Preparation, characterization and in-Vitro/in-Vivo evaluation of meloxicam extruded pellets with enhanced bioavailability and stability

References

• Emara LH , Emam MF , Taha NF , et al. In-Vitro dissolution study of meloxicam immediate release products using flow through cell (Usp Apparatus 4) under different operational conditions. Int J Pharm Pharm Sci. 2014;6:254–260. https://www.researchgate.net/publication/269222632.
   Google Scholar
• Ochi M , Inoue R , Yamauchi Y , et al. Development of meloxicam salts with improved dissolution and pharmacokinetic behaviors in rats with impaired gastric motility. Pharm Res. 2013;30(2):377–386.
   PubMed Web of Science ®Google Scholar
• Del Tacca M , Colucci R , Fornai M , et al. Efficacy and tolerability of meloxicam, a cox-2 preferential nonsteroidal anti-inflammatory drug. Clin Drug Invest. 2002;22(12):799–818.
   Web of Science ®Google Scholar
• Hughey JR , Keen JM , Brough C , et al. Thermal processing of a poorly water-soluble drug substance exhibiting a high melting point: the utility of KinetiSol® dispersing. Int J Pharm. 2011;419(1-2):222–230.
   PubMed Web of Science ®Google Scholar
• Janssens S , Van den Mooter G. Review: physical chemistry of solid dispersions. J Pharm Pharmacol. 2009;61(12):1571–1586.
   PubMed Web of Science ®Google Scholar
• Hancock BC , Shamblin SL , Zografi G. Molecular mobility of amorphous pharmaceutical solids below their glass transition temperatures. Pharm Res. 1995;12(6):799–806.:1016292416526.
   PubMed Web of Science ®Google Scholar
• Breitenbach J. Melt extrusion: from process to drug delivery technology. Eur J Pharm Biopharm. 2002;54(2):107–117.(02)00061-9.
   PubMed Web of Science ®Google Scholar
• Six K , Berghmans H , Leuner C , et al. Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, part II. Pharm Res. 2003;20(7):1047–1054.:1024414423779.
   PubMed Web of Science ®Google Scholar
• Ghareeb MM , Abdulrasool AA , Hussein AA , et al. Kneading technique for preparation of binary solid dispersion of meloxicam with poloxamer 188. AAPS PharmSciTech. 2009;10(4):1206–1215.
   PubMed Web of Science ®Google Scholar
• Maniruzzaman M , Rana M , Boateng J , et al. Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers. Drug Dev Ind Pharm. 2013;39(2):218–227.
   PubMed Web of Science ®Google Scholar
• Simões MF , Pinto RM , Simões S. Hot-melt extrusion in the pharmaceutical industry: toward filing a new drug application. Drug Discov Today. 2019;24(9):1749–1768.
   PubMed Web of Science ®Google Scholar
• Lee J-Y , Kang W-S , Piao J , et al. Soluplus®/TPGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan. Drug Des Devel Ther. 2015;9:2745–2756.
   PubMed Web of Science ®Google Scholar
• Haser A , Huang S , Listro T , et al. An approach for chemical stability during melt extrusion of a drug substance with a high melting point. Int J Pharm. 2017;524(1-2):55–64.
   PubMed Web of Science ®Google Scholar
• LaFountaine JS , Prasad LK , Brough C , et al. Thermal processing of PVP- and HPMC-Based amorphous solid dispersions. AAPS Pharm Sci Tech. 2016;17(1):120–132.
   PubMed Web of Science ®Google Scholar
• Haser A , Cao T , Lubach JW , et al. In situ salt formation during melt extrusion for improved chemical stability and dissolution performance of a meloxicam-copovidone amorphous solid dispersion. Mol Pharm. 2018;15(3):1226–1237.
   PubMed Web of Science ®Google Scholar
• Crowley MM , Zhang F , Repka MA , et al. Pharmaceutical applications of hot-melt extrusion: part I. Drug Dev Ind Pharm. 2007;33(9):909–926.
   PubMed Web of Science ®Google Scholar
• Brown C , DiNunzio J , Eglesia M , et al. Hot-melt extrusion for solid dispersions: composition and design considerations. In: Shah N. SH , Choi D. , Chokshi H. , Malick A. editor. New York (NY): Springer; 2014. 197–230.
   Google Scholar
• Huang D , Xie Z , Rao Q , et al. Hot melt extrusion of heat-sensitive and high melting point drug: Inhibit the recrystallization of the prepared amorphous drug during extrusion to improve the bioavailability. Int J Pharm. 2019;565:316–324.
   PubMed Web of Science ®Google Scholar
• Sarabu S , Bandari S , Kallakunta VR , et al. An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part II. Expert Opin Drug Deliv. 2019;16(6):567–582.
   PubMed Web of Science ®Google Scholar
• Janssens S , Denivelle S , Rombaut P , et al. Influence of polyethylene glycol chain length on compatibility and release characteristics of ternary solid dispersions of itraconazole in polyethylene glycol/hydroxypropylmethylcellulose 2910 E5 blends. Eur J Pharm Sci. 2008;35(3):203–210.
   PubMed Web of Science ®Google Scholar
• Nagy ZK , Balogh A , Vajna B , et al. Comparison of electrospun and extruded Soluplus®-based solid dosage forms of improved dissolution. J Pharm Sci. 2012;101(1):322–332.
   PubMed Web of Science ®Google Scholar
• Reintjes T. Solubility enhancement with BASF pharma polymers: solubilizer compendium. Ludwigshafen (Germany): BASF;2011.
   Google Scholar
• Djuris J , Nikolakakis I , Ibric S , et al. Preparation of carbamazepine-Soluplus solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting. Eur J Pharm Biopharm. 2013;84(1):228–237.
   PubMed Web of Science ®Google Scholar
• Gupta SS , Parikh T , Meena AK , et al. Effect of carbamazepine on viscoelastic properties and hot melt extrudability of Soluplus ®®. Int J Pharm. 2015;478(1):232–239.
   PubMed Web of Science ®Google Scholar
• Alshahrani SM , Lu W , Park J-B , et al. Stability-enhanced hot-melt extruded amorphous solid dispersions via combinations of Soluplus® and HPMCAS-HF. AAPS PharmSciTech. 2015;16(4):824–834.
   PubMed Web of Science ®Google Scholar
• Zhang Y , Liu Y , Luo Y , et al. Extruded Soluplus/SIM as an oral delivery system: characterization, interactions, in vitro and in vivo evaluations. Drug Deliv. 2016;23(6):1902–1911.
   PubMed Web of Science ®Google Scholar
• Dierickx L , Van Snick B , Monteyne T , et al. Co-extruded solid solutions as immediate release fixed-dose combinations. Eur J Pharm Biopharm. 2014;88(2):502–509.
   PubMed Web of Science ®Google Scholar
• Han SD , Jung SW , Jang SW , et al. Preparation of solid dispersion of dronedarone hydrochloride with Soluplus(®) by hot melt extrusion technique for enhanced drug release. Chem Pharm Bull (Tokyo)). 2015;63(4):295–299.
   PubMed Web of Science ®Google Scholar
• Goddeeris C , Van den Mooter G. Free flowing solid dispersions of the anti-HIV drug UC 781 with Poloxamer 407 and a maximum amount of TPGS 1000: investigating the relationship between physicochemical characteristics and dissolution behaviour. Eur J Pharm Sci. 2008;35(1-2):104–113.
   PubMed Web of Science ®Google Scholar
• Newa M , Bhandari KH , Li DX , et al. Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188. Int J Pharm. 2007;343(1-2):228–237.
   PubMed Web of Science ®Google Scholar
• Ali W , Williams AC , Rawlinson CF. Stochiometrically governed molecular interactions in drug: poloxamer solid dispersions. Int J Pharm. 2010;391(1-2):162–168.
   PubMed Web of Science ®Google Scholar
• Eloy JO , Marchetti JM. Solid dispersions containing ursolic acid in Poloxamer 407 and PEG 6000: A comparative study of fusion and solvent methods. Powder Technol. 2014;253:98–106.
   Web of Science ®Google Scholar
• Hülsmann S , Backensfeld T , Keitel S , et al. Melt extrusion–an alternative method for enhancing the dissolution rate of 17β-estradiol hemihydrate. Eur J Pharmaceut Biopharmaceut. 2000;49(3):237–242.
   PubMed Web of Science ®Google Scholar
• Feng X , Vo A , Patil H , et al. The effects of polymer carrier, hot melt extrusion process and downstream processing parameters on the moisture sorption properties of amorphous solid dispersions. J Pharm Pharmacol. 2016;68(5):692–704.
   PubMed Web of Science ®Google Scholar
• Bley H , Fussnegger B , Bodmeier R. Characterization and stability of solid dispersions based on PEG/polymer blends. Int J Pharm. 2010;390(2):165–173.
   PubMed Web of Science ®Google Scholar
• Taha NF , Emam MF , Emara LH. A novel combination of Soluplus®/Poloxamer for Meloxicam solid dispersions via hot melt extrusion for rapid onset of action. Part 2: comparative bioavailability and IVIVC. Drug Dev Ind Pharm. 2020;46(8):1362–1372.
   PubMed Web of Science ®Google Scholar
• Yang J , Grey K , Doney J. An improved kinetics approach to describe the physical stability of amorphous solid dispersions. Int J Pharm. 2010;384(1-2):24–31.
   PubMed Web of Science ®Google Scholar
• Hsu HY , Harris MT , Toth S , et al. Drop printing of pharmaceuticals: Effect of molecular weight on PEG Coated-Naproxen/PEG3350 Solid Dispersions. AIChE J. 2015;61(2):4502–4508.
   PubMed Web of Science ®Google Scholar
• Emara LH , Emam MF , Taha NF , et al. simple and sensitive HPLC/UV method for determination of meloxicam in human plasma for bioavailability and bioequivalence studies. J App Pharm Sci. 2016;6:012–019.
   Google Scholar
• Khan K , Rhodes CT. Effect of compaction pressure on the dissolution efficiency of some direct compression systems. Pharm Acta Helv. 1972;47:594–607.
   PubMedGoogle Scholar
• Guideline ICH. ICH Guidline. Stability testing of new drug substances and products. Q1A (R2), current step 4. 2003; 1–24.
   Google Scholar
• Moore JW , Flanner HH. Mathematical comparison of dissolution profiles. Pharm Technol. 1996;20:64–74.
   Google Scholar
• U.S. FDA . Dissolution testing of immediate release solid oral dosage forms; guidance for industry; 1997.
   Google Scholar
• U.S. FDA . technical Review Guide; Center For Drug Evaluation And Research (Cder), Guidance For Industry, Analytical Procedures And Methods Validation, Chemistry Manufacturing And Controls Documentation, Draft Guidance; 2001.
   Google Scholar
• Gibaldi M , Perrier D. Pharmacokinetics. 2nd ed. New York: Marcel Dekker Inc.; 1982.
   Google Scholar
• Guidance for Industry: bioavailability and bioequivalence studies for orally administered drug products – general considerations. US Department of Health and Human Services, FDA (2001), Center for Drug Evaluation and Research (CDER), Rockville, MD,USA; 2003. Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070124.pdf. [last accessed 10 March 2013].
   Google Scholar
• Kolter K , Karl M , Gryczke A. Hot-melt extrusion with BASF pharma polymers: extrusion compendium. Ludwigshafen (Germany): BASF SE. 2012.
   Google Scholar
• Leuner C , Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur J Pharmaceut Biopharm. 2000;50(1):47–60.(00)00076-X.
   PubMed Web of Science ®Google Scholar
• Rowe RC , Sheskey PJ , Owen SC. Handbook of pharmaceutical excipients. London: Pharmaceutical press; 2006.
   Google Scholar
• Guns S. Investigation of the applicability of poly (ethyleneglycol-g-vinylalcohol) as a carrier in the formulation of solid dispersions of poorly water-soluble drugs. 2012.
   Google Scholar
• Ramos L , Cavalheiro ÉT. Thermal behavior of loratadine. J Therm Anal Calorim. 2007;87(3):831–834.
   Web of Science ®Google Scholar
• Albu P , Vlase G , Vlase T. TG/DTG/DTA data used to determine the thermal behaviour of pioglitazone. Stud Univ Vasile Goldis Arad Ser Stiint Vietii. 2015;25:55–57.
   Google Scholar
• Jayaramudu T , Raghavendra GM , Varaprasad K , et al. Preparation and characterization of poly (ethylene glycol) stabilized nano silver particles by a mechanochemical assisted ball mill process. J Appl Polym Sci. 2016;133:1–8.
   Web of Science ®Google Scholar
• Han S , Kim C , Kwon D. Thermal/oxidative degradation and stabilization of polyethylene glycol. Polymer. 1997;38(2):317–323.
   Web of Science ®Google Scholar
• Swain RP , Subudhi BB. Effect of semicrystalline copolymers in solid dispersions of pioglitazone hydrochloride: in vitro-in vivo correlation. Drug Dev Ind Pharm. 2019;45(5):775–786.
   PubMed Web of Science ®Google Scholar
• Melian ME , Munguía AB , Faccio R , et al. The impact of solid dispersion on formulation, using confocal micro raman spectroscopy as tool to probe distribution of components. J Pharm Innov. 2018;13(1):58–68.
   Web of Science ®Google Scholar
• Gupta SS , Meena A , Parikh T , et al. Investigation of thermal and viscoelastic properties of polymers relevant to hot melt extrusion-I: Polyvinylpyrrolidone and related polymers. J Excipients and Food Chem. 2016;5:1001.
   Google Scholar
• Nakamichi K , Nakano T , Yasuura H , et al. The role of the kneading paddle and the effects of screw revolution speed and water content on the preparation of solid dispersions using a twin-screw extruder. Int J Pharm. 2002;241(2):203–211.(02)00134-5.
   PubMed Web of Science ®Google Scholar
• Keen JM , Martin C , Machado A , et al. Investigation of process temperature and screw speed on properties of a pharmaceutical solid dispersion using corotating and counter-rotating twin-screw extruders. J Pharm Pharmacol. 2014;66(2):204–217.
   PubMed Web of Science ®Google Scholar
• Noolkar SB , Jadhav NR , Bhende SA , et al. Solid-state characterization and dissolution properties of meloxicam-moringa coagulant-PVP ternary solid dispersions. AAPS PharmSciTech. 2013;14(2):569–577.
   PubMed Web of Science ®Google Scholar
• Etman M , Shekedef M , Nada A , et al. In vitro and in vivo evaluation of tablets containing meloxicam-PEG 6000 ball-milled co-ground mixture. J Appl Pharm Sci. 2017;7:031–039.
   Google Scholar
• Maulvi FA , Dalwadi SJ , Thakkar VT , et al. Improvement of dissolution rate of aceclofenac by solid dispersion technique. Powder Technol. 2011;207(1-3):47–54.
   Web of Science ®Google Scholar
• Mazzobre MF , Aguilera JM , Buera MP. Microscopy and calorimetry as complementary techniques to analyze sugar crystallization from amorphous systems. Carbohydr Res. 2003;338(6):541–548.
   PubMed Web of Science ®Google Scholar
• Yang Y , Ma X , Zhang L , et al. Synthesis and thermotropic liquid crystalline behavior of copolymers containing ether ketone and ester links. Polym J. 2007;39(9):923–927.
   Web of Science ®Google Scholar
• Andrews GP , Abu-Diak O , Kusmanto F , et al. Physicochemical characterization and drug-release properties of celecoxib hot-melt extruded glass solutions. J Pharm Pharmacol. 2010;62(11):1580–1590.
   PubMed Web of Science ®Google Scholar
• Fule RA , Meer TS , Sav AR , et al. Artemether-Soluplus hot-melt extrudate solid dispersion systems for solubility and dissolution rate enhancement with amorphous state characteristics. J Pharm (Cairo). 2013;2013:151432.
   PubMedGoogle Scholar
• Kabanov AV , Batrakova EV , Alakhov VY. Pluronic® block copolymers as novel polymer therapeutics for drug and gene delivery. J Control Release. 2002;82(2-3):189–212.
   PubMed Web of Science ®Google Scholar
• Knopp MM , Nguyen JH , Becker C , et al. Influence of polymer molecular weight on in vitro dissolution behavior and in vivo performance of celecoxib:PVP amorphous solid dispersions. Eur J Pharm Biopharm. 2016;101:145–151.
   PubMed Web of Science ®Google Scholar
• Bae J-W , Kim M-J , Jang C-G , et al. Determination of meloxicam in human plasma using A HPLC method with UV detection and its application to a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2007;859(1):69–73.
   PubMed Web of Science ®Google Scholar
• Bae JW , Choi CI , Jang CG , et al. Effects Of CYP2C9*1/*13 on the pharmacokinetics and pharmacodynamics of meloxicam. Br J Clin Pharmacol. 2011;71(4):550–555.
   PubMed Web of Science ®Google Scholar
• Marcelín‐Jiménez G , Hernández JA , Angeles AP , et al. Bioequivalence evaluation of two brands of meloxicam tablets (promotion® And Mobicox®): pharmacokinetics in a healthy female mexican population. Biopharm Drug Dispos. 2005;26(5):167–171.
   PubMed Web of Science ®Google Scholar
• Wiesner J , De Jager A , Sutherland F , et al. Sensitive and rapid liquid chromatography–tandem mass spectrometry method for the determination of meloxicam in human plasma. J Chromatogr B. 2003;785(1):115–121.
   PubMed Web of Science ®Google Scholar
• Narjes H , Türck D , Busch U , et al. Pharmacokinetics And Tolerability Of Meloxicam After IM Administration. Br J Clin Pharmacol. 1996;41(2):135–139.
   PubMed Web of Science ®Google Scholar