背景和目的 : Carbamazepine是治療抗痙攣、三叉神經痛藥物，不溶於水。Pentoxifylline和其代謝物可以減低血液粘度之增加，而改善血管血流的性質，因此可改善血流受損區之微細血管循環之營養狀態，可溶於水。此研究目的在研究水不溶性Carbamazepine藥物和水易溶性Pentoxifylline藥物從間質控制釋放劑型系統溶離的溶離特性及配方設計。
方法 : Carbamazepine被使用做為水難溶模式藥，各種配方改變在藥物溶離被研究，包括Carbamazepine顆粒大小；hydroxyl propyl methyl cellulose (HPMC)等級比率和錠劑膜衣包覆，HPMC聚合物系統K4M和K100LV兩等級被使用做為間質控制釋放聚合物，而ethylcellulose/polyvinylpyrrolidone K-30 (EC/PVP )複合聚合物被使用做為膜衣包覆物質。Pentoxifylline被使用做為易溶於水模式藥，HPMC K4M和carboxy methyl cellulose sodium (CMC sodium)被使用做為間質控制釋放聚合物。
結果 : 配方使用較大顆粒Carbamazepine的溶離速率比較小顆粒慢，溶離形式顯示Carbamazepine和Pentoxifylline隨著HPMC K4M聚合物量的增加而變慢，額外的膜衣包覆EC/PVP系統更降低藥物溶離速率。Pentoxifylline的溶離速率受到HPMC K4M和CMC sodium聚合物所調控，額外的添加Tween 80，可以加速Pentoxifylline藥物的溶離速率，隨著CMC sodium聚合物濃度的增加，顯示在pH值1.2和pH值4.5的溶離速率快慢是不同的。
結論 : 目前的研究清楚地顯示難溶性藥物和易溶性藥物兩種的溶離速率可以被使用在間質系統的聚合物比率所調控。 Background and Purpose: Carbamazepine is an anticonvulsant and specific analgesic for trigeminal neuragia. Carbamazepine insoluble in water. Pentoxifylline and its metabolites improve the flow properties of blood by decreasing its viscosity. In patient with chronic peripheral arterial disease , this increases blood flow to the affected microcirculation and enhances tissue oxygenation. Pentoxifylline soluble in water. The purpose of this study is to investigate the release characteristics of water insoluble Carbamazepine drug and water soluble Pentoxifylline drug from the matrix-based controlled release systems.
Methods: Carbamazepine was used as a poorly water-soluble model drug. Various formulation variables on drug release were studied, including particle size of Carbamazepine, hydroxyl propyl methyl cellulose (HPMC) grade ratio and tablet coating. Both k4M and k100LV grade of HPMC systems were used as matrix controlling polymers, whereas the ethylcellulose/polyvinylpyrrolidone k-30 (EC/PVP) system was used as film coating material. Pentoxifylline was used as a water soluble model drug. Both HPMC k4M and carboxy methyl cellulose sodium (CMC sodium) systems were used as matrix controlling polymers.
Results: Formulations with larger Carbamazepine particle size released slower than those with smaller particle size. The dissolution behavior showed that the dissolution rate of Carbamazepine and Pentoxifylline were slower as the amount HPMC k4M polymer increased. The addition of the EC/PVP system coating further decreased drug release rate. For Pentoxifylline, it appeared that the dissolution behavior was controlled by both HPMC k4M matrix and CMC sodium. The addition of Tween 80 further increased Pentoxifylline drug release rate. The dissolution behavior showed that the dissolution rate in the pH 1.2 and pH 4.5 medium was different as the amount CMC sodium polymer increased.
Conclusions: The present study clearly demonstrated that the release rate of both water insoluble drug and water soluble drug can be controlled by the ratio of polymer used in the matrix systems.
