The Effect of Wellsolve, a Novel Solubilizing Agent, on the Intestinal Barrier Function and Intestinal Absorption of Griseofulvin in Rats
スポンサーリンク
概要
- 論文の詳細を見る
The effect of Wellsolve, a new solubilizing agent, on the function of intestinal membrane barrier and transporters including P-glycoprotein (P-gp) and peptide transporter (PEPT1) was examined by an in vitro diffusion chamber and an in situ closed loop method. The model drugs used in this study were 5(6)-carboxyfluorescein (CF), rhodamine123 (a P-glycoprotein substrate), cephalexin (a typical substrate for PEPT1) and griseofulvin (a BCS Class II drug). Intestinal absorption of CF was not affected by the addition of 1—10% (v/v) Wellsolve, while 20% (v/v) Wellsolve significantly enhanced its intestinal absorption by the in situ absorption study. Therefore, this finding suggested that high concentration of Wellsolve might alter the intestinal barrier function. The mucosal to serosal (absorptive) and serosal to mucosal (secretory) transport of rhodamine123 was significantly inhibited in the presence of 5.0—20% (v/v) of Wellsolve, suggesting that Wellsolve might not affect the function of P-gp in the intestine. The intestinal transport of cephalexin was not affected in the presence of Wellsolve, suggesting that this solubilizing agent might not change the function of PEPT1 in the intestine. In the toxicity studies, we found that 1—10% (v/v) Wellsolve did not change the release of lactate hydrogenase (LDH) and protein from the intestinal membranes. Furthermore, intestinal absorption of griseofulvin in the presence of 10% (v/v) Wellsolve significantly increased as compared with the control. In summary, Wellsolve at lower concentrations might be a potent and safe solubilizing agent for improving the solubility and absorption of poorly water-soluble drugs including griseofulvin.
- 公益社団法人 日本薬学会の論文
著者
-
YAMAMOTO Akira
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
LIN Yulian
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
KATSUMI Hidemasa
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
Gao Yang
Department Of Environmental Science And Engineering Tsinghua University
-
Hamid Khuriah
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
Sakane Toshiyasu
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
Katsumi Hidemasa
Department Of Biopharmaceutics Kyoto Pharmaceutical University
-
Yamamoto Akira
Department Of Anatomy School Of Medicine University Of Tokushuma
-
Yamamoto Akira
Department Of Anatomy School Of Medicine University Of Tokushima
-
Gao Yang
Department of Biopharmaceutics, Kyoto Pharmaceutical University
関連論文
- Vaccine Efficacy of Fusogenic Liposomes Containing Tumor Cell-Lysate against Murine B16BL6 Melanoma(Pharmacology)
- 1,3-ジオキソラン環を有する新規なベタイン型界面活性剤〔英文〕
- Computed tomography-guided re-radiofrequency ablation for unresectable lung tumor with local progression previously treated with the same procedure
- Fluorine-18-fluorodeoxyglucose positron emission tomography for assessment of patients with unresectable recurrent or metastatic lung cancers after CT-guided radiofrequency ablation : Preliminary results
- Three-Year Follow-up Results of Angiographic Intervention Trial Using an HMG-CoA Reductase Inhibitor to Evaluate Retardation of Obstructive Multiple Atheroma (ATHEROMA) Study
- IS094 TFPI Competes With LPL on Endothelium : A Possible Mechanism of Low HDL.c in Atherosclerosis
- 2 Assessment of Left Ventricular Synchrony with a Novel Analysis Program (Cardio-GRAF) using ECG-gated Myocardial SPECT(Comprehensive Treatment Centered on Biventricular Resynchronization Therapy,Plenary Session 5 (PL5) (A),The 70th Anniversary Annual Sci
- Intradermal Concentration of Hydroquinone after Application of Hydroquinone Ointments Is Higher than Its Cytotoxic Concentration(Biopharmacy)
- Tumor Necrosis Factor α-Gene Therapy for an Established Murine Melanoma Using RGD (Arg-Gly-Asp) Fiber-mutant Adenovirus Vectors
- Effects of Labrasol and Other Pharmaceutical Excipients on the Intestinal Transport and Absorption of Rhodamine123, a P-Glycoprotein Substrate, in Rats(Biopharmacy)
- 難吸収性薬物の消化管吸収に対するNO供与体の吸収促進効果の特性 : 従来型の吸収促進剤との比較
- Evaluation of Insulin Permeability and Effects of Absorption Enhancers on Its Permeability by an in Vitro Pulmonary Epithelial System Using Xenopus Pulmonary Membrane
- New Diagnostic Procedure for Primary Aldosteronism: Adrenal Venous Sampling under Adrenocorticotropic Hormone and Angiotensin II Receptor Blocker-Application to a Case of Bilateral Multiple Adrenal Microadenomas
- Rupture of a Cervical Arteriovenous Fistula Associated with Neurofibromatosis Type 1. A Case Report
- IS200 Hypercholesterolemic Valvulopathy in FH
- LOW DENSITY LIPOPROTEIN (LDL) BINDING AFFINITY TO LDL RECEPTOR IN HYPERLIPOPROTEINEMIA
- Electrophysiological Studies on the Mechanism for Enhanced Intestinal Transport of Water-Soluble Compounds by Antibiotic Peptide Bacitracin
- The Formations of Two Formazans of Nitro Blue Tetrazolium (NBT) in the Histochemical Succinate Dehydrogenase Reaction.
- Effects of Various Storage Conditions and Alterations of Antioxidant Contents on Chromatic Aberration of Hydroquinone Ointment(Biopharmacy)
- THE INVESTIGATION OF RISK FACTORS FOR DEVELOPMENT OF CORONARY ARTERY DISEASE IN PARTIENTS WITH FAMILIAL HYPERCHOLESTEROLEMIA : Ichemic Heart Disease (III) : 46th Annual Scientific Meeting, Japanese Circulation Society
- Oligoarginine-Based Prodrugs with Self-Cleavable Spacers for Caco-2 Cell Permeation
- Effectiveness and Toxicity Screening of Various Absorption Enhancers Using Caco-2 Cell Monolayers
- PJ-705 Systolic and Diastolic Left Ventricular Wall motion Dyssynchrony Assessed by 99mTc-sestamibi-Gated-SPECT in Patient with Hypertension(Hypertension, clinical(09)(H),Poster Session(Japanese),The 72nd Annual Scientific Meeting of the Japanese Circulat
- PJ-332 Angiotensin II Receptor Blockade might Express Left Ventricular Remodeling Effects through Improving Left Ventricular Dyssynchrony in Hypertension(Hypertension, clinical(08)(H),Poster Session(Japanese),The 72nd Annual Scientific Meeting of the Japa
- PJ-318 Relationship Between Chronic Kidney Disease (CKD) and Left Ventricular Function/Dysynchrony Assessed by Tc99m-sestamibi-Gated-SPECT using a Novel Program "cardioGRAF"(Heart failure, clinical(16)(M),Poster Session(Japanese),The 72nd Annual Scientifi
- Assessment of Left Ventricular Dyssynchrony During Development of Heart Failure by a Novel Program Using ECG-Gated Myocardial Perfusion SPECT
- PE-522 The Relationship between Left Ventricular Systolic Dyssynchrony and Wall Stress in Patients with Hypertension and Preserved Ejection Fraction(Hypertension, clinical-08, The 71st Annual Scientific Meeting of the Japanese Circulation Society)
- Transdermal Delivery of Insulin Using Trypsin as a Biochemical Enhancer(Biopharmacy)
- Pharmaceutical and Clinical Assessment of Hydroquinone Ointment Prepared by Extemporaneous Nonsterile Compounding
- ANTIGEN-INDUCED DECREASE OF SALICYLIC ACID ABSORPTION FROM THE SMALL INTESTINE IN ACTIVELY IMMUNIZED RATS
- Relationship between left ventricular function and wall motion synchrony in heart failure assessed by ECG-gated myocardial perfusion SPECT
- Relationships among regional diastolic impairment, elongation of global time to peak filling rate, and global diastolic function using ECG-gated myocardial perfusion SPECT in heart failure
- Global and regional evaluation of systolic and diastolic left ventricular temporal parameters using a novel program for ECG-gated myocardial perfusion SPECT : Validation by comparison with gated equilibrium radionuclide angiography and speckle-tracking ra
- Quantification of left ventricular regional functions using ECG-gated myocardial perfusion SPECT : Validation of left ventricular systolic functions
- PE-271 The Role of Diastolic Dyssynchrony Assessed by a Novel Program "cardioGRAF" for Tc99m-sestamibi-gated-SPECT in the Development of Congestive Heart Failure(Nuclear cardiology-3 (I) PE46,Poster Session (English),The 70th Anniversary Annual Scientific
- A Novel Program "cardioGRAF" of Gated-SPECT for Regional Systolic-diastolic Assessment : The Predictors for Cardiac Events in Patients with Non-ischemic CHF(Nuclear Cardiology 12 (I), The 69th Annual Scientific Meeting of the Japanese Circulation Society)
- INTESTINAL ABSORPTION OF HAPTENS IN RATS IMMUNIZED WITH PROTEIN-HAPTEN CONJUGATE : COMPARISON OF SULFANILIC ACID WITH P-AMINOBENZOIC ACID
- A Microspectrophotometer for Spectral Image Analysis
- Stabilization of intracellular DNA assay with Hoechst 33258 fluorochrome (II)
- Stabilization of intra cellular DNA assay with Hoechst 33258 fluorochrome
- Subfractionation of heterochromatin
- Studies on Nucleosome Structure by Polarization Fluorometry
- Studies on Heterogeneity of Fluorescence Labeled Chromatin
- Biparametric Microfluorometry of Chlorotetracycline to Cellular DNA and Dental Structure
- Dynamic Helical CT Mammography of Breast Cancer
- Comparative Study of Vascular Enhancement on Post-contrast CT Using Three Dosages of Iodinated Contrast Media for The Aim of Detecting Brain Metastasis in Patients with Lung Cancer
- CHANGES OF SERUM TOTAL CHOLESTEROL AND TRIGLYCERIDE LEVELS IN NORMAL SUBJECTS IN JAPAN IN THE PAST TWENTY YEARS : Research Committee on Familial Hyperlipidemia in Japan
- Development of an Oral Formulation of Azetirelin, a New Thyrotropin-Releasing Hormone (TRH) Analogue, Using n-Lauryl-β-D-maltopyranoside as an Absorption Enhancer
- IMPROVEMENT OF INTESTINAL ABSORPTION OF PEPTIDES AND PROTEINS BY CHEMICAL MODIFICATION WITH FATTY ACIDS
- Enhanced Permeability of Phenylalanyl-glycine (Phe-Gly) Across the Intestinal Membranes by Chemical Modification with Various Fatty Acids
- Immunohistochemical localization of C-reactive protein-binding sites in human atherosclerotic aortic lesions by a modified streptavidin-biotin-staining method
- 消化管の efflux 機構は,"Phase ゼロ"の elimination!?
- Uptake Mechanisms of FITC-Oligoarginine Conjugates in HeLa Cells
- Design and Synthesis of Oligoarginine-Fluorescein Conjugates Possessing Novel Self-Cleavable Spacers as a Model for Effective Intestinal Absorption
- Effects of Various Absorption Enhancers on the Intestinal Absorption of Water Soluble Drugs by in Vitro Ussing Chamber Method : Correlation with an in Situ Absorption Experiment
- Effectiveness and Toxicity Screening of Various Absorption Enhancers in the Large Intestine : Intestinal Absorption of Phenol Red and Protein and Phospholipid Release from the Intestinal Membrane
- CARDIOVASCULAR FINDINGS IN FAMILIAL HYPERCHOLESTEROLEMIC CHILDREN
- Effect of Moderately Increased Intrapelvic Pressure on Renal Tissue Pressure and Vasopressin Release in Rabbits
- Laparoscopy-Assisted Abdominal Aortic Aneurysm Repair : First Case Reports From Japan
- Effects of Pretreatment of Zao Zhuang and Akabira Bituminous Coals with SiCl_4-NaI Reagents on Pyrolytic Behavior of Extracts
- On Feulgen residual DNA
- Electrophysiological Studies on the Evaluation of Absorption Enhancers in Caco-2 Cells Using a Microelectrode Technique
- Ultrasonic Heat Transfer Enhancement Using a Horn-Type Transducer
- Glycogenosomes in Hepatocyte of Diploid and Triploid Masu Salmon(Oncorhynchus masou), Mimicking Cytology of Glycogen Storage Disease Type II(Biological Chemistry)
- The Effect of Wellsolve, a Novel Solubilizing Agent, on the Intestinal Barrier Function and Intestinal Absorption of Griseofulvin in Rats
- A study of smoothed TEC precision inferred from GPS measurements
- Heterogeneous bindings of fluorescence antibiotics to chromatin subfractions.
- The Effects of Differing Amounts of Exercise Training on physical Fitness and Serum Lipids in Middle-aged Men and Women
- Lectin Histochemical Study of Squamous Carcinoma in the Head and Neck Region
- Improvement of Intestinal Absorption of Biologically Active Peptides by Chemical Modification with Fatty Acids
- LDL-apheresis ; Potential Procedure for Prevention and Regression of Atheromatous Vascular Lesion : 50th Annual Scientific Session of the Japanese Circulation Society
- Multiple Gastric Ruptures Caused by Blunt Abdominal Trauma : Report of a Case
- Double mental foramina of the mandible on computed tomography images : a case report
- Analysis of Volatile Organic Compounds (VOCs) in the Urban Atmosphere of Beijing
- Development of Interventional Radiology for the Internal Derangements of the Temporomandibular Joint
- C202 STREAMING AND HEAT TRANSFER BY AN ULTRASONIC VIBRATION IN A WATER VESSEL(Heat transfer in complex system-2)
- Measurements of Fluorescence Characteristics in Human Teeth
- Design of Drug Delivery Systems Based on Biopharmaceutical Characteristics
- Self-etching primer systems: changes in dentin bond strength with time
- Multi-sensor data fusion for land vehicle attitude estimation using a fuzzy expert system
- Optical and Electrical Properties of Boron
- In Vitro Study on the Transport of Zinc across Intestinal Epithelial Cells Using Caco-2 Monolayers and Isolated Rat Intestinal Membranes
- In Vitro Evaluation of Nasal Mucociliary Clearance Using Excised Rat Nasal Septum
- Idiopathic Localized Bronchostenosis in an Adult Man with Frequent Recurring Pneumonia
- In Vitro Evaluation of the Ciliary Beat Frequency of the Rat Nasal Epithelium Using a High-Speed Digital Imaging System
- Usefulness of Dual Echo Volumetric Isotropic Turbo Spin Echo Acquisition (VISTA) in Magnetic Resonance Imaging of the Temporomandibular Joint
- Solubility Characteristics and Selective Extraction of Jatropha Oil by Super- and Subcritical CO2 Extraction
- Influence of light intensity on contraction stress of flowable resins