Development and evaluation of clopidogrel bisulphate buccal patch for treatment of thrombosis

Abstract

Buccal delivery mucoadhesive polymer as their dosage forms should ideally adhere to the mucosa and withstands salivation, tongue movement and swallowing for a significant period of time. Moreover, buccal drug delivery offers a safer method of drug utilization, since drug absorption can be promptly terminated in case of toxicity by removing the dosage form the buccal cavity. It is also possible to administer the drug to patients, who cannot be dosed orally to prevent accidental swallowing. Buccal releases of Clopidogrel bisulphate is enabled so that it can be retained in the oral cavity from desired and localize the dosage form in a specific region and control the release rate of drug. Nine batches of Clopidogrel Bisulphate buccal patches were prepared by using three different polymers (HPMC (ESLV), pectin, sodium alginate). Based on the physico-chemical parameters such as appearance, thickness, tensile strength, uniformity of weight, drug content and in vitro diffusion studies H2, P4, and S8 were selected as best formulation. The FTIR graphs of drugs excipients and formulation showed that there is no extra peak or broadening of peaks were observed and thus it indicates that there is no incompatibility between drug and excipients. From the release kinetic results the r² value of H2 was found to be higher in zero order release kinetics. In case of korsmeyer peppas model the result indicated that release exponent ‘n’ value is 0.45<n>0.89. This indicates that the non fickian type (case – II) diffusion mechanism. The amount of drug released are 97.78% of optimized H2 formulation shows a good release. The H2 formulation was subjected to stability studies for 3 months. At the end of three months the H2 formulation showed no significant changes in appearance, colour, texture and drug content at both the room temperature and 40 ± 2ºC & RH 70 ± 5%. From the results, it may concluded that the buccal patches of H2 containing (HPMC – ESLV) in the ratio of 1:6 achieved the objectives of quick release, within 60 sec and accurate dosing (97.78%). Thus, the present study delivers the drug constantly & slowly demonstrated potentials for rapid absorption can be effective therapy, and patient compliance for the treatment of thrombosis.