Effect of Lipophilicity on in Vivo Iontophoretic Delivery. II. β-Blockers

スポンサーリンク

概要

• 論文の詳細を見る

• The objective of this study was to investigate the relationship between drug lipophilicity and the transdermal absorption proceseses in the iontophoretic delivery in vivo. Anodal iontophoresis of β-blockers as model drugs having different lipophilicity(atenolol, pindolol, achebutolol, oxyprenolol and propranolol)was performed with rats(electrical current, 0.625mA/cm^2 ; application period, 90min), and the drug concentrations in skin, cutaneous vein and systemic vein were determined. Increasing the lipophilicity of β-blockers caused a greater absorption into the skin. Exceptionally, it was found tha pindolol had high skin absorption, irrespective of its hydrophilic mnatire. Further, the drug transfer rate from skin to cutaneous vein(R_<sc>)was evaluated from the arterio-venous plasma cpncentration difference of drug in the skin. Normalized R_<sc> by skin concentration showed a negative correlation with the logarithm of n-octanol/buffer partition coefficient(Log P, pH 7.4), suggesting the partitioning betweed stratum corneum and viable epidermis was a primary process to determine the transfer properties of β-blockers to local blood circulation. Pindolol exhibited both high skin absorption and high transfer from skin[ to vutaneous vein. These characteristics of pindolol could be explained by the chemical structure, molecular size and hydrophilicity. These finding for pindolol should be valuable for the optimal design of drug vandidates for iontophoretic transdermal delivery.

• 公益社団法人日本薬学会の論文
• 2001-06-01

著者

• Kato Y

  Institute Of Cosmetic Sciences Club Cosmetics Co. Ltd.

• Ito Kunio

  Pharmaceutical Research Laboratories Kyowa Hakko Kogyo Co. Ltd.

• KATO Yasuki

  Drug Formulation Research Laboratories, Pharmaceutical Research Center, Kyowa Hakko Kogyo Co., Ltd.

• Itoh K

  Department Of Pharmaceutical Sciences Tohoku University Hospital And Division Of Clinical Pharmacy G

• Itoh Kunio

  Department Of Drug Metabolism And Pharmacokinetics Tohoku Pharmaceutical University

• Kato Yasuki

  協和醗酵工業

• Hayakawa E

  Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd

• Ito K

  Janssen Pharmaceutical K.k. Shizuoka Jpn

• TASHIRO Yoshikazu

  Drug Formulation Research Laboratories, Phaemaceutical Research Institute, Kyowa Hakko Kogyo Co., Lt

• SAMI Mari

  Drug Formulation Research Laboratories, Phaemaceutical Research Institute, Kyowa Hakko Kogyo Co., Lt

• SHICHIBE Shozo

  Drug Formulation Research Laboratories, Phaemaceutical Research Institute, Kyowa Hakko Kogyo Co., Lt

• HAYAKAWA Eiji

  Drug Formulation Research Laboratories, Phaemaceutical Research Institute, Kyowa Hakko Kogyo Co., Lt

• ITOH Kunio

  Drug Formulation Research Laboratories, Phaemaceutical Research Institute, Kyowa Hakko Kogyo Co., Lt

• Sami Mari

  Pharmaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd

• Shichibe Shozo

  Drug Formulation Research Laboratories Phaemaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.

• Tashiro Y

  Drug Formulation Research Laboratories Phaemaceutical Research Institute Kyowa Hakko Kogyo Co. Ltd.

関連論文

• Effects of Selenium Deficiency on Aldehyde Oxidase 1 in Rats(Molecular and Cell Biology)
• Granulomatous Tissue Formation of Shikon and Shikonin by Air Pouch Method
• ISOLATION OF MYCOLIC ACID-CONTAINING GLYCOLIPIDS IN NOCARDIA RUBRA AND THEIR GRANULOMA FORMING ACTIVITY IN MICE
• Murine Langerhans Cells Activation Induced by Administration of Shikon, Shikonin and Alkannin
• An Extract of the Root of Lithospermun erythrorhison Accelerates Wound Healing in Diabetic Mice
• Study of the Accelerating Effect of Shikonin and Alkannin on the Proliferation of Granulation Tissue in Rats
• Design, Production, and Characterization of Recombinant Neocarzinostatin Apoprotein in Escherichia coli
• Solid Dispersions of Benidipine Hydrochloride. II. Investigation of the Interactions among Drug, Polymer and Solvent in Preparations
• Solid Dispersions of Benidipine Hydrochloride. I. Preparations Using Different Solvent Systems and Dissolution Properties
• Reducing the Impact of Binding of UCN-01 to Human α_1-Acid Glycoprotein by Encapsulation in Liposomes(Biopharmacy)
• Evaluation of the Carrier Potential for the Lipid Dispersion System with Lipophilic Compound
• Role of the Lipid Emulsion on an Injectable Formulation of Lipophilic KW-3902, a Newly Synthesized Adenosine A_1-Receptor Antagonist
• Formulation Development of a Filter-Sterilizable Lipid Emulsion for Lipophilic KW-3902, a Newly Synthesized Adenosine A_1-Receptor Antagonist
• Asymmetric Synthesis of a Selective Endothelin A Receptor Antagonist
• Preparation of a Monoclonal Antibody Specific for 5-Methyl-2'-deoxycytidine and Its Application for the Detection of DNA Methylation Levels in Human Peripheral Blood Cells
• Comparison of Serum and Urinary Levels of Modified Nucleoside, 1-Methyladenosine, in Cancer Patients Using a Monoclonal Antibody-Based Inhibition ELISA
• Facile Formation of Chiral Calixarene Analogs Incorporating Cystine Peptide into the Macrocyclic Ring.
• Syntheses and Properties of Calixarene Analogs Containing Thiophene Ring
• Elecrochemical Stability of Desmopressin Acetate during Iontophoresis
• Effect of Pulse on Iontophoretic Delivery of Desmopressin Acetate in Rats
• Increased Expression of Queuosine Synthesizing Enzyme, tRNA-Guanine Transglycosylase, and Queuosine Levels in tRNA of Leukemic Cells
• Influence of N-Terminal Peptide and Oligosaccharide on the Clearance of t-PA
• A New Drug Delivery System Using Plasma-Irradiated Pharmaceutical Aids. IX. : Controlled-Release of Theophylline from Double-Compressed Tablet Composed of Cellulose Derivatives as Wall Material.
• A New Drug Delivery System Using Plasma-Irradiated Pharmaceutical Aids. VIII. : Delayed-Release of Theophylline from Double-Compressed Tablet Composed of Eudragit as Wall Material.
• Estimation of Radiation Exposed Area by the Nuclear Accident Occurred at Tokai Village Using ESR Measurements of Household Sugar.
• A New Drug Delivery System Using Plasma-Irradiated Pharmaceutical Aids. IX. Controlled-Release of Theophylline from Double-Compressed Tablet Composed of Cellulose Derivatives as Wall Material
• A New Drug Delivery System Using Plasma-Irradiated Pharmaceutical Aids. VIII. Delayed-Release of Theophylline from Double-Compressed Tablet Composed of Eudragit as Wall Material
• Plasma-Induced Free Radicals of Polycrystalline Carbohydrate as Spin Probe for Plasma Diagnosis of Plasma Treatment.
• Functional Analysis of Aldehyde Oxidase Using Expressed Chimeric Enzyme between Monkey and Rat(Molecular and Cell Biology)
• Properties of 130 kDa Subunit of Monkey Aldehyde Oxidase(Molecular and Cell Biology)
• Cloning, Expression, and Characterization of Male Cynomolgus Monkey Liver Aldehyde Oxidase(Biochemistry)
• Substrate Selectivity of Monoamine Oxidase A, Monoamine Oxidase B, Diamine Oxidase, and Semicarbazide-Sensitive Amine Oxidase in COS-1 Expression Systems(Biochemistry)
• Molecular Cloning and Characterization of Rat Semicarbazide-Sensitive Amine Oxidase(Biochemistry/Molecular Biology)
• Alteration in the Temperature-Dependent Content Release Property of Thermosensitive Liposomes in a Plasma
• Enhancing Effect of Switching Iontophoresis on Transdermal Absorption of Sodium Benzoate In Vivo
• Histological Study of the Accelerating Effect of Shikonin and Alkannin on the Proliferation of Granulation Tissue in Rats
• Effect of Lipophilicity on in Vivo Iontophoretic Delivery. II. β-Blockers
• Effect of Lipophilicity on in Vivo Iontophoretic Delivery.I. NSAIDs
• Biological Fate of Highly-Succinylated N-Succinyl-chitosan and Antitumor Characteristics of Its Water-soluble Conjugate with Mitomycin C at I.v. and I.p. Administration into Tumor-Bearing Mice
• Iontophoretic Transdermal Delivery of Ketoprofen : Effect of Iontophoresis on Drug Transfer from Skin to Cutaneous Blood
• Iontophoretic Transdermal Delivery of Ketoprofen : Novel Method for the Evaluation of Plasma Drug Concentration in Cutaneous Vein
• Asymmetric Synthesis of an Endothelin Receptor Antagonist
• Safe and Efficient Transdermal Delivery of Desmopressin Acetate by Iontophoresis in Rats
• Prolongation of Antidiuretic Response to desmopressin Acetate by Iontophoretic Transdermal Delivery in Rats
• Epitaxial Solution Growth of ZnTe on ZnSe
• The Effect of Eddy Current in the Feromagnetic Resonance of Spherical Specimens
• Study of White-LED Using Amorphous Carbon Nitride Grown by RF-sputtering and ECR-plasma CVD
• The Effect of Skin Depth on Ferromagnetic Resonance in Spherical Ferrites
• Ferromagnetic Crystalline Anisotropy and Transition Temperature of Ti-Substituted Magnetite
• Murine Langerhans Cells Activation Induced by Administration of Shikon, Shikonin and Alkannin
• Histological Study of the Accelerating Effect of Shikonin and Alkannin on the Proliferation of Granulation Tissue in Rats
• Design Aspects of an Ultrashort Ultraviolet Laser System
• Functional Analysis of Aldehyde Oxidase Using Expressed Chimeric Enzyme between Monkey and Rat

もっと見る 閉じる

スポンサーリンク