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1.
Article in Chinese | WPRIM | ID: wpr-872724

ABSTRACT

Objective:Arrange long-term toxicity experiments by a uniform design method, so as to explore the effect of different extracts of Psoraleae Fructus on liver toxicity in rats and mice, and find the drug factors that cause psoralen liver toxicity. Method:Based on the factors of processing, extraction technology, dosage and treatment course, each experimental group was arranged by uniform design method. A total of 220 SD rats and 220 Kunming mice with half male and half female were divided into normal groups and drug groups 1 to 8. The corresponding drugs (50% alcohol extract of salt Psoraleae Fructus in rats 2.57 g·kg-1, mice 5.14 g·kg-1, 95% alcohol extract of Psoraleae Fructus in rats 0.51 g·kg-1, mice 1.02 g·kg-1, 70% alcohol extract of salt Psoraleae Fructus in rats 1.71 g·kg-1, mice 3.42 g·kg-1, water extract of Psoraleae Fructus in rats 1.03 g·kg-1, mice 2.06 g·kg-1, water extract of salt Psoraleae Fructus in rats 1.03 g·kg-1, mice 2.06 g·kg-1, 70% alcohol extract of Psoraleae Fructus in rats 1.71 g·kg-1, mice 3.42 g·kg-1, 95% alcohol extract of salt Psoraleae Fructus in rats 0.51 g·kg-1, mice 1.02 g·kg-1, 50% alcohol extract of Psoraleae Fructus in rats 2.57 g·kg-1, mice 5.14 g·kg-1) were administered by gavage daily. The body weight and food intake of the rats and mice were measured once a week. After the treatment course, the rats were anesthetized with sodium pentobarbital, and blood was taken from the abdominal aorta, and the mice were sacrificed by removing the eyeballs, and the liver and brain were taken to calculate the organ coefficients. Serum was taken to determine liver function-related indicators, and the liver was taken for histopathological examination by hematoxylin-eosin (HE) staining. Result:The liver visceral-brain ratio of female rats in group 3 were significantly increased (P<0.05). The liver quality, visceral-body ratio and visceral-brain ratio of male mice in groups 1 to 3 were significantly increased (P<0.05, P<0.01). Histopathological manifestations in mice were more obvious than those in rats. Histopathology showed hepatocyte hypertrophy in the central area of liver lobules in mice, in particular in group 3. According to the multiple regression equation, there were interactions between extraction technology, processing, dosage and treatment course, and the extraction technology was positively correlated with the pathological score of liver injury. Based on the results of visual analysis and other indicators, it is concluded that the extraction technology factor is most relevant to psoralen liver toxicity of Psoraleae Fructus. Conclusion:Psoraleae Fructus has the hepatotoxicity, which is related to ethanol extraction technology; alcohol extraction is more toxic than water extraction, and 70% ethanol extraction is the most toxic. Besides, there are species differences, with a more significant hepatotoxicity in mice than that in rats.

2.
China Pharmacy ; (12): 196-201, 2020.
Article in Chinese | WPRIM | ID: wpr-817361

ABSTRACT

OBJECTIVE:To optimi ze the optimal composition proportion of 4 ingredients (Panax ginseng ,Astragalus membranaceus,Polygonatum sibiricum ,Lycium chinensis )in Compound ginseng immune-enhancing formula (CGIF),and to study immune activity and acute toxicity of the extracts with the optimal ratio. METHODS :The cell activity test was used to screen the crude drug concentration range of 4 ingredients. After treated with different crude drug concentrations of each medicinal material,using the contents of NO ,IL-6 and TNF-α as indexes,uniform design was used to determine the optimal ratio of each ingredient in CGIF. Totally 240 mice were taken and randomly divided into 4 batches,with 60 mice in each batch. Each batch of mice was randomly divided into blank group (normal saline ),model group (normal saline ),positive drug group [levamisole ,4 mg/(kg·d)],and optimal proportion extract of CGIF low-dose ,medium-dose and high-dose groups [ 0.952 8,1.905 6,3.811 2 g/(kg·d)],with 10 mice in each group ;they were given medicine intragastrically ,qd,for consecutive 30 d. Except for blank group,mice in the other groups were intraperitoneally injected with cyclophosphamide [ 40 mg/(kg·d)] on the 24th day after first administration,qd,for consecutive 3 d to induce immunocompromised model. The immune activity of the optimal proportion extract was evaluated by determining visceral coefficients ,spleen lymphocyte transformation capacity ,serum contents of hemolysin,IL-2,IgM,IgG and IgA ,phagocytosis function of peritoneal macrophages. Another 20 mice were collected and given the optimal proportion extract 20 mL/kg intragastrically ,twice;acute toxicity of the formula was investigated with oral maximum tolerated dose (MTD). RESULTS :The optimal ratio of CGIF was that crude drug mass ratio of P. ginseng , membranaceus,P. sibiricum ,L. chinensis was 1 ∶ 2 ∶ 2 ∶ 4. The immunological activity experiment showed that theoptimal proportion extract can significantly improve visceral indexes of mice , spleen lymphocyte proliferation ability serum contents of hemolysin ,IL-2,IgM,IgG and IgA as well as macrophage phagocy tosis ability (P<0.05 or P< 0.01). The acute toxicity test indicated that oral MTD was over 15 g/kg,which was non-toxic. CONCLUSIONS :The optimal proportion extract of CGIF can significantly enhance the immune function of mice and are non-toxic.

3.
Acta Pharmaceutica Sinica ; (12): 276-282, 2020.
Article in Chinese | WPRIM | ID: wpr-789026

ABSTRACT

Recently, the hepatotoxicity issue regarding to Psoraleae Fructus (PF) has attracted remarkable concerns, which highlights the urgent need to explore the toxicity attenuation method for PF. In this study, we proposed an alcohol soaking and water rinsing method for pre-processing PF based on the record in the classics - "Lei Gong Pao Zhi Lun", aiming to attenuate the potential hepatotoxicity of PF. The optimal pre-processing methods and parameters were investigated by U*12(108) uniform design coupled with 3D-cultured human-derived liver organoids model and high-content imaging. The results showed that there were significant variations among the hepatotoxicity intensities of different pre-processed PF products. Four factors, including the concentration of alcohol, the ratio of material and alcohol in alcohol soaking, the time of alcohol soaking and the times of water rinsing, were found as independent significant factors (all P<0.01). The optimal pre-process parameters were further predicted and verified as follows: the alcohol concentration is 80%, the times of alcohol soaking is 3, the ratio of alcohol and material of alcohol soaking is 3, the time for alcohol soaking is 30 h, the ratio of water and material of water rinsing is 2, the times of water rinsing is 3, the time water rinsing is 12 h and the time of steaming is 5 h. This research demonstrated that the alcohol soaking and water rinsing method can effectively reduce the potential hepatotoxicity of PF. This method provides a reference for reducing the risk of PF liver injury from the perspective of Chinese medicinal materials pre-processing.

4.
Article in Chinese | WPRIM | ID: wpr-802264

ABSTRACT

Objective:To optimize proportion of couplet medicine of Bupleuri Radix and Scutellariae Radix in the treatment of anti-depression, and to explore the possible antidepressant mechanism of this couplet medicine. Method:The dosages of Bupleuri Radix and Scutellariae Radix in the 2015 edition of Chinese Pharmacopoeia were taken.According to U7(72) uniform design table, Bupleuri Radix and Scutellariae Radix were carried out into 7 groups.The chronic unpredictable mild depression model mice were induced by intragastric administration of decoction of this couplet medicine and the antidepressant effect was observed by the behavior tests, which included sucrose preference test, tail suspension test, forced swimming test and open field test(crossing scores).The regression equations were established by selecting the effective indexes.The experiments of retest were taken to check the results and the possible antidepressant mechanism was primarily investigated by measuring the phosphorylation level of cyclic adenosine monophosphate(cAMP)-response element binding protein(CREB) and expression of brain-derived neurotrophic factor(BDNF). Result:Compared with the blank group, sucrose preference rate of the model group was significantly decreased(PPPPPPPPPPPPPPConclusion:Compatibility of Bupleuri Radix and Scutellariae Radix can ameliorate depressive-like behavior of model mice, and the best antidepressant compatibility proportion of Bupleuri Radix and Scutellariae Radix is 1:1, the optimal amounts of them are about 5 g.The antidepressant effect may relate to promoting phosphorylation level of CREB and the expression of BDNF in the hippocampus.

5.
Article in Chinese | WPRIM | ID: wpr-801830

ABSTRACT

Objective: To screen the best compatibility proportion of total alkaloids of Coptidis Rhizoma and Notoginseng Radix et Rhizoma total saponins (HS composition)by uniform design and pharmacological model and to observe the effect on diabetic complications. Method: The total alkaloids of Coptidis Rhizoma and Notoginseng Radix et Rhizoma total saponins were used as the research objects, U6(62) table was choosed for grouping design.The content of triglyceride fasting blood-glucose (FBG), prothrombin time (PT) and active partial thromboplastin time (APTT) was chosen as index. The best dose ratio was obtained by multipleregression analysis. Rats with type 2 diabetes mellitus induced by high-fat diet combined streptozotocin were divided into blank group, model group, metformin group (150 mg·kg-1), HS composition group (total alkaloids of Coptidis Rhizoma 360 mg·kg-1+ Notoginseng Radix et Rhizoma total saponins 40 mg·kg-1). Rats were administered orally for 10 weeks.By observing the blood glucose, glucose tolerance,area under the curve (AUC), triglyceride (TG), high-density lipoprotein (HDL-C)and low-density lipoprotein (LDL-C), hemorheological indexes and pathological changes of pancreas, heart, kidney and retina in rats of each group, the effect of this composition on diabetic complications was verified. Result: Combination of 625 mg·kg-1 total alkaloids of Coptidis Rhizoma and 60 mg·kg-1 Notoginseng Radix et Rhizoma total saponins was the optimal dosage ratio of HS composition.The validation test showed that compared with blank group, the fasting blood glucose and lipid levels in the model group were significantly increased (PPPPPPPPPPPConclusion: The optimum compatibility dose of HS composition have a good therapeutic effect on diabetic complication rats induced by high-fat diet and streptozotocin.

6.
Article in Chinese | WPRIM | ID: wpr-850877

ABSTRACT

Objective: To prepare total alkaloids of Strychni Semen (TASS) - total glucosides of paeony (TGP) lipid-based cubic liquid crystalline nanoparticles (TASS-TGP LLCN) and investigate its percutaneous absorption behavior. Methods: TASS-TGP LLCN was prepared by precursor injection method, and the encapsulation efficiency (EE) was determined by ultrafiltration centrifugation. The prescription of TASS-TGP LLCN was optimized by uniform design with the encapsulation efficiency as the index, and the basic properties of the optimized TASS-TGP LLCN were evaluated. Meanwhile, Poloxamer 407 (F127) was used as matrix to prepare gel, Franz diffusion method was used to compare the in vitro percutaneous permeability of TASS-TGP LLCN gel with TASS-TGP ordinary gel. Results: The optimal formula of TASS-TGP LLCN was glycerol monooleate (GMO) 1.0 g, F127 0.25 g, dispersed phase 60 mL. The EE of brucine, strychnine and paeoniflorin were all more than 50%, the average particle size was about (245.3 ± 16.4) nm, the pH value was 6.62, and the cubic structure was uniform in size under transmission electron microscope. The cumulate osmotic quantities in 24 h, the permeation rate and the skin retention volume of TASS-TGP LLCN gel were all better than ordinary gel of TASS-TGP. Conclusion: TASS-TGP LLCN has dual effects of promoting permeability and skin reservoir, which has a potential development prospect.

7.
Article in Chinese | WPRIM | ID: wpr-852068

ABSTRACT

Objective: The preparation process of curcumin-loaded TPGS/F127/P123 mixed micelles was optimized with uniform design method to improve the poor solubility of curcumin in water, aiming to increase entrapment efficiency (EE), drug-loading (DL), and reduce the precipitated drug (PD). Methods: Curcumin-loaded TPGS/F127/P123 mixed micelles were prepared by thin-film hydration method with modification. Before using the uniform design, a number of preliminary experiments were conducted to identify the controlled factors such as the amount of curcumin, the dosage of TPGS, and the ratio of F127/P123. The formulation was operated by uniform design of three factors and seven levels, and its results were fitted by polynomial linear equation, the response surface, and the contour line in order to choose and verify the optimal preparation process. Results: In the optimum formulation, the dosage of curcumin was 14.0 mg, TPGS 150.0 mg, and the ratio of F127/P123 was 68: 32. The solubility of optimum formulation was (3.47 ± 0.14) mg/mL, EE (87.15 ± 4.39)%, DL (4.70 ± 0.17)%, and PD (0.33 ± 0.12)% in 48 h. Conclusion: The solubility of curcumin in TPGS/F127/P123 mixed micelles was improved after the optimization of the uniform design method, and EE and DL were also improved.

8.
China Pharmacy ; (12): 958-963, 2018.
Article in Chinese | WPRIM | ID: wpr-704714

ABSTRACT

OBJECTIVE:To optimize extraction technology of cortex of Berberis dictyophylla by ethanol. METHODS:Using the contents of magnoflorine,jatrorrhizine hydrochloride,palmatine hydrochloride and berberine hydrochloride,the amount of extract as evaluation indexes,the effects of ethanol amount,volume fraction of ethanol and extraction time on extraction technology were investigated by uniform design method-comprehensive scoring method. The extraction methods of first time, second time and third time were investigated by 3 times of uniform design test. The optimal schemes of 3 times of extraction test were determined and validation test was conducted,and the transfer rates were calculated. RESULTS:The optimal technology was as follows as coarse powder of cortex of B. dictyophylla,15-fold 75% ethanol,extracting for 2 times,120 min each time. In validation test,the contents of magnoflorine,jatrorrhizine hydrochloride,palmatine hydrochloride and berberine hydrochloride were 58.96,4.82,3.07,23.29 mg/g after B. dictyophylla was extracted by optimization technology for 2 times. The transfer rates were 93.85%,95.02%,96.28%,94.88%,respectively(RSD=3.87%,2.64%,4.00%,3.91%,n=3). CONCLUSIONS:The optimal ethanol reflux extraction technology of cortex of B.dictyophylla is reasonable and feasible with good stability.

9.
Journal of Integrative Medicine ; (12): 290-296, 2018.
Article in English | WPRIM | ID: wpr-691063

ABSTRACT

<p><b>OBJECTIVE</b>The main objective of this study was to preliminarily determine the optimum formulation of a Chinese herbal formula that may have neuroprotective effects against rotenone-induced Parkinson's disease (PD).</p><p><b>METHODS</b>Seven recipes were made from Dihuang (DH, Rehmannia glutinosa Libosch), Roucongrong (RCR, Cistanche deserticola Y.C.Ma), Niuxi (NX, Achyranthes bidentata Bl.) and Shanzhuyu (SZY, Cornus officinalis Sieb. et Zucc) in different proportions, according to the principles of uniform design (4 factors 7 levels). Tyrosine hydroxylase (TH)-positive neurons in substantia nigra pars compacta (SNpc) were detected by immunohistochemistry and rotenone-exposure days necessary to induce PD symptoms were recorded. To probe one likely mechanism of the formulas, echinacoside (ECH) concentrations of all seven recipes were determined by high-performance liquid chromatography and related to number of TH-positive neurons.</p><p><b>RESULTS</b>The data showed that recipe 4 (DH:RCR:SZY:NX = 1:1:1:1) and recipe 7 (DH:RCR:SZY:NX = 7:5:3:1) partially reversed rotenone-induced death of TH-positive neurons in the SNpc and significantly increased rotenone-exposed days compared with model group. Pharmacologically, there was not a strong correlation between ECH concentration and TH-positive neurons.</p><p><b>CONCLUSION</b>The investigated formulations of Chinese herbs had neuroprotective effects against PD models, and the neuroprotective effects were weakly related to the proportion of key herbs. However the neuroprotective effects of the formula may not result from a single active constituent.</p>


Subject(s)
Animals , Disease Models, Animal , Drugs, Chinese Herbal , Chemistry , Humans , Male , Neuroprotective Agents , Chemistry , Parkinson Disease , Drug Therapy , Plants, Medicinal , Chemistry , Rats , Rats, Wistar , Rotenone
10.
China Pharmacy ; (12): 1361-1364, 2017.
Article in Chinese | WPRIM | ID: wpr-515400

ABSTRACT

OBJECTIVE:To optimize the extraction technology of Duoxuekang. METHODS:Using comprehensive score of salidroside,gallic acid content and extraction yield as indexes,U6(63)uniform design was designed to optimize the liquid-solid ra-tio,ethanol volume fraction and extraction time of Duoxuekang,then optimize extraction times,and verification test was conduct-ed. RESULTS:The optimal extraction technology was as follows as 50% ethanol,liquid-solid ratio of 1:14,soaking time of 1.5 h,reflux extraction for 1 h and repeated twice;the average extraction yield in 3 tests was 50.18%,contents of salidroside and gal-lic acid were 1.82 mg/g,16.54 mg/g (RSD≤0.84%,n=3). CONCLUSIONS:The optimized extraction technology for Duox-uekang is reasonable,simple and feasible.

11.
China Pharmacy ; (12): 1382-1385, 2017.
Article in Chinese | WPRIM | ID: wpr-515338

ABSTRACT

OBJECTIVE:To screen the matrix formulation of Indomethacin hydrophilic gel patch. METHODS:Using appear-ance,adhesion,softness,moisture retention as indexes,mixed level of uniform design was used to screen matrix formulation of patch,verification test and in vitro transdermal test were used to evaluate the patch quality. RESULTS:Optimized matrix formula-tion was as follow as PVA of 7.686 g,PVP of 9.662 g,glyceryl of 19.992 g,gelatin of 9.999 g,CMC-Na of 13.997 g,carbomer of 3.000 g,HPMC of 1.500 g. The prepared patch had smooth surface,uniform matrix,good color,strong adhesion,good soft-ness(water loss rate of 11.9%). It can be slowly released for 48 h. The in vitro transdermal release fitted the Higuchi model(R2=0.9869). CONCLUSIONS:Indomethacin hydrophilic gel patch is successfully prepared,which can slowly release drug with over-all good quality.

12.
China Pharmacy ; (12): 3976-3979, 2017.
Article in Chinese | WPRIM | ID: wpr-662029

ABSTRACT

OBJECTIVE:To optimize the extraction technology of Compound radix fici hirta granule. METHODS:Using the transfer rate of psoralen and amygdalin in extraction liquid of Compound radix fici hirta granule and extraction rate as indexes, U12(6×4×3)uniform design was used for the test,the effects of amount of adding water,extraction time,extraction times on the extraction technology were investigated,and optimized technology was verified by three pilot scale tests. RESULTS:The optimal technology was as follow as 10-fold water,extracting for 3 times,60 min each time. Under the conditions,transfer rate of pso-ralen and amygdalin and extraction rate were 82.51%(RSD=1.45%,n=3),93.69%(RSD=0.85%,n=3),18.89%(RSD=0.74%,n=3),respectively. The validated results were in the 95% confidence interval of predictive value. CONCLUSIONS:The optimized extraction technology is stable and feasible,and provides the scientific basis for the follow-up development of the prepa-ration.

13.
China Pharmacy ; (12): 3976-3979, 2017.
Article in Chinese | WPRIM | ID: wpr-659250

ABSTRACT

OBJECTIVE:To optimize the extraction technology of Compound radix fici hirta granule. METHODS:Using the transfer rate of psoralen and amygdalin in extraction liquid of Compound radix fici hirta granule and extraction rate as indexes, U12(6×4×3)uniform design was used for the test,the effects of amount of adding water,extraction time,extraction times on the extraction technology were investigated,and optimized technology was verified by three pilot scale tests. RESULTS:The optimal technology was as follow as 10-fold water,extracting for 3 times,60 min each time. Under the conditions,transfer rate of pso-ralen and amygdalin and extraction rate were 82.51%(RSD=1.45%,n=3),93.69%(RSD=0.85%,n=3),18.89%(RSD=0.74%,n=3),respectively. The validated results were in the 95% confidence interval of predictive value. CONCLUSIONS:The optimized extraction technology is stable and feasible,and provides the scientific basis for the follow-up development of the prepa-ration.

14.
China Pharmacy ; (12): 1834-1836, 2017.
Article in Chinese | WPRIM | ID: wpr-512433

ABSTRACT

OBJECTIVE:To optimize ultrasonic extraction technology for polysaccharide from Aconiti lateralis radix praepara-ta(ALRP). METHODS:Uniform design method was applied to investigate the effects of liquid material ratio,ultrasonic time and ultrasonic temperature on extraction rate of polysaccharide from ALRP. Verification test was conducted and compared with the re-sults of conventional decoction and boiling method. RESULTS:Optimized ultrasonic extraction technology was as follow as liquid material ratio of 10 mL/g,ultrasonic time of 34 min and ultrasonic temperature of 73 ℃. The polysaccharide extraction rate in veri-fication test was 19.05%(RSD=0.60%,n=3),relative error of the predicted value (19.44%) was 2.0%,while the extraction rate was higher than decoction and boiling method(16.42%). CONCLUSIONS:Optimized ultrasonic extraction technology is sim-ple,rapid and stable with high extraction rate,which is suitable for extracting polysaccharide from ALRP.

15.
Article in Chinese | WPRIM | ID: wpr-506351

ABSTRACT

Objective To study the effects of main ingredients from microemulsion extract of Compound Longqincao in vitro on anti-influenza virus H1N1 activity; To analyze effects of main ingredients from microemulsion extract on influenza virus inhibition rate.Methods Uniform design was used to conduct the experiment. MTT method was used to detect the effect rate (ER) of anti-influenza virus H1N1 on A549 cells. Setting ER as the index, Minitab17 software was used to establish mathematical model to come up with regression equations of all factors. The effects of ingredients on ER were analyzed and the efficient composition ratio of the optimum anti-influenza virus H1N1 was chosen.ResultsIn the compound compatibility, baicalin showed the most obvious antivirus activity, and licorice glycosides had certain inhibition effects on pathological changes of cells. Five ingredients had coordinative or controlled relation with ER. When per milliliter liquids containing licorice glycosides, baicalin, leucine, aspartic acid, glutamic acid was 13.94μg, 49.44μg, 0.23 mg, 1.25 mg, and 2.50 mg, ER was the best. ER was 85.34%±4.72% after verification.ConclusionThe optimized combination of main ingredients from microemulsion extract of Compound Longqincaocan better play a role in anti-influenza virus H1N1.

16.
China Pharmacy ; (12): 2635-2638, 2017.
Article in Chinese | WPRIM | ID: wpr-620739

ABSTRACT

OBJECTIVE:To study the new formula of effective components in TCM for anti-allergic rhinitis (AR),and pro-vide reference for developing TCM preparations for anti-AR. METHODS:Using pseudoephedrine hydrochloride (0-13.5 mg/kg), total alkaloid extracts of Aconitum carmichaelii (0-21.18 mg/kg),volatile oil of asari radix (0-0.0092 mL/kg) in Mahuang Fuzi Xixin decoction as formula objects,uniform design method was used for drug grouping,and multiple regression analysis was con-ducted for the behavioral scores before and after administration,contents of histamine and immunoglobulin E (IgE) in serum of AR guinea pigs to obtain the best formula. Using Xinqin granule,Loratadine tablet,Mahuang Fuzi Xixin decoction respectively as positive control,efficacy of the best formula was verified from aspects of behavioral scores before and after administration,con-tents of histamine and IgE of AR guinea pigs. And the safety of the best formula was preliminarily observed through acute toxicity test in mice. RESULTS:The best formula was as follow as pseudoephedrine hydrochloride 11.25 mg/kg,total alkaloid extracts of A. carmichaelii 21.18 mg/kg,volatile oil of asari radix 0.0045 mL/kg. Compared with each positive drug group,there were no sig-nificant differences in behavioral scores before and after administration in the best formula group(P>0.05). While compared with Xinqin granule group and Mahuang Fuzi Xixin decoction group,histamine content in serum in the best formula group was signifi-cantly reduced (P<0.05);compared with Xinqin granule and Loratadine tablet group,IgE content in serum in the best formula group was significant decreased (P<0.05). Median lethal dose of the best formula was 1822.04 mg/kg. CONCLUSIONS:The screened best formula shows better effect than Xinqin granule and Mahuang Fuzi Xixin decoction in terms of reducing histamine content in serum,better than Loratadine tablet and Xinqin granule in terms of reducing IgE content in serum,with good safety, which indicates the feasibility of TCM effective component formula to a certain degree.

17.
Article in Chinese | WPRIM | ID: wpr-853030

ABSTRACT

Objective: To establish an extraction process optimization method based on fingerprint combined with principal component analysis, which was finally applied to Compound Huzhang ethanol extraction process optimization. Methods: Taking Compound Huzhang prescription as model drug, different ethanol extraction condition fingerprint was established by HPLC, harvesting the areas of the common peaks, the total factor scores were calculated by PCA. Arranged experiments with U9(93×31) uniform design method, choosing the total factor scores as index, the influence of extration times (X1), alcohol consumption(X2), alcohol concentration(X3), and time of extracting(X4) on the yield of extract was investigated, then the technological parameters of optimum ethanol extraction condition were selected by multi-nonlinear mathematic models. Results: Multi-nonlinear mathematic models described the relationship between response indexes and factor variables with a regression coefficient of 0.997. The optimized conditions for Compound Huzhang Prescription were extracted in 90% ethanol six times as much as it for three times, 1h once. Conclusion: It is proved that the extraction method is suitable and feasible that could provide a reference for compound Chinese medicine extraction process optimization.

18.
Article in Chinese | WPRIM | ID: wpr-852675

ABSTRACT

Objective: To improve in vitro dissolution of lipophilic constituents in Compound Danshen Tablet, a novel freeze-dried emulsion was designed and developed. Methods: Compound Danshen liquid emulsion was prepared by high-speed shearing, following by high pressure homogenization process. The oil phase and cryoprotectants were optimized by uniform design test, using physical appearance and redispersibility as evaluation indexes. The in vitro dissolution profile of tanshinone IIA and borneol in the freeze-dried emulsion and Compound Danshen Tablet was determined in artificial gastric juice and artificial intestinal juice containing 0.5% sodium lauryl sulfate (SDS). Based on the appearance, average particle size and zeta potential, the stability of freeze-drying emulsion was investigated. Results: The developed Compound Danshen freeze-dried emulsion had good physical appearance, meanwhile maintained a good redispersibility and stability, when 10% medium chain triglycerides (MCT) was adopted as oil phase of liquid emulsion and 18% maltose combined with 0.25% beta-cyclodextrin was optimized as cryoprotectants. In artificial gastric juice, the accumulated dissolution rates of tanshinone IIA and borneol in Compound Danshen freeze-dried emulsion reached up to (94.8 ± 2.8)% and (97.4 ± 2.9)% at 30 min, respectively. However, the accumulated dissolution rate of borneol in the tablet was only (23.3 ± 3.4)% at 120 min, while tanshinone IIA showing no dissolution. In artificial intestinal juice, the accumulated dissolution rates of tanshinone IIA and borneol in the tablet rose to (42.5 ± 2.7)% and (74.4 ± 1.8)% at 120 min, but they were still much lower than that in the freeze-dried emulsion which reached up to (97.8 ± 1.9)% and (92.7 ± 3.5)%. After one year's storage, there were no significant changes of the stability evaluation index for freezing dry emulsion. Conclusion: The dissolution rates of lipophilic constituents in Compound Danshen freeze-dried emulsion increased significantly and exhibited a fast and fairly complete drug release, which provides a potential and promising formulation to improve bioavailability of the original dosage form of tablet. Its physical stability is good.

19.
Article in Chinese | WPRIM | ID: wpr-710126

ABSTRACT

AIM To prepare the matrine nanoparticles and their wheat germ agglutinin-modified product.METHODS Double emulsification-solvent evaporation method was employed to prepare matrine nanoparticles.In consideration of influencing factors of ratio of poly (lactic-co-glycolic acid) to matrine,rotational speed and polyvinyl alcohol concentration,as well as the evaluation indices of particle size,potential,encapsulation efficiency and drug load,the preparation was optimized by central composite design.Wheat germ agglutinin-modified matrine nanoparticles were prepared by carbodiimide method.In addition to the influencing factors of ratio of carbodiimide to N-hydroxysuccinimide,wheat germ agglutinin addition and incubation time,evaluation indices of particle size,potential and modification rate were also taken into account in the preparation optimization by uniform design.RESULTS The optimal conditions for matrine nanoparticles were determined to be 0.594 ∶ 1 for ratio of poly (lactic-co-glycolic acid) to matrine,815 r/min for rotational speed,and 0.46% for polyvinyl alcohol concentration.The average particle size,potential,encapsulation efficiency and drug loading were 112.04 nm,-15.38 mV,90.05% and 27.14%,respectively.The optimal conditions for their wheat germ agglutinin-modified product were found to be 2.8 ∶ 0.12 for ratio of carbodiimide to N-hydroxysuccinimide,3 mg for wheat germ agglutinin consumption,and 14 h for incubation time.The average particle size,potential and modification rate were 474.7 nm,-5.2 mV and 69.51%,respectively.CONCLUSION The preparation techniques are reliable,and the matrine nanoparticles and their wheat germ agglutinin-modified product show their stable properties.

20.
China Pharmacy ; (12): 3552-3554, 2016.
Article in Chinese | WPRIM | ID: wpr-504952

ABSTRACT

OBJECTIVE:To optimize the technology of supercritical CO2 extraction from Zingiberis rhizoma. METHODS:With the comprehensive score of the contents of 6-ginger phenol,8-ginger phenol and 10-ginger phenol and the extraction rate of the oil from Z. rhizoma as the index,uniform design method was adopted to investigate the effects of extraction pressure,extrac-tion temperature and extraction duration on the extraction result;verification tests were conducted. RESULTS:The optimal condi-tions were as follows as the extraction pressure of 25 MPa,extraction temperature of 30 ℃ and extraction duration of 2 h. In the verification tests,the average extraction rate of the oil from Z. rhizoma was 3.2%(n=3),and the comprehensive score was 1.874 2 (RSD=0.65%,n=3),with the relative deviation of 0.6% between the measured value and the predicted value. CONCLUSIONS:The optimal extraction technology is stable and feasible,with the advantages of low temperature,short duration.

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