Development And In-Vitro Evaluation of Pantoprazole Sodium cocrystals

Abstract

Pantoprazole is extensively metabolized in the liver and has a total serum clearance of 0.1 l/h/kg, a serum elimination half-life of about 1.1 h, and an apparent volume of distribution of 0.15 L/kg. 98% of pantoprazole is bound to serum proteins. Elimination half-life, clearance, and volume of distribution are independent of the dose. Almost 80% of an oral or intravenous dose is excreted as metabolites in urine; the remainder is found in feces and originates from biliary secretion. The clearance of pantoprazole is only slightly affected by age, with its half-life being approximately 1.25 h in the elderly. Pantoprazole is an acid labile drug that requires protection from degradation in acidic media. Hence, co-crystallization of pantoprazole sodium with appropriate co-formers will inhibit its degradation in acidic medium ensuring fast release in the stomach. The acid-labile drugs for oral administration may also be protected from gastric acidity by inhibiting its degradation upon entering into acidic environment. So, the current approach includes co-crystallization of the provided drug with appropriate co-former which prevents degradation of drug by quick absorption and protects the drug from low pH. Apart from that, the formulations also modulate or control the drug release for an immediate action.
Keywords: Pantoprazole sodium, Co-crystal, solvent drop method, Co-former.