Formulation Development and Invitro Evaluation of Mouth Dissolving Tablets of Lercanidipine Hydrochloride by Direct Compression Method: An Approach to Improving Oral Bioavailibility

AIM AND OBJECTIVES: • The present study is planned to develop Lercanidipine Hydrochloride into immediate release tablets by direct compression Method. • Lercanidipine Hydrochloride, Lercanidipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. • Lercanidipine Hydrochloride have biological half-life of 8-10 hours and duration of action upto ≥ 24 hours. • Lercanidipine Hydrochloride oral bioavailability is less than 10% due to its first pass metabolism. • Lercanidipine Hydrochloride came under BCS class II having poor solubility and high permeability. • The above said properties/characteristics which make Lercanidipine Hydrochloride suitable candidate for oral dissolving or mouth dissolving tablets. • In this study, we tried to prepare Lercanidipine Hydrochloride MDT by using various types of disintegrants by direct compression method. The present study involves formulation and evaluation of immediate release tablets of Lercandipine Hydrochloride. Endeavours with respect to Direct compression method used for formulating tablets was best suitable to achieve 100% results. Preformulation studies involving organoleptic bulk density, angle of repose, tapped density, compressibility index, hausner ratio, melting point range, pH and solubility were carried out as per USP specifications. Polymers such as CrosPovidone, Croscarmellose Sodium (CCS), Sodium Starch Glycolate (SSG), Starch 1500 were utilized in the trails. All the physical evaluations carried in preformulation studies were carried out on all the four different polymers utilized. All the formulations exhibited values within the acceptable range. Tablets were evaluated for weight variations, hardness, friability, thickness and Dissolution studies. Release studies were carried out in Phosphate buffer, for 30 minutes. Evaluated samples for all the three polymer systems. Results indicated that formulation F12, gave 99.14% release within 8 minutes which is formulated with CrosPovidone alone. Assay was carried out for formulation F12 and was found to be 99.42%. Remaining formulations gave fluctuating release profiles. The formulation F12 was considered to be better among the trails accomplished