Optimization and evaluation of immediate release pantoprazole sodium sesquihydrate capsule by buffered macro environment method

Abstract

Pantoprazole sodium inhibits gastric acid secretion through permanent prevention of (H+/K+)-ATPase function in gastric parietal cell. In case of immediate relief from ulcer and related gastrointestinal complications it is necessary to release the drug immediately. But, immediate release of proton pump inhibitors such as pentoprozole causes their degradation in gastric medium due to their acid labile nature. Due to this reason pantoprazole is available in the form of enteric coated tablets. The best approach for increasing drug stability in acidic medium is the incorporation of buffer in formulation. Macro-environment buffering method was used in which the whole gastric fluid is buffered by buffering agents. Pantoprazole immediate release granules were prepared by wet granulation method. Sodium starch glycolate and cross carmellose sodium were used as superdisintegarnts. Optimization of the formulation was done by using 2 3 factorial design on formulation P-8. Amount of sodium starch glycolate (10% and 12%) (X 1 ), amount of PVPK-30 (3.5% and 5%) (X 2 ) and amount of mannitol (45% and 50%) were used as independent variable. Coded values for 2 levels were -1 and +1. Ex vivo permeation study was performed in selected optimized batch using non-everted intestinal sac. The results showed 98.86% release after 30 min. The performance of optimized formulation was compared to the marketed formulation (Pantocid 20mg tablet: Sun Pharmaceutical Industries Ltd.). This article mainly concluded that the macro environmental buffering method can be used for the immediate release of acid labile drug.

Formulation And In-Vitro Evaluation Of Cocrystals Of Pantoprazole Sodium For Immediate Release

“…Model dependent methods are based on different mathematical functions, which describe the release profile. Once a suitable function has been selected, the release profiles are evaluated depending on the derived model parameters [19][20][21]. The data obtained from ex vivo permeation studies were plotted in different models of data treatment as follows; Zero Order model, First Order model, Higuchi"s Model and Korsmeyer-Peppas model.…”