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OBJECTIVE：To optimize the form ulation of Zuojin pectin c apsules，and to prepare modern Zuojin pectin capsules with protective effects against gastric ulcers. METHODS ：The formulation of Zuojin pectin capsules was optimized with orthogonal test with the contents of pectin ，soluble starch and dextrin as factors ，using formability ，moisture absorption and flow ability as indicators. Zuojin pectin capsule was prepared by wet granulation filling method with Zuojin extract powder as raw material. The contents of palmatine hydrochloride ，berberine hydrochloride ，evodiamine and rutaecarpin were evaluated by HPLC. Basket method was used to investigate the release behavior of the capsule in 0.1 mol/L HCl solution. The gastric ulcer model of rats was established by intragastric administration of 75％ ethanol. Gastric ulcer index ，the inhibition rate of gastric ulcer and the pathological sections were used as indexes to investigate the protective effect of Zuojin pectin capsules （the doses were 54，108， 216 mg/kg）on gastric ulcer. RESULTS ：The optimal formulation of Zuojin pectin capsules included 45％ pectin，12％ soluble starch，27％ dextrin and 1％ xylitol. Results of in vitro drug ， release showed that palmatine hydrochloride and berberine， hydrochloride in Zuojin pectin capsules released 53.76％ and No.54.82％ respectively within 1 h，completely released at about 8 h， and conformed to the zero-order release behavior. 2492109374@qq.com Different doses of Zuojin pectin capsule could improve the ulcer injury of gastric tissue in gastric ulcer model rats to different extent ，and significantly reduced the gastric ulcer index（P＜0.01），significantly increased the inhibition rate of gastric ulcer and the percentage of positive expression area of Schiff ’s iodate staining （P＜0.01）. CONCLUSIONS ：Zuojin pectin capsule with protective effect on gastric ulcer and certain sustained- release effect is successfully prepared.
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Objective: The sustained release curcumin solid lipid nanoparticles (Cur-SLN) and long circulating solid lipid nanoparticles (LSLN) were prepared, and the physicochemical properties of the two nanoparticles were investigated. Methods: Cur-SLN was prepared by emulsification ultrasonic method, and then the entrapment efficiency and drug loading of Cur-SLN prepared under the optimal formulation were determined. Cur-LSLN was prepared by back-extrapolation method, and the physicochemical properties of Cur-SLN and Cur-LSLN were evaluated by entrapment efficiency, drug loading, particle size, and Zeta potential; DSC was used to analyze, in vitro release characteristics and the transmission electron microscope (TEM) was used to observe particle appearance. Results: Based on the optimal conditions, TEM showed that the appearance of Cur-SLN and Cur-LSLN were spherical or nearly spherical, the entrapment efficiency respectively were (89.15 ± 0.66)% and (92.97 ± 0.27)%, drug loading were (1.72 ± 0.08)% and (1.98 ± 0.08)%, average diameters of particles were (144.5 ± 4.1) nm and (155.0 ± 2.6) nm, and the mean Zeta potential were (-23.6 ± 0.2) mV and (-47.8 ± 1.8) mV. Through DSC detection, it can be determined that Cur in nanoparticles had been transformed into amorphous state. In vitro release test showed that the drug release of the two preparations was divided into two stages: burst release phase and sustained released stage, the release rate was fast in 12 h, and the cumulative release of Cur-SLN in 96 h was 86.63%, and Cur-LSLN was 76.98%, so Cur-LSLN showed better sustained-release effect. Conclusion: Cur-SLN and Cur-LSLN can be successfully prepared by emulsification ultrasonic method, and PEG modified nanoparticles have better sustained-release properties and prolong the time of the presence of drug in vivo, providing reference for the development of targeted drugs.
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OBJECTIVE: To investigate the physicochemical properties of hydroxypropyl methylcellulose(HPMC)produced by different manufacturers, and to establish a link between the physicochemical properties of HPMC and its sustained release effect, which can provides a theoretical basis for further rational application. METHODS: The physicochemical properties of HPMC collected from different manufacturers, such as particle size distribution, bulk density, physical form, crystallinity and degree of substitution were characterized by laser particle size analyzer, bulk density measuring device, scanning electron microscope, X-ray diffractometer and gas chromatography, respectively. Then, the HPMC from different manufacturers were pressed into sustained release tablets, and the sustained release effect was compared by the dissolution curve. RESULTS: The physicochemical properties of HPMC produced by different factories are different, which are manifested in different particle sizes,different bulk densities, different physical shapes, whether there are differences in crystallization peaks and the content of hydroxypropoxy groups, and the different physicochemical properties directly lead to the difference of sustained release effects. CONCLUSION: The study of physicochemical properties of HPMC can better control its quality and use it more widely.