Analysis of the Release Process of Phenylpropanolamine Hydrochloride from Ethylcellulose Matrix Granules II. Effects of the Binder Solution on the Release Process

Abstract

The release properties of phenylpropanolamine hydrochloride (PPA) from ethylcellulose (EC) matrix granules prepared by an extrusion granulation method were examined. The release process could be divided into two parts; the first and second stages were analyzed by applying square-root time law and cube-root law equations, respectively. The validity of the treatments was confirmed by the fitness of a simulation curve with the measured curve. In the first stage, PPA was released from the gel layer of swollen EC in the matrix granules. In the second stage, the drug existing below the gel layer dissolved and was released through the gel layer. The effect of the binder solution on the release from EC matrix granules was also examined. The binder solutions were prepared from various EC and ethanol (EtOH) concentrations. The media changed from a good solvent to a poor solvent with decreasing EtOH concentration. The matrix structure changed from loose to compact with increasing EC concentration. The preferable EtOH concentration region was observed when the release process was easily predictable. The time and release ratio at the connection point of the simulation curves were also examined to determine the validity of the analysis.

Analysis of the Release Process of Phenylpropanolamine Hydrochloride from Ethylcellulose Matrix Granules IV.1) Evaluation of the Controlled Release Properties for in Vivo and in Vitro Release Systems

“…1,5,6) Phenylpropanolamine hydrochloride (PPA) (Powder, Alps Pharmaceutical Ind. Co., Ltd., Gifu), ethylcellulose 10 cps (EC) (ETHOCEL STD 10 cps, DOW Chemical, Tokyo), Nonpalel 103 (NP) (Sugar cube, Freund Industrial Co., Ltd., Tokyo), Talc, Polyethylenglycol (PEG), Fe 2 O 3 and 90% ethanol (EtOH) (Wako Pure Chemical Industries, Ltd., Osaka) were used.…”

“…Equipment The equipment described in the previous paper was used. 1,5,6) A high shear granulator (High Speed Mixer, LFS-GS-5, volume 5.0 l, Fukae Ind. Co., Ltd., Hyogo) and extrusion granulator (Granulator machine type of LAB, KAR-130, Tsutsui Physics and Chemistry Apparatus Co., Ltd., Tokyo) were used for granulation.…”

“…2,3) The release properties of the matrix system were mathematically assessed by Higuchi,4) and matrix systems have often been used as a method of controlled drug release; however, it was considered that the mathematical analysis of the release process was insufficient, because the equation can not explain the entire release process. 1,5,6) In previous papers, the release process was divided into two stages to understand the entire release process and these were analyzed using a combination of the square-root time law and cube-root law equations. 1,5,6) It was concluded that predicting drug release properties using this analysis was useful.…”

“…1,5,6) In previous papers, the release process was divided into two stages to understand the entire release process and these were analyzed using a combination of the square-root time law and cube-root law equations. 1,5,6) It was concluded that predicting drug release properties using this analysis was useful.…”

Influence of Swallowing Aids on the Adsorption and Palatability of Kremezin

“…[12][13][14][15] There are, however, few reports in which the effects of jellies have been evaluated as swallowing aids for Kremezin ® .…”