Porosity asymmetric membrane capsules were prepared to study the relationship between the capsule formulation and drug release. Cellulose acetate (CA) and pore formers were used in the capsule shell formulation as the main semipermeable membrane material. The capsules were permeable to both water and dissolved solutes. Using sparingly soluble drug acetaminophen as a model, cumulative release was calculated. The slope of the release profile from the distilled water had good relationship with the concentration of the pore formers F68. The release of acetaminophen was independent to the pH, osmotic pressure of dissolution medium, but influenced by intensity of agitation. When the concentration of pore former was low, zero-order release behavior was observed within 24 h which was consistent with Fickian diffusion model. When the concentration of pore former was high, however, Higuchi model release was found which is caused by Fickian diffusion and osmotic pressure release. With scanning electron microscope (SEM), the surface structure and cross-section of the capsule shell were also studied before and after drug delivery. With simple preparation and broad scope of drug application, porosity asymmetric membrane capsules can give desired drug extended release and show more convenience than controlled tablets with laser drilling.

目的:制备盐沙格雷酯不对称膜胶囊剂并研究其体外释药规律.方法:以盐酸沙格雷酯为药物模型,醋酸纤维素为囊膜材料,加入致孔剂F68,PEG-400为增塑剂,丙酮:乙醇=4:1为溶媒,采用蘸胶工艺制备囊壳.通过实验选择不同的致孔剂比例,研究其药物释放规律.结果:以60％、80％、100％ F68为致孔剂制备的胶囊,药物在24 h时有90％以上从不对称膜胶囊中释放；致孔剂F68比例为40％时,药物释放符合零级方程,致孔剂比例为100％时,药物释放符合Higuchi方程.结论:药物盐酸沙格雷酯在致孔剂含量低的不对称膜胶囊中呈缓释释药,在致孔剂含量高的不对称膜胶囊中呈控释释药.

目的:通过考察不同处方和工艺制备的吲哚美辛海藻酸钠-壳聚糖-海藻酸钠(ACA)微囊的体外释放,研究影响囊膜通透性及膜强度的因素。方法:以吲哚美辛为模型药物,采用不同的交联剂氯化钙、氯化钡,改变海藻酸钠、壳聚糖、柠檬酸钠浓度及制备工艺来制备微囊,以药物的体外释放曲线来评价囊膜的通透性,通过超声破碎评价微囊的强度。结果:影响微囊中药物释放的主要因素为处方中的交联剂,提高海藻酸钠、壳聚糖浓度、降低液化囊心时间,微囊通透性下降;氯化钙为交联剂制备的微囊强度较小。结论:通过处方和工艺调节有望得到通透性和膜强度适宜的ACA微囊。

Objective: To prepare porous membrane osmotic pump capsules and investigate the factors influencing release behavior.Methods: With cellulose acetate(CA)as capsule materials,PEG-400 and PEG-2000 as plasticizer and pore former,shell of osmotic pump capsules was prepared by dip plastic method.Different pore-forming materials and osmogents influencing release behavior were investigated with paracetamol as a model drug and the factors were identified by werapamil hydrochloride and sarpogrelate hydrochloride.surface and cross-section of capsule shell were also studied under scanning electron microscope.Results: Porosity membrane osmotic pump capsules can control the release of drug during a desired time according to optimise the pore former contents and osmogents,respectively.Conclusion: Porous membrane osmotic pump capsules enjoy more advantages than ordinary osomotic tablets,which showed poten-tial to be a new controlled-release drug delivery system.

OBJECTIVE: To establish the method for the content determining of Indomethacin colon-targeting capsule in artificial colon juice. METHODS: RP-HPLC method was adopted. The determination was performed on Hypersil ODS2 C18 column with mobile phase consisted of acetonitrile-0.1 mol·L-1 glacial acetic acid(60 ∶ 40) at flow rate of 1 mL·min-1. The detection wavelength was set at 228 nm and the column temperature was 25 ℃. The injection volume was 20 μL. RESULTS:The linear range of indomethacin was 2.0～50.0 μg·mL-1(r=0.999 9). The recovery rates of it at low, medium and high concentrations were 100.37%,99.87%,100.00% with RSD of 0.29%, 0.31%, 0.74%, respectively. CONCLUTION: The method is accurate, reliable and precision for the content determination of indomethacin in artificial colon juice.