碩士 / 國防醫學院 / 藥學研究所 / 83 / Acyclovir(ACV)為目前世界公認最可靠有效的抗病毒藥物之一,其作用機
轉主要是干擾庖疹病毒去氧核醣核酸的合成,使庖疹早日結疤,並減少病患
痛苦.但根據臨床上治療再發生單純性庖疹的經驗,發現局部給予 ACV 的
療效並不佳,主要是到達目標作用區 - 表皮基底層的量不足,導致缺乏臨
床療效,所以希望進一步改善 ACV 的經皮吸收,使藥物能進入更深層組
織. 本實驗室為增加 ACV 經皮吸收量,特別篩選傳統中藥藥引純成份,作
為經皮吸收促進劑.結果在以裸鼠為穿透的72小時體外經皮吸收實驗,及以
家兔為動物實驗研究 ACV 在各皮層組織的濃度,皆比控制組有顯著的增
加 .隨後我們在永信 GMP 製藥廠生產 5% ACV + 5% Glycyrrhizin + 1%
Ol- eanolic acid 凝膠劑和 5% ACV PEG 軟膏劑,並通過人體試驗委員會
和衛生署核准,以雙盲並行方式進行臨床試驗,治療感染帶狀庖疹的病人並
評估兩種經皮吸收劑型在治療上的差異.在安定性方面,進行兩種劑型的化
學含量在不同溫度下的經時變化,並藉由體外穿透試驗進一步探討 ACV 對
經皮吸收之滲透試驗安定性.結果顯示, ACV 兩種製劑的化學安定性在各
種溫度三個月內呈不顯著之改變;體外穿透試驗顯示 ACV 凝膠平均穿透
量(72hr)在三個月和四個月時與新鮮配製相同,但兩個月結果尚難解釋,而
凝膠劑與新鮮配製無顯著差異;初步臨床試驗已完成32人,顯示 ACV 含中
藥藥引的製劑在 50% 傷口癒合時間 (P < 0.05) 的治療上有顯著的差異.
Acyclovir is one of the most reliable and effective antiviral
drugs at the presetn time . The antivial mechanism of ACV is to
interfere with herpes virus DNA replication . According to
clini- cal study in treating recurrent cutaneous herpes simplex
virus i- nfection , topical ACV therapy shows lack of efficacy
.The insuf- ficient delivery of ACV to the target site (basal
epidermis) is the invalid reason . Therefore , the purpose of
the study is to enhance the percutaneous absorption of ACV so
as to increase its therapeutic effect . With the considerationf
to enhance acyclovir percutaneous ab- bsorption , our group
search on the most commonly used Chinese herbal enhancers for
the purpose . The cumulative amount in the 72-hour penetration
study of nude mice abdominal skin in vitro and acyclovir
concentration of the rabbit skin and tissue in vivo were
significantly higher than those in the control groups . The
formulations were invented . One is the gel formulation with
con- tains 5% ACV + 5% Glycyrrhizin + 1% Oleanolic acid . The
other is the ointment formulation which contains 5% ACV + PEG
base . The study was approved by the Istitutional Review Board
of the Natio- nal Defense Medical Center and National Health
Department . Eval- uation was by the double-blind and parallel
design . The time ef- fect on content and permeation stability
were measured under var- ious temperature .
| Identifer | oai:union.ndltd.org:TW/083NDMC0551004 |
| Date | January 1995 |
| Creators | Lin Win-Bow, 林文博 |
| Contributors | Oliver Y.P.Hu., 胡幼圃 |
| Source Sets | National Digital Library of Theses and Dissertations in Taiwan |
| Language | zh-TW |
| Detected Language | English |
| Type | 學位論文 ; thesis |
| Format | 104 |
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