共查询到19条相似文献,搜索用时 177 毫秒
1.
2.
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
3.
4.
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
5.
目的:制备复方水飞蓟素丹参素自乳化半固体胶囊剂,以期提高水飞蓟素和丹参素溶出度及生物利用度。方法:通过测定溶解度和绘制三元相图对自乳化处方进行筛选,应用单纯形网格法进行处方优化;采用熔融法制备半固体胶囊并对该半固体胶囊进行稳定性影响因素考察及药物溶出度测定。结果:制备了高载药量的水飞蓟素丹参素自乳化半固体胶囊剂,自制制剂中水飞蓟素和丹参素的溶出度超过80%,而市售参比制剂中水飞蓟素和丹参素的溶出度不超过50%。结论:复方水飞蓟素丹参素自乳化半固体胶囊剂能够显著提高水飞蓟素和丹参素的溶出度。 相似文献
6.
7.
8.
9.
10.
11.
The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p < 0.05). All preparation methods enhanced silymarin dissolution from solid dispersions of different characteristics. The co-precipitation method proved to be best and provided a stable amorphous solid dispersion with 2.5 improved dissolution compared to the pure drug. 相似文献
12.
Preparation of silymarin proliposome: a new way to increase oral bioavailability of silymarin in beagle dogs 总被引:2,自引:0,他引:2
Yan-yu X Yun-mei S Zhi-peng C Qi-neng P 《International journal of pharmaceutics》2006,319(1-2):162-168
The aim of the present study was to find a method to increase oral bioavailability of silymarin, that is to say, by the preparation of silymarin proliposome and to compare the pharmacokinetic characteristics and bioavailability after oral administration of silymarin proliposome and silymarin in beagle dogs. Silymarin proliposome was prepared by the film-deposition on carriers. After the proliposome was contacted with water, the silymarin liposome suspensions formed automatically. The tests of physicochemical properties including SEM, TEM, encapsulation efficiency, dissolution studies, particle size of the reconstituted liposome and stability of the silymarin proliposome were determined by laser-particle-sizer, HPLC, etc. The concentrations of silymarin in plasma of beagle dogs and its pharmacokinetic behaviors after oral administration of silymarin liposome suspensions and silymarin were studied by RP-HPLC. The pharmacokinetic parameters were computed by software program 3p97. The encapsulation efficiency of silymarin liposome could be more than 90%, with an average particle size of about 196.4 nm and the proliposome appeared a very stability at 40 degrees C during 3 months. It was found that mean plasma concentration-time curves of silymarin after oral administration of liposome suspensions and silymarin in beagle dogs were both in accordance with open two-compartments model and first-order absorption. Pharmacokinetic parameters of silymarin proliposome and silymarin in beagle dogs were Tmax both 30 min; Cmax 472.62 and 89.78 ng mL(-1); and AUC0-infinity 2606.21 and 697 ng mL(-1)h, respectively. The high bioavailability of silymarin proliposome could be obtained by oral administration. Silymarin proliposome was stable and did enchance the gastrointestinal absorption of silymarin. 相似文献
13.
14.
目的:通过共研磨技术改善水飞蓟素固体分散体的体外溶出度。方法:设计单因素试验考察溶出度的影响因素,如共研磨载体材料的种类及与共研磨药物的比例,研磨的时间等因素。结果:以甘露醇与PVP K30为混合亲水性载体材料,与药物的比例为1∶1∶1,研磨6 h,以pH7.4的磷酸盐缓冲溶液为溶出介质。结论:共研磨法制备水飞蓟素固体分散体能显著提高药物的体外溶出度,且制备工艺简单易行。 相似文献
15.
The effects of silymarin on bronchoconstriction induced by antigen challenge and on post-antigen challenge hyperresponsiveness to substance P were evaluated in sensitized guinea-pigs. Silymarin significantly decreased the bronchoconstriction due to antigen administration in the early phase of the response. In contrast, the dose-response curve for substance P recorded 1 h after antigen challenge was not modified by pretreatment with silymarin. The influence of the flavonoid on hyperresponsiveness to histamine in propranolol- and PAF (platelet-activating factor)-treated animals was also assessed. Silymarin did not affect hyperresponsiveness to histamine induced by either propranolol or PAF although it had inhibitory activity on the bronchial contractile response to the autacoid. These results suggest that silymarin has a protective effect in the early phase of allergic asthma, an effect, which may be related to a negative influence of the flavonoid on bronchial responsiveness to histamine. 相似文献
16.
17.
Kang JS Yoon WK Han MH Lee H Lee CW Lee KH Han SB Lee K Yang KH Park SK Kim HM 《International immunopharmacology》2008,8(10):1475-1480
Silymarin has been known to inhibit chemical-induced irritant contact dermatitis. In the present study, we report that topical application of silymarin suppresses dust mite extract (DPE)-induced atopic dermatitis (AD) in NC/Nga mice. Repeated topical application of ears with DPE caused AD-like skin lesions in NC/Nga mice. However, silymarin reduced AD-like skin lesions in these mice, resulting in decreased ear swelling and leukocyte infiltration into the ear. Moreover, our results showed that mast cell infiltration into the ear was suppressed by silymarin treatment in DPE-treated NC/Nga mice. Silymarin also reduced plasma level of IL-4 and IgE in these mice. Further study demonstrated that the mRNA expression of IL-4 was increased and that of IFN-gamma was decreased by DPE treatment in the ears of NC/Nga mice. However, DPE-induced changes in IL-4 and IFN-gamma mRNA expression were reversed by silymarin. DPE-induced increase in TNF-alpha mRNA expression was also suppressed by silymarin treatment. The results presented in this report suggest that silymarin might be beneficial for the treatment of AD. 相似文献
18.
The effect of silymarin on liver lipid peroxidation and membrane lipid alterations induced by an acute dose of CCl4 was studied. Four groups of animals were treated with CCl4, CCl4 + silymarin, silymarin and its vehicles. CCl4 was given orally (0.4 g 100 g-1 body wt.) and silymarin was administered i.p. All animals were sacrificed 24 h after the treatments. Liver lipid peroxidation was measured and plasma membranes were isolated. Alkaline phosphatase (AP) and gamma-glutamyl transpeptidase (GGTP) were measured in plasma membranes. Membrane lipids were extracted and then analysed by thin-layer chromatography by measuring the phosphorus of the phospholipids in each spot. Liver lipid peroxidation was increased about three times in the group receiving CCl4 only. Silymarin cotreatment prevented this increase. Phosphatidylethanolamine (PEA) decreased, while phosphatidylinositol (PI) increased in the plasma membranes isolated from the CCl4-treated group. Animals that received CCl4 + silymarin showed no decrease in PEA content. A partial prevention of the decrease in phosphatidylinositol content was also observed in plasma membranes of animals treated with silymarin in addition to CCl4. CCl4 decreased gamma-glutamyl transpeptidase (GGTP) and alkaline phosphatase (AP) membrane activities. Silymarin cotreatment prevented the AP (completely) and the GGTP (partially) falls caused by CCl4. Silymarin by itself increased AP membrane activity. A significant relationship between the membrane content of phosphatidylethanolamine (PEA) and the AP activity was observed in plasma membranes of treated animals and in normal liver membranes enriched with PEA. These results indicate that silymarin can protect against the alterations induced by CCl4 on the liver plasma membrane through its antioxidant properties by modifying the plasma membrane phospholipid content. 相似文献
19.
《Journal of microencapsulation》2013,30(7):619-626
AbstractA surface-attached silymarin-loaded solid dispersion with improved dissolution profile and enhanced oral bioavailability was formulated using silymarin, polyvinylpyrrolidone (PVP) and Tween 80 in water. In this solid dispersion, hydrophilic PVP was adhered onto the surface of crystalline drug rendering silymarin hydrophilic without changing its crystallinity. The drug solubility from the optimised solid dispersion prepared with silymarin/PVP/Tween 80 at the weight ratio of 5/2.5/2.5 increased by almost 650-fold compared to drug powder. The drug was physically and chemically stable in the solid dispersion for at least 6 months. Moreover, the solid dispersion enhanced the oral bioavailability of the drug in rats by almost 3-fold compared to the commercial product. The silymarin-loaded solid dispersion also exhibited advanced hepatoprotective bioactivity against CCl4-induced liver damage compared to silymarin or the commercial product. Thus, this silymarin-loaded solid dispersion would be useful for the enhancement of oral bioavailability and hepatoprotective activity of poorly water-soluble silymarin. 相似文献