节能乳化法制备水包油型乳膏基质及体外质量考察

目的: 探讨节能乳化法制备O/W型乳膏基质及对其质量的影响.方法: 分别用混合乳化法和节能乳化法制备乳膏基质,对其稳定性和释放性进行评价.结果: 节能乳化法所制得的乳膏比混合乳化法稳定性好,释药能力强,且节能、节时.结论: 节能乳化法适于配制O/W型乳膏基质.     

乳化剂后加法制备O/W型乳膏基质及质量考察

目的 探讨乳化荆后加法对O／W型乳膏基质质量的影响。方法 用乳化剂分相加入法和乳化剂后加法分别制备O／W型乳膏基质．并对稳定性和释放度进行评价。结果 乳化剂后加法所制得的乳滴粒径小，分散均匀，质量稳定，释放度高。结论 本法可在生产中推广应用。     

乳膏基质乳化方法的实验比较

乳膏剂是皮肤科应用较多的一种剂型,其稳定性取决于乳化方法。目前国内文献报道的乳化方法有3种,即油、水分相法,混合加热法和后加乳化剂法。为了探讨3种乳化方法对乳膏基质稳定性的影响,本文选择了2种O/W处方用3种乳化方法分别进行了3次实验,并对所制备的乳膏基质的稳定性进行了实验性评价。     

正交法优选O/W乳膏基质维生素E霜制备工艺

目的:探讨O/W型乳膏基质维生素E霜的最佳制备工艺.方法:工艺优选采用正交法.结果:最佳制备工艺组合为A1B2C2,即搅拌方式为变速搅拌(混相成乳时以720 r/min搅拌,继以120 r/min搅拌);成相温度为(70±0.5)℃;油相与水相比为30:70.结论:混相成乳时两相温度差、搅拌方式、油相与水相之比为影响O/W型乳膏基质维生素E霜质量的主要因素.     

3种乳化法对水包油型乳膏基质质量的影响

目的探讨O/W型乳膏基质的乳化剂添加方法对其质量的影响。方法用3种乳化方法制备乳膏基质,对稳定性和释放性进行评价。结果后加乳化剂法所制得的乳膏质量最好。结论后加乳化剂法是一种值得推广的乳膏的乳化方法。     

O/W乳膏基质配制方法的改进及质量考察

目的　通过 O/ W型乳膏基质配制方法的改进 ,制备质量稳定的基质。方法　采用温度控制、乳化剂置后加入、搅拌速度的调节以及乳化不完全基质的“返工”等方法制备 O/ W型乳膏基质。结果　按改进后的配制方法生产 12个批次 O/ W型乳膏基质 ,经质量考察 ,结果满意。结论　改进后的 O/ W型乳膏基质配制方法切实可行 ,易操作 ,主动性强 ,制备成功率高     

乳化剂的添加方法对水包油型乳膏基质质量的影响

目的探讨O／W型乳膏基质的乳化剂添加方法对其质量的影响。方法用3种乳化方法制备乳膏基质，对稳定性和释放性进行评价。结果后加乳化剂法所制得的乳膏质量最好。结论本法可推广应用。     

W/O乳膏质量稳定性探讨

目的:探讨W/O型乳膏的稳定性.方法:查阅相关文献、书籍并结合工作经验,从理论和实践两方面进行探讨.结果:配方中的油相、水相、相比例、乳化剂、增稠剂等和制备工艺中的制备方式、设备、搅拌和温度等因素对W/O型乳膏的稳定性影响较大.结论:在实践中,如果能较全面地考虑配方和制备工艺两方面的影响W/O型乳膏稳定性的诸因素,将会得到稳定性较好的膏体.     

复方氟康唑霜的试制

本品(霜剂)以氟康唑、氯霉素为主药;以薄荷脑、冰片为辅药,与乳膏基质用乳化法制成水包油(O/W)型霜剂。1 处方 水包油(O/W)型乳膏基质2 制法 A液(油相)称取(油相)中诸药置水浴上加热至70～80℃熔融。 B液(水相)取(水相)中诸药加热至70～80℃搅拌全溶。     

优选精制蛇毒酶乳膏剂制备工艺的实验分析

目的优化精制蛇毒酶乳膏制备工艺。方法以乳膏剂的稳定性及外观性状为考察指标,采用正交实验设计法,以油相、水相、乳化温度和乳化时间为可变因素,选用L9(34)表进行实验。结果最优的基质组成工艺是:硬脂酸20.0 g、植物油10.0 g、液体石蜡8.0 g、丙三醇5.0 g、三乙醇胺1.0 g;混合乳化机搅拌60min;乳化温度85℃。结论按此法制备的乳膏剂符合中国药典软膏剂的规定。     

Releasing properties of water soluble drug in internal water phase of W/O/W multiple emulsions]

A stable water/liquid paraffin system water-in-oil-in-water (W/O/W) multiple emulsion was prepared by the two-step procedure of emulsification using a variety of nonionic emulsifying agents, such as Span 80 and Tween 20. After comparison of the releasing properties of such water soluble drugs as cefadroxil, cephradine, 4-aminoantipyrine and antipyrine which were entrapped separately in the inner aqueous phase of the W/O/W multiple emulsion, a large difference was observed. It was ascertained that the difference in these releasing properties was due to no physical rupture by the microscopic observation and the results of the release test of W/O/W multiple emulsion with two kinds of drugs entrapped simultaneously in an inner aqueous phase. This reason was presumed to be dependent on permeation in the oily phase of the drug itself. It was proved that the differences of releasing properties tended to depend on the molecular weight and were closely related to the drug concentration of outer aqueous phase of W/O/W multiple emulsion containing the drug in both aqueous phases prepared as an experimental model. Therefore, two possible mechanisms for the releasing of drugs in W/O/W multiple emulsion may be interpreted as follows: the first is that the mixed and inversed micelles formed by Span 80 and Tween 20 agents in the oily phase act as a carrier of drugs, and the second is that drug molecules diffuse through small pore existing in very thin lamella of the emulsifying agents partially formed in the oil layer owing to the fluctuation of the thickness.     

Process and formulation variables in the preparation of wax microparticles by a melt dispersion technique. II. W/O/W multiple emulsion technique for water-soluble drugs.

Pseudoephedrine HCl-carnauba wax microparticles were prepared by a multiple emulsion-melt dispersion technique. A heated aqueous drug solution was emulsified into the wax melt (W/O emulsion), followed by emulsification of this primary emulsion into a heated external aqueous phase (W/O/W emulsion). The drug-containing microparticles were formed after cooling and congealing of the wax phase. The encapsulation efficiencies were above 80 per cent and actual drug loadings close to 50 per cent were achieved. The surface of the microparticles had submicron pores and drug crystals were visible on cross-sections. The drug loading depended on the rate of cooling and the volume of the internal aqueous phase but was insensitive to the volume of the continuous phase. The drug release was much faster when compared to the release from polymeric microspheres.     

Process and formulation variables in the preparation of wax microparticles by a melt dispersion technique. II. W/O/W multiple emulsion technique for water-soluble drugs

Abstract

Pseudoephedrine HCl-carnauba wax microparticles were prepared by a multiple emulsion-melt dispersion technique. A heated aqueous drug solution was emulsified into the wax melt (W/O emulsion), followed by emulsification of this primary emulsion into a heated external aqueous phase (W/O/W emulsion). The drug-containing microparticles were formed after cooling and congealing of the wax phase. The encapsulation efficiencies were above 80 per cent and actual drug loadings close to 50 per cent were achieved. The surface of the microparticles had submicron pores and drug crystals were visible on cross-sections. The drug loading depended on the rate of cooling and the volume of the internal aqueous phase but was insensitive to the volume of the continuous phase. The drug release was much faster when compared to the release from polymeric microspheres.     

Preparation of water in oil type cream with high content of water containing Kochia scoparia fruit and Cnidium monnieri fruit

Kikisui is a herbal lotion containing Kochia scoparia Fruit and Cnidium monnieri Fruit that is clinically used as an antipruritic for itchy dry skin. However, this formulation is unsuitable for inducing a prolonged effect. Here, we attempted to change the formulation from a lotion to a cream. The cream we chose was a water-in-oil (W/O) type emulsion for enhancing skin compatibility. In addition, the high water content imparts a sensation of coolness. However, it is difficult to prepare a stable W/O type cream with high water content using a mechanical mixing method. Instead, we prepared the W/O type emulsion using liquid crystals. Water containing cocamidopropyl betaine was added to a dispersed phase comprising an oil phase of oleic acid and liquid paraffin that was constantly stirred. Addition of an aqueous solution containing Kochia scoparia Fruit and Cnidium monnieri Fruit decreased the stability of the cream. However, addition of glycerin as a humectant, and ethyl p-hydroxybenzoate/n-butyl p-hydroxybenzoate as preservatives enhanced the stability of the cream. The stability of the emulsion was correlated with the apparent viscosity of the cream. The final W/O type cream had a water content of 83% and was stable for more than 6 months at 4°C. Furthermore, ostol, which is one of the main biologically active herbal compounds, was also stable for more than 6 months.     

Preparation of stable W/O/W type multiple emulsion containing water-soluble drugs and in vitro evaluation of its drug-releasing properties]

The stable water-in-oil-in-water (W/O/W) multiple emulsion was prepared by a two-step procedure for emulsification using glyceryl tricaprylate (Panasate-800) as the oil phase. The water-soluble drugs such as cefadroxil, cephradine, 4-aminoantipyrine, and antipyrine were selected and entrapped separately in the inner aqueous phase of W/O/W multiple emulsion. In consideration of parenteral administration, pH 7.4 phosphate buffered saline was used in both inner and outer aqueous phases. Moreover, these multiple emulsions could be significantly stable for a month at room temperature by the addition of hydrophilic polymer like gelatin and of amino acid like lysine to the inner aqueous phase.     

Microencapsulation of peptides and proteins

Microcapsules were prepared by using a double-emulsion technique. A new production method called 'induced phase separation method' was applied to encapsulate peptides and proteins. To find the optimal adjuvants a matrix was set up combining the appropriate organic solvents and the suitable surfactants. The polymer was chosen with regard to the required release period. The aqueous drug solution was intensively mixed with the organic polymer solution. An aqueous surfactant solution was slowly added to the O/W emulsion. The obtained W/O/W emulsion is stirred under partial vacuum conditions until the organic solvent was removed. After removing the solvent from the W/O/W emulsion the microcapsules were washed and lyophilized. The morphology of the microparticles (spheres, sponges, capsules, surplus polymer) was checked by microscopy, particle size distributions were measured by laser diffraction.     

Effect of various vehicles on diclofenac sodium and indomethacin pharmaceutical availability

The aim of the study was to determine the pharmaceutical availability of various ointment systems containing antirheumatic substances and to establish an optimal system for cutaneous application. Topical application permits elimination or at least reduction of side effects connected with oral administration. Three systems were evaluated: emulsion W/O (ointment), emulsion O/W (cream) and gel, all of them containing diclofenac sodium or indomethacin. The investigated systems are characterized by proper rheological parameters and long physicochemical stability. Studies on diclofenac and indomethacin pharmaceutical availability show a good release of the substances from cream and hydrogel bases, but a very poor release from the ointment base.     

Particle control of emulsion by membrane emulsification and its applications

Particle-size control of emulsion is very important for maintaining stability and giving emulsions new functional roles. Porous glass membrane, prepared by phase separation of a glass composition, is available as an emulsifying element, from which, one can obtain monodispersed emulsion with different particle sizes, and useful water/oil/water (W/O/W) emulsion in very high yield. The authors have called this new technology 'membrane emulsification'. Applications of membrane emulsification technology to drug delivery systems were carried out under cooperative research with Miyazaki Medical College. It was found that the clinical administration of a W/O/W drug emulsion that encapsulated an anticancer drug in its inner droplets was surprisingly effective for both terminal and multiple nodules of hepatocellular carcinoma when the drug was injected to damaged liver through a catheter inserted in the hepatic artery. Other applications have been tried and developed elsewhere.     

内水相添加氯化钠对W/O/W型复乳性质的影响

目的探讨在内水相中添加氯化钠(NaCl)对W/O/W型复乳性质的影响。方法在前期试验优选出较佳W/O/W复乳处方的基础上,以1 g/L NaCl水溶液代替处方中的纯化水作为内水相,采用二步乳化法制备复乳,从显微结构、粒径分布、稳定性等方面比较复乳性质的变化。结果在内水相中添加NaCl(1 g/L)时,复乳主要为B型结构,外观较圆整,液滴大小较均匀,且乳滴不易聚集成一团,大部分粒子粒径在20～40μm之间,稳定性良好。结论在内水相中添加NaCl(1 g/L),有助于优化W/O/W型复乳物理化学性质,提高其稳定性。