Objective To establish the determination method of gallic acid in Yuanhu Zhitong Soft Capsule by HPLC. Methods Chromatography was performed on a Unitary C18 column (250 mm× 4.6 mm, 5 μm) at 254 nm. The mobile phase consisted of a mixture of methanol and 0.5%phosphate acid (5∶95) at flow rate of 1.0 mL/min. Results The standard curve of linear relationship was 0.024 8-0.496 μg and r=0.999 9. The RSD of precision, repeatability and stability was 0.27%, 0.21%, 1.40%, respectively. The average recovery was 99.81%, RSD was 0.72%. Conclusion The established method was accurate and reliable for the determination of gallic acid in Yuanhu Zhitong Soft Capsule.

Artemisinin is the antimalarial active ingredient, which is discovered by Chinese scientists in 1970s. The chemical structure of artemisinin is modified or altered to obtain a series of analogues to satisfy the medication requirements. According to the physicochemical properties of medicines and actual clinical necessities, the preparations of artemisinins are developed and the common preparations include tablet, suppository, injection, etc.. With the developing of technology, researchers have conducted a large number of studies on the artemisinins nanoparticles injection, transdermal drug delivery systems, mucosal drug delivery systems and etc. This article systematically collected and discussed the recent studies on the antimalarial preparations of artemisinins in line with different administration routes.

Objective To analyze the composing principles of the prescriptions for the shell of Gelatin Soft Capsule (GSP). Methods Totally 41 articles related to shell of GSP published on journals, dissertation and patent literatures in recent 10 years were used to analyze the composing principles for the shell of GSP by TCM Inheritance Platform System. Results The core combination was glycerin-gelatin-water, and the peripheral combinations ingredients included sorbitol, lemon yellow, titaniaum dioxide, iron oxide, PEG400 and ethylparaben, et al. Conclusion TCM Inheritance Platform System can be used for analyzing the composing principles of GSP.

Objective:To establish a method of evaluating the reproducibility of the preparation process of Xiaozheng-Zhitong cataplasm. Methods:Used fingerprint spectrum technology and in vitro release test to evaluate the reproducibility preparation process of Xiaozheng-Zhitong cataplasm. By using HPLC to establish the fingerprint of Xiaozheng-Zhitong cataplasm. The chromatographic column was an Agilent HC-C18 column (4.6 mm×250 mm, 5 μm); the detection wavelength was 280 nm; the flow rate was 1 ml/min; the column temperature was 25 ℃. The mobile phase was acetonitrile-0.2% phosphoric acid aqueous solution, used gradient elution method. An HPLC method for the determination of tetrahydropalmatine content was established, and the vertical Franz diffusion cell method was used to investigate its in vitro release. Results:The results showed that the similarity between the 10 batches of Xiaozheng-Zhitong cataplasm and the control map was above 0.95, indicating that the process of Xiaozheng-Zhitong cataplasm was stable and feasible; the cumulative release amount of tetrahydropalmatine was 0.23 mg in 24 hours, and the cumulative release rate in 8 hours was 91.54%, and the RSD of 6 samples at each time point was <3%. Conclusion:The method of evaluating the reproducibility of the preparation process of Xiaozheng-Zhitong cataplasm was established by using fingerprint technology and in vitro release; it can provide a reference and scientific basis for the evaluation of the reproducibility of the preparation process of the plaster.

Objective To optimize refinement of water extract from Bushen Yangxue Granules by chitosan flocculation.Methods According to the content of icariin detected by HPLC, the waters amount, extraction time and extraction times were evaluated by orthogonal design. The effects of the solution concentration, clarifying temperature and the amount of clarifying agent on the flocculation clarification processes were optimized with the content of icariin and polysaccharides.Results The optimum water extraction processes A2B1C3 were follows: 10 times amount of water, three times extraction and 1 h for each extraction process. The optimized flocculation clarification processes A1B2C3 were as follows: solution concentration was 0.4 g/mL, the clarifying temperature was 40℃ and the addition of chitosan was 0.1%.Conclusion The optimized refining process is stable and feasible.

Objective To study the effects of microemulsion/ethosomes on transdermal absorption properties and efficacy of Huoxue Zhitong Cataplasm. Methods The improved Franz diffusion cells were used for the in-vitro permeation experiment with rat skins as the barriers, which was used to evaluate the transdermal absorption properties. In the erxeriment, the contents of paeonol, eugenol and methyl salicylate were used as markers, and detected by ultra performance liquid chromatography to evaluate the transdermal absorption effects. The anti-inflammatory and analgesia activity were evaluated through the writhing plate experiments. Results The cumulative release rate of paeonol in Huoxue Zhitong Cataplasm, Microemulsion Huoxue Zhitong Cataplasm and Ethosomes Huoxue Zhitong Cataplasm were, in order, 65.30%, 61.30%and 60.20%in 24 h;eugenol were, in order, 51.08%, 54.71% and 55.66% in 24 h; methyl salicylate were, in order, 49.20%, 65.17% and 72.15% in 24 h. Furthermore, Microemulsion Huoxue Zhitong Cataplasm high-dose group and Ethosomes Huoxue Zhitong Cataplasm medium-dose group had good effects on reducing the inflammatory exudate of peritoneal capillary and capillary permeability (P<0.05) in animal models. Conclusion Huoxue Zhitong Cataplasm based on microemulsion/ethosomesnano-technology has good transdermal absorption properties and efficacy.

OBJECTIVETo optimize the matrix formulation of cataplasm.

METHODFace-centered design was used in the experimental design, and response surface was produced in quadratic polynomial after data fitting in order to explore the impacts of Sodium Polyacrylate, Carbomer and the cross-linking agent on stickiness of cataplasm, optimize the prescription of the cataplasm matrix and perform the evaluation analysis.

RESULTThe multiple correlation coefficient (R2) and adjusted R2 in the fitting method using quadratic polynomial were 0.970 and 0. 952 (F = 53.953, P = 0.0001), respectively, and the model was significant different. The ratio of optimum proportion of Sodium Polyacrylate, Carbomer and the cross-linking agent in the matrix of cataplasm was determined, which was proved efficaciously.

CONCLUSIONFace-centered design-response surface method is a simple method with good prediction result for the optimization of cataplasm matrix.

Chemistry, Pharmaceutical ; methods ; Drugs, Chinese Herbal ; chemistry ; Models, Theoretical

OBJECTIVETo investigate the regularity of Yulian Cataplasm in vitro release and transdermal behaviors.

METHODImproved Franz diffusion devices was used with four index ingredients as evodiamine, rutaecarpine, palmatine and berberine that were determined by HPLC in one mobile phase.

RESULTThe release rates of evodiamine, rutaecarpine, palmatine and berberine were 0.0239, 0.0156, 0.0725, 0.8191 mg x cm(-2) x h(-1/2), respectivley. The transdermal rates of evodiamine, rutaecarpine, palmatine and berberine were 1.256, 1.0302, 2.8029, 20.919 microg x cm(-2) x h(-1), respectively.

CONCLUSIONThe releasing process of all index is in accordance with Higuchi equation and the transdermal proccess is in accordance with zero-level equation.

Animals ; Berberine ; administration & dosage ; pharmacokinetics ; Berberine Alkaloids ; administration & dosage ; pharmacokinetics ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Indole Alkaloids ; administration & dosage ; pharmacokinetics ; Mice ; Plant Extracts ; administration & dosage ; pharmacokinetics ; Quinazolines ; administration & dosage ; pharmacokinetics ; Skin ; metabolism ; Skin Absorption

Objective:To study the hypoglycemic effect of Quercus mongolica leaves total flavonoids on alloxan-induced hyperglycemia mice; To discuss its underlying mechanism and pharmacodynamic material basis.Methods:The healthy ICR mice were divided into control group and diabetic mice group according to random number table method. The diabetic mouse model was established by intravenously injected with streptozotocin solution (45 mg/kg) via the tail vein. The model diabetic mice were divided into model group, positive drug group (150 mg/kg metformin hydrochloride), total flavonoids low (100 mg/kg), medium (200 mg/kg) and high (400 mg/kg) dose groups, and monomer flavonoids low (25 mg/kg), medium (50 mg/kg) and high (100 mg/kg) dose groups. Each group of mice received 0.2 ml/10 g body weight for gavage, once a day for 14 consecutive days. The control and model group were given an equal volume of physiological saline. On the 7th and 14th day of administration, the body weight, fasting blood glucose, area under the curve (AUC) of blood glucose, serum insulin and insulin receptor beta concentrations, and insulin sensitivity index were measured. The main chemical components of total flavonoids from Quercus mongolica leaves were analyzed using ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) technology.Results:Compared with the model group, after 14 days of administration, the total flavonoids of Quercus mongolica leaves at different doses and quercetin-3-O-β-D-glucopyranoside and astragalin at different doses all significantly reduced blood glucose levels ( P<0.01 or P<0.05), decreased AUC ( P<0.01 or P<0.05), and increased insulin sensitivity index ( P<0.01 or P<0.05). The 12 flavone glycosides and aglycone components were identified by UPLC-MS/MS. Conclusions:Flavonoids are speculated to be the material basis for the hypoglycemic effect of Quercus mongolica leaves. Among them, total flavonoids of Quercus mongolica leaves and monomeric flavonoids such as quercetin 3-O-β-D-glucopyranoside and astragalin have certain hypoglycemic activity, which can lower blood glucose levels by improving insulin resistance.

OBJECTIVETo compare the pharmcoknetic parameters of six major alkaloids in the two drug delivery system of Zuojin Wan, by LC-MS assaying the six major alkaloids plasma concentration.

METHODThe blood samples were collected at different time after transdermal administration. The plasma concentration of six major alkaloids were detected by LC-MS, then the concentration-time data are modulated by software WinNonlin.

RESULTTook the six alkaloids (berberine palmatine coptisine jateorhizine evodiamine rutecarpine) as index components, the relative bioavailability were 131%, 127%, 108%, 121%, 92%, 109%, respectively, the ratio of Ka were 10.5, 5.1, 3.7, 0.8, 1.8, 1.5, respectively.

CONCLUSIONThe LC-MS can be applied in the determination of six major alkaloids plasma concentration. The pharmcoknetic parameters indicated that Zuojin Wan microemulsion gel delivery system can accelerate the transdermal absorption rate of Zuojin Wan, compared with the hydrogel drug delivery system.

Alkaloids ; administration & dosage ; chemistry ; pharmacokinetics ; Animals ; Chromatography, Liquid ; Drug Delivery Systems ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; pharmacokinetics ; Emulsions ; Female ; Gels ; Hydrogels ; chemistry ; Male ; Mass Spectrometry ; Rats