半固體藥妝品在法蘭茲式、強化式或穿流式擴散池溶離裝置中其活性成分釋放之比較研究   全文下載

A Comparative Study of the Release of Active Ingredients from Semisolid Cosmeceuticals Measured with Franz, Enhancer or Flow-Through Cell Diffusion Apparatus

本研究旨在探討不同半固體藥妝品活性成分在三種擴散池中的釋放性能比較。本試驗以法蘭茲式（Franz）、強化式（Enhancer）和穿流式（flowthrough）擴散池為釋放裝置，以水難溶性藥物皮質醇（hydrocortisone）、抗菌劑三氯生（triclosan），水溶性抗老化合物水楊酸（salicylic acid）、抗壞血酸（ascorbic acid）為模式藥物，測定上述各單方、水楊酸與三氯生複方和抗壞血酸與三氯生複方從凝膠、乳劑及軟膏中的釋放率。為了得到較穩定與變異較小（f2因數大於50）的釋放曲線，擴散所用的醋酸纖維素膜需預先浸泡於油酸與pH5.8磷酸緩衝液混液或50%乙醇與緩衝液混液處理。由皮質醇、水楊酸、抗壞血酸及三氯生從乳劑和凝膠中的釋放結果得知以穿流式擴散池為釋放裝置，其釋放速率顯著低於以法蘭茲式和強化式擴散池（p < 0.01）。在所有三種釋放系統中，在緩衝液中親水性化合物自凝膠劑的釋放較快；而在水醇混合液中水難溶性和親油性化合物從乳劑和軟膏的釋放較快。穿流式擴散池的缺點在於操作困難與樣品量小，導致結果變異較大。強化式擴散池的優點在於此法基本上應用美國藥典的溶離裝置且體積範圍較大，而利於產品含低濃度或難分析活性成分的釋放研究。

This study reports the release properties of the poorly water-soluble drug hydrocortisone, antibacterial agent triclosan, and the water-soluble anti-aging compounds salicylic acid and ascorbic acid from gels, creams, and ointments, alone or combined with triclosan. Drug release was measured with the flow-through, Franz, and Enhancer cell release testing methods. For the 3 methods, a cellulose acetate membrane soaked in lipophilic oleic acid and dissolution mediums composed of a phosphate buffer pH 5.8 or a 50% ethanol: buffer mixture gave more constant and less variable release profiles (similarity factors, f2, above 50). Comparison of the release rates of hydrocortisone, salicylic acid, ascorbic acid, and triclosan from creams and gels showed that the rates measured with the flow-through cells were significantly slower (p < 0.01) than those measured with the Franz and Enhancer cells. In all 3 systems, hydrophilic compounds released faster in the buffer solution and from the gels. Less water-soluble compounds and lipophilic compounds released faster in the hydro-alcohol mixture and from creams and ointments. The disadvantages of the flow-through cells were difficult operation and small sample sizes which caused variable results. The advantages of the Enhancer cells were that they used the basic USP dissolution apparatus and had a larger volume range making it easier to adapt the system for studying the release of products containing low concentrations of active ingredients or ingredients that are difficult to analyze. 本研究旨在探討不同半固體藥妝品活性成分在三種擴散池中的釋放性能比較。本試驗以法蘭茲式（Franz）、強化式（Enhancer）和穿流式（flowthrough）擴散池為釋放裝置，以水難溶性藥物皮質醇（hydrocortisone）、抗菌劑三氯生（triclosan），水溶性抗老化合物水楊酸（salicylic acid）、抗壞血酸（ascorbic acid）為模式藥物，測定上述各單方、水楊酸與三氯生複方和抗壞血酸與三氯生複方從凝膠、乳劑及軟膏中的釋放率。為了得到較穩定與變異較小（f2因數大於50）的釋放曲線，擴散所用的醋酸纖維素膜需預先浸泡於油酸與pH5.8磷酸緩衝液混液或50%乙醇與緩衝液混液處理。由皮質醇、水楊酸、抗壞血酸及三氯生從乳劑和凝膠中的釋放結果得知以穿流式擴散池為釋放裝置，其釋放速率顯著低於以法蘭茲式和強化式擴散池（p < 0.01）。在所有三種釋放系統中，在緩衝液中親水性化合物自凝膠劑的釋放較快；而在水醇混合液中水難溶性和親油性化合物從乳劑和軟膏的釋放較快。穿流式擴散池的缺點在於操作困難與樣品量小，導致結果變異較大。強化式擴散池的優點在於此法基本上應用美國藥典的溶離裝置且體積範圍較大，而利於產品含低濃度或難分析活性成分的釋放研究。