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鋰鹽持續釋出劑型之研究
Product Development of Lithium Salt Sustained Release Dosage Forms
摘要
本研究之目的是研究碳酸鋰之持續釋出劑型，以降低藥物副作用，提高療效。碳酸鋰持續釋出劑型是以十種不同處方組成，經由改變其重要賦型劑如普維酮（PVP K-30，1，2及4%）、澱粉（2，3，5及7%）及硬脂酸甘油脂（2，4，6及7.5%）之比例而製成基質型錠劑。碳酸鋰錠劑之重要物理性質如重量差異、硬度、脆損度及顆粒之流動性也經測定，其結果為脆損度小於0.5%，重量差異符合一般藥典規定，流動性其值為1.7至2.54cm^3/sec。此三者用以評估錠劑品質及製造之方法。各種錠劑也測定其溶離特性，以兩種不同pH（1.2及7.5）之溶離媒液，試驗結果顯示碳酸鋰之各錠劑其溶離速度在前三小時接近一定值，表示藥物具穩定釋出之特性。由多變數線性廻歸分析顯示增加普維酮及硬脂酸甘油酯之量降低溶離速率，反之澱粉則增加溶離速率，但其因素則不太顯著。經初步體內試驗亦顯示所研製之碳酸鋰製品具有適當持續釋出之特性。
並列摘要
In order to optimize the therapeutics and decrease the side effects of lithium carbonate, sustained-release delivery system was developed. Matrix-type tablets of lithium carbonate were made with ten formulations varying in the preparation of starch (2, 3, 5 and 7%), PVP k-30 (1, 2 and 4%), glyceryl monostearate (2, 4, 6 and 7.5%) and other inert ingredients. The physical properties of lithium carbonate were determined including weight variation, hardness and friability. The results showed that friability was less than 0.5%, weight variation met the specification of pharmacopeia and flowability ranged from 1.7 to 2.54 cm^3/sec. These properties were used to evaluate and control the processes of preparation. The dissolution rates of various preparations of lithium carbonate approached a constant value during the initial three hours of dissolution test. From the analysis of multiple linear regressions it showed that increasing the amount of PVP k-30 and glyceryl monostearate decreased the dissolution rate; alternatively, increasing the amount of starch increased the dissolution rate, but this effect is not remarkable. The results of in-vitro study also suggested that some lithium carbonate preparations had reasonable sustained-release behavior.