Reference

Transdermal delivery of anxiolytics: in vitro skin permeation of midazolam maleate and diazepam

Transdermal delivery of anxiolytics: in vitro skin permeation of midazolam maleate and diazepam. Touitou, Elka (Sch. Pharm., Hebrew Univ., Jerusalem, Israel). Int. J. Pharm., 33(1-3), 37-43 (English) 1986. CODEN: IJPHDE. ISSN: 0378-5173. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The skin permeation of midazolam maleate (I) [59467-94-6] and diazepam (II) [439-14-5] from various solvent systems were investigated. Results were computed using a program designed to manipulate skin permeation data. The permeation rates of I and II may be affected by using aq. mixts. of polar org. solvents. Azone [59227-89-3] (1 and 5%) increased the permeation fluxes of both drugs. In the presence of 5% Azone in a solvent system of propylene glycol [57-55-6]- EtOH [64-17-5]-H2O, the fluxes were increased <43-fold for II and 86-fold for I. The performance of a novel hydrophilic transdermal matrix contg. 50 mg I was tested in vitro. 64-17-5 and 57-55-6 are just another two chemicals used in this study. The steady-state flux obtained was used for a coarse estn. of the feasibility of transdermal administration of I. .

Enhancement of naloxone penetration through human skin in vitro using fatty acids, fatty alcohols, surfactants, sulfoxides and amides

Enhancement of naloxone penetration through human skin in vitro using fatty acids, fatty alcohols, surfactants, sulfoxides and amides.Some chemicals with cas registry numbers like 57-13-6 and 506-44-5 are also used. Aungst, Bruce J.; Rogers, Nancy J.; Shefter, Eli (Biomed. Prod. Dep., E. I. du Pont de Nemours and Co., Wilmington, DE 19898, USA). Int. J. Pharm., 33(1-3), 225-34 (English) 1986. CODEN: IJPHDE. ISSN: 0378-5173. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Human skin permeation of naloxone (I) [465-65-6] was studied in vitro using various vehicles and penetration enhancers. To screen various chem. as penetration enhancers propylene glycol [57-55-6] contg. 10% adjuvant was used. Fatty acids and fatty alcs. were very effective promoters of I flux. In both the acid and alc. series, max. flux was with C12 adjuvants, and for C18 acids and alcs. unsatd. adjuvants were more effective than satd. ones. Other effective skin penetration enhancers included some nonionic and cationic surfactants, decyl methyl sulfoxide [3079-28-5], Azone [59227-89-3], and N-alkylpyrrolidones. Lauric acid [143-07-7] and lauryl alc. [112-53-8] in iso-PrOH [67-63-0], polyethylene glycol 400 [25322-68-3], and mineral oil vehicles were not as effective in promoting I skin penetration as when dissolved in propylene glycol. Na lauryl sulfate [151-21-3] in propylene glycol slightly increased flux, but a much greater effect was obsd. using a mineral oil vehicle. Concn./enhancement profiles were detd. for lauric acid and lauryl alc. Skin penetration enhancing effects are, to some extent, specific and dependent on the drug, vehicle, enhancer concn. and probably other factors. Possible mechanisms of altering skin permeability are discussed. .