評估capsaicin衍生物-Sodium nonivamide acetate微乳劑配方對膀胱收縮功能之影響

Evaluation the effect of capsaicin derivative-Sodium nonivamide acetate microemulsion formulation on bladder contraction

林勇豪(Yong-Hao Lin)

指導教授 ： 吳寶珠

高雄醫學大學/藥學院/藥學研究所/碩士(2007年)

摘要

間質型膀胱炎（Interstitial cystitis）是一種膀胱壁發炎的疾病，每10萬名婦女中就有52∼67位罹患間質型膀胱炎，而平均發病年齡為40歲，其臨床徵狀有疼痛（pain）、頻尿（frequency）、尿急（urgency）和尿失禁（urge incontinence）等。Sodium nonivamide acetate， C19H29NO5Na 2H2O，簡稱SNA，為水溶性的capsaicin衍生物，其不會產生辛辣感與皮膚的刺激性。藥理活性和capsaicin相類似，其降低痛覺刺激的作用約capsaicin的1.75倍。故嘗試將SNA製成微乳劑型，直接灌注於膀胱中，評估SNA對膀胱收縮間隔（intercontraction interval, ICI）的影響。本研究將SNA製成以 Tween80、Span20為界面活性劑，IPM為油相，二次水為水相，乙醇為輔助界面活性劑之微乳劑系統。微乳劑處方的粒徑大小均在16∼330 nm之間，由導電度大小推斷大部分微乳劑處方均為油/水型微乳劑。實驗結果顯示將SNA製成微乳劑型，在體外穿透試驗中24小時的累積穿透量為26.99∼73.01 µg/cm2。體內實驗以皮下給藥及膀胱內治療（intravesical）給藥，其ICI的實驗結果有二：
1. SNA可增加膀胱容積，減少排尿頻率
2. SNA可以有效治療間質型膀胱炎

關鍵字

微乳劑 ； 辣椒素衍生物 ； 間質型膀胱炎

並列摘要

Interstitial cystitis (IC) is a inflammatory condition of the bladder. Women are much more frequently diagnosed with IC than men (10:1). Results of a recent questionnaire mailed to participants in the US Nurses Health Study I and II suggested a prevalence in these women of between 52 and 67 per 100 000 (Nickel, 2000). It’s more commonly found in females, with a median age of onset at 40 years. Clinical symptom were included pain, frequenycy, urgency, urge incontinence.
Sodium nonivamide acetate (SNA: C19H28NO5Na) is a hydrophilic derivative of capsaicin and without producing an over pungent sensation and skin irritation. SNA showed a higher antinociceptive potency than capsaicin did by 1.75-fold. We try to make SNA microemulation and to infuse it into the bladder. Evaluation the effect of SNA on ICI. In this study, we have developed a microemulsion system consisted of Tween 80 and Span 20 as surfactant phase, isopropyl myristate as oil phase, doubled-distilled water as aqueous phase, and ethanol as co-surfactant phase for transdermal delivery of SNA. The result showed that average size of microemulsions were from 64 nm to 210 nm. The accumulated amount at 24th hr of microemulsion formulations ranged from 26.99 to 73.01µg/cm2, were higher than that of control formulation (40% EtOH aqueous solution, 9.05 µg/cm2). The results of ICI shown：
(1).SNA can increase the volume of bladderand reduce frequency of voiding.
(2).SNA could treat of rat with interstitial cystitis

並列關鍵字

Microemulsion ； Sodium nonivamide acetate ； Intravesical ； Interstitial cystitis

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