Effects of Labrasol and Other Pharmaceutical Excipients on the Intestinal Transport and Absorption of Rhodamine123, a P-Glycoprotein Substrate, in Rats(Biopharmacy)
スポンサーリンク
概要
- 論文の詳細を見る
Effects of Labrasol and other pharmaceutical excipients on the intestinal transport and absorption of rhodamine123, a P-glycoprotein substrate (P-gp) were examined. Intestinal transport and absorption studies were examined by an in vitro diffusion chamber method and an in situ closed loop method. We evaluated the intestinal membrane damage produced by Labrasol by measuring the release of protein and alkaline phosphatase (ALP). Labrasol (0.075-0.1% (v/v)) increased the absorptive transport of rhodamine123 and decreased its secretory transport in the in vitro transport studies. However, Labrasol did not change the transport of Lucifer yellow, a non-P-gp substrate, suggesting that the effect of Labrasol on the transport of drugs was specific for rhodamine123. We observed almost no intestinal membrane damage in the presence of Labrasol. These findings suggest that the increase in the absorptive transport of rhodamine123 in the presence of Labrasol may not be due to its intestinal membrane damage. In the in situ absorption studies, we found that Labrasol (0.1% (v/v)) significantly enhanced the intestinal absorption of rhodamine123 in rats, although the absorption enhancing effect of Labrasol was much less than that of verapamil. These findings suggest that low concentrations of Labrasol might inhibit the function of P-gp in the intestine, thereby increasing intestinal absorption and bioavailability of P-gp substrates including rhodamine123. However, we may also consider the contribution to the enhanced intestinal absorption of rhodamine123 via a passive transport in addition to the inhibitory action of Labrasol for the function of P-gp in the intestine.
- 社団法人日本薬学会の論文
- 2007-07-01
著者
-
Okada Naoki
Department of Biotechnology and Therapeutics, Graduate School of Pharmaceutical Sciences, Osaka Univ
-
YAMAMOTO Akira
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
Fujita T
Division Of Oral Cytology And Cell Biology Department Of Developmental And Reconstructive Medicine N
-
Okada N
Graduate School Of Pharmaceutical Sciences Osaka University
-
LIN Yulian
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
SHEN Qi
School of Pharmacy, Shanghai Jiao Tong University
-
KATSUMI Hidemasa
Department of Biopharmaceutics, Kyoto Pharmaceutical University
-
FUJITA Takuya
Ritsumeikan University College of Information Science and Engeneering
-
JIANG Xuehua
Department of Clinical Pharmacy, Pharmacy School of Sichuan University
-
Yamamoto Akira
Dep. Of Biopharmaceutics Kyoto Pharmaceutical Univ.
-
Fujita T
Ritsumeikan University College Of Information Science And Engeneering
-
Okada Naoki
Department Of Bioppharmaceutics Kyoto Pharmaceutical University
-
Fujita T
Showa College Of Pharmaceutical Sciences
-
Fukushima Tohru
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Setsunan University
-
Shen Qi
School Of Pharmacy Shanghai Jiao Tong University
-
Shen Qi
School Of Chemistry And Chemical Engineering Suzhou University
-
Jiang Xuehua
Department Of Clinical Pharmacy Pharmacy School Of Sichuan University
-
Katsumi Hidemasa
Dep. Of Biopharmaceutics Kyoto Pharmaceutical Univ.
-
Katsumi Hidemasa
Department Of Biopharmaceutics Kyoto Pharmaceutical University
-
Yamamoto Akira
Department Of Biopharmaceutics Kyoto Pharmaceutical University
-
Okada Naoki
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
関連論文
- Optimized PEGylated Adenovirus Vector Reduces the Anti-vector Humoral Immune Response against Adenovirus and Induces a Therapeutic Effect against Metastatic Lung Cancer
- Non-Methylated CpG Motif Packaged into Fusogenic Liposomes Enhance Antigen-Specific Immunity in Mice(Highlighted paper selected by Editor-in-chief,Pharmacology)
- Vaccine Efficacy of Fusogenic Liposomes Containing Tumor Cell-Lysate against Murine B16BL6 Melanoma(Pharmacology)
- Anti-tumor Responses Induced by Chemokine CCL19 Transfected into an Ovarian Carcinoma Model via Fiber-Mutant Adenovirus Vector(Biopharmacy)
- 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〕
- Prolongation of the Effective Duration of Cytomedical Therapy by Re-injecting SK2 Hybridoma Cells Microencapsulated within Alginate-Poly(L)lysine-Alginate Membranes into Human Interleukin-6 Transgenic Mice
- Therapeutic Effect of Cytomedicine on Mesangio-Proliferative Glomerulonephritis in Human Interleukin-6 Transgenic Mice
- 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
- Cell Delivery System : A Novel Strategy to Improve the Efficacy of Cancer Immunotherapy by Manipulation of Immune Cell Trafficking and Biodistribution
- 3P-081 ファージ表面提示法を用いたTNFR1指向性リンフォトキシンαの創製とその特性評価(蛋白質工学,進化工学,第46回日本生物物理学会年会)
- 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
- Evaluation of Angiogenic Inhibitors with an in vivo Quantitative Angiogenesis Method Using Agarose Microencapsulation and Mouse Hemoglobin Enzyme-linked Immunosorbent Assay
- Selective Enhancement by Tumor Necrosis Factor-α of Vascular Permeability of New Blood Vessels Induced with Agarose Hydrogel-entrapped Meth-A Fibrosarcoma Cells
- A Quantitative in vivo Method of Analyzing Human Tumor-induced Angiogenesis in Mice Using Agarose Microencapsulation and Hemoglobin Enzyme-linked Immunosorbent Assay
- 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
- The Functional Involvement of Rac on Bone and Tooth Formation : Characteristic of N17Rac Transgenic Mice(International Symposium of Maxillofacial and Oral Regenerative Biology in Okayama 2005)
- Transactivation of Core Binding Factor α1 as a Basic Mechanism to Trigger Parathyroid Hormone-Induced Osteogenesis
- Incadronate and Etidronate Accelerate Phosphate-Primed Mineralization of MC4 Cells via ERK1/2-Cbfa1 Signaling Pathway in a Ras-Independent Manner: Further Involvement of Mevalonate-Pathway Blockade for Incadronate
- Phosphate Stimulates Differentiation and Mineralization of the Chondroprogenitor Clone ATDC5
- Bone-anabolic Effect of Salmon Calcitonin on Glucocorticoid-Induced Osteopenia in Rats
- 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
- Effects of Various Storage Conditions and Alterations of Antioxidant Contents on Chromatic Aberration of Hydroquinone Ointment(Biopharmacy)
- ANGIOGRAPHIC FINDINGS AND CLINICAL COURSE OF FAMILIAL HYPERCHOLESTEROLEMIA WITH CORONARY ARTERY DISEASE : PROCEEDINGS OF THE 47th ANNUAL SCIENTIFIC MEETING OF THE JAPANESE CIRCULATION SOCIETY : Ischemic Heart Disease (II)
- 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)
- The Utility of Poly(γ-glutamic acid) Nanoparticles as Antigen Delivery Carriers in Dendritic Cell-Based Cancer Immunotherapy
- INTESTINAL ABSORPTION OF HAPTENS IN RATS IMMUNIZED WITH PROTEIN-HAPTEN CONJUGATE : COMPARISON OF SULFANILIC ACID WITH P-AMINOBENZOIC ACID
- Characterization of Transcutaneous Protein Delivery by a Hydrogel Patch in Animal, Human, and Tissue-Engineered Skin Models
- A Microspectrophotometer for Spectral Image Analysis
- Studies on Nucleosome Structure by Polarization Fluorometry
- Studies on Heterogeneity of Fluorescence Labeled Chromatin
- Biparametric Microfluorometry of Chlorotetracycline to Cellular DNA and Dental Structure
- Improved Synthesis of Anacardic Acids, 6-Pentadecylsalicylic Acid and 6-[8(Z)-Pentadecenyl]salicylic Acid, from Aldehyde and Acetoacetate
- Synthesis of Anacardic Acids Utilizing an Annelation Reaction of Isoxazoles with Ethyl Acetoacetate
- Bone Anabolic Effects of PTH(1-34) and Salmon Calcitonin in Ovariectomy- and Ovariectomy-Steroid-Induced Osteopenic Rats: A Histomorphometric and Biomechanical Study
- Glucocorticoid-Induced Secondary Osteopenia in Female Rats : A Time Course Study as Compared With Ovariectomy-InducedOsteopenia and Response to Salmon Calcitonin
- 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
- Conformational Analysis of Febrifugines and Halofuginones in Organic Solvents
- PA42 CONFORMATIONAL ANALYSIS OF TRICHOSPORIN-B-V BY CD AND NMR SPECTROSCOPY
- 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
- Synthesis and Structure of a Novel Tetranuclear Tungsten-Bismuth-Sulfur Complex
- 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
- Enhanced Oral Bioavailability of Daidzein by Self-Microemulsifying Drug Delivery System
- Electrophysiological Studies on the Evaluation of Absorption Enhancers in Caco-2 Cells Using a Microelectrode Technique
- Modifying the antigen-immunization schedule improves the variety of monoclonal antibodies obtained from immune-phage antibody libraries against HIV-1 Nef and Vif(MEDICAL BIOTECHNOLOGY)
- 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
- 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
- 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
- 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)
- An HPLC method for the pharmacokinetic study of daidzein-loaded nanoparticle formulations after injection to rats
- Modifying the antigen-immunization schedule improves the variety of monoclonal antibodies obtained from immune-phage antibody libraries against HIV-1 Nef and Vif
- 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
- In Vitro Evaluation of the Ciliary Beat Frequency of the Rat Nasal Epithelium Using a High-Speed Digital Imaging System