Multiparticulate drug delivery system of aceclofenac: Development and in vitro studies

G.V. Shavi, U. Nayak, R.K. Averineni, K. Arumugam, S.R. Meka, U. Nayanabhirama, P. Sureshwar

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

The aim of this study was to develop an enteric-coated multiunit dosage form containing aceclofenac, a nonsteroidal anti-inflammatory drug. The pellets were prepared by using extrusion/spheronization method, and the core pellets were coated with a pH-sensitive poly(meth) acrylate copolymer (Eudragit L100-55) to achieve site-specific drug release. The formulated pellets were characterized for percentage yield, size distribution, surface morphology studies, drug content, and flow properties. In vitro dissolution test was used for comparison of drug release profiles of various coated pellets. The practical yield was found to be 90-95%. The particle size of enteric-coated pellets was found to be in the range of 0.59-0.71 mm. The pellets were spherical in shape and surfaces of pellets were found to be rough and showing micropores. Enteric-coated pellets showed good flow properties and in vitro dissolution profile. Dissolution tests were carried out in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the aceclofenac from formulated pellets was established to be minimum in the pH 1.2 (
Original languageEnglish
Pages (from-to)252-258
Number of pages7
JournalDrug Development and Industrial Pharmacy
Volume35
Issue number2
DOIs
Publication statusPublished - 2009

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Drug Delivery Systems
Dissolution
Pharmaceutical Preparations
Dosage Forms
Particle Size
Gastrointestinal Tract
Anti-Inflammatory Agents
Surface morphology
Extrusion
Copolymers
Particle size
aceclofenac
In Vitro Techniques
Drug Liberation

Cite this

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title = "Multiparticulate drug delivery system of aceclofenac: Development and in vitro studies",
abstract = "The aim of this study was to develop an enteric-coated multiunit dosage form containing aceclofenac, a nonsteroidal anti-inflammatory drug. The pellets were prepared by using extrusion/spheronization method, and the core pellets were coated with a pH-sensitive poly(meth) acrylate copolymer (Eudragit L100-55) to achieve site-specific drug release. The formulated pellets were characterized for percentage yield, size distribution, surface morphology studies, drug content, and flow properties. In vitro dissolution test was used for comparison of drug release profiles of various coated pellets. The practical yield was found to be 90-95{\%}. The particle size of enteric-coated pellets was found to be in the range of 0.59-0.71 mm. The pellets were spherical in shape and surfaces of pellets were found to be rough and showing micropores. Enteric-coated pellets showed good flow properties and in vitro dissolution profile. Dissolution tests were carried out in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the aceclofenac from formulated pellets was established to be minimum in the pH 1.2 (",
author = "G.V. Shavi and U. Nayak and R.K. Averineni and K. Arumugam and S.R. Meka and U. Nayanabhirama and P. Sureshwar",
note = "Cited By :17 Export Date: 10 November 2017 CODEN: DDIPD Correspondence Address: Meka, S. R.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, India; email: ms.reddy@manipal.edu Chemicals/CAS: aceclofenac, 89796-99-6; eudragit, 24938-16-7, 51822-44-7, 9065-11-6; Acrylic Resins; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac, 15307-86-5; Eudragit L100-55; Tablets, Enteric-Coated; aceclofenac, 89796-99-6 Manufacturers: Lupin Laboratories, India References: Aabakken, L., Olaussen, B., Mowinckel, P., Osnes, M., Gastro-duodenal lesions associated with two different piroxicam formulations. An endoscopic evaluation (1992) Scand. J. Gastroenterol, 27, pp. 1049-1054; Alvarez, L., Concheiro, A., G{\'o}mez-Amoza, J.L., Souto, C., Mart{\'i}nez-Pacheco, R., Effect of microcrystalline cellulose grade and process variables on pellets prepared by extrusion-spheronization (2002) Drug Dev. Ind. Pharm, 28, pp. 451-456; Aulton, M.E., (1990) Pharmaceutics: The Science of dosage form design, 1. , 2 ed, London: Churchill Livingstone; Bando, H., McGinity, J.W., Relationship between drug dissolution and leaching of plasticizer for pellets coated with an aqueous Eudragit{\circledR} S100:L100 dispersion (2006) Int. J. Pharm, 323, pp. 11-17; Bashaiwoldu, F., Abraham, B., Podczeck, J.M.N., The application of non-contact laser profilometry to the determination of permanent structural change induced by compaction of pellets II. Pellets dried by different techniques (2004) Eur. J. Pharm. Sci, 22, pp. 55-61; Chopra, R., Podczeck, F., Newton, J.M., Alderborn, G., The influence of pellet shape and film coating on the filling of pellets hard shell capsules (2002) Eur. J. Pharm. Biopharm, 53, pp. 327-333; Debunne, A., Vervaet, C., Mangelings, D., Remon, J., Compaction of enteric-coated pellets: Influence of formulation and process parameters on tablet properties and in vivo evaluation (2004) Eur. J. Pharm. Sci, 22, pp. 305-314; Hu, L., Liu, Y., Tang, X., Zhan, Q., Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets (2006) Eur. J. Pharm. Biopharm, 64, pp. 185-192; Huyghebaert, N., Vermeire, A., Rottiers, P., Remaut, E., Remon, J.P., Development of an enteric-coated, layered multi-particulate formulation for ileal delivery of viable recombinant Lactococcus lactis (2005) Eur. J. Pharm. Biopharm, 61, pp. 134-141; Lin, A.Y., Larry, L., Augsburger (2001) AAPS Pharm. Sci, 3 (2), pp. 1-12; Muatlik, S., Usha, A.N., Reddy, M.S., Ranjith, A.K., Pandey, S., Improved bioavailability of aceclofenac from spherical agglomerates: Development, in vitro and preclinical studies (2007) Pak. J. Pharm. Sci, 20 (3), pp. 218-226; Mutalik, S., Anju, P., Manoj, K., Usha, A.N., Enhancement of dissolution rate and bioavailability of aceclofenac: A chitosan-based solvent change approach (2008) Int. J. Pharm, 350 (1-2), pp. 279-290; Pareek, A., Chandanwale, A.S., Oak, J., Jain, U.K., Kapoor, S., Efficacy and safety of aceclofenac in the treatment of osteoarthritis: A randomized double-blind comparative clinical trial versus diclofenac - an indian experience (2006) Curr. Med. Res. Opin, 22 (5), pp. 977-988; Paulsson, M., Singh, S.K., Colloidal and thermal characteristics of concentrated dispersions of polymethacrylate-based latices for aqueous enteric coating (1999) J. Pharm. Sci, 88 (4), pp. 406-411; Rahman, N.U., Yuen, K.H., Eudragit NE40-drug mixed coating system for controlling drug release of core pellets (2005) Drug Dev. Ind. Pharm, 31, pp. 339-347; Rodriguez, E.C., Torrado, J.J., Nikoakakis, I., Torrado, S., Lastres, J.L., Malamataris, S., Micromeritic and packing properties of diclofenac pellets and effets of some formulation varibles (2001) Drug. Dev. Ind. Pharm, 27 (8), pp. 847-855; Shivakumar, H.N., Sarasija, S., Desai, B.G., Design and evaluation of pH sensitive multi-particulate systems for chronotherapeutic delivery of diltiazem hydrochloride (2006) Indian J. Pharm. Sci, 68 (6), pp. 781-787; Sriamornsak, P., Nunthanid, J., Luangtana-anan, M., Puttipipatkhachorn, S., Alginate-based pellets prepared by extrusion/spheronization: A preliminary study on the effect of additive in granulating liquid (2007) Eur. J. Pharm. Biopharm, 67, pp. 227-235; Zheng, W., McGinity, J.W., Influence of eudragit NE 30 d blended with eudragit- l 30 D-55 on the release of phenylpropanolamine hydrochloride from coated pellets (2003) Drug Dev. Ind. Pharm, 29 (3), pp. 357-366",
year = "2009",
doi = "10.1080/03639040802277680",
language = "English",
volume = "35",
pages = "252--258",
journal = "Drug Development and Industrial Pharmacy",
issn = "0363-9045",
publisher = "Informa Healthcare",
number = "2",

}

Multiparticulate drug delivery system of aceclofenac: Development and in vitro studies. / Shavi, G.V.; Nayak, U.; Averineni, R.K.; Arumugam, K.; Meka, S.R.; Nayanabhirama, U.; Sureshwar, P.

In: Drug Development and Industrial Pharmacy, Vol. 35, No. 2, 2009, p. 252-258.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Multiparticulate drug delivery system of aceclofenac: Development and in vitro studies

AU - Shavi, G.V.

AU - Nayak, U.

AU - Averineni, R.K.

AU - Arumugam, K.

AU - Meka, S.R.

AU - Nayanabhirama, U.

AU - Sureshwar, P.

N1 - Cited By :17 Export Date: 10 November 2017 CODEN: DDIPD Correspondence Address: Meka, S. R.; Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, India; email: ms.reddy@manipal.edu Chemicals/CAS: aceclofenac, 89796-99-6; eudragit, 24938-16-7, 51822-44-7, 9065-11-6; Acrylic Resins; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac, 15307-86-5; Eudragit L100-55; Tablets, Enteric-Coated; aceclofenac, 89796-99-6 Manufacturers: Lupin Laboratories, India References: Aabakken, L., Olaussen, B., Mowinckel, P., Osnes, M., Gastro-duodenal lesions associated with two different piroxicam formulations. An endoscopic evaluation (1992) Scand. J. Gastroenterol, 27, pp. 1049-1054; Alvarez, L., Concheiro, A., Gómez-Amoza, J.L., Souto, C., Martínez-Pacheco, R., Effect of microcrystalline cellulose grade and process variables on pellets prepared by extrusion-spheronization (2002) Drug Dev. Ind. Pharm, 28, pp. 451-456; Aulton, M.E., (1990) Pharmaceutics: The Science of dosage form design, 1. , 2 ed, London: Churchill Livingstone; Bando, H., McGinity, J.W., Relationship between drug dissolution and leaching of plasticizer for pellets coated with an aqueous Eudragit® S100:L100 dispersion (2006) Int. J. Pharm, 323, pp. 11-17; Bashaiwoldu, F., Abraham, B., Podczeck, J.M.N., The application of non-contact laser profilometry to the determination of permanent structural change induced by compaction of pellets II. Pellets dried by different techniques (2004) Eur. J. Pharm. Sci, 22, pp. 55-61; Chopra, R., Podczeck, F., Newton, J.M., Alderborn, G., The influence of pellet shape and film coating on the filling of pellets hard shell capsules (2002) Eur. J. Pharm. Biopharm, 53, pp. 327-333; Debunne, A., Vervaet, C., Mangelings, D., Remon, J., Compaction of enteric-coated pellets: Influence of formulation and process parameters on tablet properties and in vivo evaluation (2004) Eur. J. Pharm. Sci, 22, pp. 305-314; Hu, L., Liu, Y., Tang, X., Zhan, Q., Preparation and in vitro/in vivo evaluation of sustained-release metformin hydrochloride pellets (2006) Eur. J. Pharm. Biopharm, 64, pp. 185-192; Huyghebaert, N., Vermeire, A., Rottiers, P., Remaut, E., Remon, J.P., Development of an enteric-coated, layered multi-particulate formulation for ileal delivery of viable recombinant Lactococcus lactis (2005) Eur. J. Pharm. Biopharm, 61, pp. 134-141; Lin, A.Y., Larry, L., Augsburger (2001) AAPS Pharm. Sci, 3 (2), pp. 1-12; Muatlik, S., Usha, A.N., Reddy, M.S., Ranjith, A.K., Pandey, S., Improved bioavailability of aceclofenac from spherical agglomerates: Development, in vitro and preclinical studies (2007) Pak. J. Pharm. Sci, 20 (3), pp. 218-226; Mutalik, S., Anju, P., Manoj, K., Usha, A.N., Enhancement of dissolution rate and bioavailability of aceclofenac: A chitosan-based solvent change approach (2008) Int. J. Pharm, 350 (1-2), pp. 279-290; Pareek, A., Chandanwale, A.S., Oak, J., Jain, U.K., Kapoor, S., Efficacy and safety of aceclofenac in the treatment of osteoarthritis: A randomized double-blind comparative clinical trial versus diclofenac - an indian experience (2006) Curr. Med. Res. Opin, 22 (5), pp. 977-988; Paulsson, M., Singh, S.K., Colloidal and thermal characteristics of concentrated dispersions of polymethacrylate-based latices for aqueous enteric coating (1999) J. Pharm. Sci, 88 (4), pp. 406-411; Rahman, N.U., Yuen, K.H., Eudragit NE40-drug mixed coating system for controlling drug release of core pellets (2005) Drug Dev. Ind. Pharm, 31, pp. 339-347; Rodriguez, E.C., Torrado, J.J., Nikoakakis, I., Torrado, S., Lastres, J.L., Malamataris, S., Micromeritic and packing properties of diclofenac pellets and effets of some formulation varibles (2001) Drug. Dev. Ind. Pharm, 27 (8), pp. 847-855; Shivakumar, H.N., Sarasija, S., Desai, B.G., Design and evaluation of pH sensitive multi-particulate systems for chronotherapeutic delivery of diltiazem hydrochloride (2006) Indian J. Pharm. Sci, 68 (6), pp. 781-787; Sriamornsak, P., Nunthanid, J., Luangtana-anan, M., Puttipipatkhachorn, S., Alginate-based pellets prepared by extrusion/spheronization: A preliminary study on the effect of additive in granulating liquid (2007) Eur. J. Pharm. Biopharm, 67, pp. 227-235; Zheng, W., McGinity, J.W., Influence of eudragit NE 30 d blended with eudragit- l 30 D-55 on the release of phenylpropanolamine hydrochloride from coated pellets (2003) Drug Dev. Ind. Pharm, 29 (3), pp. 357-366

PY - 2009

Y1 - 2009

N2 - The aim of this study was to develop an enteric-coated multiunit dosage form containing aceclofenac, a nonsteroidal anti-inflammatory drug. The pellets were prepared by using extrusion/spheronization method, and the core pellets were coated with a pH-sensitive poly(meth) acrylate copolymer (Eudragit L100-55) to achieve site-specific drug release. The formulated pellets were characterized for percentage yield, size distribution, surface morphology studies, drug content, and flow properties. In vitro dissolution test was used for comparison of drug release profiles of various coated pellets. The practical yield was found to be 90-95%. The particle size of enteric-coated pellets was found to be in the range of 0.59-0.71 mm. The pellets were spherical in shape and surfaces of pellets were found to be rough and showing micropores. Enteric-coated pellets showed good flow properties and in vitro dissolution profile. Dissolution tests were carried out in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the aceclofenac from formulated pellets was established to be minimum in the pH 1.2 (

AB - The aim of this study was to develop an enteric-coated multiunit dosage form containing aceclofenac, a nonsteroidal anti-inflammatory drug. The pellets were prepared by using extrusion/spheronization method, and the core pellets were coated with a pH-sensitive poly(meth) acrylate copolymer (Eudragit L100-55) to achieve site-specific drug release. The formulated pellets were characterized for percentage yield, size distribution, surface morphology studies, drug content, and flow properties. In vitro dissolution test was used for comparison of drug release profiles of various coated pellets. The practical yield was found to be 90-95%. The particle size of enteric-coated pellets was found to be in the range of 0.59-0.71 mm. The pellets were spherical in shape and surfaces of pellets were found to be rough and showing micropores. Enteric-coated pellets showed good flow properties and in vitro dissolution profile. Dissolution tests were carried out in a USP type II dissolution apparatus in media-simulating pH conditions of the gastrointestinal tract. The release of the aceclofenac from formulated pellets was established to be minimum in the pH 1.2 (

U2 - 10.1080/03639040802277680

DO - 10.1080/03639040802277680

M3 - Article

VL - 35

SP - 252

EP - 258

JO - Drug Development and Industrial Pharmacy

JF - Drug Development and Industrial Pharmacy

SN - 0363-9045

IS - 2

ER -