Reference

2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepin-containing solutions for oral or parenteral administration

2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepin-containing solutions for oral or parenteral administration. Haeger, Bruce Edwin; Krueger, James Elwood; Lowery, James Alfred; Ritter, Lawrence (American Cyanamid Co., USA). Ger. Offen. DE 2633943 17 Feb 1977, 15 pp. (German). (Germany). CODEN: GWXXBX. CLASS: IC: A61K031-55. PRIORITY: US 75-602331 6 Aug 1975. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Stable aq. solns. of 2-chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine (I) [1977-10-2] or 1 of its salts suitable for oral or parenteral administration are prepd. by mixing I first with propylene glycol [57-55-6], adjusting the pH to 5.0-7.0 with dil. mineral acid, and then adding H2O. For example, 63.0 g I was mixed with 2100 mL propylene glycol, and 800 mL H2O was added to the mixt. The pH was adjusted to 6.2 by addn. of 10% HCl, and the mixt. was heated for 30 min at 60.degree., dild. with H2O to 3000 mL, and sterilized by filtration. The final soln. contained 2.0% I, and was placed in 2.0 ml ampuls. A conc. for oral administration comprised 2.5% I in 70% aq. propylene glycol, and was added to fruit juice in amts. of 3.5 ml/100 g juice before administration. Solns. of 10 mg I/ml in 50%, 60% and 70% aq. propylene glycol showed good stability, contg. only 120, 110, and 100 .mu.g/mL, resp., of the I hydrolysis product, 2-chloro-dibenz[b,f][1,4]oxazepin-11(10H)-one [3158-91-6], and retaining >98% of the initial I neuroleptic activity after 15 months. Encapsulated suspensions of I succinate [27833-64-3] and parenteral solns. of I as the free base showed comparable neuroleptic activity.