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TITLE:

PRECLINICAL PHARMACOKINETIC EVALUATION OF STARCH ACETATE AND CHITOSAN MICROPARTICLES OF GLICLAZIDE

AUTHORS:

P.Veera Lakshmi , K.P.R Chowdary, A.Prameela Rani, S.V.U.M.Prasad

ABSTRACT:

Recently much emphasis is being laid on the development of microparticles because of their potential benefits such as increased bioavailability, reduced risk of systemic toxicity, reduced risk of local irritation and predictable gastric emptying. The preparation and in vitro(drug release) and in vivo Pharmacodynamic evaluation of microparticles of gliclazide using i) starch acetate, a new modified starch and ii) chitosan, a new mucoadhesive polymer are reported earlier. The microparticles prepared using both the polymers exhibited good in vitro controlled release of gliclazide over 12 h and in vivo hypoglycemic effect over longer periods of time following their oral administration. The objective of the present study is preclinical pharmacokinetic evaluation of selected gliclazide microparticles (SAF2 and CHF3) in comparison to gliclazide pure drug in healthy rabbits (n=6). The products were tested orally at a dose equivalent to 3 mg/kg of gliclazide. Plasma gliclazide concentrations were determined by a reported and revalidated HPLC method. The biological half life (t1/2) of gliclazide pure drug estimated was in good agreement with the literature value. The t1/2 of gliclazide was slightly elongated with microparticles. The absorption of Gliclazide was very rapid when administered as pure drug and was slow from both the microparticles tested. Based on (AUC)oα , the relative bioavailability ( BA) of gliclazide from microparticles SAF2 and CHF3 was 85.81 % and 117.14 % respectively when compared to gliclazide pure drug (100%). A good level A correlation was observed between percent drug released (in vitro) and (AUC)oα (in vivo) with both the microparticles. Thus, the results of preclinical pharmacokinetic studies indicated that gliclazide was absorbed slowly from microparticles and the plasma drug concentrations were sustained over longer period of time when compared to gliclazide pure drug. Key Words: Gliclazide, Microparticles, Chitosan, Starch acetate, Preclinical evaluation, Pharmacokinetics.

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