共查询到20条相似文献,搜索用时 234 毫秒
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目的:探讨液固压缩技术提高葛根总黄酮溶出度的机制。方法:采用液固压缩技术制备葛根总黄酮速释片,比较液固压缩片与原料药、市售片的溶出度,通过差示扫描量热法(DSC)、粉末接触角测定仪等探讨液固压缩技术的增溶机制。结果:葛根总黄酮液固压缩片较市售片、原料药的溶出有大幅度提高。DSC表明葛根素的特征峰消失,随着添加剂PVPK30占药物溶液比例的增加,液固压缩粉末的接触角逐渐减小。结论:液固压缩技术可提高葛根总黄酮溶出时的有效表面积,改善药物润湿性,使难溶性药物快速释放。 相似文献
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提高难溶性药物固体制剂溶出度的方法研究进展 总被引:1,自引:0,他引:1
目的 了解提高难溶性药物固体制剂溶出度的方法,为制剂开发工作提供参考资料。方法 查阅最近10年的国内外专业文献,从制剂学的角度对提高难溶性药物固体制剂溶出度的方法研究概况进行归纳整理。结果 通过选择适当的辅料改进处方、改进工艺、采用新的制剂技术是提高难溶性药物固体制剂溶出度的有效途径。结论 提高难溶性药物固体制剂溶出度是必要的、可行的。 相似文献
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<正>固体分散技术是指制备制剂时将固体药物,特别是难溶性药物高度分散在另一种固体载体中的新技术。自1961年提出固体分散体(Solid dispersion,SD)概念以来,人们围绕如何利用难溶性药物与水溶性材料制成SD的技术,在提高难溶性药物的溶出度和生物利用度方面展开了大量的研究工作。近年 相似文献
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固体分散技术是指制备制剂时将固体药物,特别是难溶性药物高度分散在另一种固体载体中的新技术。固体分散体作为一种新型的载药系统,能够显著地增加难溶药物的溶出,还可根据需要制备具有缓释控释功能的制剂。丸、散、膏、汤等是 相似文献
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目的:探讨液固压缩技术对α-细辛脑溶出的影响。方法:采用液固压缩技术制备α-细辛脑液固压缩片(液体赋形剂为吐温80或聚乙二醇400,载体材料为PH-101微晶纤维素,涂层材料为微粉硅胶200),与市售细辛脑片在片剂质量和溶出度方面进行比较。结果:α-细辛脑液固压缩片中α-细辛脑在短时间内迅速溶出,5 min时达到80%以上,是市售细辛脑片溶出度的3倍,且崩解时限均<100 s。结论:液固压缩技术对难溶性药物α-细辛脑的溶出有一定帮助。 相似文献
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自乳化释药系统与液固压缩技术联合开发难溶性药物新剂型的进展 总被引:1,自引:0,他引:1
提高难溶性药物溶解度,改善难溶性口服药物的生物利用度,一直是药剂学的热点和难点。本文旨在通过对自乳化释药系统和液固压缩技术的介绍,并阐述2种技术联合开发难溶性药物新剂型的优势,说明固体自乳化释药系统可以作为液体自乳化释药系统的提高或者替代,其具有降低生产成本,简化工业生产,提高稳定性与患者耐受性等方面的优势。 相似文献
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INTRODUCTION: Today, the properties of many new chemical entities have shifted towards higher molecular weights and this in turn increases the lipophilicity hence decreasing aqueous solubility. The low solubility of drugs usually has in vivo consequences such as low bioavailability, increased chance of food effect and incomplete release from the dosage form. AREAS COVERED: The present review discusses the advantages of the liquisolid technology in formulation design of poorly water soluble drugs for dissolution enhancement and highly water soluble drugs for slow release pattern. EXPERT OPINION: With the advent of high throughput screening and combinatorial chemistry, it has been shown that most of the new chemical entities have a high lipophilicity and poor aqueous solubility, hence poor bioavailability. In order to improve the bioavailability, the release rate of these drugs should be enhanced. Although there are multiple technologies to tackle this issue, they are not cost effective due to the involvement of sophisticated machinery, advanced preparation techniques and complicated technology. As the liquisolid technology uses a similar production process as the conventional tablets, this technology to improve the release rate of poorly water soluble drugs will be cost effective. This technology also has the capability to slow down drug release and allows preparing sustained release tablets with zero order drug release pattern. The excipients required for this technology are conventional and commonly available in the market. The technology is in the early stages of its development with extensive research currently focused on. It is envisaged that the liquisolid compacts could play a major role in the next generation of tablets. 相似文献
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《Expert opinion on drug delivery》2013,10(2):191-205
Introduction: Today, the properties of many new chemical entities have shifted towards higher molecular weights and this in turn increases the lipophilicity hence decreasing aqueous solubility. The low solubility of drugs usually has in vivo consequences such as low bioavailability, increased chance of food effect and incomplete release from the dosage form. Areas covered: The present review discusses the advantages of the liquisolid technology in formulation design of poorly water soluble drugs for dissolution enhancement and highly water soluble drugs for slow release pattern. Expert opinion: With the advent of high throughput screening and combinatorial chemistry, it has been shown that most of the new chemical entities have a high lipophilicity and poor aqueous solubility, hence poor bioavailability. In order to improve the bioavailability, the release rate of these drugs should be enhanced. Although there are multiple technologies to tackle this issue, they are not cost effective due to the involvement of sophisticated machinery, advanced preparation techniques and complicated technology. As the liquisolid technology uses a similar production process as the conventional tablets, this technology to improve the release rate of poorly water soluble drugs will be cost effective. This technology also has the capability to slow down drug release and allows preparing sustained release tablets with zero order drug release pattern. The excipients required for this technology are conventional and commonly available in the market. The technology is in the early stages of its development with extensive research currently focused on. It is envisaged that the liquisolid compacts could play a major role in the next generation of tablets. 相似文献
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Nowadays, one of the most important task of the pharmaceutical technology is to optimize the dissolution of active ingredients, because most of the drug candidates have a poorly water solubility and hence a slow absorption. According to the latest examinations, the bioavailability of poorly water soluble drugs can be increased significantly by using surfactants or the mixture of surfactants and polymers. Nowadays, surfactants (like polysorbates) are generally used in the production of solid dispersions, so the use of surface-active sucrose esters can be resulted an innovative solution in the pharmaceutical technology. The aim of our investigation was to examine the applicability of sucrose laurate in hot-melt technology in order to influence the crystalline structure and dissolution rate of a poorly water soluble drug (gemfibrosil) having low-melting point. The results of the X-ray powder diffractometry have showed that the sucrose laurate had no significant effect on the crystallization degree of the drug which is important in case of the stability. On the bases of the results of in-vitro dissolution studies, it can be concluded that the sucrose laurate (using minimum 5%) can be well applied in hot-melt technology with carriers having characteristic melting point (e.g. Macrogol) to increase the dissolution rate of poorly soluble drugs. 相似文献
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Pharmacokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug 总被引:3,自引:0,他引:3
Hanafy A Spahn-Langguth H Vergnault G Grenier P Tubic Grozdanis M Lenhardt T Langguth P 《Advanced drug delivery reviews》2007,59(6):419-426
An increasing number of newly developed drugs show bioavailability problems due to poor water solubility. Formulating the drugs as nanosuspensions may help to overcome these problems by increasing saturation solubility and dissolution velocity. In the present study the bioavailability of the poorly soluble fenofibrate following oral administration was investigated in rats. Four formulations were tested: a nanosuspension type DissoCube(R), one solid lipid nanoparticle (SLN) preparation and two suspensions of micronized fenofibrate as reference formulations, one suspension in sirupus simplex and a second in a solution of hydroxyethy-cellulose in physiological saline. Both colloidal drug delivery systems showed approximately two-fold bioavailability enhancements in terms of rate and extent compared to the reference formulations. No significant differences were found in AUC(0-22 h) as well as in C(max) and t(max) between the two colloidal delivery systems. In conclusion, nanosuspensions may be a suitable delivery system to improve the bioavailability of drugs with low water solubility. 相似文献
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Kun Feng Shuzhen Wang Hairong Ma Yijun Chen 《The Journal of pharmacy and pharmacology》2013,65(1):64-71
Objectives Although drug solubilization by block copolymer micelles has been extensively studied, the rationale behind the choice of appropriate block copolymer micelles for various poorly water‐soluble drugs has been of relatively less concern. The objective of this study was to use methoxy‐poly(ethylene glycol)‐polylactate micelles (MPEG‐PLA) to solubilize glycosylated antibiotic nocathiacin I and to compare the effects of chirality on the enhancement of aqueous solubility. Methods Nocathiacin I‐loaded MPEG‐PLA micelles with opposite optical property in PLA were synthesized and characterized. The drug release profile, micelle stability and preliminary safety properties of MPEG‐PLA micelles were evaluated. Meanwhile, three other poorly water‐soluble chiral compound‐loaded micelles were also prepared and compared. Key findings The aqueous solubility of nocathiacin I was greatly enhanced by both l ‐ and d ‐copolymers, with the degree of enhancement appearing to depend on the chirality of the copolymers. Comparison of different chiral compounds confirmed the trend that aqueous solubility of chiral compounds can be more effectively enhanced by block copolymer micelles with specific stereochemical configuration. Conclusions The present study introduced chiral concept on the selection and preparation of block copolymer micelles for the enhancement of aqueous solubility of poorly water‐soluble drugs. 相似文献
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This paper describes the preparation of solid solutions of ciclosporin as model solubilizate in water-soluble sugar esters, which are solid, biodegradable, and nontoxic surfactants. Sugar esters were found to be excellent solubilizers for poorly water-soluble drugs such as ciclosporin. Such systems are suitable for the preparation of solid dosage forms for the purpose of oral administration. Addition of water to the solid solutions yields clear solutions of the solubilizate. 相似文献