QbD approach for developing Fast-dissolving Tablets containing Loperamide hydrochloride using Super Disintegrant Blends and Subliming Materials

Abstract

Mouth dissolving pills, which dissolve or disintegrate quickly on the tongue or buccal cavity, have been developed in response to the growing demand for more patient-compliant dosage forms. It is utilized to improve bioavailability by reducing dose frequency in order to reduce adverse effects and make tablets with high first-pass metabolism more cost-effective. The most commonly used drug for diarrhoea is loperamide hydrochloride. It is an opioid receptor agonist that targets the mu opioid receptors in the large intestines of the myenteric plexus. It specifically works by lowering myenteric plexus activity, which lowers the motility of the circular and longitudinal smooth muscles of the intestinal wall. It is a synthetic anti-diarrheal that is used to treat the symptoms of inflammatory bowel disease-related chronic diarrhoea as well as acute, non-specific diarrhoea. Due to substantial hepatic first-pass metabolism, loperamide hydrochloride has a very limited systemic bioavailability. Therefore, the primary goal of the study was to develop Loperamide hydrochloride orally disintegrating tablets to obtain a better breakdown rate, enhance the drug's bioavailability, and provide very rapid relief from diarrhoea. The pre-compression parameters, such as bulk density, compressibility, angle of repose, etc., for orally disintegrating tablets manufactured by direct compression and using three super disintegrants, croscarmellose sodium (CCS), Microcrystalline cellulose (MCC), and sodium starch glycolate (SSG), were prepared and assessed. The manufactured batches of tablets passed tests for satisfactory results. The highest amount of medicine was released at all-time intervals in the optimised formulation, which also displayed a favourable release profile.