Home
Resources
Publications
Stabilization of Fenofibrate in Low Molecular Weight Hydroxypropylcellulose Matrices Produced by Hot-Melt Extrusion

Stabilization of Fenofibrate in Low Molecular Weight Hydroxypropylcellulose Matrices Produced by Hot-Melt Extrusion

Weibin Deng, Soumyajit Majumdar, Abhilasha Singh, Sejal Shah, Noorullah Naqvi Mohammed, Seongbong Jo, Elanor Pinto, Divya Tewari, Thomas Durig, Michael A Repka

Drug Dev Ind Pharm. 2013 Feb;39(2):290-8.

PMID: 22524504

Abstract:

The objective of this study was to improve the dissolution rate and to enhance the stability of a poorly water-soluble and low glass-trasition temperature (T(g)) model drug, fenofibrate, in low molecular weight grades of hydroxypropylcellulose matrices produced by hot-melt extrusion (HME). Percent drug loading had a significant effect on the extrudability of the formulations. Dissolution rate of fenofibrate from melt extruded pellets was faster than that of the pure drug (p < 0.05). Incorporation of sugars within the formulation further increased the fenofibrate release rates. Differential scanning calorimetry results revealed that the crystalline drug was converted into an amorphous form during the HME process. Fenofibrate is prone to recrystallization due to its low T(g). Various polymers were evaluated as stabilizing agents among which polyvinylpyrrolidone 17PF and amino methacrylate copolymer exhibited a significant inhibitory effect on fenofibrate recrystallization in the hot-melt extrudates. Subsequently immediate-release fenofibrate tablets were successfully developed and complete drug release was achieved within 5 min. The dissolution profile was comparable to that of a currently marketed formulation. The hot-melt extruded fenofibrate tablets were stable, and exhibited an unchanged drug release profile after 3-month storage at 40°C/75% RH.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP24938167	Amino methacrylate copolymer		24938-16-7	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: