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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

Grislain L, Mocquard M T, Dabe J F, Bertrand M, Luijten W, Marchand B, Resplandy G, Devissaguet M

Bio-Pharmacie Servier, Orleans, France.

Xenobiotica. 1990 Aug;20(8):787-800. doi: 10.3109/00498259009046893.

The metabolism of perindopril (non-thiol angiotensin-converting enzyme inhibitor) was studied in rat, dog and monkey after single oral and i.v. administration of 14C-perindopril, and in man after a single oral dose. 2. Six biotransformation products of perindopril from urine, faecal and plasma samples (bile only for rats) were identified. 3. The main route of biotransformation in all species is the hydrolysis of the carboxylic ethyl ester side-chain, with the formation of perindoprilate, the active metabolite. 4. A minor route of biotransformation led to the acyl glucuronides of perindopril and perindoprilate. 5. Internal dehydration of perindopril and perindoprilate into cyclic lactam structures occurs. This route of metabolism is of minor importance except in humans.

在大鼠、犬和猴单次口服及静脉注射14C-培哚普利后，对其代谢情况进行了研究，同时也对人类单次口服剂量后的情况进行了研究。2. 从尿液、粪便和血浆样本（仅大鼠有胆汁样本）中鉴定出了培哚普利的六种生物转化产物。3. 在所有物种中，生物转化的主要途径是羧酸乙酯侧链的水解，形成活性代谢产物培哚普利拉。4. 生物转化的次要途径导致培哚普利和培哚普利拉的酰基葡萄糖醛酸苷形成。5. 培哚普利和培哚普利拉会发生内部脱水形成环状内酰胺结构。除了在人类中，这条代谢途径的重要性较低。

Grislain L, Mocquard M T, Dabe J F, Bertrand M, Luijten W, Marchand B, Resplandy G, Devissaguet M

Bio-Pharmacie Servier, Orleans, France.

Xenobiotica. 1990 Aug;20(8):787-800. doi: 10.3109/00498259009046893.

The metabolism of perindopril (non-thiol angiotensin-converting enzyme inhibitor) was studied in rat, dog and monkey after single oral and i.v. administration of 14C-perindopril, and in man after a single oral dose. 2. Six biotransformation products of perindopril from urine, faecal and plasma samples (bile only for rats) were identified. 3. The main route of biotransformation in all species is the hydrolysis of the carboxylic ethyl ester side-chain, with the formation of perindoprilate, the active metabolite. 4. A minor route of biotransformation led to the acyl glucuronides of perindopril and perindoprilate. 5. Internal dehydration of perindopril and perindoprilate into cyclic lactam structures occurs. This route of metabolism is of minor importance except in humans.

在大鼠、犬和猴单次口服及静脉注射14C-培哚普利后，对其代谢情况进行了研究，同时也对人类单次口服剂量后的情况进行了研究。2. 从尿液、粪便和血浆样本（仅大鼠有胆汁样本）中鉴定出了培哚普利的六种生物转化产物。3. 在所有物种中，生物转化的主要途径是羧酸乙酯侧链的水解，形成活性代谢产物培哚普利拉。4. 生物转化的次要途径导致培哚普利和培哚普利拉的酰基葡萄糖醛酸苷形成。5. 培哚普利和培哚普利拉会发生内部脱水形成环状内酰胺结构。除了在人类中，这条代谢途径的重要性较低。