Hypromellose Acetate Succinate Based Amorphous Solid Dispersions Via Hot Melt Extrusion: Effect of Drug Physicochemical Properties

Overview

Journal Carbohydr Polym

Specialty Biochemistry

Date 2020 Feb 16

PMID 32059882

Citations 18

Authors

Sandeep Sarabu

Venkata Raman Kallakunta

Suresh Bandari

Amol Batra

Vivian Bi

Thomas Durig

Feng Zhang

Michael A Repka

Affiliations

Soon will be listed here.

Abstract

In this study, the impact of drug and hydroxypropyl methylcellulose acetate succinate (HPMCAS) grades physicochemical properties on extrusion process, dissolution and stability of the hot melt extruded amorphous solid dispersions (ASDs) of nifedipine and efavirenz was investigated. Incorporation of drugs affected the extrusion temperature required for solid dispersion preparation. Differential scanning calorimetry and powder X-ray diffraction studies confirmed the amorphous conversion of the drugs in the prepared formulations. The amorphous nature of ASDs was unchanged after 3 months of stability testing at 40 °C and 75% relative humidity. The dissolution efficiency of the ASDs was dependent on the log P of the drug. The inhibitory effect of HPMCAS on drug precipitation was dependent on the hydrophobic interactions between drug and polymer, polymer grade, and dose of the drug. The dissolution efficiency and dissolution rate of the ASDs were dependent on the log P of the drug and solubility and hydrophilicity of the polymer grade respectively. The inhibitory effect of HPMCAS on drug precipitation was dependent on the hydrophobic interactions between drug and polymer, polymer grade, and the dissolution dose of the drug.

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