参考文献：M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. 美国食品药品监督管理局批准的药物标签用于研究药物诱导的肝损伤，《药物发现今日》，16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank：按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
References:M Chen, V Vijay, Q Shi, Z Liu, H Fang, W Tong. FDA-Approved Drug Labeling for the Study of Drug-Induced Liver Injury, Drug Discovery Today, 16(15-16):697-703, 2011. PMID:21624500 DOI:10.1016/j.drudis.2011.05.007
M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. Drug Discov Today 2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
◉ Summary of Use during Lactation:No information is available on the use of methylnaltrexone during breastfeeding. The manufacturer recommends against breastfeeding in mothers taking methylnaltrexone. Based on pharmacokinetic data, the oral absorption of methylnaltrexone appears to be very low. Observe breastfed infants who have been exposed to opioids during pregnancy or postpartum for signs of opioid withdrawal, especially diarrhea.
◉ Effects in Breastfed Infants:Relevant published information was not found as of the revision date.
◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
Process for the preparation of N-methylnaltrexone bromide, wherein a compound of the general formula (I):
wherein
X
−
represents an anion other than the bromide anion, and R represents hydrogen or a leaving group, is dissolved or dispersed in a suitable polar solvent, the solution or dispersion is mixed with a compound containing bromide anions, and the resulting reaction mixture is stirred until N-methylnaltrexone bromide has formed and crystallised, wherein, in the case where R represents a leaving group, that group is removed during or after the reaction.
Process for the Production of Seven-Membered Lactam Morphinans
申请人：Mallinckrodt LLC
公开号：US20130144053A1
公开（公告）日：2013-06-06
The present invention relates to improved processes for preparing lactam morphinans. The processes generally transform keto-morphinans to seven-membered lactam morphinans using a hydroxyamine sulfonic acid reagent and proceed in high yield and with good selectivity.
Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts
申请人：Wang Peter X.
公开号：US20100035910A1
公开（公告）日：2010-02-11
An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
将三级吗啡类生物碱进行N-烷基化，形成相应的季铵盐型吗啡类生物碱衍生物的改进过程。
[EN] LIQUID ORAL DOSAGE FORMULATIONS OF METHYLNALTREXONE<br/>[FR] FORMULATIONS POSOLOGIQUES ORALES LIQUIDES DE MÉTHYLNALTREXONE
申请人：BAUSCH HEALTH IRELAND LTD
公开号：WO2020225395A1
公开（公告）日：2020-11-12
Provided herein are pharmaceutical compositions comprising methylnaltrexone, lauryl sulfate or docusate, and at least one of an oil, a surfactant or a cosolvent, wherein the methylnaltrexone and lauryl sulfate or docusate are present as an ion pair. The pharmaceutical compositions may further comprise a surfactant so as to provide self-emulsifying methylnaltrexone delivery systems.
