Abstract

Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. Orally clopidogrel bisulfate has a short elimination half-life (7-8 h), low oral bioavailability (50 %) undergoes extensive first pass metabolism (85 %) and frequent high doses (75 mg) are required to maintain the therapeutic level as a result. The purpose of this research was formulation and evaluation of transdermal drug delivery system of clopidogrel bisulfate using various polymers such as HPMC and EC by solvent casting technique for improvement of bioavailability of drug and reducing toxic effects. The developed transdermal patches may increase the therapeutic efficacy and reduce toxic effect of clopidogrel bisulfate. The prepared transdermal drug delivery system of clopidogrel bisulfate using different polymers such as HPMC and EC had shown good & promising results for all the evaluated parameters. Based on the in vitro drug release, drug content, weight variation, tensile strength, thickness and folding endurance results formulation F2 was concluded as an optimized formulation which shows its higher percentage of drug release.
 Keyword: Clopidogrel bisulfate; Transdermal patch; TDDS; Solvent evaporation; In vitro drug release

Highlights

  • Quinazolin-4(3H)-one oximes are heterocyclic fused ring systems and are moieties of considerable interest because of the diverse range of their biological properties like anticancer, anti-inflammatory, anticonvulsant, anti hypertensive and antimicrobial activities (Desai et al, 2006)

  • 2-Methyl quinazolin-4(3H)-one oxime (4b): Anthranilic acid treated with excess of acetamide and proceeded

  • Synthesis of metal chloride complexes of quinazolin4(3H)-oneoxime was carried out via Niemantowski reaction followed by oxime formation, which in turn react with metal chlorides like zinc chloride, cobalt chloride or copper chloride in 2:1 ratio

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Summary

INTRODUCTION

Quinazolin-4(3H)-one oximes are heterocyclic fused ring systems and are moieties of considerable interest because of the diverse range of their biological properties like anticancer, anti-inflammatory, anticonvulsant, anti hypertensive and antimicrobial activities (Desai et al, 2006). Considering, the importance of transition metal complexes as active moieties in antibacterial, antitubercular and antileprotic, antiviral and antimalarial activities. Novel oxovanadium complexes with 2methyl-3-(pyridine-2-ylmethyleneamino)quinazolin4(3H)-ones were reported as antimicrobial agents by Prasad et al, 2011. Quinazoline-4-one and 8hydroxyquinoline derivatives were evaluated for antifungal activity and reported by Vashi et al, 2009. In the present paper synthesis, characterization and antibacterial activities of Co (II), Cu(II) and Zn (II) complexes with quinazolin-4(3H)-oneoxime, 2-phenyl quinazolin4(3H)-oneoxime, and 2-methyl quinazolin-4(3H)oneoxime were reported

MATERIALS AND METHODS
RESULTS AND DISCUSSION
CONCLUSION
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