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Sustained release latanoprost implant

a technology of latanoprost and implant, which is applied in the field of biodegradable intraocular implants, can solve the problems of extremely difficult molecule incorporation into biodegradable implants

Inactive Publication Date: 2012-11-01
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0035]The extruded intraocular implant (i.e., fiber) may further comprise a polyethylene glycol (PEG). The PEG can act as a plasticizing agent, making it possible to extrude the implant (i.e, to form the fiber) at temperatures lower than might otherwise be possible in the absence of the PEG. Lower extrusion temperatures are desirable to preserve latanoprost activity.
[0065]Another embodiment is a method of fabricating an intraocular implant comprising a thin film of latanoprost in a biodegradable polymer matrix by solvent casting, the method comprising dissolving one or more biodegradable polymers and latanoprost in an appropriate organic solvent, casting said solution onto a suitable substrate and removing said solvent to recover a thin film of latanoprost in a biodegradable polymer matrix. In certain embodiments the solvent is selected from the group consisting of dichloromethane, ethanol, octanol, chloroform, acetone and acetonitrile. In certain embodiments the solution comprises from 10 to 75% solids, wherein said solids comprise latanoprost, polymer and other components which are useful for modifying the release of latanoprost from the resulting film and / or plasticizers of said polymer which contribute to the flexibility of the film.

Problems solved by technology

However, its physicochemical properties make it an extremely challenging molecule to incorporate into a biodegradable implant.

Method used

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  • Sustained release latanoprost implant
  • Sustained release latanoprost implant
  • Sustained release latanoprost implant

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0110]

TABLE 1Latanoprost Containing Film Formulationsw / w, %ResomerResomerResomerResomerFormulation NoLatanoprostR208R203SRG752SRG755SR-2007-8933-16630350035R-2007-8933-16730350350R-2007-8933-16830353500R-2007-8933-16930035035R-2009-9606-01430200500R-2009-9606-01530350350R-2009-9606-01630500200R-2009-9606-01730600100

[0111]Release studies were performed in triplicates as follows. The dried film was cut using 4-mm biopsy punch (approximately 2.0-mg), and was placed into a 10-mL vial containing 0.01M phosphate buffered saline (pH 7.4)+0.1% Triton X100. The samples were then transferred into a shaking water bath set at 37° C. and 50 rpm. At various time-points, the solution was removed and analyzed by HPLC for the amount of released latanoprost. The removed solution is replaced with fresh phosphate buffered saline solution. Drug release profiles are shown in FIGS. 1A-C.

[0112]The film-shaped implants made by solvent casting can be cut to any shape and dimension. One example is a disc shap...

example 2

[0113]This example prepares an extruded solid polymer implant containing latanoprost. While the above discussion relates mainly to the problems of incorporating latanoprost in a film oily drug substances (DS) are also very difficult to incorporate into hot-melt extruded implants because they exude the oily DS when heated. It is important to keep the extrusion temperature as low as possible to avoid loss and degradation of the DS. This can be overcome by using a select combination of polymers and a plasticizer like PEG that are compatible with the drug substance. The oily DS and PEG plasticize the polymers to a degree that allows the mixture to be extruded at a temperature where the DS is not degraded or lost. Suitable formulations are shown in Table 2.

[0114]The polymer implants were made by hot-melt extrusion using a mechanically driven ram microextruder, but they can also be made by direct compression or solvent casting. The implants are rod-shaped, but they can be made into any ge...

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Abstract

The present invention provides a sustained release, biodegradable intraocular latanoprost implant for reducing elevated intraocular pressure in an individual in need thereof. The implant can be configured as a film (e.g., a rolled film) or extruded filament, either of which can be inserted into the eye of the individual to provide for extended release of latanoprost for several days. Upon insertion into the eye, a rolled film may unroll to provide a film having a high surface area to volume ratio for drug diffusion.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Application No. 61 / 480,657, filed Apr. 29, 2011, and U.S. Provisional Application 61 / 480,630, filed Apr. 29, 2011. The contents of each of these provisional applications are hereby incorporated by reference.BACKGROUND OF THE INVENTION[0002]1. Field of the Invention[0003]The present invention relates to biodegradable intraocular implants that provide for the sustained release of latanoprost, and to methods of making these implants, and to methods of using these implants to reduce elevated intraocular pressure in individuals in need thereof.[0004]2. Summary of the Related Art[0005]Latanoprost is a prostaglandin F2α analogue which is indicated in the treatment of open-angle glaucoma or ocular hypertension in patients who are intolerant of other intraocular pressure (IOP)—lowering medications or insufficiently responsive (i.e., failed to achieve target IOP after multiple measurements ove...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61F2/14A61P27/02A61K31/215
CPCA61K9/0051A61K9/7007A61K31/216A61K47/34A61F9/0017A61K31/5575A61P27/02A61P27/06
Inventor GHEBREMESKEL, ALAZAR N.SPADA, LON T.
Owner ALLERGAN INC
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