Vaginal or rectal applicator and method

ES 2 345 656 T3

DESCRIPTION

Vaginal or rectal applicator and procedure.

Field of the invention

The present invention relates to a vaginal or rectal applicator, such as for example for the transvaginal or rectal application of pharmaceutical preparations.

Background of the invention

Vaginal or rectal applicators have been used to dispense medications to treat vaginal diseases and disorders and diseases of the inner abdomen including the colon and rectum. They are sold both pre-loaded and empty. For example, SCHERING-PLOUGH® Healt Care Products, Memphis, TN, provides applicators for GYNE-LOTRIMIN^®. Likewise, Ortho McNeill and Columbia Labarotories supply pre-filled applicators to administer a contraceptive gel and a vaginal humidifier, respectively. In general, the vaginal applicator consists of a small diameter elongated cylindrical body and a plunger rod.

Vaginal and rectal applicators have traditionally been designed to deliver large volumes (eg, greater than 1 mL) of pharmaceutical preparations. Vaginal applicators are typically used to deliver large volumes of drug for the treatment of diseases and disorders within the vagina, although rectal applicators have been used to treat diseases of the lower abdomen and intestine using large volumes of drugs in the form of enemas, foams and suppositories. When such large volumes of drugs are administered, they coat the entire vaginal epithelium, in the case of vaginal administration, or the anal canal, in the case of rectal administration. The large volume of drug contained within the applicator raises aesthetic concerns and hygiene concerns. Also, the amount of drug dispensed is often imprecise, which can result in over or under dosing.

Applicators of this type have been disclosed in GB 1 248 636 A; EP 0 633 033 A; US 5 462 740 A; US 6 224 573 B1; and US 5 531 703 A. Document US 5 462 740 A discloses a cartridge 50, in which a plunger 60 is slidably housed. The cartridge can be filled with a variable amount of drug and expelled through a cannula 57 when the plunger is depressed. Document EP 0 263 976 A discloses, in combination, distinctive features that fall within the scope of the preamble of Claim 1.

Summary of the invention

In accordance with the present invention, there is provided a vaginal or rectal applicator comprising (a) a cylindrical body of the applicator, wherein the cylindrical body of the applicator is a circular member having an inner diameter and an outer diameter and a rounded tip. located at the proximal end of the applicator; (b) a plunger into which the plunger can be inserted in telescopic relationship into the barrel of the applicator; (c) a plunger tip, wherein the plunger tip is at the proximal end of the plunger; and (d) an applicator cap, wherein the applicator cap can be attached to and removed from the tip of the applicator barrel, characterized in that: the applicator barrel comprises a drug chamber that extends distally concentrically into the applicator barrel from an opening in the rounded tip at the proximal end of the applicator, wherein that of the drug has a diameter less than the inner diameter of the cylindrical body of the applicator and delimits a cavity having a small volume of 1 mL or less capable of containing said small volume of a pharmaceutical composition; and the tip of the plunger forms an airtight seal with the medication chamber and is configured to expel all of the pharmaceutical composition from the medication chamber.

It is possible in embodiments of the invention to provide vaginal or rectal applicators that are capable of accurately delivering small amounts of pharmaceutical compositions.

Likewise, it is a further possibility in embodiments of the invention to provide vaginal or rectal applicators for transvaginal or transrectal administration of pharmaceutical compositions for zonal administration.

Brief description of the figures

To enable a better understanding of the present invention, and to show how the invention can be carried out, reference will now be made, by way of example only, to the accompanying drawings, in which:

Figure 1A is a side view of the vaginal or rectal applicator assembly;

Figure 1B is a side view of the four main elements of the vaginal or rectal applicator assembly;

Figure 2A is a side view of the barrel of the applicator;

Figure 2B is a cross-sectional view of the applicator barrel;

Figure 2C is an end view of the rear end of the applicator barrel;

Figure 2D is a cross-sectional view of the tip of the applicator barrel;

Figure 3A is a side view of the plunger tip;

Figure 3B is a cross-sectional view of the end of the plunger and the tip of the plunger;

Figure 3C is an aerial view of the end of the plunger;

Figure 4A is an end view of the applicator cap;

Figure 4B is a side view of the applicator cap;

Figure 4C is a cross-sectional view of the applicator barrel tip and applicator cap; and Figure 4D is an enlarged cross-sectional view taken around lines 4-4 of Figure 4C.

Detailed description

Vaginal or rectal applicators intended for the administration of a small volume of a pharmaceutical preparation, that is, less than 1 mL, are disclosed herein. The administration of a small volume of a pharmaceutical preparation allows the transvaginal administration of the preparation to the area of ​​the upper vaginal vault or the rectum for the treatment of diseases and disorders of the woman's urogenital system, the cervix, the uterus, of the ovaries, the fallopian tubes and the peritoneal cavity and the inner abdomen. Rectal or vaginal applicators contain four main parts: an applicator barrel, a plunger, a plunger tip, and an applicator cap. The applicator works similar to a syringe. The applicator is rear-loaded with a pharmaceutical preparation with the plunger in the rearward position. The cap of the applicator is fixed to hermetically close the pharmaceutical preparation of the applicator. To use the applicator, the cap is removed, the applicator is positioned, and the plunger is depressed.

I. Assembly of the Vaginal or Rectal Applicator

As shown in Figures 1A and 1B, the vaginal or rectal applicator assembly (10) (also referred to herein as a "vaginal / rectal applicator") contains an outer tubular member or cylindrical body (15) of the applicator and an internal tubular member consisting of a plunger (20), which can be inserted in telescopic relation into the cylindrical body (15) of the applicator in order to expel a pharmaceutical composition. The vaginal / rectal applicator assembly (10) contains a plunger tip (25), which is located at the proximal end of the plunger (27), and forms an airtight seal with a drug chamber (50) located on the proximal exterior of the applicator barrel.

The vaginal / rectal applicator assembly (10) also contains an applicator cap (30), which is located at the tip of the applicator barrel (33) and constitutes an airtight seal with the applicator barrel. applicator. The vaginal / rectal applicator assembly is made from inert, pure, polymeric materials, such as polystyrene or polypropylene.

A. Cylindrical Body of Applicator

As shown in Figure 2A, the cylindrical body (15) of the applicator has a generic tube shape with a grip area (35) located at its distal end, a fin (40) located below the grip area, and an opening (45) located at its rounded tip (33). Figures 2B and 2C show that the barrel of the applicator is a thin-walled tube. The cavity at the tip of the tube is the drug chamber (50). The diameter of the drug chamber (50) is smaller than the outer diameter of the barrel of the applicator. The medicine chamber is large enough to hold a small volume of a pharmaceutical composition, which is less than 1 ml. In the preferred embodiment, the drug chamber is capable of holding 200 µΙ. of a pharmaceutical composition. Following the drug chamber is a barrier (55), which prevents the plunger from pushing past the drug chamber. After the plunger is

ES 2 345 656 T3 depressed, the barrier locks the plunger in position. In one embodiment the length from the fin to the tip of the applicator barrel is greater than or equal to 10.2 cm. Thus, when the vaginal or rectal applicator device is inserted into a patient, the tip of the applicator barrel is inserted no more than 10.2 cm into the vaginal cavity or is approximately 10.2 cm inside the vaginal cavity. Rectal administration of the length can be less than or equal to 10.2 cm. Alternatively, for some embodiments, a shorter applicator, with a length ranging from 2.5 to 5.1 cm, is useful. For example, for rectal administration, a length of 3.8 to 3.1 cm of a pharmaceutical composition to the anal canal is useful. Likewise, for applicators that are used to administer pharmaceutical compositions to children, an applicator with a shorter length, such as approximately 2.5 cm, is useful.

The diameter and shape of the cylindrical body of the applicator is large enough to prevent penetration of the vaginal wall / cervix or uterus. The tip of the applicator barrel is smooth, to facilitate insertion of the applicator barrel. The length of the drug chamber (the delivery stroke) is approximately 1.3 cm. This is a length in which the user can distinguish the location of the plunger from start to finish by noting that the drug is being delivered.

The flap (40) is wide enough to prevent over-insertion of the applicator barrel into the vagina and not injure the cervix. The cylindrical body of the applicator has a grip area (35) located behind the flap (40) to aid insertion and manipulation of the device.

B. Plunger and Plunger Tip

As shown in Figure 3B the tip (25) of the plunger surrounds the proximal end of the plunger (27). The plunger tip is designed to stop at the end of the applicator barrel so that the user can feel the stop and know that the full dose has been delivered. There is a space between the plunger and the barrel of the applicator to prevent excessive displacement of the plunger. The tip of the plunger forms an airtight seal with the drug chamber of the applicator barrel. The design of the plunger tip ensures that all of the pharmaceutical formulation has been expelled from the drug chamber delivered to the patient.

C. Applicator Cap

The applicator cap (30) has distinctive features designed to prevent insertion of the applicator into the vagina or rectum with the cap removed (see Figures 4A through D). For example, the cap (30) of the applicator is wider than the barrel (15) of the applicator to prevent its insertion into the vagina. The cap (30) of the applicator constitutes an airtight seal with the end of the cylindrical body (15) of the applicator (see Figures 4C and 4D) to prevent contamination.

II. Procedure for using the Vaginal or Rectal Applicator Assembly

The applicator is loaded from behind, that is, through the opening (45) located in the tip (33) of the cylindrical body (15) of the applicator, with a pharmaceutical preparation with the plunger in the retracted position. A small volume of pharmaceutical preparation, less than 1 mL, is placed inside the medicine chamber. In a preferred embodiment, 0.2 mL of a pharmaceutical preparation is placed inside the medicine chamber. The pharmaceutical preparations can be presented in the form of a powder, a gel, a cream, a lotion, a suppository, a module, a tablet, or a capsule. After filling the applicator, the applicator cap is attached to seal the pharmaceutical preparation within the applicator. To use the applicator, the cap is removed, the cap is placed into the vagina or rectum of the patient, and the plunger is depressed.

III. Vaginal or Rectal Applicator Mount Applications

The vaginal applicator can be used to administer pharmaceutical formulations to the vagina and rectum. The pharmaceutical compositions can be administered locally at the site of application or regionally over the surrounding area. As used herein, "locally" can refer to a generically topical application to the mucosal or endometrial surfaces of the vagina. As used herein, "regionally" refers to the reproductive organs and surrounding areas, which include the uterus, fallopian tubes, peritoneal space, pelvic cul-de-sac, ovaries, perineum, abdominal region; the rectovaginal region; and the urinogenital tract, including the bladder, urinary tract, and rectum. In the preferred method of application, drug formulations are administered transvaginally over the region of the superior regional vault for the treatment of diseases and disorders of the woman's urogenital system, of the cervix, of the uterus, of ovaries, fallopian tubes, and peritoneal cavity. In another embodiment, the formulations are administered locally into the vagina. Alternatively, the applicator can be used for rectal administration of pharmaceutical compositions, such as for administering the drug into the colon or anal canal.

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The applicator can be used to administer drugs for the treatment of diseases and disorders locally and regionally throughout the administration area. For example, the vaginal applicator can be used to treat urinary incontinence and endometriosis. The rectal applicator can be used to deliver a drug to the lower abdominal region to treat conditions such as colitis, eleitis, irritable bowel syndrome, Chron's disease, or ulcerative colitis.

The term "drug" can refer to any pharmaceutically active substance capable of being administered in a particulate formulation, which obtains the desired effect. Drugs can be organic, synthetic or natural compounds, proteins or peptides, oligonucleotics or nucleotides, or polysaccharides or sugars. The drugs can have multiple activities, which can be inhibitory or stimulatory, such as an antibiotic activity, an antiviral activity, an antifungal activity, a steroid activity, a cytotoxic or antiproliferative activity, an anti-inflammatory activity, an analgesic or anesthetic activity, or be used as a contrast or as other diagnostic agents. A description of the drug classes and species within each class can be found in Martindale, The Extra Pharmacopoeia, Thirty-First Ed., The Pharmaceutical Press, London (1996) and Goodman and Gilman, The Pharmaceutical Basis of Therapeutics, (9th Ed. ., McGraw-Hill Publishing company (1996).

Examples of compounds with steroid activity include progestins, estrogens, antiestrogens, and antiprogestins.

In a preferred embodiment, the drug is tanacol or gestrinone in a micro or nanoparticulate formulation. This can be accomplished by grinding the drug or atomizing the drug solution, for example, in a solvent extraction fluid, or with other standard techniques. Danazol or gestrinone can be presented as a complex with a cyclodextrin, eg, hydroxypropyl-jd-cyclodextrin (HPB).

In other embodiments, the drug is a polysaccharide, preferably a sulfated polysaccharide. Examples of sulfated polysaccharides include carrageenan, dextran sulfate, heparin, and fucoidin.

Unless otherwise stated, all technical and scientific terms used herein have the same meanings as those commonly used by a person skilled in the art to which the disclosed invention belongs. Although any method or similar or equivalent material described herein may be used, in the practice or evaluation of the present invention, the preferred methods, devices, and materials are as described.