HPLC法测定罗格列酮缓释片的含量

目的建立测定罗格列酮缓释片含量的方法。方法采用高效液相色谱法,以十八烷基硅烷键合硅胶为固定相,0.05 mol/L醋酸钠(用冰醋酸调pH 6.0)-甲醇(体积比25∶75)为流动相,检测波长247 nm,测定盐酸罗格列酮缓释片的含量。结果盐酸罗格列酮在10.15~60.90μg.mL浓度范围内有良好的线性关系(r=0.9998),回收率为100.3%(RSD=0.65%)。结论本法测定罗格列酮缓释片的含量,结果准确,可行。     

蔗糖基聚合物作为缓释片剂载体的应用研究

目的:研究蔗糖基聚合物作为缓释片的载体的可行性.方法:以不同相对分子质量的蔗糖基聚合物为载体制备非诺络芬钙的缓释片,于1～12 h定时地以紫外分光光度法测定缓释片在人工肠液中的释放度,绘制释放度随时间变化的释放曲线.结果:12 h内非诺络芬钙在人工肠液中能够平稳地缓慢释放,蔗糖基聚合物的相对分子质量越大,释放速率越慢.结论:蔗糖基聚合物可以作为缓释片的载体,其中以MW=79.4K的缓释效果最佳.     

全反式维甲酸-聚酸酐长效缓释剂研制及可行性分析

目的：以可生物降解高分子材料聚酸酐(Polyanhydrides,PAD) 作载体,包埋全反式维甲酸（ATRA）,研制长效缓释微球ATRA-PAD肿瘤治疗剂。建立高效液相色谱法(HPLC)测定体系,以检测缓释治疗剂中ATRA含量,探讨体内外ATRA经时缓释变化规律。方法：采用乳剂一扩散溶剂挥发法制备维甲酸长效缓释微球ATRA-PAD肿瘤治疗剂,扫描电镜检测微球外观及微球粒径,HPLC检测微球载药量、包封率及体内外释药量。结果：所制治疗剂微球光滑圆整,大小均一,平均粒径：(154．42?6.76) nm,载药率：(16.52?1.45)％,包封率：(87.84?.79)％;体外释放实验证明该微球治疗剂可持续释放ATRA约50天,将其肌肉注射到大耳白兔体内,可稳定缓释ATRA近约45天。结论：ATRA-PAD治疗剂制备工艺合理,载药量及包封率均较高,体内外释药释药平稳并且具有明显的长效缓释作用。     

一金颗粒对动物小肠与急性胰腺炎的药理作用

目的：观察一金颗粒的药效学作用。方法：通过不同动物观察一金颗粒对小肠与急性胰腺炎的药理作用，采用（1）墨汁法观察一金颗粒对小鼠肠蠕动的作用；（2）离体肠肌试验观察一金颗粒对家兔离体肠肌的作用；（3）毛细血管通透性试验观察一金颗粒对小鼠毛细血管通透性的作用；（4）3％牛磺胆酸钠胰腺被膜下注射复制急性胰腺炎模型，观察一金颗粒对急性胰腺炎大鼠的治疗作用。结果：（1）小鼠肠内墨汁的推进率在大、中剂量组明显高于阴性对照组，而小剂量组略有增加；（2）能增加肠肌蠕动的幅度和频率，其中以频率增加为主；（3）各剂量组均可使小鼠毛细血管通透性降低；（4）3、6h各剂量组均可使血淀粉酶较模型有显著降低。结论：一金颗粒具有一定的增加肠蠕动．抗炎及抗胰腺炎的作用。     

克拉霉素缓释胶囊人体相对生物利用度研究

 目的建立人血浆中克拉霉素浓度测定的LC-MS/MS方法,研究克拉霉素缓释胶囊与市售克拉霉素缓释片的药动学及人体相对生物利用度。方法以罗红霉素为内标,用乙醚-二氯甲烷(3∶2)提取处理,以甲醇-水-甲酸(80∶20∶0.05)为流动相,用C18柱分离,采用ESI源,正离子方式检测,扫描方式为多反应监测(MRM)。结果克拉霉素线性范围为10.0～4000μg·L^-1,日内、日间RSD均小于15%。应用此方法研究18名健康受试者口服0.5g受试制剂和参比制剂的药动学参数。单剂量口服受试制剂和参比制剂的t_max,ρ_max,t_1/2,AUC_0-t,AUC_0-∞,CL和Vd分别为:(5.36±1.14)和(5.25±0.88)h,(1218±433)和(1333±370)μg·L^-1,(4.59±1.67)和(4.24±2.10)h,(8239±1553)和(8467±1364)μg·h·L^-1,(8662±1829)和(8795±1331)μg·h·L^-1,(60.9±15.1)和(58.9±11.3)L·h^-1和(382±103)和(366±224)L。多剂量口服受试制剂和参比制剂的t_max,ρ_ssmax,ρ_ssmin,ρ_av,AUC_ss和DF分别为:(5.31±1.11)和(5.28±0.96)h,(1387±396)和(1488±401)μg·L^-1,(64.6±26.8)和(70.1±30.0)μg·L^-1,(399±99.2)和(410±107)μg·L^-1,(9585±2382)和(9830±2578)μg·h·L^-1,(3.32±0.62)和(3.49±0.66)。单剂量和多剂量相对生物利用度分别为(98.2±16.3)%和(99.5±19.0)%。结论本法快速、准确、专属、灵敏。统计结果表明,两制剂人体内相对生物利用度无显著性差异(P>0.05)。     

Anti-inflammatory activity of Albizia lebbeck Benth., an ethnomedicinal plant, in acute and chronic animal models of inflammation

Aim of the study

Albizia lebbeck Benth. is used both in Indian traditional system and folk medicine to treat several inflammatory pathologies such as asthma, arthritis and burns. The aim of the present study was to evaluate the scientific basis of anti-inflammatory activity of different organic solvent extracts of Albizia lebbeck.

Materials and methods

The anti-inflammatory activity of Albizia lebbeck was studied using the carrageenan, dextran, cotton pellet and Freund's complete adjuvant induced rat models. The extracts obtained using petroleum ether, chloroform and ethanol were administered at the concentrations of 100, 200 and 400 mg/kg body weight.

Results

The petroleum ether and ethanol extracts at 400 mg/kg, showed maximum inhibition of inflammation induced by carrageenan (petroleum ether—48.6%; ethanol—59.57%), dextran (petroleum ether—45.99%; ethanol—52.93%), cotton pellet (petroleum ether—34.46%; ethanol—53.57%) and Freund's adjuvant (petroleum ether—64.97%; ethanol—68.57%).

Conclusion

The marked inhibitory effect on paw edema shows that Albizia lebbeck possesses remarkable anti-inflammatory activity, supporting the folkloric usage of the plant to treat various inflammatory diseases.     

The effect of the aqueous extract of Helietta parvifolia A. Gray (Rutaceae) stem bark on carrageenan-induced paw oedema and granuloma tissue formation in mice

Aims of study

Despite the ethnopharmacological relevance of Helietta parvifolia A. Gray (Rutaceae) in Mexico, we found no significant pharmacological studies of this plant in the scientific literature. The aim of the present study was to establish the anti-inflammatory effect of an aqueous extract of the stem bark of Helietta parvifolia in mice.

Materials and methods

The anti-inflammatory activity of the aqueous extract of the stem bark of Helietta parvifolia was evaluated using carrageenan-induced paw oedema in mice, and the cotton pellet granuloma method.

Results

An extract dose ranging from 20 to 80 mg/kg p.o. showed a non-significant effect over the initial phase of carrageenan-induced oedema. However, it showed a significant inhibition of oedema after 3 h, which can be related to the inhibition of the release of kinin-like substances. An ID₅₀ value of 47.4 mg/kg was obtained for the plant extract. The extract also suppressed granulomatous tissue formation during chronic inflammation. The inhibitory values were 19.2, and 22.2, corresponding to 40 and 80 mg/kg doses of extract respectively.

Conclusions

Aqueous extract showed a statistically significant anti-inflammatory effect in mice during the late phase of acute inflammation and during chronic inflammation. However, the exact mechanism(s) of anti-inflammatory effects of Helietta parvifolia observed in this study remains unclear.     

采用多元定时释药技术制备雷公藤胃漂浮缓释胶囊的研究

目的:采用多元定时释药技术制备雷公藤胃漂浮缓释制剂.方法:采用挤出滚圆法,以90%十八醇为助漂剂制得空白胃漂浮微丸.使用流化床包衣设备,制备载药胃漂浮微丸.再以低取代羟丙基纤维素作为内溶胀层材料,以乙基纤维素水分散体作为外控释层材料进行包衣制备胃漂浮定时释药包衣微丸.等量称取控释层包衣增重分别为0%,8%,12%,15%,22%的包衣微丸,混均装入硬胶囊中,即得雷公藤胃漂浮缓释胶囊.结果:当溶胀层处方及用量固定后,通过控制控释层的厚度,可使包衣微丸在预期的不同时间定时释药.将几种控释层增重不同的包衣微丸混合后制成雷公藤胃漂浮缓释胶囊,在溶出介质中,均立即起漂,包衣微丸8 h漂浮率大于80%,并于不同时间依次释药,从而在整体上呈现出一种缓释特征.结论:采用多元定时释药技术制备而成的雷公藤胃漂浮缓释胶囊具有良好的漂浮性能和缓释特性.     

复方奥硝唑甲磺酸培氟沙星缓释牙栓的缓释抑菌作用的评价

目的 观察复方奥硝唑甲磺酸培氟沙星缓释牙栓的缓释、抑菌作用.方法 采用Kirby-Bauer纸片扩散法进行复方缓释牙栓的缓释、细菌敏感稳定性、基质影响试验. 结果复方奥硝唑甲磺酸培氟沙星缓释牙栓对牙龈卟啉单胞菌等几个菌种有明显的缓释作用,缓释时间可达12 h以上.将该牙栓4 ℃存放6个月后,仍有明显的抑菌作用,与半年前的抑菌环进行比较,无显著性差异(P＞0.05).但对于基质影响试验,加入基质组对金黄色葡萄球菌、牙龈卟啉单胞菌、具核梭杆菌、消化链球菌的抑菌作用相对减弱(P＜0.05),而对表皮葡萄球菌、中间普氏菌、变形链球菌抑菌环无显著性差别( P＞0.05).结论 复方奥硝唑甲磺酸培氟沙星缓释牙栓对牙周致病菌有明显的缓释、稳定的抑菌作用以及基质影响较小,稳定性较好.     

高效液相色谱法测定盐酸右哌甲酯缓释微丸的有关物质及含量

目的：应用高效液相色谱技术建立盐酸右哌甲酯缓释微丸有关物质检查和含量测定的方法。方法采用Agilent ZORBAX SB-C18色谱柱（250 mm ×4．6 mm,5μm）;磷酸二氢钾溶液[25 mmol／L,三乙胺0．2％（v／v）,磷酸调至pH 3．5]－甲醇（65∶35）为流动相,检测波长209 nm,流速1．0 ml／min,柱温40℃。结果在选定的色谱条件下,盐酸右哌甲酯与相关杂质分离良好,制剂辅料不干扰盐酸右哌甲酯的测定;检测限为81．12 ng／ml（S／N＝3）,在质量浓度2～30μg／ml范围内,盐酸右哌甲酯与峰面积线性关系良好,相关系数r为0．9995;平均回收率为100．83％,溶液在12 h内保持稳定（ RSD为0．10％）。结论该方法简便、准确、专属性强,可用于盐酸右哌甲酯缓释微丸有关物质及其含量的测定。