The difference between three representative components of total salvianolic acids in pharmacodynamic activity were compared by three different pharmacological experiments: HUVECs oxidative damage experiment, 4 items of blood coagulation in vitro experiment in rabbits and experimental myocardial ischemia in rats. And the effects of contribution rate of each component were calculated by multi index comprehensive evaluation method based on CRITIC weights. The contribution rates of salvianolic acid B, rosmarinic acid and Danshensu were 28.85%, 30.11%, 41.04%. Apparent oil/water partition coefficient of each representative components of total salvianolic acids in n-octyl alcohol-buffer was tested and the total salvianolic acid components were characterized based on a combination of the approach of self-defined weighting coefficient with effects of contribution rate. Apparent oil/water partition coefficient of total salvianolic acids was 0.32, 1.06, 0.89, 0.98, 0.90, 0.13, 0.02, 0.20, 0.56 when in octanol-water/pH 1.2 dilute hydrochloric acid solution/ pH 2.0, 2.5, 5.0, 5.8, 6.8, 7.4, 7.8 phosphate buffer solution. It provides a certain reference for the characterization of components.
Animals ; Benzofurans ; chemistry ; pharmacology ; Cinnamates ; chemistry ; pharmacology ; Depsides ; chemistry ; pharmacology ; Lactates ; chemistry ; pharmacology ; Male ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Solubility

Adolescent ; Adult ; Aged ; Endoscopy ; Female ; Humans ; Middle Aged ; Otorhinolaryngologic Surgical Procedures ; methods ; Paranasal Sinuses ; surgery ; Turbinates ; surgery ; Young Adult

To prepare salvianolic acid phospholipid compound. With the compound of salvianolic acids and soybean phospholipid as the index, mono-factor experiment and orthogonal design experiment were conducted to screen its technical parameters. According to the results, the optimal preparation conditions of salvianolic acid phospholipid compound were that THF were taken as the reaction solvent, the concentration time was 3 h, the reactant concentration was 5 g x L(-1), the mass ratio of salvianolic acids and phospholipid was 1: 1.5, and the reaction temperature was 40 degrees C. The oil/water partition coefficient of the prepared salvianolic acid phospholipid compound significant increased in water and buffers with different pH values. The results of phase analysis such as DSC, XRD and FTIR indicated that salvianolic acids existed in phospholipid in an amorphous state.
Alkenes ; chemistry ; metabolism ; Chemical Phenomena ; Chemistry, Pharmaceutical ; methods ; Intestinal Absorption ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; metabolism ; Soybeans ; chemistry ; Temperature

Traditional Chinese medicine (TCM) composition is a multi-component multiple drug release system and more components preparation system. How to evaluate the drug release behavior of diversification has been a block for the modernization of TCM. This article through to study of more representative components of ginkgolides drug release and similarity analysis of more representative components of ginkgolides drug release behavior and use Weight coefficient method to integrate the multicomponent drug release curve. So it can provide the idea and method for drug evaluation of TCM component preparation.
Drugs, Chinese Herbal ; chemistry ; Ginkgolides ; chemistry ; Kinetics ; Solubility

Astragalus polysaccharides was lounded to 4-(2-aminoethylphenol), followed by labeling the APS-Tyr with fluorescein-5-isothiocyanate (FITC) at the secondary amino group. The absorption enhancement effects of low molecular weight chitosan and protamine on astragalus polysaccharides were evaluated via Caco-2 cell culture model. The results show that the fluorecent labeling compound has good stability and high sensitivity. On the other hand low molecular weight chitosan and protamine also can promoted absorption of the astragalus polysaccharides without any cytotoxity, and the absorption increase was more significant with increasing the amount of low molecular weight chitosan and protamine. At the same time, the low molecular weight chitosan has slightly better effect. The transepithelial electric resistance (TEER) of Caco-2 cells show that absorption enhancers could improve its membrane transport permeability by opening tight junctions between cells and increasing the cell membrane fluidity.
Absorption ; Astragalus Plant ; chemistry ; Biological Transport ; Caco-2 Cells ; Fluorescein-5-isothiocyanate ; chemistry ; Fluorescent Dyes ; chemistry ; Humans ; Plant Extracts ; chemistry ; pharmacokinetics ; Polysaccharides ; chemistry ; pharmacokinetics

Microcrystalline cellulose and chitosan were applied to prepare ginkgolides component solid dispersions micro pill drug release unit and study the dissolution of GKS. Microcrystalline cellulose, chitosan as composite carrier, solvent method was used to prepare ginkgolides component solid dispersions. Differential scanning calorimetry was used to Characterization of ginkgolides component solid dispersions. Ginkgolides component solid dispersions as principle agent were prepared for micro-pellet. Comparison of different types, different doses of the adhesive, drug-polymer interactions, and disintegrating agent for the preparation of ginkgolides components of micro-pellet drug release unit, the optimum preparation ginkgolides components of micro-pellet drug release unit was screened by orthogonal design experiment. Preparation of ginkgolides components solid dispersions with microcrystalline cellulose and chitosan at ratio 1: 3. Drug cumulative dissolution was more than 80% in 60 min. Solid dispersion-micro-pellet drug release unit can significantly improve the dissolution of ginkgolides components, it has practical application value.
Cellulose ; chemistry ; Chitosan ; chemistry ; Drug Compounding ; methods ; Ginkgolides ; chemistry

The purpose of this research was to prepare total salvianolic acids-phytosome-HA coprecipitate to improve drug dissolution and its micromeritic properties. Firstly, the coprecipitate was prepared by solvent method and in vitro dissolution of tripterine was performed with the salvianolic acid B and danshensu as criteria. At the same time, the micromeritic properties was characterizated, the structure of samples was characterized by TEM, DSC, XRD and FTIR. Results showed that when the ratio of drug to HA was 1:2, it had a better dissolution, the accumulative drug-release percent in vitro at 60 min was over 90%. At the same time, it has good liquidity and low moisture absorption. Its micromeritic properties have improved. It is proved that the drug still existed amorphously by microstructure analysis. The preparation process is simple and feasible, it has practical value.
Alkenes ; chemistry ; Chemical Precipitation ; Chemistry, Pharmaceutical ; methods ; Durapatite ; chemistry ; Phospholipids ; chemistry ; Polyphenols ; chemistry ; Time Factors

OBJECTIVETo explore the relationship of plasma endotoxin level with TCM deficiency/excess Syndrome and the grading/staging of pathologic change of liver in patients with chronic hepatitis B (CHB).

METHODSPlasma level of endotoxin (ET) was determined using chromogenic limulus amebocyte lysate (LAL) assay in 75 patients with chronic hepatitis B (30 of excess dominance, 45 of deficiency dominance) and also in 15 healthy subjects for control. Moreover, pathological examination on liver biopsy of 20 patients was conducted.

RESULTS(1) ET level increased in all CHB patients, and the increment was higher in patients of excess dominance than that in patients of deficiency dominance, showing significant difference (P < 0.01). (2) Correlation between ET level and liver pathological grading/staging was shown in CHB patients.

CONCLUSIONPlasma level of ET could be taken as one of the criteria of TCM microcosmic diagnosis in differentiating deficiency/excess syndrome. (2) Endotoxemia plays an important role in pathologic process of liver injury.

Adolescent ; Adult ; Aged ; Diagnosis, Differential ; Endotoxins ; blood ; Female ; Hepatitis B, Chronic ; blood ; etiology ; pathology ; Humans ; Liver ; pathology ; Male ; Medicine, Chinese Traditional ; Middle Aged ; Yang Deficiency ; blood ; pathology ; Yin Deficiency ; blood ; pathology

Objective To examine mycological profile of eryptococcal meningitis in patients with non-acquired immune deficiency syndrome (AIDS) during treatment and follow-up so that to support clinical therapy. Methods Data of 28 cuhure-confirmed cryptoeoccal meningitis patients with non-AIDS were retrospectively analyzed. Fungat smear, count, culture and latex agglutination test of cerebrospinal fluid (CSF) were done during treatment and follow-up. Initial treatment included intravenous amphotericin B plus oral flucytosine or f;uconazole for at least 6 weeks, and consolidation treatment included oral fluconazole and (or) itraeonazole for at least 2 months. All 28 patients were cured. The data were analyzed by rank-sum test. Results The positive rate of CSF fungal smear was 92.9% before treatment and gradually decreased, and the fungal count was significantly reduced over time after treatment. While fungal smears of some patients were still positive after initial treatment. Fungal growth time in culture was gradually extended, and fungal culture turned to be negative in all patients after 2 weeks of treatment. The positive rate of latex agglutination test of CSF was 100%. Cryptococcal antigen titer decreased steadily after treatment, which was not correlated with the decrease of fungal count. Conclusion Mycological tests of patients with eryptococcal meningitis should be interpreted comprehensively during treatment, and result of each test should be specifically analyzed.

Objective To investigate the effect of intra-articular carboxymethylated ehitosan(CM- CTS)injection on inducible nitric oxide synthase(iNOS)expression in cartilage at the early stage of os- teoarthfitis(OA).Methods Thirty-two white rabbits were underwent unilateral anterior cruciate ligament transection(ACLT)and were randomly divided into 4 groups 5 weeks after transection.Rabbits of group A re- ceived 0.3 ml of 2% high molecular weight CMCTS(H-CMCTS)once every two weeks.Rabbits in group B were treated using 2% low molecular weight(L-CMCTS)CMCTS at:the same intervals.Group C rabbits were injected intra-articularly with 0.3 ml of 1% sodium hyaluronate(Na-HA)once a week.Animals of group D were not injected.At sacrifice,11 weeks following surgery,the expression of iNOS in cartilages was analyzed by immunohistochemistry and reverse transcription-polymerase chain reaction(RT-PCR)methods.Results Both immunohistochemistry and RT-PCR showed that the level of iNOS expression of cartilage in CMCTS in- jection groups was lower than that in Na-HA injection group and the untreated group.There was no significant difference in iNOS expression between the two different molecular weight CMCTS injection groups. No signifi- cant difference of iNOS expression in cartilage was found between Na-HA injection group and the untreated group.Conclusion CMCTS suppresses iNOS expression in cartilage during the early stage of OA.Na-HA treatment has no effect on iNOS expression in cartilage.