Patent Application
20070286890
The advantages and features of the present invention will be better understood by the following description when considered in conjunction with the accompanying drawings, in which:
With reference to the
As part of the present invention, the formulation 28, disposed in the container 14, is a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I:
wherein dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxa radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is —N(R4)2 wherein R4 is selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms,
wherein R5 is a lower alkyl radical having from one to six carbon atoms; Z is ═O; one of R1 and R2 is ═O, —OH or a —O(CO)6 group, and the other one is —OH or —O(CO)6, or R1 is ═O and R2 is H, wherein R6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or —(CH2)mR7 wherein m is 0 or an integer of from 1 to 10, and R7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above or a pharmacologically acceptable acid addition salt thereof. A pharmaceutical carrier adapter for topical application to mammalian skin may be provided.
Preferably, the compound is a cyclopentane heptanoic acid, 2-(phenyl alkyl or phenyloxyalkyl) presented by the formula II:
Wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, Y is a radical selected from the group consisting of alkyl, halo, e.g. fluoro, chloro, etc., nitro, amino, thiol, hydroxy, alkyloxy, alkylcarboxy, halo substituted alkyl wherein said alkyl radical comprises from one to six carbon atoms, etc. and n is 0 or an integer of from 1 to 3 and R3 is ═O, —OH or —O(CO)R6 wherein R6 is as defined above or a pharmaceutically acceptable salt thereof.
More Preferably the compound is a compound of formula III:
wherein y is 0 or 1, x is 0 or 1 and x and y are not both 1, Y is a radical selected from the group consisting of alkyl, halo, nitro, amino, thiol, hydroxy, alkyloxy, alkylcarboxy, halo substituted alkyl wherein said alkyl radical comprises from one to six carbon atoms, n is 0 or an integer of from 1 to about 3 and R3 is ═O, —OH or —O(CO)R6 wherein R6, hatched lines indicate α configuration and solid triangles are used to indicate β configuration.
More preferably y is 1 and x is 0 and R1, R2 and R3 are hydroxy.
Most preferably the compound is cyclopentane N-ethyl heptanamide-5-cis-2-(3α-hydroxy-5-phenyl-1trans-pentenyl)-3,5-dihydroxy, [1α,2β,3α,5α], also known as bimatoprost (Lumigan®).
A maximum of up to about 3 ml of the formulation 28 is disposed in the squeezable container 14, which may be formed from any suitable material to maintain sterility of the formulation. The container 14 size is selected for enabling convenient handling by a user. As indicated in
The applicator device 18, including brush, may be fitted to the container 14 through a threaded neck 44 by a correspondingly threaded fitting 46 supporting the brush in an extended fashion which also provides a passageway 50 interconnecting the brush 24 and the container 14.
The compound 28 being water soluble enables residue free drying of the brush 24 after each application. This is facilitated by vents, or openings, 54 in a cap end 56. Additional vents (not shown) may be provided in the cap 20 to facilitate drying of the brush 24 after use.
In order to maintain the sterility of the formulation 28, a one-way valve 60 may be provided in the passageway 50. Alternatively, although not shown, a valve may be disposed in the container 14 or the threaded neck 44.
An alternative hair growth application system embodiment 70 is shown in
With reference to both 5 and 6, the applicator device 70 includes a brush 100 securable for storage by a sheath 102 and removably affixed therein by external threads 104 in the cap 98.
As illustrated in
After application, the brush 102 and cap 98 are again reversed for insertion into the sheath 102 as illustrated in
An aqueous solution containing 5%, by weight, bimatoprost is prepared as follows. Bimatoprost is dissolved in water and the resulting solution is sterilized by filtration. The solution is aseptically filled into the sterile container 14. Thereafter, as hereinbefore stated, the container is squeezed to prevent the solution to an eyelid and/or eyelash through the brush 24.
Twenty-five healthy female volunteers completed the study
The results are shown in
Although there has been hereinabove described a specific eyelash applicator and method in accordance with the present invention for the purpose of illustrating the manner in which the invention may be used to advantage, it should be appreciated that the invention is not limited thereto. That is, the present invention may suitably comprise, consist of, or consist essentially of the recited elements. Further, the invention illustratively disclosed herein suitably may be practiced in the absence of any element which is not specifically disclosed herein. Accordingly, any and all modifications, variations or equivalent arrangements which may occur to those skilled in the art, should be considered to be within the scope of the present invention as defined in the appended claims.
