THE COMPARATIVE STEADY-STATE BIOAVAILABILITY OF THE ACTIVE INGREDIENTS OF MADECASSOL
THE COMPARATIVE STEADY-STATE BIOAVAILABILITY OF THE ACTIVE INGREDIENTS OF MADECASSOL
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DOI：
10.1007/bf03190180
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发表时间：
1993-10-01
影响因子：
1.9
通讯作者：
GRAHAM, DJM
中科院分区：
文献类型：
--
作者：
RUSH, WR;MURRAY, GR;GRAHAM, DJM
研究了12名健康男性和女性志愿者口服近似等摩尔剂量的积雪酸(12 Mg)或积雪草苷衍生物积雪草苷(24 Mg)后，积雪酸的相对稳态生物利用度。积雪草酸和积雪草苷都是市场上销售的皮肤病产品Madecasol的成分。积雪草苷在体内通过水解糖的裂解转化为积雪草酸。在这两种方案中，积雪草酸的稳态AUC0-12h值相似(亚洲酸后为614+/-250ng.h/ml，积雪草苷后为606+/-316ng.h/ml)，表明这两种成分的生物利用度大致相同。由于积雪草酸被认为是马迪卡松中最具治疗活性的成分，目前的数据表明积雪草苷的治疗作用可能是通过转化为积雪草酸来实现的。
The comparative steady-state bioavailability of asiatic acid was studied in 12 healthy male and female volunteers following oral administration of approximately equimolar doses of either asiatic acid (12 mg) or the glycoside derivative of asiatic acid, asiaticoside (24 mg). Both asiatic acid and asiaticoside are constituents of the marketed dermatological product Madecassol. Asiaticoside is converted in vivo to asiatic acid by hydrolytic cleavage of the sugar moiety.Steady-state AUC0-12h values for asiatic acid on either regime were similar (614 +/- 250 ng.h/ml following asiatic acid compared to 606 +/- 316 ng.h/ml following asiaticoside) indicating comparable bioavailability for asiatic acid with the two ingredients at approximately equimolar doses. Since asiatic acid is considered to bc the most therapeutically active ingredient of Madecassol, the current data suggest that the therapeutic effects of asiaticoside may be mediated through conversion to asiatic acid.