Incorporation of acetaminophen as an active pharmaceutical ingredient into porous lactose

International Journal of Pharmaceutics
Amirali EbrahimiTimothy Langrish

Abstract

A new formulation method for solid dosage forms with drug loadings from 0.65 ± 0.03% to 39 ± 1% (w/w) of acetaminophen (APAP) as a model drug has been presented. The proposed method involves the production of highly-porous lactose with a BET surface area of 20 ± 1 m(2)/g as an excipient using a templating method and the incorporation of drug into the porous structure by adsorption from a solution of the drug in ethanol. Drug deposition inside the carrier particles, rather than being physically distributed between them, eliminated the potential drug/carrier segregation, which resulted in excellent blend uniformities with relative standard deviations of less than 3.5% for all drug formulations. The results of DSC and XRD tests have shown deposition of nanocrystals of APAP inside the nanopores of lactose due the nanoconfinement phenomenon. FTIR spectroscopy has revealed no interaction between the adsorbed drug and the surface of lactose. The final loaded lactose particles had large BET surface areas and high porosities, which significantly increased the crushing strengths of the produced tablets. In vitro release studies in phosphate buffer (pH 5.8) have shown an acceptable delivery performance of 85% APAP release within 7 minutes...Continue Reading

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Citations

Jan 23, 2017·International Journal of Pharmaceutics·Zhe LiYi Feng
Jan 9, 2021·Expert Opinion on Drug Delivery·Prashantkumar K ParmarArvind K Bansal
Jun 3, 2021·Pharmaceutics·Wei-Feng ZhuLiang-Shan Ming

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