WO2012042331A1

WO2012042331A1 - Device for locally administering an active ingredient

Info

Publication number: WO2012042331A1
Application number: PCT/IB2011/002213
Authority: WO
Inventors: Nicola Staffolani
Original assignee: Individual
Current assignee: Individual
Priority date: 2010-09-27
Filing date: 2011-09-23
Publication date: 2012-04-05
Anticipated expiration: 2013-03-27
Also published as: ITPG20100050A1; EP2621417A1; IT1402097B1

Abstract

Device (1) for locally administering, on glans of male organ, at least one active ingredient (2) for the erection of said male organ, said device (1) comprising at least a first chamber (3) surrounding, at least partially, said glans of said male organ and containing said active ingredient (2) in solid condition, said at least one first chamber (3) being provided with at least one selective membrane (6) for passing of said active ingredient in a solid condition, disposed at the outer surface of said glans, and with at least one section (7) for entering a solvent (8) into said at least one first chamber for solubilization of said active ingredient in solid condition and passing said active ingredient in solution through said membrane (7).

Description

"DEVICE FOR LOCALLY ADMINISTERING AN ACTIVE

INGREDIENT"

* * * *

FIELD OF THE INVENTION

The present invention concerns a device for locally administering an active ingredient on glans of male organ. Particularly, such a device is applied on the male organ, or penis, before the sexual act, in such a way to administer said active ingredient, usually a vasodilatator, on the dermal surface of the glans thereof, preferably on the corona of glans, thereby allowing the user to complete the sexual act.

It has to be observed that with the term "locally" it is intended such an administration that the transdermal absorption of the active ingredient is limited to the local blood circulation and the general systemic circulation is involved only within limits. Various compositions of vasodilatator agents, or active ingredients, for local application are already known to the person skilled of the art.

KNOWN PREVIOUS ART

Active ingredients used for the erection of the male organ are known. Particularly, it is known the use of sildenafil citrate administered orally, or systemically. Such a molecule revealed to be highly effective to solve most of the problem of male impotence, however such an used administration type is not free from drawbacks because the molecule goes into the systemic circulation and reaches every organs of human body, thereby affecting their functioning, sometimes also detrimentally. For example, sildenafil citrate is highly not recommended for people suffering from cardiac pathologies, most of all in persons in therapy with nitro compounds, because the intake of also little amounts of such an active ingredient may have serious side effects up to bring on hypotension and shock.

In literature, studies on local use of sildenafil citrate (i.e. transdermally) are known, directly on glans, however in these studies the most evident problem is the difficulty in administering the molecule in recommended times and doses to obtain a lasting erection of the organ, without the onset of particular serious side effects in the user. Object of the present invention is then to realize a device allowing to administer locally, in a controlled and weighted out way, anyway effective, an active ingredient for the erection of said organ directly on glans of the male organ.

A further object of the present invention is to realize a device being structurally simple and ease to use.

SUMMARY OF THE INVENTION

These and other objects are obtained by the present device for locally administering, on glans of male organ, an active ingredient for the erection of said male organ, said device comprising at least a first chamber surrounding, at least partially, said glans of said male organ and containing said active ingredient in solid condition, said at least one first chamber being provided with at least one selective membrane for passing of said active ingredient in a solid condition, disposed at the outer surface of said glans, and with at least one section for entering a solvent into said at least one first chamber for solubilization of said active ingredient in solid condition and passing said active ingredient in solution through said membrane.

In substance, the active ingredient, preferably anhydrous and powdered, when not in use it is preserved inside said at least a first chamber, not being able to come out. When the device is placed on the male organ, with said selective membrane facing to the outer surface of glans, and it is operated, said first chamber is at least partially filled with a solvent, preferably a physiologic solution, but it may be sterile, deionized water, or similar, or even in solid condition, anyway being able to solubilize the active ingredient; the latter then entering into the solution and passing through the afore said membrane selective for said active ingredient in solid condition. The membrane, provided with passages, or holes, having a constant dimension, allows to adjust the solution flow comprising the solubilization liquid and the active ingredient dissolved therein and a constant delivering of the solution composed by the active ingredient and solvent and, thereby, a constant administration of the active ingredient onto the glans. Said active ingredient may be selected from sildenafil, alprostadil, vardenafil and tadacafil and their possible salts pharmaceutically acceptable, such ad for example sildenafil citrate. It has to be further observed that the use of an active ingredient in lyophilized, or anhydrous conditions, and powdered, has the advantage of being able to be solubilized easily and quickly and then to be used when contacting an appropriate solubilizing solution, or solvent.

Further said at least one entering section is provided with a septum punchable from the outside. In this way it is possible to fill said at least one first chamber from the outside with the afore said solubilization solvent, by insertion of a puncher conveniently dimensioned to punch said entering section.

According to an alternative embodiment, said administering device comprises at least one second chamber connected with said at least one first chamber by said at least one entering section, wherein said at least one second chamber contains said liquid for the solubilization of said lyophilized active ingredient. The afore said entering section, in such an alternative embodiment, is provided with a septum frangible by compression. However the user has to squeeze said second chamber to break said frangible septum and to obtain the passage of the solubilization solvent from said at least one second chamber into said at least one first chamber, at last to pass through said selective membrane.

Such a solubilization solvent is preferably in liquid condition, for example of physiological solution type, although other solid, gaseous solvents or, more simply, liquids may be selected based on the used active ingredient. For example adapted solvents may be selected between sterile or deionized water or similar. According to both the afore described embodiments, said at least one first chamber and / or said at least one second chamber have the shape of a circular circle, or closed or opened ring. Further, said device comprises means for retaining the prepuce of said male organ, at least when said device is placed at the glans. These retaining means comprise at least a lowered portion, or recess, disposed inside said device between said at least one first and said at least one second chamber. In practice, according to a preferred embodiment, the inner diameter of said at least one first chamber is smaller than that of said at least one second chamber so that these retaining means, besides having the function of retaining the prepuce in a stable position, have the important function of containing the liquid administered on glans and then of avoiding the dispersion outwardly thereof.

Further, according to a third embodiment of the invention, the device, according to the first or the second embodiment described above, is disposed inside a cowl, at the front portion thereof.

BRIEF DESCRIPTION OF THE FIGURES

For purposes of illustrations and not limitative, more particular preferred embodiments of the present invention will be now provided with reference to the accompanying figures, in which:

figure 1 is a schematic longitudinal section view of the administering device according to the first embodiment of the invention;

figure 2 is a schematic longitudinal section view of the administering device according to the second embodiment of the invention;

figure 3 is a schematic longitudinal section view of the administering device according to the third embodiment of the invention;

figure 4 is a schematic longitudinal section view of the administering device according to a fourth embodiment of the invention.

DETAILED DESCRIPTION OF SOME EMBODIMENTS OF THE PRESENT INVENTION

Referring particularly to these figures, with 1 an administering device according to the invention is shown.

The device 1 to locally administer on the glans of the male organ an active ingredient 2, preferably sildenafil citrate, for the erection of said male organ, comprises a first chamber 3 having a circular circle, or ring, shape, surrounding almost completely the glans of said male organ, when the device 1 is in use, and containing, in its inside, said active lyophilized and powdered ingredient 2, and then in a solid condition. Substantially, the active ingredient in solid condition, is brought into such a first chamber 3 for being preserved until its final use. The amount of active ingredient 2 inserted into said first chamber 3 is, then, determined a priori so to be the amount necessary for assuring an organ erection sufficient for the sexual act, without however causing undesirable side effects in the user, such as, for example, an excessive duration of the organ erection. So, this allows to weight out precisely and effectively the active ingredient directly on glans, preferably at the corona of glans, thereby avoiding possible and undesired effects that could arise using the systemic administration. A typical dose of such an active agent, or active ingredient, locally administered, i.e. transdermally, is generally comprised between about 0.1 and 500 mg.

It has to be observed that, as afore said, the administration used in the present invention is named local because the transdermal absorption of the active ingredient is designed to be limited to the local blood circulation of the male organ in such a way that the general systemic circulation is involved only at minimum. Various compositions of vasodilatator agents, or active ingredients, for local application are already known to the person skilled of the art and herein they are not referred.

It has to be observed that such a first chamber 3 is provided, in its inner side 5, that one in use facing and contacting, at least partially, the outer surface of the glans of the male organ, with a membrane 6 selective for the passage of said active ingredient 4, when in solid condition. Substantially, a membrane 6 able to be passed through by a liquid is selected, but not able to be passed through by a solid substance, in granular condition. For example, a semipermeable or natural or artificial membrane falls within the definition of selective membrane of said active ingredient, when in solid condition. Said first chamber 3 further comprises a section 7 for entering a solvent in liquid condition 8 into said chamber 3. Such a solvent 8, preferably physiological solution, when entered inside said chamber 3 dissolves said active ingredient 2, the latter thereby entering in the solution and becoming solute. Then the active ingredient, being completely dissolved in the solubilization solvent, passes through said membrane 6 and reaches the glans to be administered locally on the outer surface thereof. It has to be observed that the membrane 6 operates a constant filtering, i.e. it has homogeneous filtering features. For example, it is provided with holes, having dimensions substantially similar and it is further made of a material allowing just an uniform passage of the obtained solution after the active ingredient came into the solution.

In the embodiment described in figure 1 , the entering section 7 is provided with a septum punchable from the outside so that it is possible to bring the liquid 8 into said first chamber 3 by the use of a syringe or similar means having, anyway, a punching element. Although herein it is described an entering section provided with a punchable septum, however an entering section provided with a raisable element such as, for example, a cap, or a frangible septum, or similar, falls again within the protection scope of the present invention.

In figure 1 , as anyway in the further attached figures, the arrows show the route of the solubilization solvent 8 when it has been brought into the entering section 7. It is noticed that the membrane 6 is not passed through by the solvent only, in this case liquid 8 brought into the section 6, but by a liquid comprising also the active ingredient 2 of the sildenafil citrate type, as afore said, in solution.

It has to be observed that the above described features allow conveniently to obtain a device 1 assuring the local absorption of drugs containing an active ingredient and that, contacting the outer surface of the glans of the male organ, preferably at the corona of glans, render it immediately ready to sexual act assuring the necessary duration for the couple.

In figure 2 is shown a second product embodiment. The device 1, in this case, comprises a second chamber 10 connected to said first chamber 3 through said entering section 7. In this second embodiment the entering section 7 is provided with a septum frangible by compression and, then, it is different from the first above described embodiment because the solvent 8 is not brought inside from the outside, but it is already contained in said second chamber 10. In figure 2 the arrows show the route of the solubilization liquid 8 when it has been brought into the entering section 7. As it can be easily observed, the solubilization solvent 8 is not brought inside from the outside, as in the first embodiment, but it is already contained in the second chamber 10 and it comes into the first chamber 3 only when the frangible septum, disposed at the entering section 7, is broken by user compression. It has to be noticed that, in this case also, the membrane 6 is not passed through only by the liquid 8 brought into the section 6, but by a liquid comprising also the active ingredient 2 of the sildenafil citrate type, as afore said, in solution.

It has to be observed that, although so far it is referred to sildenafil citrate, however an active ingredient selected from a different salt of sildenafil, alprostadil, vardenafil and tadalafil and their possible salts pharmaceutically acceptable, is still comprised in the protection scope of the present invention. Further, it should be said that also the solubilization solvent is preferably physiological solution, although a different solvent able to solubilize the specific used active ingredient falls again within the protection scope of the present invention. For example, a solubilization liquid usable in the present invention may be sterile or deionized water.

Further it should be said that the active ingredients mentioned so far act by vasodilatation of blood vessel of said organ, however the use of an active ingredient taking advantage from a different action mechanism falls again within the protection scope of the present invention.

Further, it has to be noticed that the device may also comprise several active ingredients 2 or, as described in the embodiments here presented, only one active ingredient 2; in the same way any used active ingredient may be, if desired and / or necessary, formulated with the use of carries and / or excipients pharmaceutically acceptable, as known to a person skilled of the art.

Always according to the embodiments herein described both said first chamber 3 and said second chamber 10 have a circular circle, or ring, shape, although a different shape, for example of circular circle, or ring, partially open, that is C-shaped, or similar, falls within the protection scope of the present invention.

Further, it has also to be noticed that in both the embodiments described so far, the device 1 comprises means 20 for retaining the prepuce of said male organ such that during the operation of the device 1, an active ingredient 2 is administered on the glans without the prepuce could be an obstacle for such an operation.

These retaining means 20 comprise a recessed portion 21 having a circular circle shape. Such a recess may be disposed between said first 3 and said second chamber 10. Advantageously said first chamber 3 and said second chamber 10 have a different inner diameter so that said recess 21 is obtained because of the diameter difference between the first 3 and the second chamber 10, wherein the inner diameter of said second chamber 10 is greater than the inner diameter of said first chamber 3.

It has to be noticed that, although herein not shown so far, an embodiment of the administering device free of said retaining means 20 of the prepuce will however fall within the protection scope of the present invention.

Further, both the embodiments comprise a sponge 60, or other absorbing biocompatible material / fabric, in the shape of circular circle, or ring, connected respectively at the free end of said retaining means 20a, in case of the first embodiment of the invention (said sponge 60 is not shown in figure 1 ), or at the free end 10a of said second chamber 10, in case of said second embodiment of the invention. Such a sponge 60 has the task of absorbing part of the substance composed by said active ingredient and said physiological solution, that has passed through the afore said selective membrane 6 and that has not been absorbed completely by said glans surface. Further, such a sponge 60 has also the task of cleaning the glans, scraping on it, when the administering device 1 is taken off from the male organ. It has to be observed that, although an administering device 1 provided with a sponge 60 has been described, an embodiment of the device 1 being free of such a sponge 60 still falls in the protection scope of the present invention.

According to a third embodiment of the invention, as shown in figure 3, the device 1, comprising a first chamber 3, a second chamber 10 and said sponge 60, as described in the second embodiment of the invention, is disposed inside a cowl 30 in the inner front portion 31 thereof. It has to be observed that, although herein not shown, a cowl 30 containing in its inside a device 1 according to the first embodiment above described, falls again within the protection scope of the present invention. But in this case the entering section 7 passes through the wall of the cowl 30 to be available for the user also when the cowl is worn. In case of embodiment with a cowl 30, the device 1 may be realized integrally with the cowl 30, therefore constrained thereto, or able to move in its inside to find the better position on the glans. The cowl 30 is worn on the organ glans subjected to the administration of the said active ingredient and it has the task of avoiding the solution containing said active ingredient, when on the glans, from dispersing outside.

At last, in figure 4 is shown a fourth embodiment of the device 1. Such an embodiment is different from the others, but particularly from the second embodiment represented in figure 2, because the inner side 5 of the said first chamber 10, coincident with said membrane 6, is tapered towards the inside of the device 1, i.e. the transversal thickness of the walls of the first chamber 3 (as seen in section) decreases little by little as we move in the direction of said second chamber 10. In other words, the inner diameter of said first chamber 3 increases gradually, or linearly, in the opposite direction from the free end 3 a of the said first chamber 3, that is inside the device 1. Such a solution allows to aid a better local administration of the active ingredient on the glans because the inner shape of said first chamber 10 traces out substantially the glans' one. In fact, the membrane 6 contacts the glans for the most of its length.

Claims

1. Device (1 ) for locally administering, on glans of male organ, an active ingredient

(2) for the erection of said male organ, said device (1 ) comprising at least a first chamber (3) surrounding, at least partially, said glans of said male organ and containing said active ingredient (2) in solid condition, said at least one first chamber

(3) being provided with at least one selective membrane (6) for passing of said active ingredient in a solid condition, disposed at the outer surface of said glans, and with at least one section (7) for entering a solvent (8) into said at least one first chamber for solubilization of said active ingredient in solid condition and passing said active ingredient in solution through said membrane (7).

2. Device according to claim 1 , characterized in that said active ingredient is lyophilized.

3. Device according to claim 1 or 2, characterized in that said active ingredient is powdered.

4. Device according to one or more of the preceding claims, characterized in that said at least one membrane (6) is semipermeable.

5. Device according to claim 4, characterized in that said membrane is provided with passages, or holes, having constant dimensions.

6. Device according to one or more of the claims from 1 to 5, characterized by comprising at least one second chamber (10) connected with said at least one first chamber by said at least one entering section (7) and containing said at least one solubilization liquid (8) in its inside.

7. Device according to one or more of the claims from 1 to 7, characterized in that said at least one entering section (7) is provided with a septum frangible by compression or punchable from the outside.

8. Device according to one or more of the preceding claims, characterized in that said active ingredient (2) is selected from sildenafil, alprostadil, vardenafil and tadacafil.

9. Device according to one or more of the preceding claims, characterized in that said solvent (8) is selected from a physiological solution, sterile water or deionized water.

10. Device according to any one or more of the preceding claims, characterized in that said at least one first chamber (3) and / or said at least one second chamber (10) have substantially a closed, or partially open, annular shape.

1 1. Device according to claim 10, characterized in that said inner diameter (d) of said first chamber (3) increases little by little in a direction opposite to the free ending (3a) of said first chamber (3).

12. Device according to one or more of the preceding claims, characterized by comprising means (20) for retaining the prepuce of said male organ.

13. Device according to claim 12, characterized in that said retaining means comprise at least one recess (21) disposed inside said device.

14. Device according to one or more of the preceding claims, characterized by comprising a cowl (30) in the inner front portion (31) thereof is disposed said administering device (1) according to one or more of the preceding claims.

15. Device according to one or more of the preceding claims, characterized by comprising at least a sponge (60) connected with the free ending (20a) of said retaining means (20), or with the free ending (10a) of said second chamber (10).