The purpose of this work was to improve the oral bioavailability of poorly soluble drugs by incorporation into solid lipid nanoparticles (SLNs). All-trans retinoic acid (ATRA) was used as a poorly soluble model drug. Different formulations of SLNs loaded with ATRA were successfully prepared by a high-pressure homogenization method and using Compritol 888 ATO as lipid matrix. The particle size and distribution, drug loading capacity, drug entrapment efficiency (EE %), zeta potential, and long-term physical stability of the SLNs were investigated in detail. Drug release from two sorts of ATRA-SLN was studied and compared with the diffusion from ATRA solution in 0.1 M HCl, distilled water and phosphate buffer (pH 7.40), using a dialysis bag method. A pharmacokinetic study was conducted in male rats after oral administration of 8mgkg---1 ATRA in different formulations and it was found that the relative bioavailability of ATRA in SLNs was significantly increased compared with that of an ATRA solution. The amount of surfactant also had a marked effect on the oral absorption of ATRA with SLN formulations. Although an emulsion formulation also increased ATRA absorption, it was too unstable for use in clinical situations. The absorption mechanism of the SLN formulations was discussed. These results indicate that ATRA absorption is enhanced significantly by employing SLN formulations. SLNs offer a new approach to improve the oral bioavailability of poorly soluble drugs.

目的 以山嵛酸甘油酯（Compritol888ATO）为脂质材料，采用超声分散法制备维甲酸固体脂质纳米粒，并考察其体内外性质。方法 选用脂溶性较高的维甲酸作为模型药物，采用超声分散法制备固体脂质纳米粒，并对其各种理化性质进行研究。考察了纳米粒的体外释放，以维甲酸溶液剂为对照，测定了两种纳米粒在大鼠体内的药代动力学参数。结果 采用超声分散法可以简便、快速制备得到两种维甲酸固体脂质纳米粒，透射电镜测得纳米粒为圆球状，大小均匀。动态光散射法测得平均粒径分别为（158±9）nm和（89±ll）nm。于4℃放置1年粒径无明显变化，载药量为3.3%，包封率大于95%。药物体外释放符合Weibull方程。与对照组相比，两种维甲酸固体脂质纳米粒静脉注射后药物在血液中的滞留时间显著延长。结论 超声分散法适用于固体脂质纳米粒的制备。

目的：建立离子交换色谱法测定去甲基斑蝥素乳剂含量的方法。方法：采用HypersilSAX色谱柱（250mm×4.6mm，5μm），以0.3%磷酸一甲醇（75：25）为流动相，流速0.6mL•min-1；检测波长：210nm;柱温：室温。结果：在本色谱条件下测定去甲基斑蝥素线性范围为2～80μg•mL-l，相关系数r=0.9999；高、中、低3个浓度的平均日内精密度RSD值分别为0.41%，0.46%和0.57%，日间精密度RSD分别为4.2%，6.2%和4.5%（n=5），样品测定方法回收率平均为98.9%，最低检测浓度为0.05μg•mL-1。结论：本方法简便快捷、灵敏度高、重现性好。

目的 考察聚卡波菲等11种常用生物黏附性高分子材料的吸水性、黏附力等与制剂学有关的物理性质，为筛选处方提供可靠的依据。方法 采用离心沉降法以溶胀度为指标测定生物黏附性高分子材料的吸水性能，并且考察了高湿条件下它们的吸湿性；评价了生物黏附性高分子材料在水中分散后的流变学性质；采用简便称重法测定体外条件下不同生物黏附性高分子材料的切向黏附力和垂直方向黏附力。结果考 察的11种生物黏附性高分子材料中，溶胀度、吸湿性、黏度、黏附力均以聚卡波菲最大，同浓度下黏附力排列顺序为聚卡波菲、黄原胶、卡波沫（Carbopol1342P）、卡波沫（Carbopol974P）、甲壳素、卡波沫（Carbopol971P）、羟丙基甲基纤维素（MethacelKIOOM）、羧甲基纤维素钠、羟丙基甲基纤维素（MethacelK15M）、明胶和阿拉伯胶。结论 吸水性、吸湿性、黏度及黏附力具有一定的相关性，可以用来筛选处方工艺。

目的：建立生脉粉针剂（麦冬等）中薯蓣皂苷元的高效液相色谱含量测定方法。方法：采用ODSC18柱（5μm，4.6mm×250mm），乙腈-水（88：12）为流动相，流速1.0mL•min-l，测定波长204nm，柱温30℃下对生脉粉针剂中的薯蓣皂苷元进行含量测定。结果：薯蓣皂苷元进样量在2.46～7.38μg范围内线性关系良好（r=0.9999），平均回收率98.3%，RSD为0.95%（n=9）。结论：该方法准确可靠，专属性强，重现性好，可用于制剂的含量测定。