Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1994-11-04
1998-06-16
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424464, 424476, 424480, 424486, 424487, 424488, 514786, A61K 936, A61K 942, A61M 3100, A61F 200
Patent
active
057666199
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 PCT/FR 93/00433 filed May 5, 1993.
FIELD OF THE INVENTION
The present invention relates to pharmaceutical dosage forms intended for the ocular administration of active ingredients that it is desired to deliver in a more or less prolonged fashion, as well as to a process for preparing the dosage forms.
BACKGROUND OF THE INVENTION
The entry of active ingredients into the eye takes place essentially via the conjunctiva, which is highly vascularized. Entry via the cornea is hotly disputed; it is considered to be very selective and influenced by many factors. The epithelium is considered to play the part of a barrier.
The secretion and drainage of the lacrimal fluid bring about a rapid elimination of all conventional medicinal dosage forms applied to the surface of the eye. In the case of eyewashes, 20% of the drop instilled may be retained by the eye, and five minutes after administration only 8% of the 20% remains in the conjunctival cul-de-sac. This is due to the renewal of lacrimal fluid, which can be enhanced as a result of the irritation caused by the drop. The outcome of this brief contact time, or else of binding to proteins, is that only a small fraction enters the eye. Conventional means such as increasing the viscosity of the eyewashes, the addition of surfactants, oily solutions or ointments are relatively ineffective.
In addition to prolonging the action, the new technologies developed in recent years seek to provide other advantages, such as a steady concentration of active principles in the lacrimal fluid for a more sustained pharmacological response, a decrease in side effects and a less exacting dosage regimen, which should improve patient compliance.
With this aim in view, insoluble extraocular implants of the Ocusert.RTM. type appeared in 1973 in the USA. They take the form of two insoluble, crimped semipermeable membranes containing the solution of medicinal active principles that, over a few days, are released slowly into the conjunctival cul-de-sacs. However, this type of product gives rise to many problems of tolerance that limit their use.
Extraocular implants then underwent development. They form the subject of a Pro-Pharmacopea monograph in April-May 1988 (No. 500) under the name of ophthalmic insert. Hitoschi Ozawa (Biomaterials, vol. 4, July 1983) studied the value of ocular inserts impregnated with antibiotics (including erythromycin) in the treatment of trachoma in rabbits, and their behavior in vitro. Despite their satisfactory activity in vivo, soluble or biodegradable inserts have, however, the drawback of being able to leave debris and of giving rise to disorders of vision resulting from dissolution of the polymer. For this reason, their use in the context of a surgical procedure seems to be ruled out.
SUMMARY OF THE INVENTION
The use of an insoluble solid dosage form capable of being readily removed from the eye after releasing the active principles would be preferable. In addition, for some surgical operations on the eye, it is necessary to maintain the eye in a state of mydriasis and cycloplegia for several hours or even days.
Thus, the subject of the present invention is a pharmaceutical dosage form intended for ocular administration, characterized in that it possesses, from the inside to the outside: active ingredient,
BRIEF DESCRIPTION OF THE DRAWING
FIG. 1 shows a curve of cumulative percentages of active ingredient released for tablets of Formula 5, in relation to time.
DETAILED DESCRIPTION OF THE INVENTION
The polymer or polymers constituting the matrix of the present invention form a network that confines the molecules of active principle and release them gradually. A portion of the glycerides forming the first layer of coating can be present within the matrix. They provide for a lubricant role during tabletting. The amount thereof is adjusted so that they distribute at the surface of the core and form an even and homogeneous layer, of variable thickness in accordance with the rate of release of the active principle that is des
REFERENCES:
patent: 3630200 (1971-12-01), Higuchi
patent: 3828777 (1974-08-01), Ness
patent: 3863633 (1975-02-01), Ryde et al.
patent: 3986510 (1976-10-01), Higuchi et al.
Handbook of Pharmaceutical Excipients, Second Edition, 1994, pp. 211, 229 & 231, 362-366, and 2249.
Aiache Jean-Marc
Serpin Gilbert
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