ABSTRACT
OBJECTIVE：To optimize the formulation of Curcumin （CUR）transethosomes（CUR-TEs）. METHODS ：The contents of CUR in CUR-TEs were determined by HPLC. CUR-TEs were prepared by injection method. Using comprehensive score of encapsulation efficiency and drug loading as index ，based on signal factor test ，Box-Behnken design-response surface method was used to optimize and validate the formulation. The property of CUR-TEs prepared by the optimal formulation was investigated. RESULTS：The optimal formulation of CUR-TEs was as follows as lecithin of 4％，CUR of 0.13％，1，2-propylene glycol of 25％，tween-80 of 1％. Results of validation test of optimal formulation showed that comprehensive score of encapsulation efficiency and drug loading of CUR-TEs was 93.04±2.16，relative error of which to predicted value （91.19）was 2.03％. The encapsulation efficiency of CUR-TEs prepared by optimal formulation was （91.17±1.35）％，and its drug loading was （0.94± 0.02）％. The particle size was （190.64±15.97）nm with polydispersity index of 0.086±0.007，and Zeta potential was （－12.74± 1.60）mV. CONCLUSIONS ：The optimized formulation of CUR-TEs is stable ，feasible and repeatable ，with good stability.
ABSTRACT
Objective To optimize the processing technology of stir-frying with vinegar of Curcuma Longa Radix (CLR) by orthogonal design and Box-Behnken design-respanse surface method (BBD-RSM) based on entropy method. Methods As comprehensive evaluation indexes, the contents of curcumin, demethoxycurcumin, and bisdemethoxycurcumin in CLR processed by traditional method were determined by HPLC. The orthogonal test was adapted to examine the influence of the amount of vinegar, the moistening time, parching time, and parching temperature on processing technology of stir-frying with vinegar. Based on the results above, BBD-RSM was adopted to optimize the processing technology further using the moistening time, parching time and parching temperature as factors. Results The optimum processing technology of the orthogonal test was covered the amount of vinegar of 15%, moistening time of 10 min, parching temperature of 130 ℃, and parching time of 10 min. The optimum processing technology by BBD-RSM was covered moistening time of 12 min, parching temperature of 150 ℃, and parching time of 8 min. The verification esting indicates that the process conditions are reasonable and feasible with good reproducibility. Conclusion The method and data are precise and reliable. Besides, it established the processing technology of vinegar CLR and provided a theoretical basis for the processing technology of stir-frying with vinegar of CLR.
ABSTRACT
Objective: To optimize the composition of Compound Cheqinggao microemulsion and investigate its stability. Methods: Suitable emulsifier, co-emulsifier, and oil phase were selected by solubility method, and the pseudo ternary phase diagram was drawing by water titration. Then, the factors with the mass fraction of emulsifier, co-emulsifier, and oil phase as the independent variables, and the drug loading and particle size as response value, using Box-Behnken design-response surface method to determine the best prescription ratio and investigate its stability. Results: The optimal composition of substrate from Compound Cheqinggao microemulsion was as follows: 33% of polyoxyethylene hychogenated castor oil (RH40), 16% of polyethylene glycol (PGE400), 16% of Isopropyl palmitate, and 35% of water. Under these conditions, drug loading was 224.17 mg/mL and the particle size was 56.50 nm. Compound Cheqinggao microemulsion has good stability at 4 ℃ and 25 ℃ in dark conditions. Conclusion: The prepared microemulsion has good appearance, high drug loading, suitable particle size, and good stability, which could greatly increase the solubility of Compound Cheqinggao volatile oil.
ABSTRACT
OBJECTIVE:To optimize the extraction technology of total flavonoids from Psidium guajava leaves and investigate the effects of total flavonoids from P guajava leaves on glucose tolerance in diabetic model mice.METHODS:Based on single factor test,using extraction time,solid-liquid ratio and the amount of ethanol as independent variables,comprehensive scores of the yield of hyperin,quercetin-3-O-β-D-arabinopyranoside,quercetin-3-O-α-L-furanarabino side ethyl acetate and extract as dependent variable,Box-Behnken design-response surface method was used to optimize the reflux extraction process of total flavonoids from P guajava leaves,and validation test was also conducted.Sixty mice were randomly divided into blank group,model group,metformin group (170 mg/kg),P.guajava leaves total flavonoids low-dose,medium-dose and high-dose groups (23.41,46.81,93.62 mg/kg,by the content of total flavonoids),with 10 mice in each group.Except for blank group,diabetic model was induced in those groups,and then model mice were given relevant medicine intragastrically once a day for consecutive 21 d,6 h after last medication given glucose 2.0 g/kg intragastrically.The levels of blood glucose were determined 0,0.5,1.0,2.0 h after intragastric administration of glucose,and the area under the curve (AUC) of blood glucose was calculated.RESULTS:The optimal technology of P guajava leaves total flavonoids was as follows as extracting twice,lasting for 1.0 h each time,solid-liquid ratio of 1 ∶ 17,ethanol volume fraction of 56％.In validation test,the contents of hyperin,quercetin-3-O-β-D-arabinopyranoside and quercetin-3-O-α-L-furanarabino side ethyl acetate were 2.57,3.38,2.26 mg/g(RSD＜2％,n=3);the yield of extract was 25.71％ (RSD=1.19％,n=3);average comprehensive score was 96.41 (RSD=l.34％,n=3);relative error was 3.57％ with the predicted value of 99.98.Compared with blank group,AUC of mice were increased significantly in each group;compared with model group,AUC of metformin group,P.guajava leaves total flavonoids medium-dose and high-dose groups were all decreased significantly,with statistical significance (P＜0.05 or P＜0.01).CONCLUSIONS:The optimal extraction technology is stable,feasible and controllable in quality.Total flavonoids from P.guajava leaves can promote the recovery to normal level of blood glucose.
ABSTRACT
Objective To optimize the dry granules process of Typha Pollen. Methods The particle size and particle friability were selected as evaluation indexes. The inspect factors were water content, compression frequency, and granulation frequency. Influence of inspect factors on evaluation indexes was investigated by single factor test, the influence of inspect factors on OD value was investigated by Box-Behnken design, and response surface method was adopted to predict, analyze and choose optimal process. Results The optimal dry granulation technology was as follows: the water content was 35.0%; the frequency of tabletting was 27 Hz; the granulating frequency was 15 Hz. Conclusion The selected process is stable, feasible and reproducible, which can be used for granulation of Typha Pollen granules.
ABSTRACT
Objective: To optimize the preparation technology for total glucosides from Paeonia lactiflora (TGP) liposome and study on its in vitro release. Methods: Liposomes were prepared by reverse-phase evaporation technique. Taking the entrapment efficiency (EE) as indexes, the preparation of liposome was optimized using Box-Behnken design-response surface method (BBD-RSM), and the in vitro release was studied. Results: The optimal formulation was cholesterol-lecithin (1:2.7), TGP-lipid (1:29), and hydrated medium of 5.1 mL. The average EE were 73.0% and the 12 h in vitro accumulative release rate was 42.18%. Conclusion: The optimized process is rational and feasible, and the TGP liposome has the higher EE and good stability with better sustained release in vitro.