GB2325855A - Preparation for topical application to the male sexual organ comprising at least one vasodilator & an aloe extract as active ingredients in an aq cream or gel - Google Patents

Abstract

The preparation for topical application to the male sexual organ to overcome erectile dysfunction comprises, as active ingredients, at least one vasodilator and an aloe extract. The preparation includes adjuvants such as one or more of stearic acid, triethanolamine, silicone oil, cetyl alcohol, glycerol, acidic carboxyvinyl gelling agents, methyl cellulose, wax emulsifiers, methyl paraben and propyl paraben so as to form an aqueous cream or gel. The aloe extract is preferably prepared using an extract prepared from the plant aloe ferox which contains at least 30 per cent by weight amino acids and also includes polysaccharides. The vasodilator may comprise glyceryl trinitrate and/or isosorbide dinitrate, or combination of theophylline and ethylene diamine, or co-dergocrine mesylate (ie a combination of dihydroergocornine mesylate and dihydroergocristine mesylate with alpha- and beta- dihydroergocryptine mesylate). To assist penetration the adjuvants may include one or more of propylene glycol, isopropyl palmitate and isopropyl myristate. Preferably the preparation is substantially thixotropic and supplied in unit dosage form. The preparation is preferably manufactured by mixing the active ingredients as a finely divided solid or as a solution to form a solution or dispersion in an aqueous cream or gel composition. The aloe extract and one or more gelling agents are advantageously prepared as one batch, a soap composition is prepared as a second batch and thereafter the two batches are mixed to form a homogeneous mixture to which the vasodilator is admixed.

Description

PREPARATION FOR TOPICAL APPLICATION TO THE MALE SEXUAL ORGAN This invention relates to a preparation for topical application to the male sexual organ. The preparation in many cases overcomes erectile dysfunction.

Erectile dysfunction is a widespread problem with human males. The consequences result in psychological damage and in many cases frustrate the normal fertilisation processes so that artificial insemination procedures must be used if procreation is required. The causes of this dysfunction may be physical or mental. Procedures for overcoming this problem have been proposed which can involve the surgical implantation of stiffening devices as described in GB-A-1 476 804, US-A-5 242 391 and other patents. Chemotherapeutical approaches have been proposed which require the injection of vasodilator compositions immediately prior to intercourse. The injection takes place on or near the penile shaft. Neither procedure is attractive and both approaches can result in revulsion or distress on the part of the partners involved. US-A-5 059 603 and US-A-4 801 587 propose topical application of compositions containing vasodilators. In both documents dimethylsulphoxide is a preferred component of the compositions due to its ability to carry compounds through the skin barrier. Unfortunately this compound is considered to be deleterious to health.

The present invention provides a preparation for topical application to the male sexual organ which causes the erectile tissue to engorge and, in many cases, enable normal sexual intercourse to take place which does not use dimethyl sulphoxide as a carrier.

According to the present invention there is provided a preparation for topical application to the male sexual organ comprising as active ingredients at least one vasodilator and an aloe extract together with adjuvants to form an aqueous cream or gel.

The vasodilator may be any of the compounds known to have this property such as glyceryl trinitrate and isosorbide dinitrate or compositions supplied for this purpose such as aminophylline, a combination of theophylline and ethylene diamine, and co-dergocrine messylate, a combination of dihydroergogornime messylate and dihydroergocristinne messylate with alpha and beta dihydroergocrytine messylate.

The aloe extract is preferably one prepared using an extract prepared from the plant aloe ferox. Such extracts contain at least 30 per cent amino acids and have a high level of polysaccharides. Extracts from some other species of aloe may be used such as those called aloe vera and also aloe peryi.

The adjuvants used to ensure consistency and easy application of the preparation include stearic acid, triethanolamine, silicone oils, cetyl alcohol, glycerol, acidic carboxyvinyl gelling agents, such as those sold under the trade mark Carbopol, methyl cellulose, wax emulsifiers, such as those sold under the trade mark Brij, and antibacterial and antifungal preservatives such as propyl and methyl paraben.

The the penetration and absorption of the active components through the skin can be enhanced by the inclusion of compounds such as propylene glycol, isopropyl palmitate, isopropyl myristate, glycerine and a silicone liquid supplied by Dow Corning under the designation Silicone 344.

Other ingredients can include fragrances and/or colorants.

The active ingredients are mixed as finely divided solid or as a solution to form a solution or dispersion in an aqueous cream or gel composition. When appropriate, such as when using Carbopol type thickeners, pH adjustment is carried out to provide a suitable consistency for topical application. Preferably the preparation is thixotropic so that the effect of temperature variations on viscosity and flow are minimised and after application the preparation does not flow.

In a preferred method the aloe extract and suitable gelling agents are prepared in one batch and a soap composition in a separate batch. The two components are mixed to form a homogenous mixture at which stage the vasodilator is admixed followed by any fragrance and/or colourant to complete the composition for packaging in dosage form.

The final preparation is preferably packaged in dosage form so that application can be controlled. Such packaging can comprise sachets containing a measured quantity of the cream or gel preferably one or two grams.

The sachets are constructed in conventional manner from polymer film with tags or other known means to assist bursting at on end enabling the contents to be extruded by squeezing the body of the sachet. Alternatively the preparation may be enclosed in small tubes with removable caps. To maintain a partial or complete erection the preparation may also be enclosed within a condom.

In order that the invention may be clearly understood a series of preparations according to the invention will now be described.

EXAMPLE I A cream composition was prepared containing the following ingredients as percentages by weight: aminophylline vasodilator 2.50 isosorbide dinitrate vasodilator 0.50 co-dergocrine messylate vasodilator 0.10 aloe extract 10:1 enhancer 15.00 these active ingredients were formed into a cream by admixture with: stearic acid 24.00 triethanolamine 2.20 Silicone 344 2.00 cetyl alcohol 1.00 glycerol 0.60 methyl paraben 0.25 fragrance 0.15 colorant 0.05 The cream was completed by the incorporation of 51.65 percent demineralised water.

The active ingredients and the soap composition were separately mixed before admixture in a manner conventional in the cosmetics industry.

EXAMPLE II A cream composition was prepared containing the following ingredients as percentages by weight: glyceryl trinitrate vasodilator 10.00 (as 10t solution in propylene glycol) aloe extract enhancer 15.00 these active ingredients were formed into a cream by admixture with: isopropyl palmitate 2.00 triethanolamine 1.20 Carbopol 940 0.70 polyethylene glycol 0.60 Brij 99 0.50 methyl cellulose 0.25 propyl paraben 0.15 methyl paraben 0.15 fragrance 0.15 colorant 0.05 The cream was completed by the incorporation of 69.00 percent demineralised water.

EXAMPLE III A gel composition was prepared containing the following ingredients as percentages by weight: aminophylline vasodilator 2.50 isosorbide dinitrate vasodilator 0.50 aloe extract enhancer 15.00 these active ingredients were formed into a gel by admixture with: triethanolamine 2.00 Silicone 344 2.00 glycerine 2.00 Cremophor RH40 0.80 methyl paraben 0.20 fragrance 0.15 colorant 0.05 The gel was completed by the incorporation of 74.00 percent demineralised water.

EXAMPLE IV A gel composition was prepared containing the following ingredients as percentages by weight: glyceryl trinitrate vasodilator 9.00 (as 10% solution in propylene glycol) aminophylline 2.50 aloe extract enhancer 15.00 these active ingredients were formed into a gel by admixture with: triethanolamine 2.00 Silicone 344 2.00 glycerine 2.00 Cremophor RH40 0.80 Carbopol 940 0.80 methyl paraben 0.15 fragrance 0.15 colorant 0.05 The gel was completed by the incorporation of 65.55 percent demineralised water.

In all the Examples the aloe extract was a composition sold under the name 'aloe vera 10:1' produced by extraction from aloe ferox. The extract was ten times the constituent strength of standard 'aloe vera' compositions.

In use two grams of one of the cream or gel compositions was applied to the glans penis and penile shaft and gently massaged into the skin. The effect was to produce an erection of the penis which was maintained for around 45 minutes. In an alternative mode of use one gram of the cream or gel was applied about two hours before an erection was desired. A second application was applied 30 minutes later resulting in an erection a short time later. The effect achieved by use of the cream or gel is enhanced by the types of audio, visual and tactile stimuli which in many cases initiate a penile erection.

Claims (14)

1. A preparation for topical application to the male sexual organ comprising as active ingredients at least one vasodilator and an aloe extract together with adjuvants to form an aqueous cream or gel.

2. The preparation as claimed in claim 1, in which the aloe extract is prepared using an extract prepared from the plant aloe ferox.

3. The preparation as claimed in claim 1 or claim 2, in which the aloe extract contains at least 30 per cent by weight amino acids and also includes polysaccharides.

4. The preparation as claimed in any of the preceding claims, in which the vasodilator comprises glyceryl trinitrate and/or isosorbide dinitrate.

5. The preparation as claimed in any of the claims 1 to 3, in which the vasodilator comprises a combination of theophylline and ethylene diamine, co-dergocrine messylate, a combination of dihydroergogornime messylate and dihydroergocristinne messylate with alpha- and betadyhydroergocrytine messylate.

6. The preparation as claimed in any of the preceding claims, in which the adjuvants comprise one or more of stearic acid, triethanolamine, silicone oil, cetyl alcohol, glycerol, acidic carboxyvinyl gelling agents, methyl cellulose, wax emulsifiers, methyl paraben and propyl paraben.

7. The preparation as claimed in any of the preceding claims, in which the adjuvants further comprise one or more of propylene glycol, isopropyl palmitate and isopropyl myristate.

8. The preparation as claimed in any of the preceding claims in which the preparation is substantially thixotropic.

9. The preparation as claimed in any of the preceding claims in unit dosage form.

10. Preparations for topical application to the male sexual organ as claimed in claim 1 and as herein described.

11. A method of manufacturing a preparation as claimed in any of the claims 1 to 10, wherein the active ingredients are mixed as a finely divided solid or as a solution to form a solution or dispersion in an aqueous cream or gel composition.

12. The method as claimed in claim 11, wherein the aloe extract and one or more gelling agents are prepared as one batch, a soap composition is prepared as a second batch and thereafter the two batches are mixed to form a homogeneous mixture to which the vasodilator is admixed.

13. The method as claimed in claims 11 or 12, wherein the manufactured preparation is packaged in unit dosage form.

14. Methods of manufacturing a preparation as claimed in claim 1 and as herein described.