新規非ステロイド性抗炎症剤2-[3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-1-yl]ethyl Acetateの消化管吸収の改善
スポンサーリンク
概要
- 論文の詳細を見る
The effects of triglycerides on the gastrointestinal absorption of 2-[3-(3,5-di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo [3,4-b] pyridin-1-yl] ethyl acetate (1) were investigated in dogs. The enhancing abilities of the triglycerides on the absorption of 1 were demonstrated as in the order of trilinolein>triolein>tristearin>tripalmitin. Among the series of fatty acids and monoglycerides, namely, digestive products of triglycerides by pancreatic lipase, linoleic acid and monolinolein showed the most potent solubilizing activities of 1 in a solution of bile salt. The incorporation of 1 into mixed micelle formed by lipids and bile salts was presumed to play an important role in the accelerated absorption of 1 after ingestion of triglycerides. On the basis of these findings, an emulsion containing 1 was prepared with soybean oil. The emulsion exhibited a remarkable improvement of the absorption of 1 compared to a suspension of the drug in methylcellulose solution.
- 社団法人日本薬学会の論文
- 1991-08-25
著者
-
小川 建志
Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.
-
水田 博彰
吉富製薬株式会社中央研究所
-
小川 建志
吉富製薬株式会社中央研究所
-
水田 博彰
Research Laboratories Yoshitomi Pharmaceutical Industries Ltd.
-
鮫元 博文
吉富製薬株式会社中央研究所
-
鮫元 博文
Pharmaceutical Development Analytical & Pharmaceutical Research Laboratories Yoshitomi Pharmaceu
関連論文
- Nitrofurantionの消化管吸収 : イヌにおける消化管通過時間の新規な測定法の有用性評価
- Effect of Small Intestinal Transit Time on Gastrointestinal Absorption of 2-[3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-1-yl]ethyl Acetate, a New Non-steroidal Anti-inflammatory Agent
- Gastrointestinal Absorption of Chlorothiazide : Evaluation of a Method Using Salicylazosulfapyridine and Acetaminophen as the Marker Compounds for Determination of the Gastrointestinal Transit Time in the Dog
- 新規非ステロイド性抗炎症剤2-[3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-1-yl]ethyl Acetateの消化管吸収における胆汁の寄与及び食餌の影響
- Effects of Meals on Gastric Emptying and Small Intestinal Transit Times of a Suspension in the Beagle Dog Assessed Using Acetaminophen and Salicylazosulfapyridine as Markers
- Salicylazosulfapyridine法によるビーグル犬の小腸通過時間の測定
- 高速液体クロマトグラフィーによるシステインアルキルエステルの定量
- Utility of Gastrointestinal Physiology Regulated-Dogs : Bioavailability Study of a Commercial sustained-Release Dosage Form of Theophylline
- Gastrointestinal Physiology-Regulated Dogs : Utilization of a Bioavailability Study of a New Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]-diazepine, an Antagonist of Platelet-Activating Factor, and Its Preparations
- Biovavailability Study of Commercial Sustained-Release Preparations of Diclofenac Sodium in Gastrointestinal Physiology Regulated-Dogs
- 新規非ステロイド性抗炎症剤2-[3-(3,5-Di-tert-butyl-4-hydroxyphenyl)-1H-pyrazolo[3,4-b]pyridin-1-yl]ethyl Acetateの消化管吸収の改善
- Comparative Pharmacokinetics of Sulpiride and N-[(1-Butyl-2-pyrrolidinyl)methyl]-2-methyl-5-sulfamoyl-2,3-dihydrobenzofuran-7-carboxamide Hydrochloride, a New Lipophilic Substituted Benzamide in Rats
- Effect of Gastric Acidity on Bioavailability of N, N-Dimethylcarbamoylmethyl α, 2-Dimethyl-5H-[1]benzopyrano[2,3-b]pyridine-7-acetate, a New Prodrug-Type Anti-inflammatory Agent
- Gastric pH Profile and Its Control in Fasting Beagle Dogs
- (RS)-7-(2-Aminomethylmorpholino)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic Acidの結晶水の挙動
- N, N-Dimethylcarbamoylmethyl α, 2-Dimethyl-5H-[1]benzopyrano[2,3-b]pyridine-7-acetateと各種添加剤との混合粉砕物の溶出特性とバイオアベイラビリティー
- Powder Coating Mixture of a Novel Anxiolytic, Y-23684 : Dissolution Characteristics and Bioavailability
- Gastric Acidity-Dependent Bioavailability of Commercial Sustained Release Preparations of Indomethacin, Evaluated by Gastric Acidity-Controlled Beagle Dogs
- 胃酸度調整ビーグル犬を用いたシンナリジンのバイオアベイラビリティーの評価
- Pharmacokinetics and neuroendocrinological studies of bromperidol in schizophrenic patients.