Skip to main content
Erschienen in: Cellulose 6/2013

01.12.2013 | Original Paper

Preparation of hydroxypropylmethyl cellulose-based porous matrix for gastroretentive delivery of gabapentin using the freeze-drying method

verfasst von: Ju-Young Kim, Sang-hyub Kim, Yun-Seok Rhee, Chun-Woong Park, Eun-Seok Park

Erschienen in: Cellulose | Ausgabe 6/2013

Einloggen

Aktivieren Sie unsere intelligente Suche, um passende Fachinhalte oder Patente zu finden.

search-config
loading …

Abstract

The aims of the present study were to prepare hydroxypropylmethyl cellulose (HPMC)-based porous matrix tablets for gastroretentive drug delivery and to characterize their physicochemical properties. Gabapentin (GBP) was used as a model drug. Paste containing GBP, HPMC and water was molded and freeze-dried to prepare freeze-dried gastroretentive matrix tablet (FD-GRT). In vitro drug release and erosion studies were also performed. Although FD-GRT exhibited porous structure, they had good tablet strength and friability. Density of FD-GRT ranged from 0.402 to 0.509 g/cm3 and thus they could float on the medium surface without any lag time. FD-GRT was remained floated until the entire matrix erosion or end of drug release during in vitro release test. Release behavior of GBP could be modulated by the amount and the viscosity grade of HPMC. However, large amount and high viscosity of HPMC caused trouble in molding prior to freeze-drying. Addition of ethylcellulose could retard the release rate of GBP, with relatively low increase in viscosity of paste. Since pores generated by freeze drying imparted buoyancy for gastric retention to FD-GRT, additional materials for buoyancy was not necessary and FD-GRT had no lag time for buoyancy due to low density. Therefore it could be a promising tool for gastroretentive drug delivery.

Sie haben noch keine Lizenz? Dann Informieren Sie sich jetzt über unsere Produkte:

Springer Professional "Technik"

Online-Abonnement

Mit Springer Professional "Technik" erhalten Sie Zugriff auf:

  • über 67.000 Bücher
  • über 390 Zeitschriften

aus folgenden Fachgebieten:

  • Automobil + Motoren
  • Bauwesen + Immobilien
  • Business IT + Informatik
  • Elektrotechnik + Elektronik
  • Energie + Nachhaltigkeit
  • Maschinenbau + Werkstoffe




 

Jetzt Wissensvorsprung sichern!

Springer Professional "Wirtschaft+Technik"

Online-Abonnement

Mit Springer Professional "Wirtschaft+Technik" erhalten Sie Zugriff auf:

  • über 102.000 Bücher
  • über 537 Zeitschriften

aus folgenden Fachgebieten:

  • Automobil + Motoren
  • Bauwesen + Immobilien
  • Business IT + Informatik
  • Elektrotechnik + Elektronik
  • Energie + Nachhaltigkeit
  • Finance + Banking
  • Management + Führung
  • Marketing + Vertrieb
  • Maschinenbau + Werkstoffe
  • Versicherung + Risiko

Jetzt Wissensvorsprung sichern!

Literatur
Zurück zum Zitat Andre V, Fernandes A, Santos PP, Duarte MT (2011) On the track of new multicomponent gabapentin crystal forms: synthon competition and pH stability. Cryst Growth Des 11:2325–2334CrossRef Andre V, Fernandes A, Santos PP, Duarte MT (2011) On the track of new multicomponent gabapentin crystal forms: synthon competition and pH stability. Cryst Growth Des 11:2325–2334CrossRef
Zurück zum Zitat Arora S, Ali J, Ahuja A, Khar RK, Baboota S (2005) Floating drug delivery systems: a review. AAPS PharmSciTech 6:E372–E390CrossRef Arora S, Ali J, Ahuja A, Khar RK, Baboota S (2005) Floating drug delivery systems: a review. AAPS PharmSciTech 6:E372–E390CrossRef
Zurück zum Zitat Baki G, Bajdik J, Pintye-Hodi K (2011) Evaluation of powder mixtures and hydrophilic gastroretentive drug delivery systems containing zinc acetate and sodium bicarbonate. J Pharm Biomed Anal 54:711–716CrossRef Baki G, Bajdik J, Pintye-Hodi K (2011) Evaluation of powder mixtures and hydrophilic gastroretentive drug delivery systems containing zinc acetate and sodium bicarbonate. J Pharm Biomed Anal 54:711–716CrossRef
Zurück zum Zitat Braga D, Grepioni F, Maini L, Rubini K, Polito M, Brescello R, Cotarca L, Duarte MT, Andre V, Piedade MFM (2008) Polymorphic gabapentin: thermal behaviour, reactivity and interconversion of forms in solution and solid-state. New J Chem 32:1788–1795CrossRef Braga D, Grepioni F, Maini L, Rubini K, Polito M, Brescello R, Cotarca L, Duarte MT, Andre V, Piedade MFM (2008) Polymorphic gabapentin: thermal behaviour, reactivity and interconversion of forms in solution and solid-state. New J Chem 32:1788–1795CrossRef
Zurück zum Zitat Chimatadar SA, Basavaraj T, Thabaj KA, Nandibewoor ST (2007) Ruthenium(III) catalysed oxidation of gabapentin (neurontin) by diperiodatocuprate(III) in aqueous alkaline medium: a kinetic and mechanistic study. J Mol Catal A Chem 267:65–71CrossRef Chimatadar SA, Basavaraj T, Thabaj KA, Nandibewoor ST (2007) Ruthenium(III) catalysed oxidation of gabapentin (neurontin) by diperiodatocuprate(III) in aqueous alkaline medium: a kinetic and mechanistic study. J Mol Catal A Chem 267:65–71CrossRef
Zurück zum Zitat Costa P, Sousa Lobo JM (2001) Modeling and comparison of dissolution profiles. Eur J Pharm Sci 13:123–133CrossRef Costa P, Sousa Lobo JM (2001) Modeling and comparison of dissolution profiles. Eur J Pharm Sci 13:123–133CrossRef
Zurück zum Zitat Desai J, Alexander K, Riga A (2006) Characterization of polymeric dispersions of dimenhydrinate in ethyl cellulose for controlled release. Int J Pharm 308:115–123CrossRef Desai J, Alexander K, Riga A (2006) Characterization of polymeric dispersions of dimenhydrinate in ethyl cellulose for controlled release. Int J Pharm 308:115–123CrossRef
Zurück zum Zitat Efentakis M, Koutlis A, Vlachou M (2000) Development and evaluation of oral multiple-unit and single-unit hydrophilic controlled-release systems. AAPS PharmSciTech 1:E34CrossRef Efentakis M, Koutlis A, Vlachou M (2000) Development and evaluation of oral multiple-unit and single-unit hydrophilic controlled-release systems. AAPS PharmSciTech 1:E34CrossRef
Zurück zum Zitat Felix F (2007) Freeze-drying of pharmaceuticals and biopharmaceuticals. RSC Publishing, Cambridge Felix F (2007) Freeze-drying of pharmaceuticals and biopharmaceuticals. RSC Publishing, Cambridge
Zurück zum Zitat Gordi T, Hou E, Kasichayanula S, Berner B (2008) Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive-extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in healthy subjects. Clin Ther 30:909–916CrossRef Gordi T, Hou E, Kasichayanula S, Berner B (2008) Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive-extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in healthy subjects. Clin Ther 30:909–916CrossRef
Zurück zum Zitat Hsu CH, Lin SY (2009) Rapid examination of the kinetic process of intramolecular lactamization of gabapentin using DSC-FTIR. Thermochim Acta 486:5–10CrossRef Hsu CH, Lin SY (2009) Rapid examination of the kinetic process of intramolecular lactamization of gabapentin using DSC-FTIR. Thermochim Acta 486:5–10CrossRef
Zurück zum Zitat Hsu CH, Ke WT, Lin SY (2010) Progressive steps of polymorphic transformation of gabapentin polymorphs studied by hot-stage FTIR microspectroscopy. J Pharm Pharm Sci 13:67–77 Hsu CH, Ke WT, Lin SY (2010) Progressive steps of polymorphic transformation of gabapentin polymorphs studied by hot-stage FTIR microspectroscopy. J Pharm Pharm Sci 13:67–77
Zurück zum Zitat Hutmacher DW (2000) Scaffolds in tissue engineering bone and cartilage. Biomaterials 21:2529–2543CrossRef Hutmacher DW (2000) Scaffolds in tissue engineering bone and cartilage. Biomaterials 21:2529–2543CrossRef
Zurück zum Zitat Katikaneni PR, Upadrashta SM, Neau SH, Mitra AK (1995) Ethylcellulose matrix controlled-release tablets of a water-soluble drug. Int J Pharmaceut 123:119–125CrossRef Katikaneni PR, Upadrashta SM, Neau SH, Mitra AK (1995) Ethylcellulose matrix controlled-release tablets of a water-soluble drug. Int J Pharmaceut 123:119–125CrossRef
Zurück zum Zitat Khan GM, Meidan VM (2007) Drug release kinetics from tablet matrices based upon ethylcellulose ether-derivatives: a comparison between different formulations. Drug Dev Ind Pharm 33:627–639CrossRef Khan GM, Meidan VM (2007) Drug release kinetics from tablet matrices based upon ethylcellulose ether-derivatives: a comparison between different formulations. Drug Dev Ind Pharm 33:627–639CrossRef
Zurück zum Zitat Klausner EA, Lavy E, Friedman M, Hoffman A (2003) Expandable gastroretentive dosage forms. J Control Release 90:143–162CrossRef Klausner EA, Lavy E, Friedman M, Hoffman A (2003) Expandable gastroretentive dosage forms. J Control Release 90:143–162CrossRef
Zurück zum Zitat Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA (1983) Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 15:25–35CrossRef Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA (1983) Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 15:25–35CrossRef
Zurück zum Zitat Lin SY, Hsu CH, Ke WT (2010) Solid-state transformation of different gabapentin polymorphs upon milling and co-milling. Int J Pharm 396:83–90CrossRef Lin SY, Hsu CH, Ke WT (2010) Solid-state transformation of different gabapentin polymorphs upon milling and co-milling. Int J Pharm 396:83–90CrossRef
Zurück zum Zitat Lingam M, Ashok T, Venkateswarlu V, Rao YM (2008) Design and evaluation of a novel matrix type multiple units as biphasic gastroretentive drug delivery systems. AAPS PharmSciTech 9:1253–1261CrossRef Lingam M, Ashok T, Venkateswarlu V, Rao YM (2008) Design and evaluation of a novel matrix type multiple units as biphasic gastroretentive drug delivery systems. AAPS PharmSciTech 9:1253–1261CrossRef
Zurück zum Zitat Murphy CS, Pillay V, Choonara YE, du Toit LC (2009) Gastroretentive drug delivery systems: current developments in novel system design and evaluation. Curr Drug Deliv 6:451–460CrossRef Murphy CS, Pillay V, Choonara YE, du Toit LC (2009) Gastroretentive drug delivery systems: current developments in novel system design and evaluation. Curr Drug Deliv 6:451–460CrossRef
Zurück zum Zitat Nunthanid J, Luangtana-anan M, Sriamornsak P, Limmatvapirat S, Huanbutta K, Puttipipatkhachorn S (2009) Use of spray-dried chitosan acetate and ethylcellulose as compression coats for colonic drug delivery: effect of swelling on triggering in vitro drug release. Eur J Pharm Biopharm 71:356–361CrossRef Nunthanid J, Luangtana-anan M, Sriamornsak P, Limmatvapirat S, Huanbutta K, Puttipipatkhachorn S (2009) Use of spray-dried chitosan acetate and ethylcellulose as compression coats for colonic drug delivery: effect of swelling on triggering in vitro drug release. Eur J Pharm Biopharm 71:356–361CrossRef
Zurück zum Zitat Quinten T, De Beer T, Onofre FO, Mendez-Montealvo G, Wang YJ, Remon JP, Vervaet C (2011) Sustained-release and swelling characteristics of xanthan gum/ethylcellulose-based injection moulded matrix tablets: in vitro and in vivo evaluation. J Pharm Sci 100:2858–2870CrossRef Quinten T, De Beer T, Onofre FO, Mendez-Montealvo G, Wang YJ, Remon JP, Vervaet C (2011) Sustained-release and swelling characteristics of xanthan gum/ethylcellulose-based injection moulded matrix tablets: in vitro and in vivo evaluation. J Pharm Sci 100:2858–2870CrossRef
Zurück zum Zitat Rajinikanth PS, Balasubramaniam J, Mishra B (2007) Development and evaluation of a novel floating in situ gelling system of amoxicillin for eradication of Helicobacter pylori. Int J Pharmaceut 335:114–122CrossRef Rajinikanth PS, Balasubramaniam J, Mishra B (2007) Development and evaluation of a novel floating in situ gelling system of amoxicillin for eradication of Helicobacter pylori. Int J Pharmaceut 335:114–122CrossRef
Zurück zum Zitat Ravindra R, Rao AK, Khan AA (1999) A qualitative evaluation of water and monomethyl hydrazine in ethylcellulose membrane. J Appl Polym Sci 72:689–700CrossRef Ravindra R, Rao AK, Khan AA (1999) A qualitative evaluation of water and monomethyl hydrazine in ethylcellulose membrane. J Appl Polym Sci 72:689–700CrossRef
Zurück zum Zitat Rhee YS, Park S, Lee TW, Park CW, Nam TY, Oh TO, Jeon JW, Han SB, Lee DS, Park ES (2008) In vitro/in vivo relationship of gabapentin from a sustained-release tablet formulation: a pharmacokinetic study in the beagle dog. Arch Pharmacal Res 31:911–917CrossRef Rhee YS, Park S, Lee TW, Park CW, Nam TY, Oh TO, Jeon JW, Han SB, Lee DS, Park ES (2008) In vitro/in vivo relationship of gabapentin from a sustained-release tablet formulation: a pharmacokinetic study in the beagle dog. Arch Pharmacal Res 31:911–917CrossRef
Zurück zum Zitat Ritger PL, Peppas NA (1987) A simple equation for description of solute release I. Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J Control Release 5:23–36CrossRef Ritger PL, Peppas NA (1987) A simple equation for description of solute release I. Fickian and non-fickian release from non-swellable devices in the form of slabs, spheres, cylinders or discs. J Control Release 5:23–36CrossRef
Zurück zum Zitat Rowe RC, Sheskey PJ, Owen SC (2006) Handbook of pharmaceutical excipients, 5th edn. Pharmaceutical Press, London, UK Rowe RC, Sheskey PJ, Owen SC (2006) Handbook of pharmaceutical excipients, 5th edn. Pharmaceutical Press, London, UK
Zurück zum Zitat Rujivipat S, Bodmeier R (2010) Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends. Eur J Pharm Biopharm 76:486–492CrossRef Rujivipat S, Bodmeier R (2010) Improved drug delivery to the lower intestinal tract with tablets compression-coated with enteric/nonenteric polymer powder blends. Eur J Pharm Biopharm 76:486–492CrossRef
Zurück zum Zitat Sankalia JM, Sankalia MG, Mashru RC (2008) Drug release and swelling kinetics of directly compressed glipizide sustained-release matrices: establishment of level A IVIVC. J Control Release 129:49–58CrossRef Sankalia JM, Sankalia MG, Mashru RC (2008) Drug release and swelling kinetics of directly compressed glipizide sustained-release matrices: establishment of level A IVIVC. J Control Release 129:49–58CrossRef
Zurück zum Zitat Seager H (1998) Drug-delivery products and the Zydis fast-dissolving dosage form. J Pharm Pharmacol 50:375–382CrossRef Seager H (1998) Drug-delivery products and the Zydis fast-dissolving dosage form. J Pharm Pharmacol 50:375–382CrossRef
Zurück zum Zitat Siepmann J, Peppas NA (2001) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev 48:139–157CrossRef Siepmann J, Peppas NA (2001) Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev 48:139–157CrossRef
Zurück zum Zitat Siepmann J, Kranz H, Bodmeier R, Peppas NA (1999) HPMC-matrices for controlled drug delivery: a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res 16:1748–1756CrossRef Siepmann J, Kranz H, Bodmeier R, Peppas NA (1999) HPMC-matrices for controlled drug delivery: a new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics. Pharm Res 16:1748–1756CrossRef
Zurück zum Zitat Singh BN, Kim KH (2000) Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release 63:235–259CrossRef Singh BN, Kim KH (2000) Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release 63:235–259CrossRef
Zurück zum Zitat Stewart BH, Kugler AR, Thompson PR, Bockbrader HN (1993) A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma. Pharm Res 10:276–281CrossRef Stewart BH, Kugler AR, Thompson PR, Bockbrader HN (1993) A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma. Pharm Res 10:276–281CrossRef
Zurück zum Zitat Streubel A, Siepmann J, Bodmeier R (2006) Gastroretentive drug delivery systems. Expert Opin Drug Deliv 3:217–233CrossRef Streubel A, Siepmann J, Bodmeier R (2006) Gastroretentive drug delivery systems. Expert Opin Drug Deliv 3:217–233CrossRef
Zurück zum Zitat Tang XC, Pikal MJ (2004) Design of freeze-drying processes for pharmaceuticals: practical advice. Pharm Res 21:191–200CrossRef Tang XC, Pikal MJ (2004) Design of freeze-drying processes for pharmaceuticals: practical advice. Pharm Res 21:191–200CrossRef
Zurück zum Zitat Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB (2003) Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech 4:18–23CrossRef Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdary PB (2003) Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech 4:18–23CrossRef
Zurück zum Zitat Toti US, Soppimath KS, Mallikarjuna NN, Aminabhavi TM (2004) Acrylamide-grafted-acacia gum polymer matrix tablets as erosion-controlled drug delivery systems. J Appl Polym Sci 93:2245–2253CrossRef Toti US, Soppimath KS, Mallikarjuna NN, Aminabhavi TM (2004) Acrylamide-grafted-acacia gum polymer matrix tablets as erosion-controlled drug delivery systems. J Appl Polym Sci 93:2245–2253CrossRef
Zurück zum Zitat Uchino H, Kanai Y, Kim DK, Wempe MF, Chairoungdua A, Morimoto E, Anders MW, Endou H (2002) Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition. Mol Pharmacol 61:729–737CrossRef Uchino H, Kanai Y, Kim DK, Wempe MF, Chairoungdua A, Morimoto E, Anders MW, Endou H (2002) Transport of amino acid-related compounds mediated by L-type amino acid transporter 1 (LAT1): insights into the mechanisms of substrate recognition. Mol Pharmacol 61:729–737CrossRef
Zurück zum Zitat USP (2011) US pharmacopeia, 35th edn. The United States Pharmacopeial Convention, Rockville, MD, USA USP (2011) US pharmacopeia, 35th edn. The United States Pharmacopeial Convention, Rockville, MD, USA
Metadaten
Titel
Preparation of hydroxypropylmethyl cellulose-based porous matrix for gastroretentive delivery of gabapentin using the freeze-drying method
verfasst von
Ju-Young Kim
Sang-hyub Kim
Yun-Seok Rhee
Chun-Woong Park
Eun-Seok Park
Publikationsdatum
01.12.2013
Verlag
Springer Netherlands
Erschienen in
Cellulose / Ausgabe 6/2013
Print ISSN: 0969-0239
Elektronische ISSN: 1572-882X
DOI
https://doi.org/10.1007/s10570-013-0048-7

Weitere Artikel der Ausgabe 6/2013

Cellulose 6/2013 Zur Ausgabe