Development and Evaluation of Sublingual Tablet of Lercanidipine by Solid Dispersion Method

The purpose of this study was to develop and evaluate a sublingual tablet of lercanidipine hydrochloride for the direct compression method of treating hypertension by using a solid dispersion technique. The dihydropyridine calcium-channel blocker lercanidipine Hydrochloride is used to treat hypertension, Prinz metal’s variant angina, and chronic stable angina pectoris. It can be administered alone or in combination with an angiotensin-converting enzyme inhibitor. The biological half-life of lercanidipine hydrochloride is 8–10hours, and its duration of action is up to 24hours. Because of its first pass metabolism, lercanidipine hydrochloride has a less than 10% oral bioavailability. BCS class II was applied to lercanidipine hydrochloride due to its high permeability and poor solubility. The aforementioned features and attributes render Lercanidipine Hydrochloride a fitting contender for a sublingual tablet created by robust dispersion and integrating Gelucire 50/13. When compared to pure lercanidipine Hydrochloride, the solubility is high when Gelucire 50/13 was used at the highest concentration. This is the first attempt to improve the solubility of pure lercanidipine HCl free base by the use of various solid dispersion methods, including solvent evaporation, fusion, and physical mixing. Lercanidipine HCl kneading solid dispersion, made with Gelucire 50/13 (1:1)., The prepared lercanidipine HCl sublingual tablets prevent first pass metabolism, avoid swallowing-related issues, particularly in elderly patients, and enhance solubility. The tablet disintegrated in 50 seconds, according to the results. Similarly, a dissolution study conducted in vitro revealed 96.68% drug release in 10 minutes. The prepared lercanidipine HCl sublingual tablets containing a complex with Gelucire 50/13 solid dispersion were found to significantly improve patient compliance and bioavailability.