Wang Li-Fang, Chen Xiao-Nan, Li Jun, Tu Peng-Fei, Wang Jin-Ling
School of Chinese Materia Medica, Modern Research Center for Traditional Chinese Medicine,Beijing University of Chinese Medicine Beijing 100029, China.
Zhongguo Zhong Yao Za Zhi. 2019 Jun;44(11):2236-2243. doi: 10.19540/j.cnki.cjcmm.20181221.005.
The single-factor test was used to optimize the high-pressure homogenization method to prepare the phenolic extract nanosuspensions(DBNs). The physicochemical properties of the obtained nanosuspensions were characterized and the cumulative release in vitro was evaluated. The results showed that the drug concentration was 0.5 g·L(-1), the mass concentrations of PVPK30 and SDS were 0.5 and 0.25 g·L(-1), respectively, the probe ultrasonic time was 5 min, the homogenization pressure was 900 bar, and the number of homogenization was 2 times. The prepared DBNs had an average particle size of(168.80±0.36) nm, polydispersity index(PDI) of 0.09±0.04, stability index(SI) of 0.85, and DBNs were stable for storage within 30 days. Scanning electron microscopy showed that the particle size of the dragon's blood extract was reduced and the uniformity was improved in the obtained nanosuspensions. X-ray diffraction pattern and differential scanning calorimetry showed that the phenolic extract of dragon's blood was still in an amorphous state after being prepared into nanosuspensions. The results of saturated solubility measurement showed that the solubility of DBNs lyophilized powder reached 6.25 g·L(-1), while the solubility of DB raw powder was only 28.67 mg·L(-1). The in vitro dissolution experiments showed that DBNs lyophilized powder accumulated in gastrointestinal fluid for 8 h. The release amount was 90%,the cumulative release of the raw powder in the gastrointestinal fluid for 24 h was less than 1%, and the solubility and dissolution rate of the DBNs lyophilized powder were significantly higher than the DB raw powder. The method is simple in process and convenient in operation, and can successfully prepare uniform and stable nanosuspensions to improve its solubility, and provides a research basis for solving the application limitation of dragon's blood extract.
采用单因素试验对高压均质法制备血竭酚提取物纳米混悬液（DBNs）进行优化。对所得纳米混悬液的理化性质进行表征，并评价其体外累积释放度。结果表明，药物浓度为0.5 g·L⁻¹，PVPK30和SDS的质量浓度分别为0.5和0.25 g·L⁻¹，探头超声时间为5 min，均质压力为900 bar，均质次数为2次。所制备的DBNs平均粒径为（168.80±0.36）nm，多分散指数（PDI）为0.09±0.04，稳定性指数（SI）为0.85，且DBNs在30天内储存稳定。扫描电子显微镜显示，所得纳米混悬液中血竭提取物的粒径减小且均匀性提高。X射线衍射图谱和差示扫描量热法表明，血竭酚提取物制成纳米混悬液后仍为无定形状态。饱和溶解度测定结果显示，DBNs冻干粉末的溶解度达到6.25 g·L⁻¹，而血竭原料粉末的溶解度仅为28.67 mg·L⁻¹。体外溶出实验表明，DBNs冻干粉末在胃肠液中累积8 h，释放量为90%，原料粉末在胃肠液中24 h的累积释放量小于1%，DBNs冻干粉末的溶解度和溶出速率显著高于血竭原料粉末。该方法工艺简单、操作方便，能成功制备均匀稳定的纳米混悬液以提高其溶解度，为解决血竭提取物的应用局限提供了研究依据。
