制备盐酸小檗碱脂质体,并测定其包封率和脂质体各成分含量。方法:采用硫酸铵梯度法制备盐酸小檗碱脂质体,以超速离心法、微柱法、超滤法对盐酸小檗碱脂质体包封率的测定方法进行研究,以HPLC-ELSD测定脂质体各成分含量。结果:超速离心法能将未包封药物与脂质体很好地分离,最佳超速离心条件:离心速度为60 000 r·min-1,离心时间为1h,离心温度为10℃,脂质浓度为6 mg·ml-1。结论:包封率测定方法具有简单、快速分离等优点。HPLC-ELSD能够同时测定脂质体各成分含量。

Objective:To prepare bererine hydrochloride ( BER) liposomes and establish an effective method for the determination of content and entrapment efficiency. Methods:BER liposomes were prepared by ammonium sulfate gradient method. The encapsula-tion efficiency of BER liposomes was respectively determined by supercentrifugation method, microcolumn gel method and ultrafiltration method, and the content of every component in BER liposomes was detected by HPLC-ELSD. Results:The results showed that super-centrifugation method could precisely separate the free drug from the liposomes. The optimum parameters of supercentrifugation method were the centrifugal speed of 60 000 r·min-1 , the centrifugal time of 1 h, the centrifugal temperature of 10℃ and the lipid concentra-tion of 6 mg·ml-1 . Conclusion:The method is simple and sensitive with good separation efficiency. HPLC-ELSD can be used to de-termine the content of every component in BER liposomes.

目的：：优选愈烧伤脂质体凝胶的提取工艺条件。方法：以盐酸小檗碱含量及浸膏得率为评价指标,采用正交试验法考察加水量、粒度、提取时间对提取工艺的影响。结果：优化工艺为：将黄连粉碎成10目大小的颗粒,加热提取3次,加水量分别为药材量的10倍、8倍、8倍,提取时间分别为3,2,2 h。结论：优选的工艺稳定可靠,可用于愈烧伤脂质体凝胶的制备。

Objective:To optimize the conditions in the extraction process of Yushaoshang liposomal gels. Methods: Using the content of hydrobererine and extract yield as the indices, the optimum extraction conditions were screened by orthogonal test. Results:The optimum extraction conditions were as follows:Rhizoma coptidis was crashed into small particles as 10 mesh sieve, heating extrac-ted three times with 10-fold,8-fold and 8-fold water, and extracting 3h, 2h and 2h,respectively. Conclusion:The extraction technology is reliable and available in the preparation of Yushaoshang liposomal gels.

目的：：建立盐酸罗哌卡因多囊脂质体中药物含量及包封率的测定方法。方法：采用低速离心法分离游离药物和多囊脂质体,采用高效液相色谱法检测多囊脂质体中游离药物含量和总药量,并计算包封率。结果：盐酸罗哌卡因在1.0~80.0μg·ml-1范围内线性关系良好(r=0.9998)；平均回收率为99.95%,RSD为0.72%(n=9)。用此方法测定3批盐酸罗哌卡因多囊脂质体的主药含量和包封率,结果分别在99.1%~100.3%及80.06%~82.14%之间。结论：该方法操作简单,结果准确,适合用于盐酸罗哌卡因多囊脂质体含量和包封率测定。

Objective:To establish a determination method for the content and entrapment efficiency of ropivacaine hydrochloride-loaded multivesicular liposomes. Methods: The separation of the multivesicular liposomes from the free drug was achieved by low-speed centrifugation. The concentration of ropivacaine hydrochloride in the supernatant and the multivesicular liposomes was determined by HPLC, and the entrapment efficiency was calculated. Results: The linear range of ropivacaine hydrochloride was 1. 0-80. 0μg· ml-1(r=0. 999 8). The average recovery was 99. 95% and RSD was 0. 72%(n=9). The content and entrapment efficiency of three batches of ropivacaine hydrochloride-loaded multivesicular liposomes was within the range of 99. 1%-100. 3% and 80. 06%-82. 14%, respectively. Conclusion:The method is simple and accurate, and can be used in the determination of content and entrapment efficien-cy of ropivacaine hydrochloride-loaded multivesicular liposomes.

目的在动物体内检验盐酸米诺环素脂质体控释凝胶的生物相容性及其对牙周炎动物模型的修复效果。方法毒性实验:用质量分数2%盐酸米诺环素脂质体控释凝胶溶液给SD大鼠灌胃,观察长期应用该制剂有无全身不良反应及其反应程度。牙周炎动物模型实验:将实验性牙周炎建模成功的SD大鼠分为3组,A组为派丽奥组,B组为实验药物组,C组为阴性对照组;A、B组每周牙周袋内给药1次,连续56 d,C组给予生理盐水;分别在给药7、14、28、56 d后测量各组动物的牙周探诊深度(PD)和牙龈指数(GI),并进行组织学观察,计算单核细胞和破骨细胞的数目。结果盐酸米诺环素脂质体控释凝胶具有良好的生物相容性;给药14 d后,PD、GI,以及单核细胞和破骨细胞数目均较其他两组明显降低,组织学观察可见新骨及部分新纤维形成。结论牙周袋内使用盐酸米诺环素脂质体控释凝胶可减轻牙周炎症,提示该制剂对改善牙周炎有一定的疗效,具有临床应用前景。

Objective To evaluate the therapeutic effects of 2% minocycline hydrochloride liposome controlled-release gel on the periodontitis in an established rat periodontitis model. Methods Biocompatibility was tested by oral perfusion sample solution for long-term observation. Minocycline hydrochloride liposome controlled-release gel was utilized to treat the established rat periodontitis model. The rats were selected randomly and divided into three groups: group A (PERIO-treated group), group B (minocycline hydrochloride liposome controlled-release gel treated group), and group C (negative control group). The gingival index (GI) and probing depth (PD) were detected, and the number of mononuclear and broken bone cells were examined after 7, 14, 28, and 56 d. Results The minocycline hydrochloride liposome controlled-release gel exhibited excellent biocompatibility based on weight measure and tissue section evaluation. The rats with periodontitis demonstrated that GI, PD, and the number of mono