ABSTRACT
The research on biopharmaceutics classification system of Chinese materia medica( CMMBCS) should be finally implemented to the holistic research level of traditional Chinese medicine compounds,while the overall biopharmaceutical properties of traditional Chinese medicine compounds are not only the sum of solubility and permeability of each component. In this study,Gegen Qinlian Tablets was used as the research object,and the contents of 12 representative components,i.e. puerarin,daidzin,baicalin,daidzein,wogonoside,baicalein,wogonin,glycyrrhizic acid,coptisine hydrochloride,epiberberine,berberine hydrochloride and palmatine hydrochloride,were simultaneously determined by HPLC to obtain the mass weight of each component. The in vitro lipopolysaccharide( LPS)-induced RAW264. 7 cells inflammation model was established to investigate the anti-inflammatory effects of 12 representative components and obtain the efficacy weight of each component. In order to obtain the number of doses and effective permeability coefficient which can represent the overall biopharmaceutical properties of Gegen Qinlian Tablets,mass weight was combined with efficacy weight to integrate the solubility and permeability data of each component determined by typical shake flask method and in situ single pass intestinal perfusion model respectively. The results indicated that Gegen Qinlian Tablets should be categorized â £ drug of the CMMBCS with low solubility and low permeability.
Subject(s)
Anti-Inflammatory Agents/pharmacology , Biopharmaceutics/classification , Drugs, Chinese Herbal/classification , Materia Medica/classification , Drugs, Chinese Herbal/pharmacology , TabletsABSTRACT
To illustrate the intrinsic dissolution rate(IDR) involved in biopharmaceutics classification system of Chinese materia medica(CMMBCS), investigate the effect of artificial multicomponent environment on IDR of berberine, by using a non-disintegrating disk, and summarize related rules by using the obtained data. Progressive levels design was used to investigate the effects of single component environment (puerarin, baicalin, and glycyrrhizic acid); double-component environment(puerarin+baicalin, puerarin+ glycyrrhizic acid, baicalin+glycyrrhizic acid); and triple-component environment(puerarin+baicalin+glycyrrhizic acid) on IDR of berberine, laying a foundation for further researches on the absorption mechanism of multiple components.
Subject(s)
Berberine/chemistry , Drugs, Chinese Herbal/chemistry , Materia Medica , Biopharmaceutics , SolubilityABSTRACT
One of the advantages of biopharmaceutics classification system of Chinese materia medica (CMMBCS) is expanding the classification research level from single ingredient to multi-components of Chinese herb, and from multi-components research to holistic research of the Chinese materia medica. In present paper, the alkaloids of extract of huanglian were chosen as the main research object to explore their change rules in solubility and intestinal permeability of single-component and multi-components, and to determine the biopharmaceutical classification of extract of Huanglian from holistic level. The typical shake-flask method and HPLC were used to detect the solubility of single ingredient of alkaloids from extract of huanglian. The quantitative research of alkaloids in intestinal absorption was measured in single-pass intestinal perfusion experiment while permeability coefficient of extract of huanglian was calculated by self-defined weight coefficient method.
Subject(s)
Drugs, Chinese Herbal/chemistry , Materia Medica/classification , Plant Extracts/chemistry , Animals , Biopharmaceutics , Drugs, Chinese Herbal/classification , Intestinal Absorption , Plant Extracts/classificationABSTRACT
Silicosis is an occupational pulmonary fibrosis caused by inhalation of silica (SiO2) and there are no ideal drugs to treat this disease. Earthworm extract (EE), a natural nutrient, has been reported to have anti-inflammatory, antioxidant, and anti-apoptosis effects. The purpose of the current study was to test the protective effects of EE against SiO2-induced pulmonary fibrosis and to explore the underlying mechanisms using both in vivo and in vitro models. We found that treatment with EE significantly reduced lung inflammation and fibrosis and improved lung structure and function in SiO2-instilled mice. Further mechanistic investigations revealed that EE administration markedly inhibited SiO2-induced oxidative stress, mitochondrial apoptotic pathway, and epithelial-mesenchymal transition in HBE and A549 cells. Furthermore, we demonstrate that Nrf2 activation partly mediates the interventional effects of EE against SiO2-induced pulmonary fibrosis. Our study has identified EE to be a potential anti-oxidative, anti-inflammatory, and anti-fibrotic drug for silicosis.
Subject(s)
Antioxidants/therapeutic use , Disease Models, Animal , Lung/drug effects , Materia Medica/therapeutic use , Oligochaeta/chemistry , Pulmonary Fibrosis/prevention & control , Silicosis/drug therapy , Tissue Extracts/therapeutic use , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Antioxidants/administration & dosage , Antioxidants/pharmacology , Apoptosis/drug effects , Cell Line , Cells, Cultured , Epithelial-Mesenchymal Transition/drug effects , Injections, Intraperitoneal , Lung/metabolism , Lung/pathology , Lung/physiopathology , Male , Materia Medica/administration & dosage , Materia Medica/pharmacology , Mice, Inbred C57BL , NF-E2-Related Factor 2/agonists , NF-E2-Related Factor 2/antagonists & inhibitors , NF-E2-Related Factor 2/genetics , NF-E2-Related Factor 2/metabolism , Oxidative Stress/drug effects , Pulmonary Fibrosis/etiology , Pulmonary Fibrosis/immunology , RNA Interference , Random Allocation , Respiratory Mucosa/cytology , Respiratory Mucosa/drug effects , Respiratory Mucosa/metabolism , Respiratory Mucosa/pathology , Silicosis/metabolism , Silicosis/pathology , Silicosis/physiopathology , Specific Pathogen-Free Organisms , Tissue Extracts/administration & dosage , Tissue Extracts/pharmacologyABSTRACT
To explore one-step method for the preparation of Ganoderma lucidum multicomponent microemulsion, according to the dissolution characteristics of triterpenes and polysaccharides in Ganoderma lucidum, formulation of the microemulsion was optimized. The optimal blank microemulsion was used as a solvent to sonicate the Ganoderma lucidum powder to prepare the multicomponent microemulsion, besides, its physicochemical properties were compared with the microemulsion made by conventional method. The results showed that the multicomponent microemulsion was characterized as (43.32 +/- 6.82) nm in size, 0.173 +/- 0.025 in polydispersity index (PDI) and -(3.98 +/- 0.82) mV in zeta potential. The contents of Ganoderma lucidum triterpenes and polysaccharides were (5.95 +/- 0.32) and (7.58 +/- 0.44) mg x mL(-1), respectively. Sonicating Ganoderma lucidum powder by blank microemulsion could prepare the multicomponent microemulsion. Compared with the conventional method, this method is simple and low cost, which is suitable for industrial production.
Subject(s)
Fungal Polysaccharides/analysis , Materia Medica/chemistry , Reishi/chemistry , Technology, Pharmaceutical/methods , Triterpenes/analysis , Emulsions , Medicine, Chinese Traditional , Particle Size , Powders , SolubilityABSTRACT
OBJECTIVE: To study the effect of Xianlong granules (XLG) on immunological function in the rat of adjuvant arthritis (AA). METHOD: Rats were randomly divided into normal group, AA model group, prednisone group and low, middle and high dose XLG groups, 10 rats in each group. All rats were treated by intragastric administration from the 18 days after arthritis was induced by the complete Freud's adjuvant and the effect of XLG on toes swelling was observed. On the 30th days after modeling, proliferation of the splenic and thymic lymphocytes, and IgG secreted by splenocytes were detected respectively by MTT assay and ELISA. RESULT: Compared with the model group, both the high and middle dose XLG groups had significant therapeutic effects on toes dwelling in the rat of AA (P < 0.05 or P < 0.01); The low, middle and high dose XLG groups strengthened the PHAM-inhibited proliferation of splenic lymphocytes (P < 0.05), and inhibited the PHAM-augmented proliferation of thymic lymphocytes (P < 0.05); XLG did not significantly effect on IgG level secreted by splenocytes in rats of AA. CONCLUSION: XLG can cure toes swelling in rats of AA, which is related with regulation of the abnormal immunlological function.
Subject(s)
Arthritis, Experimental/prevention & control , Drugs, Chinese Herbal/pharmacology , Materia Medica/pharmacology , Medicine, Chinese Traditional , Animals , Arthritis, Experimental/immunology , Arthritis, Experimental/pathology , Cell Proliferation/drug effects , Colubridae , Drug Combinations , Drugs, Chinese Herbal/isolation & purification , Edema/immunology , Edema/pathology , Edema/prevention & control , Female , Immunoglobulin G/metabolism , Lymphocytes/drug effects , Lymphocytes/metabolism , Lymphocytes/pathology , Male , Materia Medica/isolation & purification , Plants, Medicinal/chemistry , Random Allocation , Rats , Rats, Wistar , Spleen/metabolism , Spleen/pathology , Thymus Gland/pathology , Toes/pathologyABSTRACT
OBJECTIVE: To evaluate the clinical efficacy and security of super crush-run tong xinluo capsule (SCTXLC) for apoplexy due to energy-deficiency and blood-stasis. METHOD: The randomised controlled double blind non-inferiority trial versus paroxetine, parallel contrast, different Kinds of Techniques and dosage, the clinical trial design was adopted, 144 patients with stroke of convalescent stage were selected by 2 group, which course of diseases was in 2 weekens to 3 months, neurological deficit scores was 8 to 30, grade of acaties of daily living scores was 2 to 5. the treatment group (n = 72) received SCTXLC 0.26 g (a capsule), 4 capsules at a time, three times a day, while that of the control group (n = 72) received common crush-run tong xinluo capsule (CCTXLC) 0.38 g (a capsule), 4 capsules at a time, three times a day, the therapeutic course for both groups was 28 d. RESULT: The synthesis total effective rates of the stroke in treatment group and control group were 91.3% and 87.3% respectively, showing no significant difference. The Lower Bound Upper Bound of Asymptotic 95% Confidence Interval of the total effective rates difference is -4.57%, over the beforehand Lower Bound of 15%, non-inferiority trial versus paroxetine was eligible. The adverse reactions occurred was 1 patient in the treatment group and 2 patients in control group in clinical trial. CONCLUSION: SCTXLC has definite effect for apoplexy due to energy-deficiency and blood-stasis, the efficacy in the treated group was equal to that in the control group, and favourable satety for usage.
Subject(s)
Drugs, Chinese Herbal/therapeutic use , Materia Medica/chemistry , Plants, Medicinal/chemistry , Stroke/drug therapy , Activities of Daily Living , Adult , Aged , Animals , Capsules , Double-Blind Method , Drug Administration Schedule , Drug Combinations , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/isolation & purification , Female , Humans , Male , Middle Aged , Powders , Stroke/physiopathology , Treatment OutcomeABSTRACT
With the fast development of medicinal animals as new drugs, research on Periplaneta americana become hot recently. Several drugs which mainly consisted of P. americana were approved for clinical applications. The chemical constituents and pharmacological bioactivities of this insect were summarized herein, which provides informativon for further researches on this medicinal animal.