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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Ichihashi T, Kinoshita H, Yamada H

Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.

Xenobiotica. 1991 Jul;21(7):873-80. doi: 10.3109/00498259109039527.

Absorption of mepitiostane (MP) from the gastrointestinal tract was examined using thoracic duct-cannulated rats. 2. When 14C-MP was administered into the small intestine, 34% of the radioactivity was recovered in the 6-h thoracic duct lymph. More than 90% of this radioactivity was due to unchanged MP and most of the MP in the lymph was carried in the lipid core of the chylomicrons and VLDL. 3. Radioactivity in the portal blood was extensively extracted by the liver and excreted into bile as polar metabolites. Thus, most unchanged MP which entered the systemic circulation following oral administration was drug absorbed via the intestinal lymphatics. 4. MP avoids the first-pass effect by lymphatic adsorption.

使用胸导管插管大鼠研究了美替奥斯坦（MP）从胃肠道的吸收情况。2. 当将14C-MP注入小肠时，在6小时的胸导管淋巴液中回收了34%的放射性。该放射性的90%以上归因于未变化的MP，并且淋巴液中的大多数MP存在于乳糜微粒和极低密度脂蛋白的脂质核心中。3. 门静脉血中的放射性被肝脏大量摄取并作为极性代谢产物排泄到胆汁中。因此，口服给药后进入体循环的大多数未变化的MP是通过肠淋巴管吸收的药物。4. MP通过淋巴吸附避免首过效应。

Ichihashi T, Kinoshita H, Yamada H

Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.

Xenobiotica. 1991 Jul;21(7):873-80. doi: 10.3109/00498259109039527.

Absorption of mepitiostane (MP) from the gastrointestinal tract was examined using thoracic duct-cannulated rats. 2. When 14C-MP was administered into the small intestine, 34% of the radioactivity was recovered in the 6-h thoracic duct lymph. More than 90% of this radioactivity was due to unchanged MP and most of the MP in the lymph was carried in the lipid core of the chylomicrons and VLDL. 3. Radioactivity in the portal blood was extensively extracted by the liver and excreted into bile as polar metabolites. Thus, most unchanged MP which entered the systemic circulation following oral administration was drug absorbed via the intestinal lymphatics. 4. MP avoids the first-pass effect by lymphatic adsorption.

使用胸导管插管大鼠研究了美替奥斯坦（MP）从胃肠道的吸收情况。2. 当将14C-MP注入小肠时，在6小时的胸导管淋巴液中回收了34%的放射性。该放射性的90%以上归因于未变化的MP，并且淋巴液中的大多数MP存在于乳糜微粒和极低密度脂蛋白的脂质核心中。3. 门静脉血中的放射性被肝脏大量摄取并作为极性代谢产物排泄到胆汁中。因此，口服给药后进入体循环的大多数未变化的MP是通过肠淋巴管吸收的药物。4. MP通过淋巴吸附避免首过效应。