Evaluation of percutaneous absorption performance for XXXX female sexual steroids into pentravan cream.

@entity1 @entity1420 @entity11111 @entity53 @entity1445
There is a lack of studies on Pentravan cream, a widespread transdermal vehicle which is used by compounding pharmacies. The purpose of this study was to evaluate this transdermal vehicle. The permeation performance for @entity1420 , @entity53 , and @entity11111 in formulations containing each of those drugs separately, as well as an association of @entity53 + @entity11111 (Biest), was evaluated regarding their compounding process and their potential biological application. An excised female @entity1 skin model was used to predict the permeation and the retention of the active compounds in every skin layer in lieu of conventional tape stripping. @entity1420 was the drug with the highest permeation (37.02 mcg cm(-2) at the end of the experiment). @entity53 and @entity11111 in Biest had permeations approximately 4-fold lower (9.44 mcg cm(-2) for @entity53 -Biest and 14.02 mcg cm(-2) for @entity11111 -Biest), and the profiles of @entity53 in Eemuls and in Biest were almost the same (9.46 mcg cm(-2) for Eemuls). All permeations followed pseudo- first order kinetics. For @entity1420 , using the percentage of permeation by dose, one can infer that a @entity1 using the 1-g emulsion dose released by the pump containing 50 mg of @entity1420 will have 38.4 mg of @entity1420 liberated into his bloodstream, gradually and continuously for 48 hours. The results indicate that the vehicle was able to provide percutaneous absorption rates compatible with and higher than clinical treatment needs. Using the same rationale, the Eemuls would deliver practically the entire amount of @entity53 load per dose (1.0 mg), approximately 0.5 mg of @entity53 per day. As for the Biest, the dosing used would deliver almost 0.5 mg @entity53 /day and 2.0 mg @entity11111 / day. Thus, according to the results, @entity1 female sexual hormones incorporated in the oil-in-water vanishing cream base and applied topically are expected to exert their biological activities systemically with good efficacy due to their satisfactory permeation through @entity1 skin. However, one must take into account that a high quantity of drug was delivered. Thus, to avoid @entity1 @entity1445 , care has to be taken regarding the quantity of emulsion used.
