Oxymatrine is an alkaloid from Traditional Chinese Medicine, Sophora flavescens Ait. which has many pharmacological effects. We studied the effects of oxymatrine on the proliferation of human tonsillar cells and mouse splenocytes with or without mitogens. The results show that oxymatrine can augment the proliferation of the human tonsillar cells which show low PHA & tSAC response capacity. On the other hand, oxymatrine can inhibit the proliferation of the human tonsillar cells which show high PHA & SAC responses capacity. The effects of oxymarine on mouse splenocytes are the same with the latter.

This study was aimed to develop an ICP-MS method to determine contents of six types of heavy metals, which include Cr, Pb, Cd, As, Hg and Cu, in Pian-Zai-Huang Gan-Bao (PZHGB) tablets. The samples were pro-cessed by microwave digestion. And then, they were determined by ICP-MS. The results showed that the working curves of Cr, Cu, As, Cd, Hg and Pb had good linear relationships with the correlation coefficient which was more than 0.9993. The average recovery rate of Cr was 101.2%. The relative standard deviation (RSD) was 7.6%. The av-erage recovery rate of Cu was 96.4%, with the RSD of 3.5%. The average recovery rate of As was 101.3%, with the RSD of 1.8%. The average recovery rate of Cd was 100.2%, with the RSD of 0.3%. The average recovery rate of Hg was 100.5%, with the RSD of 4.2%. The average recovery rate of Pb was 104.2%, with the RSD of 5.6%. It was concluded that the method was stable and reliable, with high sensitivity and repeatability. This method can be used in the content determination of six types of heavy metals, which include Cr, Pb, Cd, As, Hg and Cu in PZHGB tablets.

Objective To optimize the matrix formulation of the extract of Chuanxiong Rhizoma cataplasm. Methods The optimal proportion of matrix formulation was selected by uniform design and response surface method. The primary adhesion force, lasting adhesion force, peel strength and residuals on the anti-sticking paper were used as test parameters. The optimal ratios of NP-700, glycinate aluminum, glycerin, tartaric acid, the concentration of drug, and the volume of drug were acquired. Results The matrix formulation of the cataplasm was made with NP-700∶glycinate aluminum∶glycerin∶tartaric acid∶concentration of drug∶volume of drug=1.1∶0.08∶7∶0.04∶4∶5. Conclusion Uniform design combined with response surface method can be used for the optimization of the matrix formulation of cataplasm. The optimal matrix prescription has higher drug-loading, with good spreadability, moisture-retention capability and adhesive force.

Objective To establish a high purity primary culture methods of human nasal epithelial cells (HNEC) in vitro and to provide a successful primary culture model for evaluation experiments of the nasal preparation .Methods Primary culture of human nasal epithelial cells were performed with enzymatic dissociation of isolated tissue and cultured in serum-free medium .HNEC were separated through magnetic field by immunomagnetic beads .We determined the purity of the separated cells by light microscopy and flow cytometry .The morphology of HNEC was observed with a scanning electron microscope .Results Under an inverted phase microscope ,the cells morphology was paving stone shaped .Under the scanning electron microscopy ,abundant microvilli and cilia differentiation were observed .Flow cytometry showed the epithelial cells accounted for 99% .Conclusion The highly purified HNEC can be directly isolated by the magnetic cell sorting system .The cell model can be used for the basic research of nasal cavity preparation .

OBJECTIVETo study the factors that affect mucosal absorption of gardenia extract.

METHODTake vitro frog skin as a model to study the vitro mucosal permeation. The impacts of the osmotic pressure and the pH value of permeation medium on the Papp of the Jasminoidin were studied, and the effect of frog skin on the stability of Jasminoidin was investigated also.

RESULTThe Papp of Jasminoidin were (0.53 +/- 0.01), (0.21 +/- 0.05), (0.44 +/- 0.12), (0.42 +/- 0.13), (0.26 +/- 0.03) cm x min(-1) by using the normal saline (pH 6.88), pure water, 1.8 % NaCl solution, normal saline (pH 4.05) and normal saline (pH 10.05) as permeation medium for each. The accumulated permeation rate was (55.69 +/- 9.81)% by 12 h, using normal saline as permeation medium respectively, and there was no obvious time lag. Jasminoidin began to degrade around 8 h by affectedof frog skin, the constant of degradation rate (K) was 1.999, and the t1/2 was 0.347 h.

CONCLUSIONThe mucosal permeability of gardenia extract by using the vitro model of frog skin is good, and consistent with zero level absorption process. The osmotic pressure and pH value significantly affected the permeation and the isotonic and partial neutral permeation medium are more conducive to the permeation and absorption of Jasminoidin. The degradation effect of frog skin to the Jasminoidin will not affect mucosal permeation research. In vitro model of frog skin is a suitable way to simulate mucosal permeation process of the gardenia extract.

Gardenia ; chemistry ; Hydrogen-Ion Concentration ; Mucous Membrane ; drug effects ; physiology ; Permeability ; drug effects ; Plant Extracts ; chemistry ; pharmacology ; Skin ; drug effects ; Skin Absorption ; drug effects ; physiology ; Solubility

OBJECTIVETo determine the O/W partition coefficient of geniposide in fructus gardeniae extract and investigate the absortion kinetics of geniposide in whole small intestine and different intestinal segments of rats.

METHODThe shake-flask method was employed to determine the O/W partition coefficient of geniposide; an in situ intestinal perfusion model was employed to investigate the absorptive kinetics of geniposide.

RESULTThe partition coefficient (P) of geniposide was 0.1077, logP was -0.9678; the absorptive rate constants (K) of geniposide at the concentration of 0.078, 0.311, 0.780 g x L(-1) were (0.130 +/- 0.007), (0.056 +/- 0.003), (0.031 +/- 0.006) h, respectively. The K of geniposide were (0.019 +/- 0.003), (0.015 +/- 0.002), (0.012 +/- 0.002) h at duodenum, jejunum, ileum, respectively.

CONCLUSIONAccording to the P and the logP, it could be indicated that the absorption of geniposide at small intestine was poor absorption; The absorption rate was increased with the decrease of the extract concentration; Their absorption was first-order process besides the passive diffusion mechanism, and facilitated diffusion and active transport may also take part in the transport process. Geniposide was absorbed at all smallintestinal segments of rats, but the duodenal absorption ratewas higher more than other section.

Animals ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; Gardenia ; chemistry ; Intestinal Absorption ; drug effects ; Intestines ; drug effects ; physiology ; Iridoids ; chemistry ; pharmacokinetics ; Kinetics ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo optimize the extraction technology for Psoralea corylifolia and Salvia miltiorrhiza.

METHODAn orthogonal test was adopted in this study. The contents of Tanshinone IIA, Salvianolic acid B, Psoralen and Isopsoralen were used as indices of appraisal. Data processing was carried out with the multiple guidelines grading method for optimizing the extraction condition.

RESULTThe best extraction technology was to extract for 2 times with 8 fold ethanol solution (70%) and 1.5 h each time.

CONCLUSIONThe optimized extraction technology was rational and the extraction rate of the active principles is high.

Chemical Fractionation ; methods ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Furocoumarins ; chemistry ; Organic Chemicals ; chemistry ; Salvia miltiorrhiza ; chemistry

OBJECTIVETo study the in vitro mucosal permeation properties of paeonol and the factors that affect such permeability.

METHODBullfrog skin was selected as the permeation model, and the modified Franz diffusion cell was adopted to investigate the percutaneous adsorption in vitro. Content of paeonol was quantified by HPLC. Kinds of receiving solution, parts of bullfrog skin and impacts of drug concentration on percutaneous adsorption in vitro were systematically studied.

RESULTPercutaneous permeation of paeonol was to some extent affected by osmotic pressure and pH value of the receiving solution. Abdominal skin, lateral abdominal skin and dorsal skin, with the permeability coefficient form high to low, had great influence on the permeation of paeonol. There existed a good percutaneous permeation of paeonol. And the relationship between the cumulative permeability rate and time was coincided with the first order kenetical process.

CONCLUSIONTake the in vitro abdominal skin of bullfrog as the permeation model, some similarities are revealed between in vitro percutaneous permeation of paeonol and mucosal adsorption.

Acetophenones ; metabolism ; Animals ; Chromatography, High Pressure Liquid ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Mucous Membrane ; metabolism ; Osmotic Pressure ; Permeability ; Rana catesbeiana ; metabolism ; Skin ; metabolism

OBJECTIVETo study the variation in plasma concentration after oral administration of Danshen multi-component osmotic pump tablets in Beagle dogs with conventional Danshen tablets as the control preparation, in order to assess the sustained release of Danshen multi-component osmotic pump tablets.

METHODHPLC was adopted for determination, with Shimadzu's ODS-SP column (4.6 mm x 150 mm, 5 microm), flow rate of 1 mL x min(-1), and column temperature of 30 degrees C. Protein in plasma samples of tanshinone II(A) and salvianolic acid B was removed by ethyl acetate extract and acetone precipitation method respectively. Their pharmacokinetic parameters were calculated based on determination results.

RESULTThe methodology study on the two constituents with different polarity showed conformity to the requirements. Compared with conventional Danshen tablets, Danshen multi-component osmotic pump tablets showed decrease in Cmax and extension in Tmax after oral administration in Beagle dogs.

CONCLUSIONDanshen multi-component osmotic pump tablet has a good sustained-release effect compared with conventional Danshen tablets.

Animals ; Dogs ; Drugs, Chinese Herbal ; pharmacokinetics ; Male ; Osmosis ; Salvia miltiorrhiza ; chemistry ; Tablets ; Time Factors

OBJECTIVETo develop a sensitive and specific LC-MS/MS method for determination of Yizhi osmotic pump tablets active ingredient in Beagle dog plasma.

METHODBeagle dog plasma pre-treatment methods were established. Geniposide, notoginsenoside R1, ginsenoside Rg1 and Rb1 notoginsenoside molecular ions and fragment ions peaks were separated well and detected synchronously by LC-MS/MS with digoxin as internal standard.

RESULTUnder the selected LC-MS/MS conditions, the characteristic fragment ions of the four components could be well separated and quantified, and the calibration curves showed good linearity within a certain concentration range of each component; extraction recoveries of those four compounds in plasma were higher than 75%, method recoveries were higher than 90%; day precision (RSD <10%) and inter-day precision (RSD <15%) were generally fine; freeze-thaw and room temperature experiments showed good stability (RSD <15%).

CONCLUSIONThe method is proved to be suitable for pharmacokinetic studies of Yizhi active ingredients in Beagle dog plasma.

Animals ; Blood Chemical Analysis ; methods ; Calibration ; Chromatography, Liquid ; methods ; Dogs ; Drug Stability ; Drugs, Chinese Herbal ; analysis ; pharmacokinetics ; Male ; Osmosis ; Tablets ; Tandem Mass Spectrometry ; methods ; Temperature ; Time Factors