Formulation and Evaluation of Floating In-Situ Gel of Nicardipine Hydrochloride

Abstract

The present research work aimed to formulate and evaluate a gastro retentive in situ gelling system of Nicardipine Hydrochloride using Sodium Alginate as gelling polymer, HPMC K100M as release retard polymer, calcium carbonate as a cross-linking agent, and tri-sodium citrate as fluidity enhancer agent to treat hypertension. The mechanism for the floatation was based on ionic cross-linking. Several evaluation tests were carried out for pre and final formulation evaluation. Based on the outcomes white-colored, viscous solution of uniform consistency was obtained. Batch B1 was very well prepared for the ability to control long-term drug release. The drug content was found to be > 97 %, the viscosities were in the acceptable range suitable for swallowing, and pH was found to be in the range of 7.33 – 7.68 which was compatible with oral digestion. Design expert 13 Software was used to derive results of interaction and responses based on the concentration of polymer and statistical analysis. The optimized formulation i.e., Batch B1 (0.6 % w/v and 0.5 % w/v HPMC K100M) showed a slow drug release of 96.44 % up to 12 hours. The best fit model for the drug release followed the Higuchi model which explained that the drug release occurred by the Fiskian mechanism i.e., a combination of both diffusion and erosion. The in-situ gel prepared can ultimately provide prolonged release, enhance the bioavailability of the drug and increase patient compliance.
 Keywords: - In situ gel, Ionic cross linking, Sodium alginate, HPMC K100M, Nicardipine Hydrochloride.

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“…The room temperature storage condition was 298 K and 65% RH and the condition for accelerated stability studies was 313 K temperature at a relative humidity of 348 K stability to be tested for 30 days. [29]…”