摘要
目的研究黄芩总黄酮及其单体成分的溶解性及体外经皮渗透性,为其经皮给药研究与开发提供依据。方法采用摇瓶法测定黄芩总黄酮及其单体成分的油水分配值;体外扩散池法测定体外经皮渗透参数。结果黄芩总黄酮难溶于水,在丙三醇和50%乙醇中溶解性最好;在pH值2.0～6.8的磷酸盐缓冲溶液中,黄芩总黄酮及其单体成分的溶解性均随着pH值增大而增大,油水分配值(lgP)随着pH值增大而减小,当pH值为7.4和8.0时,黄芩苷的溶解性逐渐降低,总黄酮及其他单体成分的溶解性逐渐增大,黄芩苷的lgP值逐渐增大,其他单体成分的lgP值逐渐减小;总黄酮、黄芩苷、千层纸素A苷、汉黄芩苷、黄芩素、汉黄芩素、木蝴蝶素体外累积透过率分别为(191.31±13.01)×10-4、(2.86±0.06)×10-4、(1.29±0.13)×10-4、(1.33±0.22)×10-4、(17.78±1.12)×10-4、(16.10±1.16)×10-4、(6.42±0.71)×10-4,稳态透皮速率分别为(18.14±1.21)、(0.30±0.01)、(0.13±0.03)、(0.13±0.04)、(1.92±0.19)、(1.90±0.25)、(0.77±0.13)μg/(cm2·h)。结论黄芩总黄酮及其单体成分均有一定的经皮渗透性能,为制备黄芩经皮给药制剂提供实验依据。
Objective To study the solubility and percutaneous penetration characteristics of the total flavones from Scutellariae Radix （TFSR） and their monomer composition, and to provide the basis for the development of transdermal delivery. Methods Bottle-shaking method was used to determine the apparent oil/water distribution value, and in vitro diffusion cell method was used to measure the percutaneous penetration parameters of TFSR and their monomer composition. Results TFSR and their monomer composition slightly dissolved in water, and the solubility in glyceryl alcohol and 50% ethanol was the best. In the phosphate buffer solution （pH 2.0-6.8）, the solubility of TFSR and their monomer composition increased with the pH value increasing, and the oil/water distribution value lgP decreased as the pH value increasing. As the pH values were 7.4 and 8, the solubility of baicalin decreased gradually, the solubility of flavonoids and other compounds increased gradually, lgP value of baicalin increased gradually, while the lgP values of other ingredients decreased. The in vitro cumulative permeation rates of the total flavonoids, baicalin, oroxylin-A-glucoside, wogonoside, baicalein, wogonin, and oroxylin were （191.31 ± 13.01） × 10^-4, （2.86 ± 0.06）× 10^-4, （1.29 ± 0.13） × 10^-4, （1.33 ±0.22） × 10^-4, （17.78 ± 1.12） × 10^-4, （16.10 ± 1.16） × 10^-4, and （6.42 ± 0.71）× 10^-4, respectively. The percutaneous penetration rates were （18.14± 1.21）, （0.30 ± 0,01）, （0.13 ± 0.03）, （0.13 ± 0.04）, （1.92 ± 0.19）, （1.90 ± 0.25）, and （0.77 ± 0.13） μg.cm-2.h^-1. Conclusion TFSR and their monomer composition have certain percutaneous permeability, which could provides the experimental basis for the preparation of ScuteIIariae Radix transdermal drug delivery.
出处
《中草药》
CAS
CSCD
北大核心
2014年第2期200-207,共8页
Chinese Traditional and Herbal Drugs
基金
江苏省高校优势学科建设项目资助(PADA
2011年)
关键词
黄芩总黄酮
溶解性
油水分配值
经皮渗透性
黄芩苷
黄芩素
total flavones from Scutellariae Radix
solubility
oil/water distribution value
percutaneous penetration
baicalin
baicalein
