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Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery.
Int J Pharm. 2005 Nov 23; 305(1-2):22-30.IJ

Abstract

The objective of this study was to evaluate the effect of two factors (ratio of Eudragit S100 and Eudragit L100 and the coating level) on indomethacin release from pellets in order to optimize coating formulations for colonic delivery. Coating formulations were designed based on the full factorial design. Two independent variables were the ratio of Eudragit S100:Eudragit L100 (1:4, 1:1 and 1:0) and the level of coating (10%, 15% and 20%, w/w), respectively. The evaluated responses were lag time prior to drug release at pH 6.8 (the time required for drug release up to 2%) and percent of drug release at pH 6.8 in 5h. Polymers were coated onto the pellets containing 20% (w/w) indomethacin, using a fluidized bed coating apparatus. Dissolution test was carried out in media with different pH (1.2, 6.5, 6.8 and 7.2). The dissolution data revealed that the level of coating and the ratio of polymers are very important to achieve optimum formulation. Using responses and resulted statistical equations, optimum formulation consisted of Eudragit S100:L100 in 4:1 ratio and the level of coating (20%) was predicted. Practical results showed that the pellets prepared according to above formulation released no indomethacin at pH 1.2 (simulating stomach pH) and pH 6.5 (simulating proximal part of small intestine pH); drug release was slowly at pH 6.8 (simulating lower part of small intestine pH), but it was fast at pH 7.2 (simulating terminal ileum pH). The results of this study revealed that factorial design is a suitable tool for optimization of coating formulations to achieve colon delivery. It was shown that coating formulation consisted of Eudragit S100:Eudragit L100 in 4:1 ratio at 20% coating level has potential for colonic delivery of indomethacin loaded pellets. The optimized formulation produced dissolution profiles that were close to predicted values.

Authors+Show Affiliations

School of Pharmacy and Pharmaceutical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran. akhgari_a@yahoo.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16236475

Citation

Akhgari, A, et al. "Statistical Optimization of Indomethacin Pellets Coated With pH-dependent Methacrylic Polymers for Possible Colonic Drug Delivery." International Journal of Pharmaceutics, vol. 305, no. 1-2, 2005, pp. 22-30.
Akhgari A, Afrasiabi Garekani H, Sadeghi F, et al. Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery. Int J Pharm. 2005;305(1-2):22-30.
Akhgari, A., Afrasiabi Garekani, H., Sadeghi, F., & Azimaie, M. (2005). Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery. International Journal of Pharmaceutics, 305(1-2), 22-30.
Akhgari A, et al. Statistical Optimization of Indomethacin Pellets Coated With pH-dependent Methacrylic Polymers for Possible Colonic Drug Delivery. Int J Pharm. 2005 Nov 23;305(1-2):22-30. PubMed PMID: 16236475.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Statistical optimization of indomethacin pellets coated with pH-dependent methacrylic polymers for possible colonic drug delivery. AU - Akhgari,A, AU - Afrasiabi Garekani,H, AU - Sadeghi,F, AU - Azimaie,M, Y1 - 2005/10/19/ PY - 2004/11/22/received PY - 2005/05/13/revised PY - 2005/08/17/accepted PY - 2005/10/21/pubmed PY - 2006/3/29/medline PY - 2005/10/21/entrez SP - 22 EP - 30 JF - International journal of pharmaceutics JO - Int J Pharm VL - 305 IS - 1-2 N2 - The objective of this study was to evaluate the effect of two factors (ratio of Eudragit S100 and Eudragit L100 and the coating level) on indomethacin release from pellets in order to optimize coating formulations for colonic delivery. Coating formulations were designed based on the full factorial design. Two independent variables were the ratio of Eudragit S100:Eudragit L100 (1:4, 1:1 and 1:0) and the level of coating (10%, 15% and 20%, w/w), respectively. The evaluated responses were lag time prior to drug release at pH 6.8 (the time required for drug release up to 2%) and percent of drug release at pH 6.8 in 5h. Polymers were coated onto the pellets containing 20% (w/w) indomethacin, using a fluidized bed coating apparatus. Dissolution test was carried out in media with different pH (1.2, 6.5, 6.8 and 7.2). The dissolution data revealed that the level of coating and the ratio of polymers are very important to achieve optimum formulation. Using responses and resulted statistical equations, optimum formulation consisted of Eudragit S100:L100 in 4:1 ratio and the level of coating (20%) was predicted. Practical results showed that the pellets prepared according to above formulation released no indomethacin at pH 1.2 (simulating stomach pH) and pH 6.5 (simulating proximal part of small intestine pH); drug release was slowly at pH 6.8 (simulating lower part of small intestine pH), but it was fast at pH 7.2 (simulating terminal ileum pH). The results of this study revealed that factorial design is a suitable tool for optimization of coating formulations to achieve colon delivery. It was shown that coating formulation consisted of Eudragit S100:Eudragit L100 in 4:1 ratio at 20% coating level has potential for colonic delivery of indomethacin loaded pellets. The optimized formulation produced dissolution profiles that were close to predicted values. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/16236475/Statistical_optimization_of_indomethacin_pellets_coated_with_pH_dependent_methacrylic_polymers_for_possible_colonic_drug_delivery_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(05)00605-8 DB - PRIME DP - Unbound Medicine ER -