Lymphatic Absorption of Hypolipidemic Compound, 1-O-[p-(Myristyloxy)-α-Methylcinnamoyl] Glycerol (LK-903)

スポンサーリンク

概要

• 論文の詳細を見る

• The intestinal absorption process of 1-O-[p-(myristyloxy)-α-methylcinnamoyl] glycerol (LK-903), a new hypolipidemic compound, was studied in rats. When ^3H-LK-903 or ^3H-LKA [^3H-p-(myristyloxy)-α-methyl cinnamic acid], labeled at the cinnamic acid moiety, or ^<14>C-LK-903,labeled at the glycerol moiety, were administered orally to thoracic duct-cannulated rats at a dose of 0.233 mmol/kg, 31.1,6.7 and 18.1% of the dose, respectively, appeared in the lymph within 24 h. In this case, radioactive compounds in the lymph lipids consisted of LKA (radioactivity was not detected in the fraction of LKA with ^<14>C-LK-903), LK-903,diglyceride analogues and triglyceride analogues. The percentages of the triglyceride analogues were the highest, followed by the diglyceride analogues. On the other hand, when doubly labeled LK-903 (^3H/^<14>C=1,corrected ratio) was administered orally, the values of ^3H/^<14>C for the monoglyceride, diglyceride and triglyceride analogues in the lymph were 1.2-1.5,1.7-1.9 and 1.9-2.7,respectively. The lymphatic absorption of LK-903 was stimulated by the presence of lecithin but inhibited by a high dose of triolein. The results indicated that (1) LK-903 formed micelles in the intestine, (2) a large part of LK-903 was absorbed as such, (3) a part of LK-903 was hydrolyzed in the intestinal mucosa, and (4) a part of LKA formed by hydrolysis was again utilized to synthesize the higher glycerides and absorbed via the lymphatic absorption route for lipids.

• 公益社団法人日本薬学会の論文

著者

• SUGIHARA Juko

  Pharmaceutical Development Research Laboratory, Tanabe Seiyaku Co., Ltd.,

• Furuuchi S

  Biological Research Laboratory Tanabe Seiyaku Co. Ltd.

• SUGIHARA Juko

  Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.

• FURUUCHI Satoshi

  Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.

関連論文

• Distribution of Thyrotropin-Releasing Hormone (TRH) Receptors in the Brain of the Ataxic Mutant Mouse, Rolling Mouse Nagoya
• Chronic Anti-ataxic Actions of the Novel Thyrotropin-Releasing Hormone (TRH) Analog, TA-0910,during and after Repeated Administration in Rolling Mouse Nagoya : Behavioral and Pharmacokinetic Studies
• Accumulation of Radioactivity in Rat Brain and Peripheral Tissues Including Salivary Gland after Intravenous Administration of 14C-D-aspartic Acid
• Studies on Intestinal Lymphatic Absorption of Drugs. II. Glyceride Prodrugs for Improving Lymphatic Absorption of Naproxen and Nicotinic Acid
• Studies on Intestinal Lymphatic Absorption of Drugs. I. Lymphatic Absorption of Alkyl Ester Derivatives and α-Monoglyceride Derivatives of Drugs
• STUDIES ON THE METABOLISM OF DILTIAZEM IN MAN
• Lymphatic Absorption of Hypolipidemic Compound, 1-O-[p-(Myristyloxy)-α-Methylcinnamoyl] Glycerol (LK-903)

スポンサーリンク