氟罗沙星与替硝唑注射液配伍的稳定性考察

目的：考察氟罗沙星注射液与替硝唑注射液、替硝唑葡萄糖注射液配伍的稳定性。方法：模仿临床常用的浓度，在25℃和37℃避光或室内自然光条件下，观察氟罗沙星分别与替硝唑、替硝唑葡萄糖注射液配伍6h内混合液的外观、pH值及氟罗沙星和替硝唑的含量变化。结果：氟罗沙星注射液与替硝唑注射液混合，2h 内有白色沉淀产生；与替硝唑葡萄糖注射液混合，6h内混合液外观、pH值、氟罗沙星和替硝唑的含量均变化不大。结论：氟罗沙星注射液与替硝唑注射液不可配伍使用，与替硝唑葡萄糖注射液可配伍使用。     

甲磺酸帕珠沙星与利巴韦林注射液在葡萄糖注射液中的配伍稳定性

目的考察注射用甲磺酸帕珠沙星与利巴韦林注射液在葡萄糖注射液中的配伍稳定性。方法采用紫外分光光度法,测定注射用甲磺酸帕珠沙星与利巴韦林注射液在5％葡萄糖中配伍后,在室温（22℃）下6h内甲磺酸帕珠沙星与利巴韦林含量变化,观察外观并测定pH值。结果两种药物配伍后,6h内外观、pH值及含量均无明显变化。结论注射用甲磺酸帕珠沙星与利巴韦林注射液在5％葡萄糖注射液中配伍后6h内可以使用。     

头孢他啶与利巴韦林的配伍稳定性

目的：考察注射用头孢他啶与利巴韦林注射液在0．9%氯化钠及5％葡萄糖注射液中的配伍的稳定性。方法：在室温[（25±1）℃]条件下，观察两药配伍后的外观、pH值变化，并用紫外分光光度法测定头孢他啶与利巴韦林的含量。结果：两药配伍后，4h内的外观、pH值及含量均无明显变化。结论：头孢他啶可在0．9％氯化钠及5％葡萄糖注射液中与利巴韦林注射液配伍应用。     

氟罗沙星葡萄糖注射液与4种止血药配伍的稳定性考察

目的考察氟罗沙星葡萄糖注射液与4种止血药配伍的稳定性。方法分别在20℃及37℃;自然光与避光环境下,模拟临床常用的浓度,观察氟罗沙星葡萄糖注射液与氨甲苯酸、酚磺乙胺、肾上腺色腙及氨基己酸注射液配伍6h内混合液的外观、pH值和氟罗沙星含量的变化。结果氟罗沙星葡萄糖注射液与酚磺乙胺注射液混合时,马上出现白色混浊,产生沉淀;与肾上腺色腙注射液混合时,马上出现橙红色凝乳状沉淀;与氨基己酸注射液混合时,1h内有白色沉淀产生;与氨甲苯酸注射液混合,在避光条件下6h内混合液外观、pH值、含量均无明显改变。结论氟罗沙星葡萄糖注射液与酚磺乙胺、肾上腺色腙和氨基己酸注射液不能配伍使用;与氨甲苯酸注射液配伍,在避光条件下,6h内性质稳定。     

探究喜炎平注射液与氟罗沙星配伍的稳定性

目的:针对喜炎平注射液与氟罗沙星配伍稳定性进行探讨。方法:观察溶液配伍后的外观色泽、含量、pH值、微粒数等变化情况,采用高效液相色谱仪检测配伍后溶液的两组份含量。结果:在常温条件中,喜炎平注射液在5%葡萄糖注射液与氟罗沙星配伍后6小时内外观无明显变化,喜炎平注射液主要成分穿心莲内酯磺化物的含量下降明显,而氟罗沙星的含量未见明显变化,不溶性微粒在指定范围内有所增加;配伍后溶液的pH值也有明显下降。结论:喜炎平注射液在5%葡萄糖注射液中与氟罗沙星不可以配伍使用。     

氟罗沙星与莪术油葡萄糖注射液配伍的稳定性考察

目的:考察氟罗沙星注射液与莪术油葡萄糖注射液配伍的稳定性.方法:采用分光光度法测定混合液中氟罗沙星与莪术油含量的变化情况.结果:混合液在0～6 h内外观、pH值、微粒数及含量均无明显变化.结论:两药按治疗剂量配伍并于6 h内静脉滴注完毕是安全有效的.     

氟罗沙星葡萄糖注射液与11种药物配伍的稳定性考察

目的考察氟罗沙星葡萄糖注射液与11种注射液配伍的稳定性。方法模拟临床常用药物质量浓度分别将注射用头孢唑啉钠等11种药物与氟罗沙星葡萄糖注射液进行配伍实验,观察配伍后在22℃下0,1,2,3h后药液外观性状及pH值变化,并以紫外分光光度法在286nm波长处测定氟罗沙星含量。结果氟罗沙星葡萄糖注射液与注射用头孢唑啉钠配伍2h后产生白色颗粒状沉淀,二者不能配伍;与酚磺乙胺注射液配伍10min后产生白色针状结晶,二者不能配伍;与维生素C注射液、三磷酸腺苷二钠注射液配伍后外观颜色由黄色立即变淡近无色;其余各药液均无外观性状及pH值变化。紫外分光光度法测定氟罗沙星含量在22℃下3h后均在90.0%～110.0%范围内变化。结论氟罗沙星葡萄糖注射液除与注射用头孢唑啉钠、酚磺乙胺注射液不能配伍使用外,与其他9种药物3h内配伍稳定,无理化配伍禁忌。     

注射用氟罗沙星在葡萄糖注射液中的稳定性考察

目的考察注射用氟罗沙星在葡萄糖注射液中的稳定性。方法模拟临床用药浓度,将注射用氟罗沙星加入5%、10%葡萄糖注射液中,室温下避光放置,用紫外分光光度法测定不同时间配伍液的吸收度(A),同时检查配伍液的pH值、外观变化。结果配伍液在24h内外观、pH值、紫外吸收光谱、含量等基本不变。结论注射用氟罗沙星与葡萄糖注射液配伍,室温避光条件下24h内稳定,可提前配制。     

利巴韦林注射液与3种常用输液的配伍稳定性

目的研究室温6h内利巴韦林注射液与50g·L-1葡萄糖注射液、9g·L-1氯化钠注射液和复方葡萄糖氯化钠注射液的配伍稳定性,为临床用药提供科学依据。方法采用反相高效液相色谱法测定利巴韦林注射液与输液配伍后,6h内利巴韦林的含量及有关物质,同时考察配伍液的外观和pH值。结果利巴韦林与输液配伍6h后,外观、pH值、含量和有关物质均无明显变化。结论利巴韦林注射液可与50g·L-1葡萄糖注射液、9g·L-1氯化钠注射液和复方葡萄糖氯化钠注射液配伍使用。     

头孢米诺钠与利巴韦林配伍稳定性考察

目的分别于25℃和37℃条件下考察头孢米诺钠与利巴韦林注射液在0．9％氯化钠注射液（NS）及5％葡萄糖注射液（5％GS）中8h内的配伍稳定性。方法采用紫外分光光度法测定配伍后8h内不同时间点配伍液中头孢米诺钠与利巴韦林的含量，同时考察配伍后pH值、外观及吸收曲线的变化。结果配伍液在8h内外观、pH值及含量无明显变化。结论两药在NS及5％GS中配伍稳定性良好。     

磷酸吡哆醛的差热分析法鉴定

目的:改进多效胃镜乳的处方,提高多效胃镜乳的稳定性,控制制剂的质量。方法:通过外观质量、显微镜检、离心试验、耐寒耐热试验、常温留样以及含量测定等为指标,考察不同的乳化剂对多效胃镜乳质量的影响,确定最优处方。结果:以0．8％司盘-80、1．6％西黄蓍胶和5％司盘-80、2％CMC-Na配制的多效胃镜乳,稳定性好。结论:改进后的多效胃镜乳处方可应用于制剂生产。     

多效胃镜乳的处方改进及稳定性考察

目的改进多效胃镜乳处方，提高多效胃镜乳的稳定性，控制制剂的质量。方法通过外观质量检查、显微镜观察、离心试验、耐寒耐热试验、常温留样及含量测定等，考察了不同乳化剂对多效胃镜乳质量的影响，确定最优处方。结果以0．8％司盘-80，1．6％西黄蓍胶和5％司盘-80，2％CMC—Na配制的多效胃镜乳稳定性好。结论改进后的多效胃镜乳处方可用于制剂生产。     

多效胃镜乳的制备与临床应用

目的：研究多效胃镜乳的处方、制备工艺、质量标准及临床疗效。方法：用研磨乳化法将油相和水相混合制备成乳剂，并对其稳定性、主药含量进行测定。对506例胃镜检查患者进行疗效观察。用法：胃镜检查前30 min口服，每次10 mL。结果：一次性口服给药，同时达到局麻、解痉、消泡、减少分泌、润滑等多种效果，总有效率达100.0%。结论：多效胃镜乳处方合理、工艺成熟、质量稳定、疗效显著，值得推广使用。     

正交设计法优选多效胃镜乳的制备工艺

目的优选多效胃镜乳的制备工艺。方法以乳剂的稳定性和外观为考察指标,以乳化剂用量、水相（未加单糖浆）pH和乳化温度为可变因素,用L9（3^4）表进行正交试验。结果最优的制备工艺是7mL乳化剂司盘-80和14g西黄蓍胶,水相（未加单糖浆）pH=4,乳化温度85℃。结论按最佳工艺制备的多效胃镜乳符合2000年版《中国药典》的规定。     

镰形棘豆总黄酮霜剂的处方筛选及稳定性考察

目的筛选镰形棘豆总黄酮霜剂的处方,并考察各产品的稳定性。方法选取组成不同的水包油（O/W）乳膏基质,采用研和法制备霜剂。采用外观、显微观察、含量变化等方面评价各处方的优劣及产品的稳定性。结果以硬脂酸3g、白凡士林3 g、单硬脂酸甘油酯1 g、司盘-60 0.8 g、液体石蜡4.5 g为油相,吐温-80 2.5 g、甘油5 g、尼泊金0.1 g、蒸馏水40ml为水相制得的霜剂具有良好的稳定性,易涂抹、易清洗,质量稳定。结论镰形棘豆总黄酮霜剂的处方得到了优选,产品质量稳定。     

超细胃镜在胆管疾病诊治中的应用效果

目的 探讨超细胃镜在胆管疾病诊治中的应用价值。方法 以2013年2月至2015年2月河南大学第一附属医院接受胃镜检查的60例胆管疾病患者为研究对象,随机双盲法将其分为十二指肠镜组（36例）与超细胃镜组（24例）,比较两组患者围检查期生命体征变化、反应分级,同时观察记录超细胃镜插镜情况及检查结果。结果 超细胃镜组24例一次性操作成功率100.0%,进镜视野A级占95.8%。3例超细胃镜直视下活检证实为腺瘤恶性病变,12例巨大嵌顿直视下激光碎石成功,3例疑似残余结石通过单纯胆总管探查排除结石残留。无胆管炎等并发症发生。超细胃镜组患者检查中收缩压为（96.40±9.18）mmHg,血氧饱和度为（97.85±1.37）%,优于十二指肠镜组的（103.42±10.74）mmHg、（95.71±3.05）%,差异均有统计学意义（P<0.05）;超细胃镜与十二指肠镜检查,患者反应分级差异无统计学意义（P>0.05）。结论 超细胃镜作为经口胆道镜诊治胆管疾病安全可行。     

Influence of phenolic acids on the storage and digestion stability of curcumin emulsions based on soy protein-pectin-phenolic acids ternary nano-complexes

Abstract

Aim: To design novel emulsifiers with the ability to improve the storage and digestion stability of curcumin emulsions, besides to investigate the influence of phenolic acids types on the emulsify ability of soy protein-pectin-phenolic acids complexes obtained by ultrasonication.

Methods: The ternary complexes were characterised by particle size, morphology, zeta potential, X-ray diffraction, Fourier transform infra-red and fluorescence spectroscopy. Additionally, changes in droplet size, charge, and microstructure were monitored as quantitative stability index of curcumin emulsions.

Results: Phenolic acid types significantly affected the formation of ternary complexes. Soy protein-pectin-ferulic acid complex (S-P-F) stabilised curcumin emulsion had the best emulsifying property, followed by soy protein-pectin- ellagic acid (S-P-E), and soy protein-pectin-tannic acid complexes (S-P-T). Moreover, S-P-F emulsion was found to retain efficiently cucumin within 30?days storage (77.35%) and simulated gastrointestinal tract (64.09%).

Conclusion: Protein-polysaccharide-phenolic acids emulsions are effective oral delivery systems for hydrophobic bioactives.     

A novel vesicular transdermal delivery of nifedipine – preparation,characterization and in vitro/in-vivo evaluation

Abstract

Nifedipine is a calcium channel blocker extensively used in the treatment of anginal and hypertension. On oral administration it undergoes extensive first pass metabolism, which outweighs its absorbance through gastrointestinal tract (GIT) and bioavailability of the drug in systemic circulation. As an alternative to oral route transdermal route of drug delivery was developed. In the present investigation, proniosomes are prepared by varying the ratio of span-40, lecithin, aqueous phase and polymer. Formulation containing span-40, lecithin, isopropyl alcohol, 0.1% glycerol (5:5:4) and HPMC (2%) showed smaller vesicle size, high entrapment efficiency. The niosomal formation after hydration and their surface morphology of optimized formulation was studied by Motic and transmission electron microscopy. FTIR and differential scanning calorimetry studies were performed to unravel and understand the solid state properties of the drug and chemical interaction with formulation excipients. The ex-vivo Franz-diffusion studies were carried out in pH 6.8 using rat skin and the results showed better permeability of niosomes with good steady state flux and enhancement ratio suggesting the potential of proniosomal carriers for improved transdermal delivery of nifedipine. Skin irritation studies for 7 days, showed that the drug when formulated as proniosomes to be non-irritant with no erythemia development compared to pure drug. From the bio-distribution studies, the vesicles prepared with hydroxy propyl methyl cellulose with span-40 was found to be ideal batch as the concentration of drug at target site was higher.     

Formulation Development and Antitumor Activity of a Filter-Sterilizable Emulsion of Paclitaxel

Purpose. Paclitaxel is currently administered i.v. as a slow infusion of asolution of the drug in an ethanol:surfactant:saline admixture. However,poor solubilization and toxicity are associated with this drug therapy.Alternative drug delivery systems, including parenteral emulsions, areunder development in recent years to reduce drug toxicity, improveefficacy and eliminate premedication. Methods. Paclitaxel emulsions were prepared by high-shearhomogenization. The particle size of the emulsions was measured by dynamiclight scattering. Drug concentration was quantified by HPLC and invitro drug release was monitored by membrane dialysis. The physicalstability of emulsions was monitored by particle size changes in boththe mean droplet diameter and 99% cumulative distribution. Paclitaxelpotency and changes in the concentration of known degradants wereused as chemical stability indicators. Single dose acute toxicity studieswere conducted in healthy mice and efficacy studies in B16 melanomatumor-bearing mice. Results. QW8184, a physically and chemically stable sub-micronoil-in-water (o/w) emulsion of paclitaxel, can be prepared at high drugloading (8-10 mg/mL) having a mean droplet diameter of <100 nmand 99% cumulative particle size distribution of <200 nm. In vitro release studies demonstrated low and sustained drug release both inthe presence and absence of human serum albumin. Based on singledose acute toxicity studies, QW8184 is well tolerated both in miceand rats with about a 3-fold increase in the maximum-tolerated-dose(MTD) over the current marketed drug formulation. Using the B16mouse melanoma model, a significant improvement in drug efficacywas observed with QW8184 over Taxol^®. Conclusions. QW8184, a stable sub-micron o/w emulsion of paclitaxelhas been developed that can be filter-sterilized and administered i.v.as a bolus dose. When compared to Taxol^®, this emulsion exhibitedreduced toxicity and improved efficacy most likely due to thecomposition and dependent physicochemical characteristics of the emulsion.     

Interfacial Properties as Stability Predictors of Lecithin-Stabilized Perfluorocarbon Emulsions

ABSTRACT

The purpose of this study was to determine whether the addition of small quantities of minor lecithin components (phosphatidylinositol, phosphatidic acid, lysophosphatidylethanolamine, and cholesterol) and Pluronic F68 to lecithin could improve the stability of lecithin-stabilized perfluorocarbon emulsions. Attempts were made to correlate emulsion stability with interfacial properties (tension and charge). Dynamic interfacial tension was determined using a Teflon Wilhelmy plate method [reported previously (1)]. Emulsions were prepared by microfluidization. Microelectrophoresis was used to measure emulsion droplet charge, and photon correlation spectroscopy and Coulter analysis were used to determine emulsion stability as a function of droplet size. Thermal kinetic accelerated stability testing was conducted. Various droplet size parameters were used to compare emulsion stabilities, and an overall stability ranking, based on these parameters, was obtained for each emulsion. Small quantities of additives altered emulsion stability and these data were correlated with interfacial properties and initial droplet diameters. The addition of cholesterol to lecithin resulted in the most stable perfluorocarbon emulsion.