Simultaneous Transport and Metabolism of Nicotinic Acid Derivatives in Hairless Mouse Skin
スポンサーリンク
概要
- 論文の詳細を見る
In vitro simultaneous transport and metabolism of three ester prodrugs of nicotinic acid (NA), methyl nicotinate (MN), ethyl nicotinate (EN) and butyl nicotinate (BN) were studied using excised skin from hairless mouse. Hydrolysis studies of these esters with and without skin homogenate were also done at 37℃. Both the ester and NA were detected in all receiver solutions in permeation studies, and no chemical hydrolysis of the esters was found, indicating that the esters were hydrolyzed during the skin permeation process. The total (ester+NA) flux from a saturated solution of ester prodrugs was higher than that of NA and was highest for MN, followed by EN and BN, whereas the total permeability coefficient of ester prodrugs increased from MN to BN. A difference in the NA/total flux ratio was found among these prodrugs; thus, esterase activity was also dependent on the alkyl chain length of the esters. The total flux from each ester solution increased linearly with the donor concentration. NA flux from MN and EN solutions increased with an increase in the donor concentration and reached a plateau at the high concentration range, suggesting that metabolic saturation occurred. NA fluxes at the plateau were similar among ester prodrugs and corresponded to the V_<max> estimated from the hydrolysis experiment. The order of donor concentration at which NA reched a plateau also corresponded to the order of K_m. It was confirmed that a difference in alkyl chain length of the ester prodrugs affected not only permeability but also metabolism in the skin permeation process.
- 社団法人日本薬学会の論文
- 1999-03-15
著者
-
KATAYAMA Kazunori
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
-
KOIZUMI Tamotsu
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
-
Koizumi T
Toyama Medical & Pharmaceutical Univ. Toyama Jpn
-
Katayama K
Toyama Medical And Pharmaceutical Univ. Toyama Jpn
-
Katayama K
Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University
-
HATANAKA Tomomi
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
-
RITTIROD Theera
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
-
KAGAMI Naoki
Faculty of Pharmaceutical Sciences, Toyama Medical and Pharmaceutical University
-
Hatanaka Tomomi
Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University
-
Hatanaka Tomomi
Faculty Of Pharmaceutical Sciences Josai University
-
Koizumi T
Toyama Medical And Pharmaceutical Univ. Toyama Jpn
-
Katayama Kazunori
Faculty Of Pharmaceutical Science Toyama Medical And Pharmaceutical University
-
Koizumi Tamotsu
Faculty Of Pharmaceutical Science Toyama Medical And Pharmaceutical University
-
Kagami Naoki
Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University
-
Rittirod Theera
Faculty Of Pharmaceutical Sciences Toyama Medical And Pharmaceutical University
関連論文
- 臭化水素酸エプタゾシン注射剤の不溶性異物および着色に対する安定化
- Kinetic Analysis of Neuromuscular Blockade. II. Train-of-Four Fade Induced by d-Tubocurarine and α-Bungarotoxin
- 条件的不死化ラット網膜毛細血管内皮細胞株(TR-iBRB2)へのL-leucine取り込みにおける中性アミノ酸輸送担体LAT1, LAT2の寄与
- 条件的不死化ラット網膜毛細血管内皮細胞株(TR-iBRB2)におけるタウリントランスポーター(TAUT)の役割
- DESENSITIZING NEUROMUSCULAR BLOCKADE BY p-PHENYLENE-POLYMETHYLENE BIS-AMMONIUM COMPOUNDS DEVELOPED FROM SUCCINYLCHOLINE
- A Kinetic Study on Drug Distribution : Furosemide in Rats
- Kinetic Studies on Drug Disposition in Rabbits. III. Effect of Tolbutamide on Renal Excretion of Sulfamethizole
- Kinetic Studies on Drug Disposition in Rabbits. II. Dose Dependent Pharmacokinetics of Sulfamethizole
- Kinetic Studies on Drug Disposition in Rabbits. I. Renal Excretion of Iodopyracet and Sulfamethizole
- ミニコンによる非線形最小二乗あてはめ計算の一改良案
- Drug Targeting Efficacy to Underlying Muscle Following Topical Application. I. Evaluation Based on a Physiological Pharmacokinetic Model
- Single Dose Pharmacokinetics and Pharmacodynamics of Oxazepam in Normal and Renal Dysfunction Rats
- Influence of Enzyme Distribution and Diffusion on Permeation Profile of Prodrug through Viable Skin : Theoretical Aspects for Several Steady-State Fluxes in Two Transport Directions
- Simultaneous Transport and Metabolism of Nicotinic Acid Derivatives in Hairless Mouse Skin
- Influence of Plasma Dialysate from Normal and Renal Dysfunction Rats on the Electroencephalogram and γ-Aminobutyric Acid_A Receptor Complex Modulation of Thiopental
- Pharmacokinetic and Pharmacodynamic Consequences of Thiopental in Renal Dysfunction Rats : Evaluation with Electroencephalography
- SPECIES DIFFERENCE IN SIMULTANEOUS TRANSPORT AND METABOLISM OF ETHYL NICOTINATE IN SKIN
- A Study of the Hydrophilic Cellulose Matrix : Effect of Drugs on Swelling Properties
- Effect of Iodopyracet on Renal Excretion of Sulfamethizole in Rabbits
- Kinetic Studies of the Pharmacologic Response to Captopril in Rats. II. Hypotensive Effect and Plasma Angiotensin Converting Enzyme Activity
- Kinetic Studies of the Pharmacologic Response to Captopril in Rats. I. Role of the Renin-Angiotensin System
- Pharmacokinetic and Pharmacodynamic Studies of Piretanide in Rabbits. IV. Effect of Piretanide on the Proximal Tubules and the Loop of Henle under a Hydrated Condition
- A Kinetic Study of Chlorpromazine on the Hyperglycemic Response in Rats. II. Effect of Chlorpromazine on Plasma Glucose
- A Kinetic Study of Chlorpromazine on the Hyperglycemic Response in Rats. I. Effect of Chlorpromazine on Plasma Catecholamines
- Pharmacokinetic and Pharmacodynamic Studies of Piretanide in Rabbits. III. Sodium and Potassium Excretion under Different Hydrated Conditions
- Pharmacokinetic and Pharmacodynamic Studies of Piretanide in Rabbits. II : Effects on the Proximal Tubules and the Loop of Henle
- The Pharmacodynamic and Pharmacokinetic Interaction of Pentobarbital and Chlorpromazine in Rats
- 30C-04 生薬を用いた浴湯剤に関する研究 (III) : 生薬成分の皮膚透過に対する中国産川〓の吸収促進効果
- ラットにおけるSuccinylcholineの筋弛緩効果におよぼす血清Cholinesterase活性の影響
- In Vitro-in Vivo Correlation of Percutaneous Absorption : Isosorbide Dinitrate and Morphine Hydrochloride
- Anodization of Glassy Carbon Electrodes in Oligomers of Ethylene Glycol and Their Monomethyl Ethers as a Tool for the Elimination of Protein Adsorption
- PHARMACOKINETIC AND PHARMACODYNAMIC STUDIES OF PIRETANIDE IN RABBITS. I. EFFECT OF DIFFERENT HYDRATED CONDITIONS
- Pharmacokinetic and Pharmacodynamic Studies of Centrally Acting Drugs in Rat : Effect of Pentobarbital and Chlorpromazine on Electroencephalogram in Rat
- Effect of Chlorpromazine on the Pharmacokinetics and Pharmacodynamics of Pentobarbital in Rats
- PHARMACOLOGIC EFFECTS OF CHLORPROMAZINE IN RELATION TO ITS DISPOSITION IN RATS : BODY TEMPERATURE, BLOOD GLUCOSE AND HEART RATE
- EFFECT OF ENVIRONMENTAL TEMPERATURE ON THERMAL RESPONSE TO CHLORPROMAZINE. I. SIMULATION OF TEMPERATURE REGULATION IN RATS
- Kinetic Analysis of Neuromuscular Blockade. I. Relationship between Twitch Depression and Stimulation Frequency after d-Tubocurarine Administration
- Enantioselective Fluorination of Organic Molecules. I. Synthetic Studies of the Agents for Electrophilic, Enantioselective Fluorination of Carbanions
- Pharmacokinetics of Two Rectal Dosage Forms of Ketoprofen in Patients after Anal Surgery
- A Note on Diffusion in Finite Composite Media
- 血液網膜関門における vitamin C 輸送機構の解析
- シンバスタチン錠剤からの溶出挙動に及ぼすラクトン体とヒドロキシアシド体の相互変換速度の影響
- イオンペア形成によるCephalexinの皮膚透過促進に及ぼすカウンターイオンの構造の影響
- シスプラチンとオンダンセトロンの薬動学的相互作用
- 非線形型拡散モデルの薬物腎挙動解析への適用
- 硫酸エステル類の立体選択的皮膚透過性に関する熱力学的検討
- オレイン酸の透過促進機構に関する研究 : 皮膚インピーダンス解析のよる評価
- 生薬を用いた浴湯剤に関する研究(第2報) : 黄連エキスの皮膚透過促進効果
- A Study of the Hydrophilic Cellulose Matrix : Effect of Indomethacin and a Water-Soluble Additive on Release Mechanisms
- Two-Layer Membrane Model for Iontophoretic Drug Transport through Excised Rat Skin
- Effect of l-Menthol on the Permeation of Indomethacin, Mannitol and Cortisone through Excised Hairless Mouse Skin
- 生薬を用いた浴湯剤に関する研究 : 川〓エキスの経皮吸収促進効果
- I-B-5 生薬を用いた浴湯剤に関する研究 1 : 川〓エキスの経皮吸収および経皮吸収促進作用について
- Transfer of Diclofenac Sodium across Excised Guinea Pig Skin on High-Frequency Pulse Iontophoresis. II. : Factors Affecting Steady-State Transport Rate
- Transfer of Diclofenac Sodium across Excised Guinea Pig Skin on High-Frequency Pulse Intophoresis. I. : Equivalent Circuit Model
- 高周波パルス型イオントフォレシスによるフマル酸フォルモテロールの経皮吸収促進(第2報)通電方法, 周波数及び通電率の影響
- Chemical Structural Requirement in Gingerol Derivatives for Potentiation of Prostaglandin F_-Induced Contraction in Isolated Mesenteric Veins of Mice
- Bioavailability of Morphine in Rabbits after Rectal Administration of Suppository Containing Controlled Release Morphine Tablet
- Factors Affecting Sulfisoxazole Transport through Excised Rat Skin during Iontophoresis
- 立体異性体の皮膚透過に及ぼす組織結合と代謝の役割-理論的考察
- プロピオン酸系抗炎症薬の立体選択的皮膚透過挙動の解析
- Ecabet sodium のラット腎排泄の性差に関する速度論的解析
- 薬物生体内挙動と薬物反応の速度論的解析
- 生理的要因を介した薬物反応と薬物動態の速度論的解析
- 日本薬学会奨励賞受賞山岡清氏の業績
- Significant Expression of Functional Human Type 1 Mitochondrial ADP/ATP Carrier in Yeast Mitochondria
- Irreversible Extrusion of the First Loop Facing the Matrix of the Bovine Heart Mitochondrial ADP/ATP Carrier by Labeling the Cys^ Residue with the SH-Reagent Methyl Methanethiosulfonate^1
- PHARMACOKINETIC STUDIES ON PHARMACOLOGIC RESPONSE OF CAPTOPRIL IN RATS
- PHARMACOLOGIC EFFECTS OF METFORMIN IN RELATION TO ITS DISPOSITION IN ALLOXAN DIABETIC RATS
- INFLUENCE OF ETHANOL AND POLYETHYLENE GLYCOL UPON THE SKIN PERMEATION OF DRUGS
- 高周波パルス型イオントフォレシスによるフマル酸フォルモテロールの経皮吸収促進(第1報) : 一定電流及び一定電圧の影響
- Biological Effects of Furosemide in Relation to Its Disposition in Rabbits
- Microdialysis 法による血液網膜関門を介した薬物排出輸送能の解析
- 血液網膜関門GLUT1を介したvitamin C網膜供給機構 (第25回生体膜と薬物の相互作用シンポジウム--ダイナミックインターフェイスとしての生体膜 講演要旨集)
- フェニトインのファルマコキネティックスに及ぼす柴胡桂枝湯の影響
- 新鎮痛剤1,4-Dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine Hydrobromide(ST-2121)の生体内運命(第2報)光学異性体間におけるラット尿中代謝物の比較
- Applecation of a Non-linear Dispersion Model to Analysis of the Renal Handling of p-Aminohippurate in Isolated Perfused Rat Kidney
- Effect of Dosage Form on Stereoisomeric Inversion of Ibuprofen in Volunteers
- A KINETIC STUDY ON CHLORPROMAZINE DISPOSITION AND HYPOTHERMIC RESPONSE IN RATS
- PHARMACOKINETIC EVIDENCE FOR BLOOD FLOW DEPRESSION IN DOSE DEPENDENT DISPOSITION OF 4-AMINOANTIPYRINE IN RABBITS
- A NOTE ON SATURABLE AND INHIBITORY KINETICS OF p-AMINOHIPPURATE RENAL TRANSPORT IN RABBITS
- A PHARMCOKINETIC MODEL FOR ENTEROHEPATIC CIRCULATION OF AN ANALGESIC l-1,4-DIMETHYL-10-HYDROXY-2,3,4,5,6,7-HEXAHYDRO-1,6-METHANO-1H-4-BENZAZONINE HYDROBROMIDE (l-ST-2121) IN RATS
- PHARMACOKINETIC ANALYSIS OF PHARMACOLOGICAL EFFECTS AND DRUG DISPOSITION. HYPOGLYCEMIC EFFECT OF TOLBUTAMIDE IN RABBITS
- 新鎮痛剤l-1,4-Dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine Hydrobromide(l-ST-2121)の生体内運命(第3報)マウス, ラット, ウサギ, イヌ, サルおよびヒトにおける吸収, 排泄および代謝について
- 新鎮痛剤l-1,4-Dimethyl-10-hydroxy-2,3,4,5,6,7-hexahydro-1,6-methano-1H-4-benzazonine Hydrobromide(l-ST-2121)の生体内運命(第1報)ラット皮下投与における吸収, 分布, および排泄について
- An Interpretation of the Hill Equation : Time Course of Diuretic Response after Furosemide Administration in Man
- A STUDY ON FUROSEMIDE DISPOSITION IN MAN
- Study on Baths with Crude Drug. III. The Effect of Ligustici Chuanxiong Rhizoma Extract on the Percutaneous Absorption of Some Natural Compounds
- Difference of train-of-four fade induced by nondepolarizing neuromuscular blocking drugs: a theoretical consideration on the underlying mechanisms
- KINETICS OF p-AMINOHIPPURATE RENAL EXCRETION IN RABBITS
- THE DIURETIC EFFECT OF FUROSEMIDE IN RELATION TO ITS DISPOSITION IN MAN
- 健やかに生きるために : 富山医科薬科大学公開講座(公開講座-地域社会への貢献-)
- Doctor=教師(「薬学博士の学位-授与規定を考える」)