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Baloglu E Ay Senyıgıt Z Karavana SY Vetter A Metın DY Hilmioglu Polat S Guneri T Bernkop-Schnurch A 《Chemical & pharmaceutical bulletin》2011,59(8):952-958
The main objective of this work was to develop antifungal matrix tablet for vaginal applications using mucoadhesive thiolated polymer. Econazole nitrate (EN) and miconazole nitrate (MN) were used as antifungal drugs to prepare the vaginal tablet formulations. Thiolated poly(acrylic acid)-cysteine (PAA-Cys) conjugate was synthesized by the covalent attachment of L-cysteine to PAA with the formation of amide bonds between the primary amino group of L-cysteine and the carboxylic acid group of the polymer. Vaginal mucoadhesive matrix tablets were prepared by direct compression technique. The investigation focused on the influence of modified polymer on water uptake behavior, mucoadhesive property and release rate of drug. Thiolated polymer increased the water uptake ratio and mucoadhesive property of the formulations. A new simple dissolution technique was developed to simulate the vaginal environment for the evaluation of release behavior of vaginal tablets. In this technique, daily production amount and rate of the vaginal fluid was used without any rotational movement. The drug release was found to be slower from PAA-Cys compared to that from PAA formulations. The similarity study results confirmed that the difference in particle size of EN and MN did not affect their release profile. The release process was described by plotting the fraction released drug versus time and n fitting data to the simple exponential model: M(t)/M(∞)=kt(n). The release kinetics were determined as Super Case II for all the formulations prepared with PAA or PAA-Cys. According to these results the mucoadhesive vaginal tablet formulations prepared with PAA-Cys represent good example for delivery systems which prolong the residence time of drugs at the vaginal mucosal surface. 相似文献
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Zegers RG van Den Berg AM Brandenburg S Fleurot FR Fujiwara M Guillot J Hannen VM Harakeh MN Laurent H van Der Schaaf K van Der Werf SY Willis A Wilschut HW 《Physical review letters》2000,84(17):3779-3782
The (nat)Pb(3He,tp) reaction at E(3He) = 177 MeV was studied to identify 2Planck's over 2piomega isovector monopole strength in Bi isotopes. Monopole strength was found in the region -45
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The dynamics of a single strain HIV model is studied.The basic reproduction number R_0 used as a bifurcation parameter shows that the system undergoes transcritical and saddle-node bifurcations.The usual threshold unit value of R_0 does not completely determine the eradication of the disease in an HIV infected person.In particular,a sub-threshold value R_C is established which determines the system's number of endemic states:multiple if R_c Ro 1,only one if R_C = R_0 = 1,and none if R_0 R_C 1. 相似文献
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