Systems for the controlled release of pilocarpine

Details Systems for the controlled release of pilocarpine Systems for the controlled release of pilocarpine

1996-03-26

1999-02-09

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424443, 424446, 424447, 424448, A61F 1300, A61L 1516

Patent

active

058690867

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a transdermal therapeutic system for the controlled pilocarpine release to the skin having a backing layer and a pressure sensitive adhesive reservoir layer, to a process for the production of this system, and to the use of a capsule made of a semipermeable membrane for the controlled release of pilocarpine ((3S, 4R)-3-ethyl-4,5-dihydro-4-(1-methyl-1H-imidazole-5-ylmethyl)-2(3H)-furanon e).
Pilocarpine is an alkaloid which is recovered from different kinds of the genus pilocarpus (Rutaceae (Rutales)), e.g., Pilocarpus Jaborandi Holmes etc., and has been used in ophthalmology for more than 100 years. Pilocarpine drops are used by patients suffering from glaucoma; they have to be instilled into the conjunctival sac several times a day. In glaucoma there is an increased intraocular pressure which may result in damages of the retina and the optic nerve if left untreated. If applied to the eye, pilocarpine causes a contraction of the pupil, the outflow of the aqueous humor in the eye is facilitated and thus the intraocular pressure reduced. One application persists for 4 to 6 hours so that several applications per day are required to lower the intraocular pressure throughout the day. For this reason an uncontrolled increase in the pressure values particularly occurs in the early morning due to the subsiding action of the dosage instilled in the evening and because of the fact that the intraocular pressure physiologically increases at this time of the day.
Another disadvantage of this form of application is the fact that older patients, who mainly suffer from glaucoma, find it difficult to instil the eye drops and that--due to the repeated instillation--the patients are reminded of their complaints several times a day and cannot dissociate themselves from their disease, resulting in mental strain. Moreover, it is disadvantageous that pilocarpine eye drops--immediately after their administration--result in difficulties in focussing accompanied by impairment of vision.
This problem led to the development of a system similar to contact lenses and containing pilocarpine, described in U.S. Pat. No. 4,144,317. This system known under the trade name Ocusert.RTM. was worn in the conjunctival sac for seven days. Although it met all requirements, there were cases where Ocusert.RTM. got out of place within the conjunctival sac and could hardly be removed, therefore the drug had to be withdrawn from the market.
Accordingly, there is a demand for pharmaceutical products lowering the intraocular pressure without applying pilocarpine directly to the eye.
Accordingly, it is the object of the present invention to provide a pharmaceutical product for the systemic release of pilocarpine for lowering the intraocular pressure while simultaneously suppressing the side effects.
The above object is achieved by a transdermal therapeutic system according to the invention and by the semipermeable capsule according to the invention. Particularly preferred embodiments of the present invention and to a process for the production of the transdermal therapeutic system are disclased.
The present invention relates to a transdermal therapeutic system having a backing layer and a pressure sensitive adhesive reservoir layer for the controlled active substance release to the skin; the system is characterized by the fact that the reservoir layer comprises a polymeric material, a plasticizer, and a pilocarpine base or one of its pharmaceutically acceptable salts.
Furthermore, the present invention relates to using a capsule made of a semipermeable membrane for the controlled release of pilocarpine, which comprises pilocarpine in encapsulated form and has an aperture in the capsular material, for the treatment of glaucoma.
This solution is surprising all the more, since it is accepted that only extremely high pilocarpine doses--if at all--are suitable to lower the intraocular pressure if the drug is not applied locally, i.e., as eye drops or ointments, or as ocular system, but is administered systemically. Because of it

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Kuschinsky et al., Kurzes Lehrbuch der Pharmakologie und Toxikologie, 9th edition (George Thieme Verlag. Stuttgart, New York 1981, p. 54.

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