Title:  Buccal drug delivery system for use in male contraception

United States Patent:  6,180,682

Assignee:  Place; Virgil A. (Kawaihae, HI)

Filed:  January 26, 1999

A buccal dosage unit is provided for administering a contraceptive composition to fertile mammalian males. The buccal dosage unit comprises a an androgenic agent and a progestin in a polymeric carrier that bioerodes and provides for delivery of the active agents throughout a predetermined drug delivery period that is preferably in the range of approximately 8 to 24 hours.

SUMMARY OF THE INVENTION

Accordingly, it is a primary object of the invention to address the aforementioned need in the art by providing a drug dosage unit for buccally administering to a male individual a pharmaceutical composition comprising an androgenic agent and a progestin.

It is another object of the invention to provide a method for effecting contraception in a male individual by buccally administering a contraceptive composition using the aforementioned drug dosage unit.

Additional objects, advantages and novel features of the invention will be set forth in part in the description which follows, and in part will become apparent to those skilled in the art upon examination of the following, or may be learned by practice of the invention.

Accordingly, in a first embodiment, then, a pharmaceutical composition is provided in the form of a simple, compact buccal dosage unit comprising therapeutically effective amounts of an androgenic agent and a progestin in a bioerodible polymeric carrier, wherein the carrier is such that it enables the dosage unit to adhere to the buccal mucosa. Following application to the buccal mucosa, gradual and complete erosion of the unit occurs over a predetermined time period, thus providing drug delivery throughout that time period. In a preferred embodiment, the dosage unit contains only the active agents to be administered and the polymeric carrier. However, other components, particularly a lubricant, may be incorporated to facilitate manufacture of the unit or if otherwise found to be necessary or desirable. The buccal dosage units are typically far smaller than conventional buccal delivery systems--the present tablets are on the order of 5-20 mg, typically 10-15 mg--and do not require a plurality of excipients, disintegrants, adhesives, or the like, nor are fragrances or permeation enhancers necessary. Accordingly, the novel dosage units are more comfortable than conventional systems because of their compact size. The novel units are also highly effective in providing effective contraceptive levels of steroidal agents. While the dosage units are designed to erode and thus deliver the active agents over a predetermined time period that is generally in the range of about 8 hours to about 24 hours, 12-hour dosage units are preferred, such that the individual receiving drug therapy can conveniently use two dosage units in a 12-hour period, enabling two "breaks" for dental hygiene or the like during the day. In this regard, the dosage units can be applied to an area of a subject's buccal mucosa such that the subject can eat and/or drink with the unit in place.

In another embodiment of the invention, a method is provided for effecting contraception in a mammalian male, comprising buccally administering the aforementioned contraceptive composition comprising an androgenic agent and a progestin. The composition is administered through the buccal mucosa by affixing a dosage unit as provided herein to the buccal mucosa and allowing the dosage unit to remain in place until erosion is complete.

In an additional embodiment of the invention, a kit is provided to assist an individual in buccal drug adminstration. Generally, the kit includes the following components: a buccal dosage unit comprising a contraceptive composition and a bioerodible polymeric carrier; a container housing the dosage unit prior to use; and written instructions for carying out administration of the composition

Claim 1 of 40 Claims

What is claimed is:

1. A buccal dosage unit for use in male contraception, comprising a compressed tablet of a polymeric carrier which adheres to the oral mucosa and erodes upon sustained contact therewith over a period of approximately eight to twenty-four hours, and, incorporated in the polymeric carrier, a contraceptive composition comprising an androgenic agent and a progestin, wherein the weight of the tablet is in the range of approximately 5 mg to 20 mg.

____________________________________________
If you want to learn more about this patent, please go directly to the U.S. Patent and Trademark Office Web site to access the full patent.