Abstract

FORMULATION DEVELPOMENT AND OPTIMIZATION OF LORATIDINE TABLETS EMPLOYING SOLID DISPERSIONS IN MCC PH102 AND POLOXAMER188 AS PER 22 FACTORIAL DESIGN

V. Ramesh*, J. Janardhana Gupta, P. Praveen Srikumar, S. Meenakshi,
N. Jyothirmayee, G. Rajeswari and D. Madhavi

ABSTRACT

Loratadine has anti-histamine that reduces the effect of natural chemical histamine in the body. Histamine can produce symptoms of sneezing, itching, watery eyes and runny nose. Loratadine is used to treat sneezing, runny nose, watery eyes haves skin rash, itching & other cold or allergy symptoms. The present investigation concerns the formulation development & optimization of loratadine which after oral regulation or disintegration to enhance the solubility of solution and increase drug bioavailability. The loratadine prescribes anti histamic drug belongs to class-II and BCS classification & exhibit low and variable oral bioavailability due to its poor aqueous solubility. In the present study solid dispersion in microcrystalline cellulose and Poloxamer188 tried alone and in combination to enhance dissolution rate of loratadine in its tablet formulation development. The objective of the present study is to optimize loratadine in its tablet formulation by 22 factorial design using solid dispersions. MCC PH 102 and Poloxamer188 (surfactant) to achieve NLT 85% dissolution in 15 minutes. For optimization of loratadine tablet or 22 factorial design using solid dispersion MCC PH 102 and Poloxamer188 are considered as two factors the two levels of the A (MCC) are 1:1 and 1:5 ratio of Drug:MCC PH 102 at the two levels of factor B (Poloxamer188) are 1% and 5% of drug conent. Four loratadine tablet formulations employing selected combination of two factors i.e. MCC PH 102 and Poloxamer188 as per 22 factorial design were formulated. Solid dispersions of loratadine in combined carries were initially prepared and were used to prepare the tablets. The tablets were prepared by direct compression method and were evaluated. Loratadine tablet formulations LSDFa disintegrated rapidly with in 25 seconds and gave very rapid dissolution of loratadine, 100% in 15 min. The increasing order of dissolution rate (K1) observed with various formulations was LSDFa>LSDFab>LSDFb>LSDF1. The polynomial equation describing the relationship between the response, Y and the variables X1 & X2 based on the observed data was found to be Y= 60.73+37.93(X1)+4.49(X2)-5.83(X1X2). Based on the above polynomial equation, the optimized loratadine tablet formulations with NLT 86.42% dissolution in 15 min could be formulated employing MCC PH 102 at 1: 4.52 ratio of drug : MCC PH 102 , Polaxamer188 at 3% of drug content. The optimized loratadine tablet formulations gave 86.42% of dissolution in 15 min fulfilling the target dissolution set. Hence optimization by 22 factorial design employing solid dispersion MCC PH 102 and Poloxamer 188 could be used to formulate loratadine tablets with the desired dissolution i.e ,,,, NLT 85% and 15 min.

Keywords: Optimization, Loratadine tablets, Factorial design, Solid dispersion, MCC PH102, Poloxamer188.