Detail of "2898-12-6"

Reference

Interactions between macromolecular excipients and drugs

Interactions between macromolecular excipients and drugs. Part 25: The effect of cellulose ethers on dissolution characteristics of benzodiazepines. Keipert, S.; Alde, D. (Sekt. Chem., Humboldt-Univ., Berlin, Ger. Dem. Rep.). Pharmazie, 41(12), 845-9 (German) 1986. CODEN: PHARAT. ISSN: 0031-7144.There are some reagents with their cas registry numbers 12794-10-4 and 58-25-3 are used in this study. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The effect of Me cellulose [9004-67-5], and hydroxyethyl cellulose [9004-62-0] on the dissoln. behavior of chlordiazepoxide [58-25-3], medazepam [2898-12-6], nitrazepam [146-22-5], diazepam [439-14-5], and clonazepam [1622-61-3] was studied. Phys. mixts., evaps., lyophilizates and microcapsules improved the dissoln. of the drugs. No relation between satn. soly. and dissoln. was obsd. An increase in soly. was obsd. with the only nitrazepam and clonazepam when a Me cellulose-triturate was used. The interaction of diazepam, clonazepam and medazepam with the cellulose was concn. and temp. dependent. No interactions were detected with chlordiazepoxide. It is assumed that a high distribution of drug particles in the dissoln. medium by treatment with cellulose ether was the reason for an increase in the dissoln. rate. .

Effects of drug bindings on the esterase-like activity of human serum albumin

Effects of drug bindings on the esterase-like activity of human serum albumin. VII. Subdivision of R-type drugs inhibiting the activity towards p-nitrophenyl acetate. Kurono, Yukihisa; Ozeki, Yoshiro; Yamada, Hideto; Takeuchi, Toshimasa; Ikeda, Ken (Fac. Pharm. Sci., Nagoya City Univ., Nagoya 467, Japan). Chem. Pharm. Bull., 35(2), 734-9 (English) 1987. CODEN: CPBTAL. ISSN: 0009-2363. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The subdivision of R-type drugs, which inhibit the reaction of p-nitrophenyl acetate [830-03-5] with an active site (R site) located near the tyrosine-411 residue of human serum albumin (HSA), is proposed based on the results of kinetic and fluorometric studies. Two kinds of R-type drugs were found with regard to the influence on the reaction rate of 3,5-dinitroaspirin (DA) [19073-90-6] at a site (U site) near the lysine-199 and tryptophan-214 (Trp-214) residues of HSA. One of them (R2-type drug, e.g., diazepam [439-14-5] or medazepam [2898-12-6]) greatly accelerates the reaction of DA with HSA, and the other (R1-type drug, e.g., octanoic acid [124-07-2]) does not affect the reaction. 830-03-5 and 58-25-3 which are cas registry numbers of substances are two of reagents here. The R2-type drug quenches the fluorescence originating from the Trp-214 residue in the U site of HSA, and the R1-type drug hardly influences this fluorescence. The acceleration of the reaction was considered to be due to the conformational change of the U site caused by binding of the R2-type drug to a part of the R site on HSA. Five benzodiazepines, 3 sulfonylureas, and 3 other drugs were classified into R1-type and R2-type drugs. .