Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
  • A61M35/00—Devices for applying media, e.g. remedies, on the human body
  • A61M35/003—Portable hand-held applicators having means for dispensing or spreading integral media
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/04—Antibacterial agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/10—Antimycotics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/08—Vasodilators for multiple indications

Definitions

• the present invention relates to a device for the application of a formulation of a pharmaceutical active ingredient on a mucosa, and more particularly, the application of a vasodilator active ingredient on the penile mucosa in order to treat erectile dysfunction.
• Erectile dysfunction or impotence is characterized by the inability to obtain and / or maintain an erection sufficient to allow sufficient sexual intercourse.
• the causes of this impotence can be multiple and be of physiological or psychological origin.
• vasodilator active ingredients A particular problem lies in the route of administration of the vasodilator active ingredient. Indeed, it is essential that the vasodilatation effect is obtained as quickly as possible after administration of the active ingredient with the shortest latency possible.
• intra-urethral delivery systems or intra-cavernous injection of vasodilator active principles have been developed in order to treat these erectile dysfunctions.
• intra-urethral administration involves the use of a medical device that is often complicated and uncomfortable for the patient.
• transmucosal topical mode of administration is well suited to the intended application and there are various products on the market formulated from a vasodilator agent combined with one or more penetrating agent or absorption facilitator to facilitate and accelerate the migration of the vasodilator active principle into the cavernous body where it can perform its physiological role.
• vasodilator active principles commonly used in the indication erectile dysfunction there may be mentioned, for example, prostaglandins, particularly prostaglandins E1 (PGE1) or prostaglandins E2 (PGE2).
• PGE1 prostaglandins E1
• PGE2 prostaglandins E2
• the application of transmucosal topical formulations for erectile dysfunction is performed by the patient by manually spreading an adequate amount of product from a tube containing the preparation.
• Such a manual application can cause some problems.
• the repeated contact of the hands or fingers with the product is not always desirable on a sanitary level because such multiple contacts can cause contamination of the product.
• Another major problem is that the manual application of vasodilators causes a residual amount of product to remain in the skin of the fingers.
• the transmucosal topical formulations comprise one or more agents that promote the transfer of the active ingredient, the absorption thereof is rapid, including at the level of the hands.
• the inflow of blood thus generated in the hands and fingers causes discomfort or pain for the user when applying such products.
• a topical application on the penile mucosa there is a device of "wafer” type, that is to say a very thin fast disintegrating film intended to be deposited at the level of the glans.
• This film comprises a vasodilator active ingredient which is absorbed once said film deposited at the level of the penile mucosa.
• the manufacture of such a "wafer" is complex.
• the packaging and application systems for the cream-like products, gels, ointments and ointments described today are generally in the form of a container, possibly under pressure, which is also possibly associated with a generally tubular applicator for directing the product. produced to the area to be treated.
• This kind of packaging and application device does not does not respond optimally to the specificity of the topical implementation of vasodilator agent for which a certain massage time is useful to ensure the proper absorption of the active ingredient and this despite the possible presence of penetration agent.
• Said devices described in the prior art do not allow application by direct contact for obvious hygiene reasons in the case of application to a mucosa.
• the present invention relates to a packaging device for the topical application of a formulation comprising an active ingredient on a mucosa, said conditioning system comprising: a body (1) having an open base (2) intended to receiving the end of at least one finger and an applicator head (3) provided with at least one opening (4), body in which is disposed a movable means (5) defining a cavity (6) filled with the formulation (7) and allowing the expulsion of said formulation through the opening (4) when exerting pressure on this moving means.
• Such a device has many advantages. Thus there is no contact between the active ingredient and the skin of the user except at the level of the mucosa, where the application is desired and therefore no side effect of an active ingredient to an undesired level.
• the implementation of such a device is adapted to the application of said active ingredient by a person other than the patient himself.
• the single FIGURE shows a longitudinal section of a particular embodiment of the device according to the present invention.
• the open base 2 located at the body 1 has dimensions and shapes adapted to the implementation of the applicator at the tip of a finger or several fingers which facilitates the application of the active ingredient topically .
• this open base 2 will preferentially have an annular section to fit the finger of a user.
• the diameter of the opening is not critical and it can be chosen according to the intended audience.
• the applicator head 3 has at least one closable opening 4 for dispensing the formulation 7 comprising the active ingredient contained in the cavity 6 of said device.
• the size and shape of the opening 4 are not critical and they may be chosen according to the viscosity of said formulation comprising the active ingredient, for example. It may be a single opening or a plurality of circular or ovoid shaped openings for example.
• the closure of this opening can be achieved through any closure means 8 known to those skilled in the art bearing in mind that there should be no salient residue at the applicator head so avoid any risk of injury during application. Indeed, the use according to the present invention is intended for application to a mucosa, a particularly sensitive and fragile tissue.
• a self-adhesive seal, screwed or welded closing the opening can be considered as a sealing means 8, which cap is removed at the time of use of 1'applicateur.
• a shutter-type cap that can be held by screwing or clipping, for example.
• the applicator head 3 is preferably of hemispherical shape to ensure accuracy and comfort during application. But one can also consider a flat applicator head or having a very slight convexity or a combination of these profiles. In particular a truncated hemispherical profile is preferred because it allows a better closure of the opening. It must be kept in mind, however, that we try to avoid having too sharp angles that could injure the user or the patient during the application.
• the device according to the present invention will not present sharp corners or salient residues with regard to the areas intended to come into contact with a mucosa during application. This avoids any injury knowing that the use according to the present invention is for a mucosa.
• the application according to the present invention relates to a healthy or damaged mucosa, preferably healthy.
• the moving means 5 present in the body of the device and delimiting a cavity 6 containing the formulation 7 comprising the active ingredient serves as a piston for expelling the active ingredient in use.
• the user has one or more fingers at the open base of the body and, by exerting pressure in the longitudinal axis, expels the formulation containing the active ingredient through the opening once it released its closure.
• the moving means 5 will be designed to ensure the best possible seal at its junction with the body of the device so as to avoid leakage of formulation containing the active ingredient.
• This movable means may be an annular piston optionally equipped with an annular folding membrane.
• This piston may also be provided with two sliding lips along the wall of the body.
• a convex piston that will adapt to the shape of the applicator head to allow the most complete expulsion of the formulation contained in the cavity once said piston has come into abutment. It is also possible to envisage a diaphragm or a deformable wall defining a cavity filled with a formulation containing the active principle and allowing the active ingredient to be expelled through the opening once pressure is exerted on it and is deformed.
• the material used for said piston will be compatible with the pharmaceutical active ingredient (s) included in the formulation contained.
• This material may thus be selected from the group polyolefins or elastomers for example.
• polyethylene (PE) is particularly suitable and more preferably High Density Polyethylene (HDPE).
• the use of such a device is particularly suited to the application of active principle to a mucosa.
• the use of such a device makes it possible to overcome the drawbacks mentioned above.
• the application can be done without contacting the active ingredient with the skin other than that of the penile mucosa to which is intended such an active ingredient.
• the present invention also relates to a method of treating erectile dysfunction in which an active ingredient contained in a pharmaceutical formulation for the topical treatment of said erectile dysfunction is applied to the penile mucosa using a device comprising: a body 1 having an open base 2 intended to receive the end of at least one finger and an applicator head 3 provided with at least one opening 4, body in which is disposed a moving means 5 defining a cavity 6 filled with the formulation 7 and allowing the expulsion of said formulation through the opening 4 when exerting pressure on the moving means.
• the expression "penile mucosa” is understood to mean the surface of the glans. It may be the external mucosa but also the internal mucosa, namely the urethral end at the meatus. It is also possible to envisage the use according to the present invention to dispense an active ingredient topically on any other mucosa for which direct contact with the hand or the fingers is undesirable or impractical.
• the oral, anal or vaginal mucosa may be concerned with a use according to the present invention.
• the use of such a device is particularly suitable for the local application of antibiotics or antimycotics. It is also possible to envisage the use of said device according to the invention for the topical oral application of an active principle intended for the treatment of mouth ulcers and / or gingivitis, for example.
• the active ingredient concerned by the use according to the present invention may be any active principle of application that is at least potentially topical on the mucosa.
• it is a vasodilator active ingredient.
• Suitable vasodilator active principles include alpha-1 blockers and / or alpha-2 blockers such as phentolamine, moxisylyte and PDE5 inhibitors (Phosphodiesterase 5). More preferably still it is at least one prostaglandin and preferably prostaglandin E1, alprostadil.
• any active ingredient vasodilator aiming topically is conceivable within the scope of the present invention.
• the vasodilator active ingredient may be chosen from the group comprising alprostadil, misoprostol, papaverine and phentolamine. It may also be misoprostol as described in EP 980245 for example. As indicated above, in the case of application to vaginal mucosa, the active ingredient delivered may be selected from the group comprising antibiotics and antimycotics.
• the active vasodilator active principle used in the use according to the present invention can be formulated according to common compositions and known to those skilled in the art.
• a suitable formulation may be a formulation in the form of a gel or a cream whose viscosity may reach 45,000 centipoise at an ambient temperature of about 20 ° C., containing an effective amount of vasodilator active ingredient.
• vasodilator active principle any formulation of a vasodilator active principle from the moment this formulation ensures an adequate viscosity for the expulsion of the composition containing the active principle and the topical application at the level of the mucosa.
• An appropriate formulation containing a vasodilator active ingredient such as misoprostol is described in EP 980245.
• the formulation volume comprising the active ingredient contained in the cavity defined by the body and the moving means will be selected according to the target indication.
• the amount of product may be from about 0.1 to 3 ml, preferably from about 0.2 to 2 ml, and still more preferably from about 0.5 to 1 ml. This amount will however be limited by the size of the packaging system, itself adapted to the size of one or more fingers because it is configured for such a fingerstall use.
• the volume of formulation to be delivered topically will be chosen so as to ensure comfort and convenience of use to the patient while ensuring the delivery of an effective amount of vasodilator active ingredient assuring sufficient erection.
• the mucosal surface to be treated in this case is relatively limited and too large a formulation containing a vasodilator active ingredient would be inadequate because a quantity of formulation, so active ingredient, could be lost.
• the body of the packaging and application system according to the present invention may be tinted with an agent rendering it opaque, thus avoiding any risk of degradation of the active ingredient by ultraviolet rays .
• the body of this system will be made of a rigid material it may be a rigid material such as a polymer selected from the group comprising polyolefins, polyesters and styrenic compounds.
• it may be polypropylene.
• the packaging system and application and the dose contained will be sized for a unit application. Such a single dose combines the inherent and necessary benefits for this indication. Thus the active ingredient is kept protected from external degradation agents and the extemporaneous opening ensures optimal hygiene for the patient.
• the packaging and application systems that can be used according to the present invention may be individually packaged in a blister or bag, optionally aluminized, under a protective atmosphere, for example.

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• Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Life Sciences & Earth Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Engineering & Computer Science (AREA)
• Organic Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Heart & Thoracic Surgery (AREA)
• Anesthesiology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Communicable Diseases (AREA)
• Oncology (AREA)
• Biomedical Technology (AREA)
• Hematology (AREA)
• Cardiology (AREA)
• Gynecology & Obstetrics (AREA)
• Endocrinology (AREA)
• Reproductive Health (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Containers And Packaging Bodies Having A Special Means To Remove Contents (AREA)

Applications Claiming Priority (2)

Publications (1)

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Family Applications (1)

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• 2004
  • 2004-09-29 FR FR0410301A patent/FR2875704A1/fr not_active Withdrawn
• 2005
  • 2005-09-27 JP JP2007534017A patent/JP2008514326A/ja not_active Withdrawn
  • 2005-09-27 US US11/663,972 patent/US20080021422A1/en not_active Abandoned
  • 2005-09-27 CA CA002581739A patent/CA2581739A1/fr not_active Abandoned
  • 2005-09-27 EP EP05789622A patent/EP1804896A2/de not_active Withdrawn
  • 2005-09-27 WO PCT/EP2005/054857 patent/WO2006035032A2/fr active Application Filing

Non-Patent Citations (1)

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