Enhancement of Loperamide Dissolution Rate by Liquisolid Compact Technique.

Kambham Venkateswarlu,Jami Komala Preethi,Kothapalli Bonnoth Chandrasekhar

doi:10.15171/apb.2016.050

Kambham Venkateswarlu, Jami Komala Preethi + Show 1 more

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https://doi.org/10.15171/apb.2016.050

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Abstract

Purpose: The aim of present study was to improve the dissolution rate of poorly soluble drug Loperamide (LPM) by liquisolid compact technique. Methods: Liquisolid compacts of LPM were prepared using Propylene glycol (PG) as a solvent, Avicel pH 102 as carrier, Aerosil as coating material and Sodium Starch Glycolate (SSG) as superdisintegrant. Interactions between the drug and excipients were examined by Fourier Transform Infrared (FTIR) spectroscopy. The dissolution studies for LPM liquisolid formulation, marketed product and pure drug were carried out in pH 1.2 HCl buffer as dissolution media. Results: Results confirmed the absence of chemical interactions between the drug and excipients. From the solubility studies, it was observed the LPM was highly soluble in PG thereby it was selected as a solvent. The dissolution efficiency of LPM at 15 min was increased from 9.99 % for pure drug and 54.57% for marketed product to 86.81% for the tablets prepared by liquisolid compact technique. Stability studies showed no significant change in percent cumulative drug release, hardness, disintegration time, friability and drug content for 3 months. Conclusion: Formulation F2 showed significant increase in dissolution rate compared to the marketed product at pH 1.2 where LPM is largely absorbed. Around 90% of the drug was released from F2 in 30 min compared to the marketed product and it might be due to the increased wetting and surface area of the particles. Hence, the liquisolid compact technique appears to be a promising approach for improving the dissolution rate of poorly soluble drug.

Highlights

The most preferred route of drug administration is oral route due to its ease, patient compliance and low production cost
There are various techniques reported to improve the dissolution of poorly water soluble or water insoluble drugs like microinization,[4,5] complex formation with β-Cyclodextrins,[6] eutectic mixtures,[7] spray drying technique[8] and recently liquisolid technique has shown promise for improved dissolution
Based on the solubility data, Propylene glycol (PG) was selected as a vehicle for LPM

Summary

Introduction

The most preferred route of drug administration is oral route due to its ease, patient compliance and low production cost. The drug must be presented in solution form for absorption through gastro intestinal tract (GIT) when given orally. There are various techniques reported to improve the dissolution of poorly water soluble or water insoluble drugs like microinization,[4,5] complex formation with β-Cyclodextrins,[6] eutectic mixtures,[7] spray drying technique[8] and recently liquisolid technique has shown promise for improved dissolution. The concept behind the liquisolid system was developed from powdered solution technology and it can be used to formulate the liquid medication. In this technique, insoluble or poorly soluble drugs are dispersed or incorporated into suitable non-volatile solvent and converted to dry, free flowing and compressible solids suitable for tableting or encapsulation using carrier and coat materials. The drug LPM comes under BCS class II drugs[11] and has low solubility profile.[10]

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