- 學位論文
Nicardipine HCl長期性間質錠之製備與評估
Preparation and Evaluation of Nicardipine HCl Matrix Tablet for Extended Release
摘要
控釋劑型為一種在固定時間以一定速率將藥物有效的傳遞到作用部位，產生預期效果的一種劑型。而本研究的目的乃是製備Nicardipine長時間釋放劑型。 在初步篩選數種賦形劑之後以HPMC來當做載體，並以Avicel®及Sodium alginate來當做修飾藥物溶離速率之添加劑。 為快速獲得具有理想釋出速率之Nicardipne extended release錠劑，本實驗利用Response surface methodology(RSM)之技術來尋求符合多項目標在第3、6和12小時之藥物釋放百分比分別為不可大於30％，介於40~65％和大於80％之合適化處方。其中以HPMC、Avicel®、Sodium alginate的含量設為indepensent factor，依限制性混合實驗法來設計一系列模式配方，所有配方依pH change溶媒進行藥物釋出試驗，以藥物在第3、6和12小時釋出量為dependent facto利用一次多項式方來分析independent factor及dependent factor之關係並找出符合理想之配方。 結果顯示，所得合適化處方在第3、6和12小時之預估溶離率值與與實際實驗觀察值經由RE％來評估，發現其RE％≦5％，因此確認了RSM的可用性；而且Nicardipine間質型長期釋放錠之釋出機轉則近似零級模式。
並列摘要
Controlled release may be defined as a technique by which drug are made available to a target at a fixed rate and duration to produce a desirable therapeutic effect. The purpose of the study was to prepare nicardipine matrix for extended release. HPMC was selected as carrier to prepare nicardipine tablets and Sodium alginate and Avicel® were used to confer the release of drug. The response surface methodology (RSM) and multiple responses optimization polynomial equation were used to obtain optimal nicardipine matrix for extended release. First of all the release rate at 3, 6, 12 hr were not more than 30%, not less than 40~65% and not less than 80%, respectively. The amounts of HPMC, Avicel® and Sodium alginate were defined as independent factors. Limit mixture method was used to design an array of formulations. Dissolution test with pH change buffer was used to obtain the release percentages at the 3, 6 and 12 hr. Multiple responses optimization polynomial equation was used to analyze the relationship between independent factor and dependent factor to obtain an optimal formulation. The result showed the optimized formulation provided a dissolution profile equivalent to that of predict and its RE%±5% was not more than 5%, indicating that the optimal formulation could be obtained by using response surface methodology. The mechanism of drug release from optimal nicardipine matrix tablets was found to follow quasi Zero-order model.