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題 名 | Preparation and Pharmacological Evaluation of Physostigmine-loaded Polyisobutylcy Anoac-rylate Nanoparticles in Rats=Physostigmine毫微粒小球之製備及其在大白鼠體內藥理作用之評估 |
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作 者 | 蔡東榮; 卓玟禾; 林清維; 詹道明; | 書刊名 | The Kaohsiung Journal of Medical Sciences |
卷 期 | 14:1 1998.01[民87.01] |
頁 次 | 頁13-18 |
分類號 | 418.1 |
關鍵詞 | Physostigmine毫微粒小球; 大白鼠; 體內; 藥理作用; Nanoparticles; Acetylcholine; Microdialysis; |
語 文 | 英文(English) |
中文摘要 | 以氰基丙烯酸異丁醋為載體材料,利用乳化聚合法製備physostigmine毫微粒小球,並檢測其粒子大小分佈及包埋率並比較含藥之毫微粒子與溶液劑在體外溶出試驗。結果顯示,粒揮大小約250nm,包埋率為62%。在體外溶出試驗,毫微粒子則表現出有緩釋效果。以大白鼠為實驗動物,測其投藥後腦中乙醜膽鹼的濃度,做為physostigmine 藥理作用的評估。實驗的方法為在大白鼠腦部紋狀體區插入微透析管,以高效液相層析儀聯接電化學法在線上(on-line)直接測出乙醱膽鹼。為了消除膽鹼的干擾,在分離管柱前加裝充填膽鹼氧化酵素和催化酵素等固定化酵素之前管柱。這種串連的管柱可單獨且靈敏的測得腦中乙醱膽鹼的濃度(5 fmol / μl )。以此方法檢測分別注射physostigmine毫微粒小球及溶液劑兩種劑型後,大白鼠腦部紋狀體乙醞膽鹼濃度的經時變化。比較曲線下的面積(AUC),毫微粒小球為溶液劑的2.3倍,顯示毫微粒小球有延長及增加physostigmine 藥理作用的效果。 |
英文摘要 | The nanoparticles of physostigmine were prepared by an emulsion polymerization of polyisobutylcyanoacrylate. The drug content, release and particle size distribution of the nanoparticles were characterized. In vitro drug release profiles displayed a retardation by the nanoparticles In comparison to the aqueous solution. Pharmacological evaluation of physostigmine nanoparticles in vivo were carried out with SpragueDawley rats. The endogenous acetylchollne was sampled by on-line microdialysis and determined by a sensitive microbore HPLC/ED system in the striatum of rats. The choline oxidase and catalase immobilized enzyme reactors were used as the precolumn to erase choline. Accordingly, this chromatographic flow sequence could be utilized for the quantitative assay of acetylcholine without interference. The results indicate that the increase of acetylcholine(%) in the rats striatum by the nanoparticle was 2.3 times (AUC) higher than that of aqueous solution. |
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