and Assessment of Hydroxypropyl Cellulose As Functional Additive for Enabling Formulations Containing Itraconazole

Overview

Journal Int J Pharm X

Specialty Pharmacology

Date 2021 Apr 14

PMID 33851133

Citations 5

Authors

Rafael D Bachmaier

Marius Monschke

Thilo Faber

Anna K Krome

Yann Pellequer

Edmont Stoyanov

Alf Lamprecht

Karl G Wagner

Affiliations

Soon will be listed here.

Abstract

Using polymers as additives to formulate ternary amorphous solid dispersions (ASDs) has successfully been established to increase the bioavailability of poorly soluble drugs, when one polymer is not able to provide both, stabilizing the drug in the matrix and the supersaturated solution. Therefore, we investigated the influence of low-viscosity hydroxypropyl cellulose (HPC) polymers as an additive in HPMC based ternary ASD formulations made by hot-melt extrusion (HME) on the bioavailability of itraconazole (ITZ). The partitioning potential of the different HPC grades was screened in biphasic supersaturation assays. Solid-state analytics were performed using differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD). The addition of HPCs, especially HPC-UL, resulted in a superior partitioned amount of ITZ in biphasic supersaturation assays. Moreover, the approach in using HPCs as an additive in HPMC based ASDs led to an increase in partitioned ITZ compared to Sporanox® in biorelevant biphasic dissolution studies. The results from the biphasic dissolution experiments correlated well with the studies, which revealed the highest oral bioavailability for the ternary ASD comprising HPC-UL and HPMC.

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