL JG, KOSUTIC G: Oral modified insulin (HIM2) in patients with type 1 diabetes mellitus: results from a Phase I/II clinical trial. Metabolism (2004) 53(1):54–58
- CHIN CM, GUTIERREZ M, STILL JG, KOSUTIC G: Pharmacokinetics of modified oral calcitonin product in healthy volunteers. Pharmacotherapy (2004) 24(8):994–1001
- RAOOF AA, RAMTOOLA Z, MCKENNA B, YU RZ, HARDEE G, GEARY RS: Effect of sodium caprate on the intestinal absorption of two modified antisense oligonucleotides in pigs. Eur. J. Pharm. Sci. (2002) 17(3):131–138
- RAOOF AA, CHIU P, RAMTOOLA Z et al.: Oral bioavailability and multiple dose tolerability of an antisense oligonucleotide tablet formulated with sodium caprate. Pharm. Sci. (2004) 93(6):1431–1439
- NISSAN A, ZIV E, KIDRON M et al.: Intestinal absorption of low molecular weight heparin in animals and human subjects. Haemostasis (2000) 30(5):225–232
- BAUGHMAN RA, KAPOOR SC, AGARWAL RK, KISICKI J, CATELLA-LAWSON F, FITZGERALD GA: Oral delivery of anticoagulant doses of heparin. A randomized, double-blind, controlled study in humans. Circulation (1998) 98(16):1610–1615
- GONZE MD, MANORD JD, LEONE-BAY A et al.: Orally administered heparin for preventing deep venous thrombosis. Am. J. Surg. (1998) 176(2):176–178
- MONEY SR, YORK JW: Development of oral heparin therapy for prophylaxis and treatment of deep venous thrombosis. Cardiovasc. Surg. (2001) 9(3):211–218
- LEONE-BAY A. SATO M, PATON D et al.: Oral delivery of biologically active parathyroid hormone. Pharm. Res. (2001) 18(7):964–970
- PINEO GF, HULL RD, MARDER VJ: Orally active heparin and low-molecular-weight heparin. Curr. Opin. Pulm. Med. (2001) 7(5):344–348
- BUCLIN T, COSMA ROCHAT M, BURCKHARDT P, AZRIA M, ATTINGER M: Bioavailability and biological efficacy of a new oral formulation of salmon calcitonin in healthy volunteers. J. Bone Miner. Res. (2002) 17(8):1478–1485
- BERKOWITZ SD, MARDER VJ, KOSUTIC G, BAUGHMAN RA: Oral heparin administration with a novel drug delivery agent (SNAG) in healthy volunteers and patients undergoing elective total hip arthroplasty. j Thromb. Haemost. (2003) 1(9):1914–1919
- KIDRON M, DINH S, MENACHEM Y et al.: A novel per-oral insulin formulation: proof of concept study in non-diabetic subjects. Diabet. Med. (2004) 21(4):354–357
- PINEO G, HULL R, MARDER V: Oral delivery of heparin: SNAG and related formulations. Best Pract. Res. Clin. Haematol (2004) 17(1):153–160
- TANKO LB, BAGGER YZ, ALEXANDERSEN P et al.: Safety and efficacy of a novel salmon calcitonin (sCT) technology-based oral formulation in healthy postmenopausal women: acute and 3-month effects on biomarkers of bone turnover. J. Bone Miner. Res. (2004) 19(9):1531–1538
- MAJURU S: Advances in the oral delivery of heparin from solid dosage forms using Emisphere's Eligen® oral drug delivery technology. Drug Deliv. Technol (2004) 4(8):84–89
- MEHTA NM: Oral delivery and recombinant production of peptide hormones. Part I: making oral delivery possible. BioPharm International (2004) 7:44–46
- MODI P, MIHIC M, LEWIN A: The evolving role of oral insulin in the treatment of diabetes using a novel RapidMist System. Diabetes Metab. Res. Rev. (2002) 18\(Suppl. 1):S38–S42
- GUEVARA-AGUIRRE J, GUEVARA M, SAAVEDRA J, MIHIC M, MODI P: Beneficial effects of addition of oral spray insulin (Oralin) on insulin secretion and metabolic control in subjects with type 2 diabetes mellitus suboptimally controlled on oral hypoglycemic agents. Diabetes Technol Ther. (2004) 6(1):1–8
- GUTNIAK MK, LARSSON H, HEIBER SJ, JUNESKANS OT, HOLST JJ, AHREN B: Potential therapeutic levels of glucagon-like peptide I achieved in humans by a buccal tablet. Diabetes Care (1996) 19(8):843–848
- GUTNIAK MK, LARSSON H, SANDERS SW, JUNESKANS O, HOLST JJ, AHREN B: GLP-1 tablet in type 2 diabetes in fasting and postprandial conditions. Diabetes Care (1997) 20(12):1874–1879