ABSTRACT
For the effects of multi-component environment on the solubility and permeability of single components,and the problems of biopharmaceutical attribute classification of single components in the compound prescriptions environment,baicalein was used as the research object in this study to investigate the biopharmaceutic attributes of single-component and their traditional Chinese medicine( TCM) biopharmaceutic attributes in the multi-component environment of Gegen Qilian Decoction. Shaking flask method,intrinsic dissolution rate test and HPLC were used to determine solubility of baicalein. Markers specified by FDA were utilized as permeable boundary reference materials to verify the applicability of the single-pass intestinal perfusion method( SPIP),and the quantitative research on the permeability of baicalein was also conducted. It is concluded that baicalein could be categorized as BCS-â ¡ drug based on its low solubility and high intestinal permeability values,and it may be categorized into CMMBCS-I in the multi-component environment of Gegen Qilian Decoction due to its poor solubility but enhanced solubility and permeability in compound environment. This study could provide verification ideas for clinical determination of the best human oral dose of baicalein,and provide the data basis for the study of biopharmaceutics classification system of Chinese materia medica( CMMBCS).
Subject(s)
Biopharmaceutics/classification , Drugs, Chinese Herbal/chemistry , Flavanones/chemistry , Materia Medica/classification , Humans , Intestinal Absorption , Permeability , SolubilityABSTRACT
The evaluation of permeability in biopharmaceutics classification system of Chinese materia medica (CMMBCS) requires multicomponent as a whole in order to conduct research, even in the study of a specific component, should also be put in the multicomponent environment. Based on this principle, the high content components in Gegen Qinlian decoction were used as multicomponent environmental impact factors in the experiment, and the relevant parameters of intestinal permeability about puerarin were measured with using in situ single-pass intestinal perfusion model, to investigate and evaluate the intestinal permeability of puerarin with other high content components. The experimental results showed that different proportions of baicalin, glycyrrhizic acid and berberine had certain influence on intestinal permeability of puerarin, and glycyrrhizic acid could significantly inhibit the intestinal absorption of puerarin, moreover, high concentration of berberine could promote the absorption of puerarin. The research results indicated that the important research ideas of permeability evaluation in biopharmaceutics classification system of Chinese materia medica with fully considering the effects of other ingredients in multicomponent environment.
Subject(s)
Drugs, Chinese Herbal/pharmacokinetics , Intestinal Mucosa/metabolism , Isoflavones/pharmacokinetics , Materia Medica/pharmacokinetics , Animals , Berberine/pharmacokinetics , Biopharmaceutics , Chromatography, High Pressure Liquid , Flavonoids/pharmacokinetics , Glycyrrhizic Acid/pharmacokinetics , Intestines/chemistry , Kinetics , Male , Permeability , Rats , Rats, WistarABSTRACT
BACKGROUND: The purpose of the present study was to develop intranasal delivery systems of the homeopathic anti-asthmatic remedy Blatta orientalis mother tincture (Q) using thermoreversible polymer Pluronic F127 (PF127) and mucoadhesive polymer Carbopol 934P (C934P). METHODS: Formulations were modulated so as to have a gelation temperature below 34 degrees C to ensure gelation at physiological temperature after intranasal administration. Its gelation temperature, mucoadhesive strength, viscosity and gel strength were studied. B. orientalis (Q) nasal gel was tested with recurrent milk aspiration to determine whether it produces changes in eosinophilia in a murine model of asthma. RESULT: The gelation temperatures of the formulations and mucoadhesive strength, determined using sheep nasal mucosal membrane, increased by the addition of increasing concentrations of Carbopol. The results of milk aspiration induced eosinophilia, B. orientalis (Q) nasal gel significantly (P < 0.001), decreased eosinophil cell count as compared with toxicant by using in absolute eosinophilia count method. Finally, histopathological examination did not detect any damage during in vivo studies. CONCLUSION: The PF127 gel formulation of B. orientalis (Q) with in situ gelling and mucoadhesive properties with increased permeation rate is promising for prolonging nasal residence time and thereby nasal absorption.
Subject(s)
Cockroaches/chemistry , Excipients/chemistry , Pulmonary Eosinophilia/drug therapy , Respiratory Aspiration/complications , Acrylates/chemistry , Adhesiveness , Administration, Intranasal , Animals , Asthma/drug therapy , Asthma/physiopathology , Disease Models, Animal , Drug Delivery Systems , Female , Gels , Guinea Pigs , Homeopathy , Male , Mice , Milk , Nasal Mucosa/metabolism , Permeability , Poloxamer/chemistry , Pulmonary Eosinophilia/etiology , Rats , Rats, Wistar , Sheep , Temperature , ViscosityABSTRACT
OBJECTIVES: The primary biomolecular target of a homeopathic potency is unknown. If it is a plasma membrane protein such as water-channel protein, the drug would alter water permeation in cells. Therefore, the objective is to see if potentized homeopathic drugs like Mercuric chloride 30c and Nux vomica 30c could alter permeation of water through the erythrocytes of a fresh water fish under acute ethanol intoxication. LOCATION: The work was carried out in the Zoology Laboratory of Visva Bharati University, Santiniketan, West Bengal, India. SUBJECT: Live freshwater catfish. DESIGN: Erythrocytes collected from fish with and without ethanol intoxication were incubated in distilled water at 30 degrees C for 30 minutes with Ethanol 30c (control), Merc cor 30c (test 1), and Nux vomica 30c (test 2). Merc cor 30c and Nux vom 30c were prepared by successive dilution of the respective mother tinctures with 90% ethanol (1:100) followed by sonication at 20 kHz for 30 seconds in 30 steps. Ethanol 30c was prepared in the same way from 90% ethanol diluted with 90% ethanol. In another experiment, fish were pretreated with Ethanol 30c and Nux vom 30c followed by ethanol injection at 2 g/kg of body weight. Then their erythrocytes were tested in vitro with the same potencies. After centrifugation of blood samples, fluid part was removed, erythrocyte pellets dried in a BioChemical Oxygen Demand (BOD; Atlas Surgical, New Delhi, India) incubator at 90 degrees C for 12 hours and intracellular water content measured. RESULTS: Red blood cells (RBCs) from ethanol-injected fish permeated more water than those from normal fish. Water permeation was enhanced with Merc cor 30c and Nux vom 30c. RBCs from fish pretreated with Nux vom 30c imbibed more water in in vitro treatments than those from fish pretreated with Ethanol 30c. CONCLUSION: Because water channel proteins or aquaporins are mainly responsible for water transport through the plasma membrane of RBCs, it is thought that potentized drugs interact with these proteins, thereby facilitating water influx in the cells.