Comparison of thymoxamine permeation between hairless rat and horse penile mucous membrane using an in vitro diffusion model.
Moxisylyte (or thymoxamine) administered intracavernously is known to improve erection in organically impotent patients. Prior to drug administration by percutaneous route, we have to define its in vitro permeation parameters after application of thymoxamine on both rat skin and horse penile mucous membrane. 24 h after drug application, the percentages of thymoxamine which diffused through the penile mucous and the rat skin were 88 and 75%, respectively. Thymoxamine flux varied according to the biological membrane tested. With regard to the penile mucous membrane, a maximal flux (1,774 nmol.h-1.cm-2) was observed 2.5 h after drug application, whereas for the rat skin a maximal flux (657 nmol.h-1.cm-2) was noted at 3.5 h. Thymoxamine flux decreased rapidly in the penile mucous membrane. This decrease was slower when thymoxamine penetrated the rat skin; the difference could be due to a different morphology of the tested biological membranes. In contrast to the rat skin, the external keratinized layer was absent in the penile mucous membrane. In conclusion, the ability of thymoxamine to penetrate easily and rapidly the biological membrane, and particularly the penile mucous membrane, suggests that thymoxamine could reach the pharmacological target represented by the corpus cavernosum of the penis.
Neau
B
B
Sarget Laboratories, Mérignac, France.
Lozano
P
P
Gomond
P
P
Roux
J
J
Grislain
L
L
Lambrey
B
B
D000818:Animals; D004058:Diffusion; D005260:Female; D006736:Horses; D066298:In Vitro Techniques; D008297:Male; D013948:Moxisylyte / Q000493:pharmacokinetics*; D009092:Mucous Membrane / Q000166:cytology / Q000378:metabolism; D010413:Penis / Q000166:cytology / Q000378:metabolism*; D051381:Rats; D012867:Skin / Q000166:cytology; D012869:Skin Absorption / Q000502:physiology*
D013948:Moxisylyte