Reference

Evaluation of a new antinauseant drug for the prevention of motion sickness

Evaluation of a new antinauseant drug for the prevention of motion sickness. Graybiel, Ashton; Knepton, James (Nav. Aerosp. Med. Res. Lab., Nav. Air Stn., Pensacola, Fla., USA). Aviat., Space Environ. Med., 48(9), 867-71 (English) 1977. CODEN: ASEMCG. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The antimotion sickness efficacy of AHR 5645B (I) [63307-61-9], administered orally in 20, 50, and 100 mg doses, was compared with that of l-scopolamine 0.3 mg and of a placebo in volunteers. Promethazine-HCl [58-33-3] 12.5 mg and ephedrine sulfate [134-72-5] 12.5 mg alone and combined, and meclizine [569-65-3] 50 mg plus ephedrine 25 mg. were also evaluated. Each subject was tested individually in a slow rotation room where the stressful stimuli were generated by requiring the subject to execute standardized head movements at 1-r.p.m. increments until either the motion-sickness endpoint or the ceiling on the test (30 r.p.m.) was reached. The effects of scopolamine were beneficial in 50% of the subjects. All of the responses to I were inconsequential except for 1 beneficial effect (100 mg) and 2 detrimental responses, 1 each with doses of 20 and 50 mg. Among the other drugs tested, only 1 of the responses was detrimental. Beneficial responses were 62.5% for promethazine 12.5 mg plus ephedrine 12.5 mg, 50% for promethazine 12.5 mg, 37.5% for ephedrine 12.5 mg, and 25% for meclizine 50 mg plus ephedrine 25 mg.

In vitro release of meclozine hydrochloride from lipophilic suppository bases with or without surfactants

In vitro release of meclozine hydrochloride from lipophilic suppository bases with or without surfactants. Becirevic, Mira; Petricic, Vanda; Kallay, Nikola (Fac. Pharm. Biochem., Univ. Zagreb, Zagreb YU-41000, Yugoslavia). Pharmazie, 39(12), 828-30 (English) 1984. CODEN: PHARAT. ISSN: 0031-7144. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Meclozine (I) [569-65-3] suppositories were prepd. with lipophilic bases, and the release rate of the drug from molten suppositories was investigated in vitro. Among various suppository bases, the highest rate was obtained when Witepsol H15 [12699-05-7] was used. The release rates were affected if nonionic surfactants, Tween 20 [9005-64-5] and Tween 80 [9005-65-6] were incorporated. In comparison to the surfactant-free suppositories, the rates obtained with suppositories contg. 5, 20 and 30% surfactants were higher, approx. the same, and lower, resp. The results were interpreted in terms of the micellar solubilization of the drug with nonionic tensides.