Effect of Vehicle Properties on Skin Penetration of Emedastine
スポンサーリンク
概要
- 論文の詳細を見る
We investigated sorption and permeation of emedastine with 11 different vehicles, composed of single or binary solvents, in excised rat skin. In the sorption study, partition parameters of the drug with each vehicle were obtained by dividing the drug amount in skin at equilibrium by its donor concentration. When the logarithm of the partition parameters for the stratum corneum/vehicle partitioning (K_s') was plotted against the dielectric constants of the vehicles, a bi-liner relationship was obtained. The skin flux of emedastine largely differ among the vehicles. A quasi-steady-state flux of emedastine exhibited a good linear relationship with K_s', except for ethanol (EtOH)/isopropyl myristate (IPM) systems, indicating that the partitioning process is critical in determining the permeation rate. Delineation of the EtOH/IPM systems would be due to an increase in the diffusivity of the drug in the stratum corneum, as indicated by the analysis using a two-layer diffusion model. Thus, differential evaluation of partitioning and diffusion processes by both sorption and permeation studies would give further insights into the effects of vehicles on skin permeation of drugs.
- 公益社団法人日本薬学会の論文
- 2000-10-01
著者
-
Yamashita Fumiyoshi
Department Of Drug Delivery Research Graduate School Of Pharmaceutical Sciences Kyoto University
-
Hashida Mitsuru
Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University
-
Takahashi Yoshiteru
Pharmaceutical Development Group Pharmaceutical Engineering Department Manufacturing & Technolog
-
HARADA Shoichi
Pharmaceutical Development Group, Pharmaceutical Engineering Department, Manufacturing & Technology
-
NAKAGAWA Hiroshi
Pharmaceutical Development Group, Pharmaceutical Engineering Department, Manufacturing & Technology
-
Harada Shoichi
Pharmaceutical Development Group Pharmaceutical Engineering Department Manufacturing & Technolog
-
Nakagawa Hiroshi
Pharmaceutical Development Group Pharmaceutical Engineering Department Manufacturing & Technology Division Nippon Organon K.k.
-
Harada Schoichi
Pharmaceutical Development Group, Pharmaceutical Engineering Department, Manufacturing & Technology Division, Nippon Organon K.K.
関連論文
- Biliary Excretion of Mitomycin C Dextran Conjugates in Relation of Physicochemical Characteristics of Carrier Dextran
- Formulation and pharmacokinetic evaluation of tetracycline-loaded solid lipid nanoparticles for subcutaneous injection in mice
- Intracellular Trafficking Is the Important Process That Determines the Optimal Charge Ratio on Transfection by Galactosylated Lipoplex in HepG2 Cells(Biopharmacy)
- Effect of the Particle Size of Galactosylated Lipoplex on Hepatocyte-Selective Gene Transfection after Intraportal Administration(Biopharmacy)
- Effect of Low-Molecular-Weight β-Cyclodextrin Polymer on Release of Drugs from Mucoadhesive Buccal Film Dosage Forms(Biopharmacy)
- Lipid Carrier Systems for Targeted Drug and Gene Delivery
- Analysis of Hepatic Disposition of Native and Galactosylated Polyethylenimine Complexed with Plasmid DNA in Perfused Rat Liver
- Formulation and Pharmacokinetic Evaluation of Tetracycline-Loaded Solid Lipid Nanoparticles for Subcutaneous Injection in Mice
- Effect of Co-administration of Cationic Macromolecules on the In Vivo Disposition and situ Renal Disposition Characteristics of rhIL-11
- Hepatic Disposition Characteristics of Recombinant Human Interleukin-11 (rhIL-11) in the Perfused Rat Liver
- Development of the inclusive evaluation method for the percutaneous absorption III : Prediction of human dermal concentration of chemicals in various vehicles
- Prediction of skin permeability of compounds from their molecular structure
- 2D- and 3D-QSAR of carrier-mediated transport of beta-lactam antibiotics in Caco-2 cells
- Prediction of Human Skin Permeability Using a Combination of Molecular Orbital Calculations and Artificial Neural Network
- QSPR analysis on inhibition of recombinant CYP3A4 activity by structurally diverse compounds using genetic algorithm combined partial least squares method
- Theoretical Analysis of the Effect of Cutaneous Metabolism on Skin Permeation of Parabens Based on a Two-Layer Skin Diffusion/Metabolism Model
- Pharmacokinetic analysis of ^I-labeled medium chain fatty acid as a radiopharmaceutical for hepatic function based on beta-oxidation
- Effect of Medium-Chain Glycerides on the Membrane Transport of D-Glucose and Sulfanilic Acid in the Intestinal Brush-Border Membrane Vesicles
- EFFECT OF MEDIUM-CHAIN GLYCERIDES (MGK^[○!R]) ON THE INTESTINAL ABSORPTION AND THE HEPATOBILIARY TRANSPORT OF BROMTHYMOL BLUE
- Pharmacokinetic considerations regarding non-viral cancer gene therapy
- Pharmacokinetic Evaluation of Biodistribution Data Obtained with Radiolabeled Proteins in Mice
- Pharmacokinetic Analysis of the in Vivo Disposition of Chemically Modified Proteins in Rats : Effect of Radiolabeling Method
- STUDY ON THE ACTION OF PERCUTANEOUS PENETRATION ENHANCERS : EFFECT ON VARIOUS DRUGS WITH DIFFERENT PHYSICOCHEMICAL PROPERTIES
- Analysis of Drug Penetration through Skin Considering Donor Concentration Decrease
- EFFECTS OF MITOMYCIN C, 5-FLUOROURACIL AND CYCLOPHOSPHAMIDE ON DRUG ABSORPTION, ENZYME ACTIVITIES AND MUCOSAL LIPID COMPOSITION OF INTESTINE
- BIOPHARMACEUTICAL STUDIES ON ANTITUMOR DRUG-INDUCED GASTROINTESTINAL DAMAGES
- Role of Tyrosine and Tryptophan in Chemically Modified Serum Albumin on Its Tissue Distribution(Biopharmacy)
- Control of Plasma Cholesterol-Lowering Action of Probucol with Various Lipid Carrier Systems
- Exogenous Expression of Interferon-β in Cultured Brain Microvessel Endothelial Cells(Biochemistry/Molecular Biology)
- Expression and Visualization of a Human Interferon-β-Enhanced Green Fluorescent Protein Chimeric Molecule in Cultured Cells (Biochemistry/Molecular Biology)
- Cationic Liposome-Mediated Efficient Induction of Type I Interferons by a Low Dose of Poly I:Poly C in Mouse Cell Lines
- Transport Characteristics of Ebastine and Its Metabolites across Human Intestinal Epithelial Caco-2 Cell Monolayers
- Cellular Interaction and in Vitro Antitumor Activity of Lipophilic Mitomycin C Prodrugs(Pharmaceutical)
- Key Physiological Phenomena Governing Transgene Expression Based on Tissue Pressure-Mediated Transfection in Mice
- EVALUATION OF DRUG DISPOSITION IN BRAIN BY MOMENT ANALYSIS (II)
- Enhanced Gene Transfection in Macrophages by Histidine-Conjugated Mannosylated Cationic Liposomes
- Relationship between Drug Release of DE-310, Macromolecular Prodrug of DX-8951f, and Cathepsins Activity in Several Tumors(Biopharmacy)
- Hydrogen peroxide-mediated nuclear factor κB activation in both liver and tumor cells during initial stages of hepatic metastasis
- Influence of Cholesterol Composition on the Association of Serum Mannan-Binding Proteins with Mannosylated Liposomes(Analytical Biochemistry)
- Tissue-specific in vivo gene transfer characteristics following direct injection of plasmid DNA
- IMMUNOLOGICAL CONTROL OF DRUG ABSORPTION FROM THE GASTROINTESTINAL TRACT : EFFECT OF LOCAL ANAPHYLAXIS ON THE INTESTINAL ABSORPTION OF LOW MOLECULAR WEIGHT DRUGS IN THE RAT
- DRUG ABSORPTION FROM THE GASTROINTESTINAL TRACT AND IMMUNITY : THE MECHANISM OF THE DECREASED ABSORPTION OF SALICYLIC ACID DURING SYSTEMIC ANAPHYLAXIS. II
- DRUG ABSORPTION FROM THE GASTROINTESTINAL TRACT AND IMMUNITY : THE MECHANISM OF THE DECREASED ABSORPTION OF SALICYLIC ACID DURING SYSTEMIC ANAPHYLAXIS.I
- Deconvolution Analysis for Absorption and Metabolism of Aspirin in Microcapsules
- Effect of Vehicle Properties on Skin Penetration of Emedastine
- Molecular and Pharmacokinetic Properties of 222 Commercially Available Oral Drugs in Humans
- Nonviral Approaches Satisfying Various Requirements for Effective in Vivo Gene Therapy
- Tissue Distribution of ^In-Labeled Uricase Conjugated with Charged Dextrans and Polyethylene Glycol
- CONTROL OF IN VIVO FATE OF PROTEIN DRUGS USING CHEMICAL MODIFICATION WITH SUGARS
- INTESTINAL ABSORPTION OF HAPTENS IN RATS IMMUNIZED WITH PROTEIN-HAPTEN CONJUGATE : COMPARISON OF SULFANILIC ACID WITH P-AMINOBENZOIC ACID
- EVALUATION OF ABSORPTIVE BARRIER TO PEPTIDES AND IMPROVEMENT OF MUCOSAL ABSORPTION OF PEPTIDES BY VARIOUS APPROACHES
- Design and Evaluation of Monoclonal Antibody-Antitumor Agent Conjugate
- Cellular Interaction and in Vitro Antitumor Effect of Various Mitomycin C Prodrugs in Mitomycin C-Resistant L1210 Leukemia Cell Lines(Pharmaceutical)
- EFFECT OF TEMPERATURE ON INTESTINAL TRANSFER AND TISSUE UPTAKE OF SULFANILAMIDE AND AMINOPROPYRON IN VITRO
- CELLULAR INTERACTION AND ANTITUMOR ACTIVITY OF MITOMYCIN C PRODRUGS
- URINARY EXCRETION CHARACTERISTICS OF A POLYMERIC PRODRUG OF MITOMYCIN C, MITOMYCIN C-DEXTRAN CONJUGATE
- ENHANCED LYMPHATIC DELIVERY OF MIYOMYCIN C BY POLYMERIC MODIFICATION
- Effect of Polycyclic Aromatic Hydrocarbons on Generation and Efflux of Glutathione Conjugates in Primary Cultured Alveolar Epithelial Cells
- In Silico Approaches for Predicting ADME Properties of Drugs
- Biodistribution Characteristics of Surface Charge Improved Lysine Dendrimers after Intravenous Injection in Mice
- ANTITUMOR ACTIVITY OF LIPOPHILIC PRODRUGS OF MITOMYCIN C ENTRAPPED IN LIPOSOME OR O/W EMULSION
- DEVELOPMENT OF LIPOPHILIC MITOMYCIN C PRODRUGS AND THEIR APPLICATION TO LIPID DISPERSION SYSTEMS
- SOLID DISPERSIONS OF POORLY WATER-SOLUBLE DRUGS WITH ENTERIC COATING AGENTS
- Bovine Serum Albumin as a Lyoprotectant for Preparation of DNA Dry Powder Formulations Using the Spray-Freeze Drying Method
- Evaluation of Long-Term Gene Expression in Mouse Liver Using PhiC31 Integrase and Hydrodynamic Injection
- Combination of Bubble Liposomes and High-Intensity Focused Ultrasound (HIFU) Enhanced Antitumor Effect by Tumor Ablation
- Sedative Effects of Inhaled Benzylacetone and Structural Features Contributing to Its Activity