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OBJECTIVE： To optimize the formulation of Diosmin gel and to investigate its in vitro release property. METHODS： Diosmin gel were prepared by using Carbomer 940 as matrix. Using accumulative release rate as index， with the amount of Carbomer 940， ethanol， acetone and pH as factors， L9（34） orthogonal test was conducted. The formulation of Diosmin gel was optimized and validated. Using Diosmin ointment as reference， dialysis bag diffusion method was used to investigate in vitro release property of Diosmin gel prepared by optimal formulation. RESULTS： The optimal formulation of Diosmin gel included Carbomer 940 1.5 g， ethanol 15 mL， glycerol 8 g， pH 6. The gel prepared with optimal formulation was sticky brown-yellow semi solid， and had good coating and spreading properties. The average accumulative release rate （2 h） was （12.67±0.12）％. Results of drug release test showed that Diosmin gel released rapidly within 12 h， then gradually slowed down. The accumulative release rates were （71.93±0.42）％ （12 h） and （80.47±0.54）％ （24 h）， drug release of which were in line with Higuchi equation. Diosmin ointment was released slowly. The accumulative release rates were （41.74±0.18）％ （12 h） and （62.63±0.59）％ （24 h）. Drug release of it were in line with first-order equation. CONCLUSIONS： The formulation of Diosmin gel is optimized successfully. Prepared Diosmin gel has good drug release property.
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Diosmin, a vascular-protecting agent, is practically insoluble in water, and its oral absorption is limited by its extremely low dissolution rate. In this study, beta -cyclodextrin [beta CD] and 2-hydroxypropyl-beta -cyclodextrin [HPbeta CD] were obtained to improve the solubility and dissolution rate of diosmin. Phase solubility studies of diosmin with beta CD and HPbeta CD in distilled water were conducted to characterize the complexes in liquid state. The solid-state characterization of the complexes prepared with different methods was performed by fourier transform-infra red spectroscopy [FTIR], optical microscopy analyses, and differential scanning calorimetry [DSC]. Dissolution studies were carried out in distilled water using US pharmacopeia dissolution rate testing equipment. The complexation of diosmin with beta CD and HPbeta CD both indicated an A[L] type of phase-solubility diagrams, and the apparent stability constants [Kc] was found to be 222.13 and 200.08 M[-1], respectively. The Kc values indicated the beta CD and HPbeta CD showed the similar equal complexation ability with diosmin, HPbeta CD provided higher solubility for diosmin due to its higher water solubility. The dissolution studies suggest that the inclusion complexes provide higher dissolution rate compared with the physical mixtures and the drug alone. Furthermore, the inclusion complex prepared by freeze drying method presented higher dissolution rate than kneading method
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<p><b>OBJECTIVE</b>To study the chemical constituents of Saussurea involucrata.</p><p><b>METHOD</b>Compounds were isolated and purified by column chromatography, and their structures were elucidated by chemical and spectroscopic methods.</p><p><b>RESULT</b>Eight compounds were yielded and identified as beta-sitosterol (1), dotriacontanoic acid (2), hexacosan-4-olide (3), (+)-11alpha, 13-dihydrodehydrocostuslactone (4), 8alpha-acetoxydehydrocostus lactone (5), zaluzanin C (6), 11,13beta-dihydrozaluzanin C (7), 8alpha-hydroxy-11beta-11,13-dihydrodehydrocostuslactone (8).</p><p><b>CONCLUSION</b>Compounds 2-7 were first isolated from S. involucrate.</p>
Subject(s)
Chromatography , Lactones , Chemistry , Magnetic Resonance Spectroscopy , Plant Extracts , Chemistry , Saussurea , ChemistryABSTRACT
Objective: Bilberry extract can inhibit the growth of cancer cells,but its effect on cervical carcinoma is rarely reported.This study was to explore the effects of bilberry extract on the expressions of Bcl-2,Bax,Fas and FasL in Hela cells.Methods: We determined the apoptosis of Hela cells by Hoechst33342/PI fluorescent staining and DNA ladder and Annexin V/PI double-staining after exposed to bilberry extract at the concentrations of 0.025-25 ?g/ml for 24 hours,and the protein expressions of Bcl-2,Bax,Fas and FasL were detected by Western blotting.Results: Obvious apoptosis-associated morphological changes and specific DNA ladder bands were observed in the Hela cells after exposed to bilberry extract at the concentrations of 0.025,0.25,2.5 and 25 ?g/ml,and the apoptosis rates of the cells were(4.13 ? 0.63)%,(5.41 ? 0.77)%,(8.74 ? 1.27)% and(12.05 ? 1.03)%,respectively.Western blot showed increased expressions of bax,Fas and FasL,and a decreased expression of bcl-2.Conclusion: Bilberry extract induces the apoptosis of Hela cells by up-regulating the protein expressions bax,Fas and FasL and down-regulating that of bcl-2.
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Object To establish a method for chemical pattern recognition on the quality assessment of Radix Astragali. Methods The contents of astragaloside in 18 samples of Astragalus Linn. in different species and origins were determinated by dual-wavelength TLCS method. The developing solvent was CHCl 3-MeOH-H 2O (65∶30∶10,), the UV detection was set at ? s=390 nm; ? R=590 nm. Astragaloside was regarded as the quality assurance of medicinal Radix Astragalus. Based on the TLCS method, the chemical data were obtained. Hierarchical clustering analyses were applied to the chemical pattern recognition. Results The content of astragaloside in Astragalus mongholicus (Bge.) Hsiao and A. membranaceus (Fisch.) Bge. was relatively higher than that in the other samples. This is consistent with the Pharmacopoeia of the People's Republic of China in which the two sorts of Astragalus Linn. were regarded as goods. Conclusion This method is a practicable in the quality assessment of Radix Astragali.