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Objective To prepare silymarin phospholipids complex（SM-PC） and investigate its physicochemical properties. Methods On the basis of single-factor tests, the drug-lipid ratio, drug concentration and reaction temperature were selected as the factors of the central composite design and response surface methodology in the preparation of SM-PC by solvent volatilization, and the best process was optimized with the compound rate as the index. And its in vitro dissolution was measured. Results The optimum preparation technology of SM-PC was as follows: acetone was used as compound solvent, the concentration of SM was 8.0 mg/ml, the mass ratio of SM to phospholipid was 1∶1.8, the reaction temperature was 56 ℃ and the recombination rate was（95.15±1.55）% with deviation of less than 3%. The in vitro dissolution test showed that the dissolution of SM-PC was close to 90% in 60 min. The dissolution behavior of main component of silybin was similar to that of silymarin capsules（Legalon ®）, which was higher than SM-API. Conclusion SM-PC was successfully prepared by central composite design response surface method, which significantly improved the dissolution and laid a foundation for the study of subsequent preparations.
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Objective: To prepare and optimize tilianin loaded solid lipid nanoparticles (T-SLNs), and investigate the physicochemical properties, absorption and transport behavour of T-SLNs in vitro. Methods: T-SLNs were prepared by high shear homogenization followed by ultrasonication and optimized by central composite design and response surface methodology. In the study, the physicochemical properties of T-SLNs including size, polydispersity (PDI), Zeta potential, shape, entrapment efficiency and release profile in vitro were investigated, the absorption and transport behavour of T-SLNs in Caco-2 cell model were also measured. Results: The optimum formulation of T-SLNs consisted of: drug/lipid of 0.11, soy lecithin/lipid of 1.26, and content of tween-80 was 5.05%. The prepared T-SLNs were spherical and uniform with the mean particle diameter at (86.40 ± 0.62) nm, PDI (0.165 ± 0.080) and Zeta potential of (-24.2 ± 0.6) mV, respectively. The average EE was (89.81 ± 1.07)%, and the release in vitro showed that tilianin was released about (98.72 ± 1.57)% in 48 h. Besides, the absorption and transport assays of T-SLNs in Caco-2 cells model indicated that T-SLNs had a higher absorption and transport than tilianin. Conclusion: The method of high shear homogenization followed by ultrasonication is suitable for T-SLNs preparation. The optimal T-SLNs have a smaller particle size and high EE. Moreover, in the same concentration of tilianin, the absorption and transport amounts of T-SLNs in Caco-2 cell model were higher than tilianin.
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Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for industrial production of the formulation. Method With the release degree as index, the influences of single factors on the release, such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials, ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone (PVP)as adhesive, were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows: rhynchophylline 9.5%, HPMC: 19%, EC: 7%, PVPP:2.2%, starch:61.5% and talcum powder: 0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The optimized recipe is reasonable and meets the requirements of sustained release formulation, which means it can provide a reference for industrial production of the formulation.
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Objective To optimize the recipe of rhynchophylline sustained release tablet in order to provide a reference for in?dustrial production of the formulation. Method With the release degree as index,the influences of single factors on the release,such as hydroxypropyl methyl cellulose(HPMC)used as an skeleton materials,ethyl cellulose(EC)as blockers and the mass fraction of polyvinylpyrrolidone(PVP)as adhesive,were evaluated to screen the optimal preparation by central composite design and response surface methodology based on the single factor investigation. Result The optimal preparation was as follows:rhynchophylline 9.5%, HPMC:19%,EC:7%,PVPP:2.2%,starch:61.5%and talcum powder:0.8%. The sustained release tablet prepared by the optimized recipe of rhynchophylline had no sudden release effect and the release degree in 12 h was more than 84%. Conclusion The opti?mized recipe is reasonable and meets the requirements of sustained release formulation,which means it can provide a reference for in?dustrial production of the formulation.
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Objective: To optimize the formula and preparation process of docetaxel-loaded pluronic P123 micelles. Methods:Docetaxel-loaded pluronic P123 micelles were prepared by a thin-film hydration method and optimized by central composite design and response surface methodology. The influencing factors including the quantity of docetaxel, volume of organic phase, volume of hydra-tion and temperature of hydration were investigated with the entrapment efficiency as the index. The morphology of micelles was ob-served under a transmission electron microscope. The particle diameter and zeta potential were determined. The in vitro release property was measured by a dialysis method. Results:The relationship between the influencing factors and the evaluation parameter was fitted by multi-linear equation, quadratic polynomial equation and cubic polynomial equation, respectively. The results showed that the cubic polynomial equation was superior to the others according to the correlation coefficient. Docetaxel-loaded pluronic P123 micelles were spherical with the mean diameter, zeta potential, polydispersity index, encapsulation efficiency and drug loading of 108. 3 nm,-3. 99 mV, 0. 265, (97. 91 ± 0. 28)% and (3. 72 ± 0. 12)%, respectively. The cumulative release in vitro reached 95. 03% in 120 h, and docetaxel-loaded pluronic P123 micelles had notable sustained-release property. Conclusion: The technical process for do-cetaxel-loaded pluronic P123 micelles is simple and usable, and docetaxel-loaded pluronic P123 micelles show high encapsulation effi-ciency and notable sustained-release property.
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This study was aimed to optimize the extraction process of double-marker components for Arctium lappa L. The central composite design and response surface methodology was used. According to 3 main factors, the extraction rates of arctiin and arctigenin was used as evaluation indexes. Multiple linear regression and two-order polynomial equation were used. The binomial fitting model was performed in the optimization of arctiin and arctigenin extraction technology. The results showed that the indentified optimized extraction technology of arctiin and arctigenin was 70% ethanol, 24-fold, ultrasonic solvent extraction for 15 minutes. It was concluded that this technology was able to extract large amount of arctiin and arctigenin, which provided experiment evidences for arctiin and arctigenin preparation. It also provided references for the development and utilization of arctiin and arctigenin.