Carbonizing by stir-frying (CSF) is the most common technology in botanical folk medicines to enhance the convergence, hemostasis, and antidiarrheal effects. Sanguisorbae Radix (SR), a well-known herbal medicine in China, has extensive therapeutic functions, while charred SR is known as an additional product obtained from SR after CSF. In this study, mass spectrometry was used to investigate the effect of charring on tannins transformation of SR. The findings showed that the content level of tannins in SR decreased significantly after carbonizing process, while their three categories, gallotannins, ellagitannins, and procyanidins, had downward trends in general. Moreover, CSF also induced the polyphenol in SR to release relevant monomers from its origins. Significant amount of hydrolyzable tannins were detected by mass spectrometry, including gallotannins and ellagitannins, suggesting that hydrolysis during CSF yielded gallic and ellagic acid and their derivatives, in addition to sugar moieties. Subsequently, gallic and ellagic acid can further polymerize to form sanguisorbic acid dilactone. The amount of proanthocyanidins, the oligomers of catechin, including procyanidin, procyanidin C2, procyanidin B3, and 3-O-galloylprocyanidin B3, decreased to form catechin and its derivatives, which may further degrade to protocatechualdehyde. Quantitative analysis illustrated that the amount of gallic, pyrogallic, and ellagic acid and methyl gallate, the essential effectors in SR, significantly increased after CSF, with increased ratios of 1.36, 4.28, 10.33, and 4.79, respectively. In contrast, the contents of cathechin and epigallocatechin dropped remarkably with increased ratios of 0.04 and 0.02. Tannins exhibit moderate absorption, while their relevant monomers have a higher bioavailability. Therefore, CSF is proved here to be an effective technique to the release of active monomers from the original polyphenol precursor. This study explored the mechanism by which tannins are transformed upon CSF of SR.

目的 从药效与灰化2个角度阐释"炒炭存性"原理,并优选地榆炒炭工艺及探讨炮制质量标志物(qualitymarker,Q-Marker)与灰化临界点参数.方法 考察炒炭温度、时间对地榆炮制品外观性状、提取物得率、指标性成分、金黄色葡萄球菌抑制效果的影响,以此优选炮制工艺.结果 随炒炭程度增加,地榆炭提取物中没食子酸含量先增后减,鞣花酸一直增加.地榆在抗菌效果方面炮制增效,从而阐释"炒炭存性";地榆炭对金黄色葡萄球菌的抑菌效果与提取物中没食子酸的含量呈较强正向相关性.地榆炭提取物得率与提取物中鞣花酸含量呈极强的反向相关性(r=-0.96403),地榆炭提取物得率突然下降时,饮片质地开始出现脆化、灰化现象.获得的最优地榆炒炭工艺:在250℃温度条件下炒炭6min,此时提取物得率约30％,没食子酸在提取物[(46.41±0.06)μg/mg]和饮片中[(14.20±0.02)μg/mg]含量相较于其他炮制条件最高.结论 提出用没食子酸含量指导地榆炒炭工艺,用提取物得率控制灰化临界点的研究思路,并优化了基于抑菌效应的地榆炮制工艺.

目的 研究钙黄绿素神经酰胺脂质体(calcein-loaded cerasomes,CA-CS)的体外皮内递送效果,并推测其皮内递送的主要机制.方法 采用薄膜水化-冻融法制备CA-CS和钙黄绿素传统脂质体(calcein-loaded conventional liposomes,CA-CL),并对其理化性质和体外释放行为进行表征;采用改良的Franz透皮扩散仪和大鼠皮肤进行体外皮内递送实验;使用荧光显微镜观察药物在皮肤中的分布.结果 CA-CS和CA-CL的粒径均在200 nm左右,且分散均匀(PDI ＜0.3),体外释放结果显示,CA-CS和CA-CL均具有良好的缓释作用;体外皮内递送实验和荧光显微镜结果显示,8h内CA-CS的皮内滞留量显著高于CA-CL和钙黄绿素溶液,分别约是它们的2倍和1.6倍,且神经酰胺脂质体能将钙黄绿素递送至更深的皮肤层.结论 神经酰胺脂质体与皮肤角质层具有较强的相互作用,能显著提高水溶性药物的皮内递送效果,实现皮肤靶向给药的目的 ,为皮肤局部给药提供了一种有效的药物载体.

中药经皮给药有悠久的应用历史,脂质体作为新型载体用于中药活性成分的经皮给药可以提升药物在局部的皮内滞留或(和)透皮吸收效果,从而显著改善药效.该文从皮肤屏障的特点、中药经皮给药概况、脂质体促进经皮吸收的机制与影响因素、中药经皮给药脂质体的皮内滞留、中药经皮给药脂质体的透皮吸收等5个方面对相关研究进展进行了综述,涉及常规脂质体以及传递体、醇质体、萜质体、甘油体、表面修饰脂质体等新型脂质体的应用,并提出了坚持正确的研究方向、提升制剂技术水平和提高研究技术水平三方面的展望.

目的 比较生姜炮制成千姜前后挥发油透皮吸收促进作用及成分的变化.方法 将生姜炮制成干姜前后提取挥发油,皮肤电阻动力学实验和体外布洛芬透皮实验比较二者的促渗能力,ATR-FTIR红外分析挥发油透皮促渗主要机制,皮肤细胞毒性实验比较了生姜和干姜挥发油的细胞毒性,GC-MS分析成分变化.结果 干姜挥发油的透皮吸收促进作用显著优于生姜挥发油,其透皮促渗机制主要为对皮肤角质层脂质的萃取,而生姜和干姜挥发油的皮肤细胞毒性均显著低于化学促渗剂氮酮,炮制后干姜挥发油的倍半萜类成分比例高于生姜挥发油,透皮后干姜挥发油组皮内的倍半萜类成分比例也高于生姜挥发油组.结论 炮制后的干姜挥发油的透皮吸收作用优于生姜挥发油,验证了中药挥发油透皮吸收促进剂存在“热者易效”的规律.

分析整理《雷公炮炙论》《炮炙大法》《修事指南》三部炮制专书中炮制辅料的应用情况,探索炮制辅料应用的发展历史,为现代炮制研究提供更多线索.