消炎痛对白色念珠菌菌丝形成的影响

目的:探讨环氧化酶抑制剂消炎痛对白色念珠菌形态发育的影响。方法:分别用含不同浓度消炎痛的RPM I1 640加10%小牛血清的液体培养基和玉米-吐温80固体培养基培养3株白色念珠菌,观察白色念珠菌形态发育变化。结果:消炎痛对白色念珠菌芽管和菌丝形成的抑制作用与其剂量相关。在液体培养基中,消炎痛浓度为0.75 mM时可抑制50%芽管形成,浓度为2.0mM时可完全抑制芽管和菌丝形成;而在固体培养基中,消炎痛浓度为1.0mM时可抑制菌丝和厚壁孢子的形成,浓度为2.0 mM时,几乎没有菌丝形成。结论:消炎痛可以抑制白色念珠菌芽管、菌丝的形成,阴道内给予消炎痛将有助于治疗念珠菌性阴道炎。     

替硝唑栓剂的制备及质量控制

OBJECTIVETo prepare tinidazole suppository and establish quality control method. METHODThe suppository were prepared by using PEG-400 and PEG-6000. The tinidazole content in suppository were determined by UV-spectrophometry at 317nm. RESULTSThe tinidazol     

吡喹酮水凝胶栓剂的含量测定

目的:制备吡喹酮水凝胶栓剂,并建立其含量测定方法。方法:用紫外分光光度法测定凝胶栓剂中吡喹酮的含量。结果:吡喹酮在0.2￣1.0mg/ml(r=0.9999)浓度范围内呈良好线性关系。平均加样回收率和相对标准偏差(RSD)为(102.44±0.69)%。结论:该处方设计合理,制备工艺可靠,质量稳定。     

对乙酰氨基酚栓剂人体相对生物利用度和生物等效性

目的:研究进口试验制剂与国产对乙酰氨基酚栓剂(参比制剂)的相对生物利用度和生物等效性.方法:采用HPLC法测定18例健康男性志愿者单次交叉直肠给予参比制剂2粒(300mg)及试验制剂2粒(250mg)后的血药浓度,经CRFB软件处理,计算其药动学参数和相对生物利用度,评价两制剂的生物等效性.结果:试验制剂和参比制剂的t1/2分别为(3.94±1.54)和(3.81±1.24)h;Tmax分别为(1.56±0.57)和(1.58±0.43)h;平均滞留时间MRT0～tn分别为(5.67±1.44)和(5.40±1.28)h;Cmax分别为(1.73±0.38)和(1.61±0.34)μg·mL-1;AUC0～tn分别为(8.01±2.20)和(7.54±1.82)μg·h·mL-1.试验品与参比品的相对生物利用度为(109.07±27.92)%,经统计学处理,试验品AUC0～t的90%置信区间为97.20%～115.85%,Cmax的90%置信区间为98.64%～116.97%.结论:两制剂生物等效.     

HPLC测定腰痛灵栓中桂皮醛的含量及对麝香酮的鉴别

目的建立腰痛灵栓中桂皮醛的含量测定及麝香酮鉴别的方法.方法采用RP-HPLC,以乙腈-0.1%磷酸(38:62)为流动相,在检测波长285 nm处测定桂皮醛含量;以2,4-二硝基苯肼为衍生试剂,乙腈-0.1%磷酸(90:10)为流动相,在检测波长365 nm处鉴定麝香酮.结果桂皮醛平均回收率为98.75%,RSD=2.22%;样品中麝香酮衍生物得到良好分离.结论桂皮醛HPLC含量测定方法可行;麝香酮HPLC鉴别方法可行.     

水杨酸咪唑栓的稳定性考察

目的考察光、温度、湿度等多种因素对水杨酸咪唑栓稳定性的影响。方法建立质量标准,分别进行各影响因素试验、加速试验、室温留样检查观察和分析水杨酸咪唑栓的性状、含量及其他项目。结果本制剂对高湿度、低温(4℃)稳定,但光照对本品外观颜色有一定影响,在高温40～80℃放置会软化变形。结论本品应避光,35℃以下温度保存。     

Potentiation of Reduced Uteroplacental Perfusion Pressure Hypertension in Pregnant Rabbits

Objective: We tested whether indomethacin (IND) potentiates the elevation of blood pressure induced by the reduction of the uteroplacental perfusion pressure (RUPP).

Methods: In pregnant rabbits on the 21st day of the 30-day gestation, the uteroplacental perfusion pressure was reduced by 68 ± 5% using a clip placed on the abdominal aorta below the renal arteries. IND suppositories (15 mg/kg each) were administered 1 and 2 days following surgery.

Results: After the second dose, MAP of IND-treated RUPP rabbits was higher (92 ± 9 mm Hg, n = 10) than in those receiving placebo (78 ± 12, n = 9, P <. 01). MAP of sham-operated pregnant rabbits with or without IND was 61 ± 9 and 58 ± 8 mm Hg, respectively (NS). Placebo-treated RUPP animals evidenced an enhanced urinary sodium excretion as compared to nor-motensive control rabbits receiving placebo (3.27 ± 0.69 mmol/kg/day vs. 1.49 ± 0.74, P <. 001). Enhanced urinary sodium excretion was blunted by IND in RUPP rabbits (1.25 ± 0.37, P <. 001).

Conclusion: (1) IND potentiates the hypertensive response induced by RUPP. (2) the reduction of urinary sodium excretion may be one of the several pharmacological effects of IND aggravating hypertension in this state.     

Development and characterisation of levosulpiride-loaded suppositories with improved bioavailability in vivo

The purpose of this study was to develop and characterize levosulpiride loaded liquid suppository with improved bioavailability. The content of levosulpiride-loaded liquid suppositories were optimized in a series of experiments using various weight ratios of P188, P407, Tween 80, and drug. The suppositories were liquid at room temperature, however, when rectally administered, they became gel at body temperature. Their rheological properties and release characteristics were determined in vitro while pharmacokinetic study was performed after its rectal administration in rats and compared with drug suspension. Poloxamer 188 and Twee 80 decreased the gelation temperature and gelation time, but increased the gel strength and mucoadhesive force of liquid suppositories. Liquid suppository composed of [Levosulpiride/P 188/P 407/Tween 80 (1/15/17/3%)] with a gelation temperature of about 30.7?°C remained liquid at 25?°C, but converted to gel at 30–36.5?°C, resulting in easy administration and rapid gelation inside the body. This liquid suppository gave a considerably increased dissolution rate reflected in a meaningfully higher plasma concentration and 7.1-fold AUC values of levosulpiride in rats as compared to the drug suspension. Hence, liquid suppository system could be used for enhanced bioavailability of levosulpiride-loaded pharmaceutical products.