| Literature DB >> 32059882 |
Sandeep Sarabu1, Venkata Raman Kallakunta2, Suresh Bandari3, Amol Batra4, Vivian Bi5, Thomas Durig6, Feng Zhang7, Michael A Repka8.
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.Entities:
Keywords: Efavirenz; HME; HPMCAS; Nifedipine; Solid dispersions; Supersaturation
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Year: 2020 PMID： 32059882 PMCID： PMC7082948 DOI： 10.1016/j.carbpol.2020.115828
Source DB: PubMed Journal: Carbohydr Polym ISSN： 0144-8617 Impact factor: 9.381