Abstract:
:The major route of degradation of tetrazepam (1) is oxidation to 7-chloro-5-(3-keto-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (3) via the stable 7-chloro-5-(3-hydroperoxy-cyclohexen-1-yl)-1,3-dihydro-1-methyl-2H -1, 4 benzodiazepin-2-one (2). Minor degradation products are 7-chloro-5-(1,2-epoxycyclohexan-1-yl)-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2-one (5) and 7-chloro-1,3-dihydro-1-methyl-2H-1, 4-benzodiazepin-2,5-dione (4), resulting from cleavage of the C-C bond between the cyclohexene ring and the benzodiazepine ring. After 48 h, AIBN (2,2'-azobis[2-methyl-propanenitrile]) in acetonitrile at 40 degrees C produced qualitatively the same impurities as those observed in the stability study of tablets of 1. Other stress tests (thermal stress at 80 degrees C, heavy metal oxidation, hydrogen peroxide, acid-catalyzed oxidation) caused qualitatively different profiles of degradation.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Boccardi G,Deleuze C,Gachon M,Palmisano G,Vergnaud JPdoi
10.1002/jps.2600810216subject
Has Abstractpub_date
1992-02-01 00:00:00pages
183-5issue
2eissn
0022-3549issn
1520-6017pii
S0022-3549(15)48746-5journal_volume
81pub_type
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