Exploring effect Of Mesoporous Carrier in improving in-vitro performance of Dronedarone HCl Formulation

Abstract

Introduction: Dronedarone HCl, a versatile antiarrhythmic drug for atrial fibrillation, has poor aqueous solubility and dissolution, resulting in less 0ral bi0availability of nearby 4% lacking meal, and rises to 15% with a high-fat meal.

Objectives: This study investigated the complexation of DRN HCl with Montmorillonite (MMT) & SYLOID® 244FP as a mesoporous carrier to increase the solubility and dissolution-rate.

Methods: Physical blends developed using mix them accurately weighed quantity of dronedarone hydrochloride with MMT & SYLOID®244FP in a glass mortar. These complexes were characterized by FTIR, DSC, and P-XRD, showing different properties from the pure drug. The physical mixture was evaluated for solubility study to optimize the ratio. Different type of medium intended for the s0lubility study (buffers of pH1.2, pH4.5, pH6.8 & water) at 37˚C.

Results: The solubility of batch B2 (Drug: MMT,1:2) increased twofold compared to batch B1 (Drug: MMT,1:1), while batch B4 (Drug: Syloid,1:2) showed a onefold increase over batch B3 (Drug: Syloid,1:1). Therefore, Batch B2 was selected for further formulation. The optimized drug: carrier (1:2) ratio was selected, with MMT being a better carrier than syloid. The formulation can be optimized by using factorial design. The optimized mixture's tablet form significantly increases drug release in at pH4.5 and 6.8 compared to standard by using pure drug.

Conclusions: So, the overall results suggest that complex of drug-MMT may be potentially useful in the preparation of novel pharmaceutical formulation containing DRN HCl. Also, this mesoporous carrier can protect the drug at lower pH which is one of the reasons for its limited oral bioavailability.