醋酸泼尼松龙脂质纳米球的制备

目的:制备高分散、高包封率的醋酸泼尼松龙脂质纳米球(PA-LN).方法:采用高速匀质法,制备脂质纳米球.探讨其制备工艺条件及影响因素.结果:制得的醋酸泼尼松龙脂质纳米球粒径在28.6 nm左右,粒度分布15～45 m;包封率大于70%.结论:本方法制备工艺简单,稳定性好,分散性好,包封率较高.     

纳米乳的研究及其在制剂学领域的应用

综述纳米乳的制备方法及其粒径和稳定性的影响因素以及在制剂学领域的新应用。纳米乳是由油相、水相、乳化剂和助乳化剂组成的透明或者半透明系统。粒径为10-100nm，具有很窄的粒径分布。近年来成为药剂学领域的研究热点。     

利多卡因纳米乳的制备及质量控制

目的制备利多卡因纳米乳并建立其质量控制的方法.方法伪三元相图法结合origin 7.0软件分析确定制备5%利多卡因纳米乳的最佳Km值(表面活性剂/助表面活性剂)及各组分的比例;对利多卡因纳米乳的外观及稳定性进行考察;马尔文Zeta粒径分析仪测定利多卡因纳米乳粒径大小及分布范围;透射电镜观察利多卡因纳米乳的形态及体系类型;HPLC法对利多卡因纳米乳进行质量控制考察.结果Km=3时利多卡因纳米乳形成区域的面积值最大,利多卡因纳米乳的平均粒径为36.4 nm,其中98%的粒径范围介于17.1～57.5 nm之间,2%介于77.9～261.3 nm之间;其分布体系为大小不均的球形多分散体系;利多卡因进药量与色谱峰面积在10～200 mg·L-1范围内线性关系良好(r=0.999 4),平均回收率为99.45%,RSD为1.08%.结论伪三元相图法结合origin 7.0软件分析并确定利多卡因纳米乳各组分比例的方法简便、准确;马尔文粒径测定结合透射电镜观察测定利多卡因纳米乳的粒径、分布、形态及体系类型的方法较为全面;利多卡因纳米乳样品的处理和HPLC测定方法简便、快速、准确,可作为利多卡因纳米乳的质量控制考察.     

多西他赛纳米乳注射液的制备与质量控制

目的制备多西他赛纳米乳注射液,并对其质量进行控制。方法采用高压均质法制备多西他赛纳米乳注射液;在最佳处方的基础上,考察工艺因素对纳米乳剂的性质及稳定性的影响,并对其理化性质进行考察。结果多西他赛纳米乳注射液载药量为2 g.L-1,粒径为(46.7±35.0)nm,含量质量分数为96.69%;与质量分数为0.9%的氯化钠配伍后24 h内使用安全;在(4±2)℃条件下,稳定性良好。结论该处方及工艺可行,所制备的多西他赛纳米乳注射液质量稳定,使用方便,具有临床应用价值。     

薄荷素油纳米乳的制备

目的：研究探索制备薄荷素油纳米乳的处方。方法：采用转向法制备薄荷素油纳米乳,通过滴定法绘制伪三元相图,以纳米乳区域的面积、稳定性为考察指标,筛选薄荷素油纳米乳最佳处方。通过稀释法鉴定薄荷素油纳米乳类型、透射电子显微镜观察其外观形态、激光粒度测定仪测定其粒径分布、电位。结果：薄荷素油纳米乳优选处方结果为：表面活性剂为蓖麻油聚氧乙烯醚（EL-40）、助表面活性剂为聚乙二醇400（PEG-400）,K_m为3：1,薄荷素油、复表面活性剂、蒸馏水含量为56.62%：23.67%：19.72%;所制得薄荷素油纳米乳为澄清透明,平均粒径为19.55 nm,PDI为0.183,呈正态分布,Zeta电位为3.10 mV。结论：薄荷素油纳米乳制备工艺简单,采用优选处方制备的薄荷素油纳米乳粒径小、大小均匀。     

原花青素纳米乳的制备及其质量评价*

目的:研制原花青素纳米乳制剂并对其进行质量评价。方法:采用伪三元相图法进行处方筛选,并考察纳米乳的理化性质、稳定性及安全性。结果:制备的原花青素纳米乳,在透射电镜下观察为球状液滴,平均粒径为40 nm,影响因素实验表明该纳米乳制剂稳定,并对完整皮肤无毒性和刺激性。结论:原花青素纳米乳制备简单,性质稳定,有望成为原花青素新制剂。     

硝酸益康唑纳米乳滴眼剂的制备及理化性质研究

目的:制备硝酸益康唑(ECZ)纳米乳并对其性质进行考察。方法:在制备三元相图的基础上,优选硝酸益康唑纳米乳的最佳处方及制备工艺,并通过形态观察、ξ电位的测定、稳定性的考察等研究了硝酸益康唑的性质。结果:硝酸益康唑纳米乳的最佳处方工艺组合为聚氧乙烯40氢化蓖麻油(PEG-40氢化蓖麻油)/辛酸/癸酸三甘酯(M-812)/水,ξ电位为1.968 mV,平均粒径为64.06 nm。稳定性考察表明纳米乳在强光及高温加速试验中均较稳定。结论:硝酸益康唑纳米乳增加了益康唑的溶解度,而且剂型稳定,HPLC法检测方便。     

新型肝靶向微乳的制备及其性质研究

目的合成含有半乳糖残基的N-十八烷基乳糖酰胺,制备N-十八烷基乳糖酰胺修饰的肝靶向性姜黄素微乳,考察该微乳的制备条件、处方优化、载药性及稳定性等,为进一步研究肝靶向微乳的抗肿瘤作用提供实验依据。方法采用酰胺化法合成N-十八烷基乳糖酰胺,1H-NMR与FT-IR对其进行结构表征。以油酸乙酯作为油相,吐温-80作为表面活性剂,乙醇为助表面活性剂,N-十八烷基乳糖酰胺作为肝靶向配体,蒸馏水作为水相,水滴定法制备肝靶向微乳,根据伪三元相图筛选该微乳制备处方。以姜黄素为模型药物,制备载药微乳,考察其载药、释药性及稳定性等性质,表征其粒径、Zeta电位等参数。结果 1H-NMR与FT-IR测试证明十八烷基乳糖酰胺结构与设计一致。制得的姜黄素肝靶向微乳载药量达95%,平均粒径为(93.23±3.43)nm,呈电中性。且载药微乳在不同浓度、不同放置时间、高速离心等条件下均保持良好的稳定性。结论制得肝靶向性微乳外观澄清透明,粒径纳米级(<100nm),载药量较高,且稳定性良好,是一种适用于中药成分靶向输送的药物载体。     

雷公藤多苷纳米乳的制备及其理化性质评价

目的:研制雷公藤多苷纳米乳并对其理化性能、稳定性等进行评价。方法:结合雷公藤多苷在不同的油和表面活性剂中的溶解度以及伪三元相图的绘制,研制雷公藤多苷纳米乳,并对其类型、形态、粒径、理化参数及稳定性进行考察。结果:雷公藤多苷在聚氧乙烯氢化蓖麻油(RH-40)和肉豆蔻酸异丙酯(IPM)中溶解度较大,且以RH-40为表面活性剂,IPM为油相时纳米乳形成区域最大,最终纳米乳配方确定为RH-40∶IPM∶水,重量比为27∶3.3∶69.7,其中可添加浓度小于5%的透皮促渗剂氮酮;制备的雷公藤多苷纳米乳为棕黄色,澄清透明,流动性良好的O/W型纳米乳,该纳米乳粒子形态主要为圆球形,平均粒径为23.6nm,稳定性良好。结论:研制的雷公藤多苷纳米乳是质量稳定的新制剂。     

纳米乳的优化方法与不稳定机制的研究进展

文中介绍纳米乳的基本概念与两种制备方法：低能法与高能法,综述了纳米乳处方及制备工艺的优化方法：相行为的研究与实验设计。针对不同方法制备的纳米乳,选择合适的优化方法筛选处方与制备工艺,可以达到提高纳米乳稳定性和减小粒径的目的。同时讨论两种主要的纳米乳不稳定机制：奥斯特瓦尔德熟化和合并,并且介绍了两种理论分别对奥斯特瓦尔德熟化和合并进行数学表征,可以通过考察粒径的变化模式来判断究竟是奥斯特瓦尔德熟化还是合并引发纳米乳的稳定性破坏。     

纳他霉素纳米乳的制备及其质量评价

目的:研制纳他霉素纳米乳制剂并对其进行质量评价。方法:采用伪三元相图法进行配方筛选,并观测纳米乳的形态、粒径分布、Zeta电位。通过紫外分光光度法测定纳他霉素纳米乳中纳他霉素的含量。最后通过光照和加速实验对其稳定性进行考察。结果:制备的纳他霉素纳米乳,在透射电镜下观察为球状液滴,平均粒径为10.5 nm(25℃),Zeta电位为+13.0 mV(25℃,pH 3.5)。纳他霉素纳米乳中纳他霉素的平均含量为(17.31±0.02)g.L-1。在避光条件下保存,可长期保持稳定。结论:纳他霉素纳米乳制备工艺简单,切实可行,性质稳定,是一种很有前途的纳他霉素新制剂。     

硫酸沙丁胺醇油包水型口服纳米乳的制备及小肠吸收考察

目的研究硫酸沙丁胺醇油包水(W/O)型口服纳米乳的成乳条件及小肠吸收情况。方法采用两种制备方法考察不同制备条件对纳米乳形成的影响;采用伪三元相图法考察油相与司盘80的不同配比对成乳区域的影响,求出W/O型纳米乳形成区域;采用HPLC法测定纳米乳中硫酸沙丁胺醇的含量;采用大鼠在体小肠循环法初步考察该纳米乳的口服吸收情况。结果在本实验范围内,稳定且含水量较高、有实际应用价值的W/O型纳米乳的优化处方为豆油、司盘80、吐温80、蒸馏水的质量比为22.8∶22.8∶45.5∶8.9。根据最优处方,将水溶性药物硫酸沙丁胺醇溶于水相中,制得了W/O型纳米乳。大鼠在体小肠循环吸收试验初步证明了该纳米乳具有缓释作用。结论W/O型纳米乳可作为水溶性药物的缓控释制剂的载体。     

复方氧氟沙星口腔溃疡膜的制备及临床应用

本文介绍了复方氧氟沙星口腔溃疡膜的处方、制备工艺、质量控制及临床疗效。结果表明：口腔溃疡膜治疗组总有效率为９７．９％；双料喉风散对照组为８６．２％。治疗组显著高于对照组（Ｐ＜０．０５）。     

Accelerated Stability Testing of a Clobetasol Propionate-Loaded Nanoemulsion as per ICH Guidelines

The physical and chemical degradation of drugs may result in altered therapeutic efficacy and even toxic effects. Therefore, the objective of this work was to study the stability of clobetasol propionate (CP) in a nanoemulsion. The nanoemulsion formulation containing CP was prepared by the spontaneous emulsification method. For the formulation of the nanoemulsion, Safsol, Tween 20, ethanol, and distilled water were used. The drug was incorporated into an oil phase in 0.05% w/v. The lipophilic nature of the drug led to the O/W nanoemulsion formulation. This was characterized by droplet size, pH, viscosity, conductivity, and refractive index. Stability studies were performed as per ICH guidelines for a period of three months. The shelf life of the nanoemulsion formulation was also determined after performing accelerated stability testing (40°C ± 2°C and 75% ± 5% RH). We also performed an intermediate stability study (30°C ± 2°C/65% RH ± 5% RH). It was found that the droplet size, conductivity, and refractive index were slightly increased, while the viscosity and pH slightly decreased at all storage conditions during the 3-month period. However, the changes in these parameters were not statistically significant (p≥0.05). The degradation (%) of the optimized nanoemulsion of CP was determined and the shelf life was found to be 2.18 years at room temperature. These studies confirmed that the physical and chemical stability of CP were enhanced in the nanoemulsion formulation.     

Novel nanoemulsion for minimizing variations in bioavailability of ezetimibe

The objectives of the present study were to develop an optimal nanoemulsion of ezetimibe and evaluate its stability, lipid lowering and pharmacokinetic potential. Solubility of ezetimibe was determined in various vehicles. Pseudoternary phase diagrams were constructed to determine the existence of nanoemulsion region. Formulations were selected from the oil/water nanoemulsion region and subjected to various thermodynamic stability and dispersibility tests. Release rate of optimized formulations was determined using in vitro dissolution test. The formulation used for evaluation contained Capryol 90 (10% v/v), Tween 80 (15% v/v), Transcutol^® P (30% v/v), double distilled water (45% v/v). The release of drug from the nanoemulsion was highly significant (P <0.001) when compared to the drug suspension. The value of total cholesterol in the group administered with the formulation TF1 was highly significant (P <0.001) with respect to the group administered with the suspension of the drug. The plasma concentration time profile of ezetimibe from nanoemulsion represented greater improvement of drug absorption than the marketed formulation and drug suspension. The shelf life of the nanoemulsion was found to be 5.94 years at room temperature. The present study established nanoemulsion to be a possible alternative for minimizing variation in bioavailability of ezetimibe.     

The effect of food and tablet formulation on plasma prednisolone levels following administration of enteric-coated tablets.

1 Plasma prednisolone levels have been compared following the administration of enteric-coated prednisolone to fasted and non-fasted subjects. The effect on plasma levels of altering the formulation of the enteric-coating has also been studied. 2 The presence of food in the stomach at the time of administration does not affect the absorption of enteric-coated prednisolone tablets. 3 There was considerable inter-subject variation in plasma prednisolone levels after administration of shellac based enteric-coated tablets. However, plasma levels were more consistent when a preparation whose formulation was based upon cellulose acetate phthalate (CAP) was given. 4 It is concluded that the pattern of absorption and plasma prednisolone levels depend on the formulation of the enteric coating. The bioavailability of the CAP based preparation is similar to that of plain prednisolone.     

Development and bioavailability assessment of ramipril nanoemulsion formulation.

The objective of our investigation was to design a thermodynamically stable and dilutable nanoemulsion formulation of Ramipril, with minimum surfactant concentration that could improve its solubility, stability and oral bioavailability. Formulations were taken from the o/w nanoemulsion region of phase diagrams, which were subjected to thermodynamic stability and dispersibility tests. The composition of optimized formulation was Sefsol 218 (20% w/w), Tween 80 (18% w/w), Carbitol (18% w/w) and standard buffer solution pH 5 (44% w/w) as oil, surfactant, cosurfactant and aqueous phase, respectively, containing 5 mg of ramipril showing drug release (95%), droplet size (80.9 nm), polydispersity (0.271), viscosity (10.68 cP), and infinite dilution capability. In vitro drug release of the nanoemulsion formulations was highly significant (p<0.01) as compared to marketed capsule formulation and drug suspension. The relative bioavailability of ramipril nanoemulsion to that of conventional capsule form was found to be 229.62% whereas to that of drug suspension was 539.49%. The present study revealed that ramipril nanoemulsion could be used as a liquid formulation for pediatric and geriatric patients and can be formulated as self-nanoemulsifying drug delivery system (SNEDDS) as a unit dosage form.