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BR-102020016764-B1 - Intraurethral drug dosage form and device.

BR102020016764B1BR 102020016764 B1BR102020016764 B1BR 102020016764B1BR-102020016764-B1

Abstract

INTRAURETHRAL DOSAGE FORM FOR MEDICATION AND DEVICE. The present invention is situated in the fields of Pharmacy and Medicine. More specifically, the invention provides an intraurethral dosage form for liquid or gel medication for men or women. In one embodiment, an applicator provides advantages in its use, facilitating the application of pharmaceutical compositions directly into the urethral canal and providing a rapid local effect without substantial risks. The invention provides a dosage form and route of administration for various medications, being particularly useful for the application of anti-inflammatory and/or anesthetic medications, for the treatment of female cystitis, for modulating female genital sensitivity and/or for modulating erectile function in men – being an advantageous alternative dosage form to oral or injectable administration of medications or even to intraurethral administration of tablets.

Inventors

  • MARIA REGINA JARDIM GUARÉ
  • CRISTIAN HUGO GIL

Assignees

  • INSTITUTO DE PESQUISA, ENSINO, CIENCIA E TECNOLOGIA APLICADA - INSTITUTO GALZU

Dates

Publication Date
20260310
Application Date
20200817

Claims (11)

  1. 1. Intraurethral drug dosing device characterized by comprising: two concave and opposite faces (11) and (12) that fit together for finger support, defining an internal space of a receptacle (10) that houses a dedicated and disposable syringe, wherein: - the concave face (11) comprises a groove (13) positioned on an internal surface of the internal space of the receptacle (10), where a posterior part of the syringe is inserted into the groove (13), fixing the syringe in the internal space of the receptacle (10), and - a tip of the syringe is disposed in the anterior part of the syringe, outside the receptacle (10) and distanced from the groove (13), and - the posterior part of the syringe receives a rod (14) for displacement of the syringe plunger, dispensing the unit dose through the tip of the syringe.
  2. 2. Device according to claim 1, characterized in that the concave face (12) comprises a hollow region (16) providing visualization of the contents of the syringe (15) inside the receptacle (10).
  3. 3. Device according to claim 2, characterized by further comprising a stroke limiter for use in the female urethra (20).
  4. 4. Intraurethral dosage form of medication comprising a unit dose of a pharmaceutical composition in liquid or gel form comprising: one or more anti-inflammatory agents; one or more anesthetics; one or more active ingredients for the treatment of female cystitis; one or more active ingredients to modulate female genital sensitivity; one or more active ingredients to modulate erectile function in men; or combinations thereof; characterized by the unit dose being administered by an intraurethral applicator device being defined in claim 1 and comprising two concave and opposite faces (11) and (12) that fit together for finger support, defining an internal space of a receptacle (10) that houses a dedicated and disposable plastic syringe, wherein: - the concave face (11) comprises a groove (13) positioned on an internal surface of the internal space of the receptacle (10), where a posterior part of the syringe is inserted into the groove (13), fixing the syringe in the internal space of the receptacle (10), - a tip of the syringe is disposed in the anterior part of the syringe, outside the receptacle (10) and distanced from the groove (13), and - the posterior part of the syringe receives a rod (14) for displacement of the syringe plunger, dispensing the unit dose through the tip of the syringe.
  5. 5. Unit dosage form, according to claim 4, characterized in that the concave faces (11) and (12) comprise a convex perimeter.
  6. 6. Unit dosage form, according to claim 4, characterized in that the posterior part of the syringe is associated with a cylinder disposed within the receptacle (10), wherein the cylinder and the tip form a single body.
  7. 7. Unit dosage form according to claim 4, characterized in that said device additionally comprises one or more of the following aspects: the plastic syringe is of the extended Luer-Slip type; a cap (17) for the syringe; a limiter (20); four locks (19).
  8. 8. Unit dosage form, according to claim 4, characterized in that said device additionally comprises a hollow region (16) in the concave face (12).
  9. 9. Unit dosage form, according to claim 4, characterized in that one or both of the outer parts of the concave faces of said device additionally comprise protrusions (18).
  10. 10. A method for dispensing medication, using an intraurethral dosing applicator device defined in claim 1, wherein the method comprises administering a unit dose of a pharmaceutical composition in liquid or gel form comprising: one or more anti-inflammatory agents; one or more anesthetics; one or more active ingredients for the treatment of female cystitis; one or more active ingredients for modulating female genital sensitivity; one or more active ingredients for modulating erectile function in men; or combinations thereof, characterized in that the device comprises: two concave and opposite faces (11) and (12) that fit together for finger support, defining an internal space of a receptacle (10) that houses a dedicated and disposable syringe, wherein: - the concave face (11) comprises a groove (13) positioned on an internal surface of the internal space of the receptacle (10), where a posterior part of the syringe is inserted into the groove (13), fixing the syringe in the internal space of the receptacle (10), - a tip of the syringe is disposed on the anterior part of the syringe, outside the receptacle (10) and distanced from the groove (13), and - the posterior part of the syringe receives a rod (14) for displacement of the syringe plunger, dispensing the unit dose through the tip of the syringe.
  11. 11. Method, according to claim 10, characterized by comprising at least one of the following steps: - positioning the syringe (15), previously filled with a single dose of the medication and/or fillable at the time of application, in the receptacle (10) of the device; and/or - actuating the rod (14) that moves the plunger of the syringe (15), which contains a single dose of the medication, dispensing the medication.

Description

Field of Invention [0001] The present invention is situated in the fields of Pharmacy and Medicine. More specifically, the invention provides an intraurethral dosage form for liquid or gel medication for men or women. In one embodiment, an applicator provides advantages in its use, facilitating the application of pharmaceutical compositions directly into the urethral canal and providing a rapid local effect without substantial risks. The invention provides a dosage form and route of administration for various medications, being particularly useful for the application of anti-inflammatory and/or anesthetic drugs, for the treatment of female cystitis, for modulating female genital sensitivity and/or for modulating erectile function in men, being an advantageous alternative dosage form to oral or injectable administration of medications or even to intraurethral administration of tablets. Background of the Invention [0002] Dosage forms that provide routes of administration for various medications are known and available. However, there are several medical conditions requiring therapeutic intervention that still suffer from a lack of dosage form options that provide risk reduction, better therapeutic effect, greater ease of use, lower dose, among other technical limitations. The present invention aims to fill this important gap by solving these and other technical problems. [0003] Among the various medical conditions that can benefit from the present invention, those in which intraurethral administration of medications still has limited dosage options stand out. Among these, special emphasis is given to anti-inflammatory therapies; anesthetics; treatment of female cystitis or in the modulation of female genital sensitivity; therapies that modulate erectile function in men, among others. [0004] In this context, INTRACAVERN INJECTIONS with phentolamine, papaverine, and alprostadil are considered second-line treatment for erectile dysfunction, although alprostadil is more commonly used. Intracavernous therapy is also frequently effective in erectile dysfunction refractory to treatment with oral PDE5 inhibitors, especially in post-radical prostatectomy patients. Despite these benefits, intracavernous therapy is an invasive procedure that is associated with dropout rates of 40% to 50% due to pain, priapism, penile fibrosis, hematoma, ecchymosis, or fear of the needle (Anaissie, J. & Hellstrom, W. J. (2016). Clinical use of alprostadil topical cream in patients with erectile dysfunction: a review. Research and reports in urology, 8, 123-131.doi:10.2147/RRU.S68560). [0005] A comparative study in 103 unselected patients with erectile dysfunction between MUSE™ (intraurethral tablet up to 1000 μg of Alprostadil) and intracavernous Prostavasin™ up to 20 μg provided total responses of 43% (MUSE™) vs 70% (Prostavasin™). Full rigid erections were achieved in 10% (MUSE™) vs 48% (Prostavasin™). In terms of side effects, the reported penile pain/burning rate after MUSE™ was 31.4%, compared to 10.6% after i.c. Alprostadil. Urethral bleeding after MUSE™ application was observed in 4.8%. Despite this, Alprostadil remains the "Gold Standard" in the treatment of male impotence, but MUSE™ should be reserved for a subset of patients who suffer of erectile dysfunction (PORST, H. Transurethral alprostadil with MUSETM (medicated urethral system for erection) vsintracavernousalprostadil— a comparative study in 103 patients with erectile dysfunction. International journal of impotence research, v. 9, n. 4, p. 187, 1997). [0006] Another study with 60 patients (31 Alprostadil and 29 placebo) applying 1% alprostadil + 5% SEPA CREAM, improved vaginal penetration 12/31 (39%) with alprostadil versus 2/29 (7%) with placebo, P<0.005 (Goldstein I, Payton TR, Schechter PJ. A double-blind, placebo-controlled, efficacy and safety study of topical gel formulation of 1% alprostadil (Topiglan) for the in-office treatment of erectile dysfunction. Urology. 2001;57(2):301-305). [0007] Another study with 1,732 patients (1,298 alprostadil, 434 placebo) applying 100, 200, or 300 μg alprostadil CREAM had the following positive results: 12% - placebo, 46% - 100 μg, 62% - 200 μg, 67% - 300 μg, with a discontinuation rate of 2.7% (Padma-Nathan H, Yeager JL. An integrated analysis of alprostadil topical cream for the treatment of erectile dysfunction in 1732 patients. Urology. 2006;68(2):386-391). [0008] External application of a gel containing 1% alprostadil + 5% SEPA, in another study with 48 patients, demonstrated a positive correlation with erectile response, since 67 to 75% of patients had an erection compared to 17% of controls (p <0.001). Blood pressure and heart rate varied minimally. No serious adverse effects were observed in the 48 patients, although most reported skin discomfort (MCVARY, KEVIN T. et al. Topical prostaglandin E1 SEPA* gel for the treatment of erectile dysfunction. The Journal of urology, v. 162, n. 3, p. 726-730, 1999). In this case, pate