Publication Type:

Journal Article

Source:

International Journal of Pharmacy and Technology, Volume 3, Number 2, p.2297-2305 (2011)

URL:

http://www.scopus.com/inward/record.url?eid=2-s2.0-79960136783&partnerID=40&md5=517dab9ee22dd1eee8ef43b122c818fc

Keywords:

animal experiment, animal model, antiinflammatory activity, area under the curve, article, cellulose acetate, clinical effectiveness, controlled study, drug bioavailability, drug blood level, drug dosage form comparison, drug formulation, drug half life, drug release, drug synthesis, drug tissue level, emulsion, ethyl cellulose, eudragit, eudragit rs, female, in vitro study, indometacin, male, maximum plasma concentration, microsphere, nonhuman, particle size, paw edema, polymer, rat, time to maximum plasma concentration

Abstract:

The main objective of any drug therapy is to achieve a desired concentration of the drug in blood or tissue which is therapeutically effective and non-toxic for an extended period of time. The aim of present work is to increase the biological half life and patient compliance of Indomethacin. For that purpose Indomethacin Microspheres were prepared using different polymers by Emulsion Solvent Evaporation Technique. The cumulative percentage drug release for all formulations of Indomethacin microspheres follow first order kinetics and they show increased dissolution rates. The result showed that the cumulative percentage release of Indomethacin from the formulations D:EC:HPMC(1:1:1), D:CE:EuRS100(1:1:1) D:EC:EuRL100(1:1:1), D:CA:EuRL100(1:1:1), D:CA:EuRS100(1:1:1) were 77.4%,78.2%,80.2%,88.74%and 83.5% respectively. Among these formulations D: CA: EuRL100 (1:1:1) shows similar percentage release as that of marketed drug (Indocide SR). Pharmacokinetic studies show that Cmax,tmax,AUC,t1/2 and MRT values of D:EC:EuRS100 and D:CA:EuRL100 formulations were increased compared to the marketed drugs The pharmacodynamic study revealed that anti inflammatory activity was well noticed in the microsphere formulation D:CA:EuRL100(1:1:1) than the marketed sample of Indomethacin and other microspheres formulation. So thereby these formulations have several advantages over the conventional form that the prolongation of drug action, improvement of bioavailability, patient compliance and reduction of gastro intestinal and centrally mediated side effects. In future the invitro-invivo correlation of the prepared formulation has to be done. Clinical evaluation is also under consideration.

Notes:

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Cite this Research Publication

F. Ra Sheeba, Chandran, Lb, Saroj, Sb, Nair, S. Cb, Anju, P. Ga, and Verjina, C. Ua, “Pharmacokinetic, pharmacodynamic and invitro evaluation of the prepared microspheres of indomethacin”, International Journal of Pharmacy and Technology, vol. 3, pp. 2297-2305, 2011.