Hey Leute!

Kennt Jemand eine zuverlässige Bezugsquelle für RU-Myristate?

Grüße

Hey Leute!

Kennt Jemand eine zuverlässige Bezugsquelle für RU-Myristate?

Grüße

K&B verzögert den release von RU in die Haut und verhindert, dass sich zu große Ansammlungen bilden, die - weil sie keinen Rezeptor besetzen können - ins Blut gehen.

Zitat aus dem Patent:

"[0082]The compositions according to the invention are primarily distinguished by a uniform release, proceeding over a certain period of time, of the compound of the formula I from the elastic film which forms after application of the composition and adheres firmly to the skin. This ensures that therapeutically active antiandrogen concentrations are achieved at the target organ--the hair root-over a relatively long period of time, without high blood level concentrations occurring in the short term, which of course lead to a systemic stress on the patient.
"

Was soll sich denn mit der komischen K&B-solution ändern? Diese besteht ja zum grössten teil auch nur aus Wasser und Alkohol.

"
[0105]100 μL of the test composition (control example) are applied to a defined area of the upper side of the human skin, covered with hair and without hair cover, lying on the measurement crystal. The permeation of the active compound can be observed with the aid of the IR band at 1323 cm-1 characteristic of 4-[3-(4-hydroxybutyl)-4,4-dimethyl-2,5-dioxo-1-imidazolidinyl]-2-(trifluo- romethyl)benzonitrile.

[0106]It was found here that about 90% of the amount of active compound applied permeates within 24 hours both through the skin covered with hair and through the skin without hair cover.

[0107]However, there were differences in the rate of permeation between the two pieces of skin. While the amount of active compound which has permeated already asymptotically approaches the end value after about 7 hours when skin covered with hair is used, the substance permeates virtually uniformly through skin without hair cover over 24 hours.

[0108]After application of a composition according to the invention, for example according to Example 1, to skin containing hair follicles--such as exists with and alopecia--a uniform permeation of the active compound over 24 hours, as after application of the control composition to skin without hair cover, was likewise achieved.
"

Das bedeutet, dass der release Allgemein verzögert wird. Das Kriterium 'mit Haar' unterscheidet sich demnach bei K&B und einem Kontrollvehikel.
Ich gebe allerdings zu, dass keine Aussage zum systemischen Load getroffen wird. Für die heißt es einfach: keine cluster, also geht weniger ins Blut - was aber nicht bewiesen wird.

Gibt es denn kein sicheres Vehikel für RU?