背景:穿心莲(AP)已被泰国政府批准用于治疗轻度病例的COVID-19患者。越来越多地使用AP产品需要质量控制以确保疗效和安全性。目前,泰国草药药典(THP)中没有对AP产品的溶出度测试的要求。
目的:这项工作旨在研究活性二萜的含量和溶出曲线,穿心莲内酯(AP1),14-脱氧-11,12-二脱氢穿心莲内酯(AP3),新穿心莲内酯(AP4),和14-脱氧穿心莲内酯(AP6)的AP胶囊在泰国市场有售。
方法:四种提取物产品(EXT。A-D)和三种粗粉末产品(CRD。通过使用HPLC-DAD测试A-C)的内容物。用装置II(桨式)在不同的介质(pH1.2、4.5、6.8和0.01NHClSLS)中研究了四种二萜的溶出曲线。
结果:粗胶囊的AP1含量为1.99%-2.90%w/w,提取物胶囊的AP1含量为2.84%-16.27%w/w。在溶出试验中,除EXT外,粗胶囊中四种二萜的溶出百分比均高于提取物胶囊。A.大多数提取物产品中的AP1(EXT。B,C,D)以低于其他三种二萜的百分比溶解在所有溶解介质中。EXT.A(水性提取物)是唯一的提取物胶囊,其显示在45分钟内溶解于所有介质中的所有二萜的量>80%。
结论:研究表明,AP产品中的AP1含量符合THP的验收标准(80%-120%),重量变化也符合美国药典(USP)的要求。然而,AP产品的不同溶出曲线可能导致二萜的生物利用度不同,进而影响其疗效。
BACKGROUND: Andrographis paniculata (AP) has been approved by the Thai government for the treatment of mild cases of COVID-19 patients. Increasing use of AP products requires quality control to ensure efficacy and safety. At present, there is no requirement for dissolution test of AP products in the Thai Herbal Pharmacopoeia (THP).
OBJECTIVE: This work aimed to examine the contents and dissolution profiles of active diterpenoids, andrographolide (AP1), 14-deoxy-11,12-didehydroandrographolide (AP3), neoandrographolide (AP4), and 14-deoxyandrographolide (AP6) in AP capsules available in Thai markets.
METHODS: Four extract products (EXT. A-D) and three crude powder products (CRD. A-C) were tested for contents by using HPLC-DAD. Dissolution profiles of four diterpenoids were investigated in different media (pH 1.2, 4.5, 6.8, and 0.01 N HCl + SLS) with apparatus II (paddle type).
RESULTS: The AP1 contents were 1.99%-2.90% w/w for crude capsules and 2.84%-16.27% w/w for extract capsules. In the dissolution test, the dissolution percentages of four diterpenoids from crude capsules were higher than those from extract capsules except EXT. A. AP1 in most extract products (EXT. B, C, D) was dissolved in all dissolution media at a lower percentage than the other three diterpenoids. EXT. A (aqueous extract) was the only extract capsule showing the amounts of all diterpenoids dissolved in all media >80% in 45 min.
CONCLUSIONS: The study demonstrated that AP1 content in AP products complied with the acceptance criteria in the THP (80%-120%), and the weight variation also met the United States Pharmacopeia (USP) requirements. However, different dissolution profiles of AP products may lead to different bioavailability of diterpenoids and further affect their efficacy.