FORM 2
THE PATENTS ACT, 1970
(39 of 1970)
&
The Patents Rules, 2003
PROVISIONAL SPECIFICATION (See section 10 and rule 13)
POLYMER-BASED CONTROLLED RELEASE DELIVERY SYSTEM FOR
PROTEINS AND PEPTIDES


Intas Biopharmaceuticals Limited
An Indian company having its registered office at:
Plot No: 423/P/A/GIDC
Sarkhej-Bavla Highway
Moraiya, Tal.: Sanand
Ahmedabad-382 210
Gujarat, India

The following specification describes the invention.


INTRODUCTION TO THE INVENTION
The present invention relates to a composition and method of preparing biodegradable polymer-based delivery system, loaded with peptides and proteins as drugs for its sustained and controlled release over an extended period of time.
Two general properties of microparticles can be distinguished - microcapsules and microspheres. Microspheres are defined as microparticles in which the drug substance is either homogeneously dissolved or dispersed in a polymeric matrix. Microparticles are particularly interesting for development of control or prolong release dosage forms. They play an important role as a drug delivery system to improve bioavailability of conventional drugs over extended periods.
Pharmaceutical application of microspheres involves different routes of administration among them oral, pulmonary and parenteral delivery after reconstituting lyophilized formulation in appropriate solvent, or an aqueous suspension to be administered directly. The present invention is mainly limited to the parenteral route of administration.
United States patent no. 5716644 describes a composition and methods of forming and using the said composition, for the sustained release of non-aggregated, biologically active, erythropoietin (EPO), wherein the polymeric matrix of a biocompatible polymer entraps biologically active, aggregation-stabilized EPO. These particles are dispersed within the biocompatible polymer. This invention provides a composition for the sustained release of biologically active EPO, by dissolving the biocompatible polymer in a solvent to form a solution, dispersing particles of biologically active, aggregation-stabilized EPO in the polymer solution, and then solidifying the polymer to form a polymeric matrix containing a dispersion of said EPO particles. The method for using a
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composition of the invention is a method for providing a therapeutically effective blood level of biologically active, non-aggregated erythropoietin in subjects for a sustained period. In this method, subjects are administered an effective dose of the sustained release composition of the present invention.
SUMMARY OF THE INVENTION
The present invention relates to a composition and method of preparing biodegradable polymer-based delivery system, loaded with peptides and proteins as drugs for its sustained and controlled release over an extended period of time.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to a composition and method of preparing biodegradable polymer-based delivery system, loaded with peptides and proteins as drugs for its sustained and controlled release over an extended period of time. The method of the present invention is found to be economically viable and easy to prepare, which is different from that of the prior art.
In an embodiment of the present invention the sustained release composition comprises a polymeric matrix of biocompatible and biodegradable polymers and copolymers thereof; surface active agents, co-surfactants and mixtures thereof; stabilizers; cryoprotectants; salting-out salts; and pharmaceutically acceptable buffers optionally with an anti-oxidant; prepared by using different organic solvents or mixtures of organic solvents.
In one embodiment of the present invention, wherein the said composition having the particle size, ranging from 1nm (nano meter) to 500 urn (micro meter).
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In one embodiment of the present invention, wherein polymeric matrix of biocompatible and biodegradable polymers are selected from poly lactic acid/s, poly glycolic acid/s, poly lactic co-glycolic acid/s and copolymers thereof.
In another embodiment of the present invention, wherein stabilizers are selected from monosaccharides, disaccharides and mixtures thereof.
In yet another embodiment of the present invention, wherein the cryoprotectant are disaccharides.
In another embodiment of the present invention, wherein the salting-out salts are selected from the group consisting of salts containing one or more of the cations Mg+2, Li+, Na+, K+, Zn+2 and NH4+; and also contain one or more of the anions SO4+2, HPO4", CI", NO3", CIO3", I" and OH'.
In yet another embodiment of the present invention further comprises of pharmaceutically acceptable buffer having pH between 3 to 9.
Jn another embodiment of the present invention, wherein organic solvents are selected from a group of dichloromethane, ethyl acetate, acetone, chloroform, tetrahydrofuran and mixtures thereof.
The present invention also provides the method of producing a composition for the sustained release of biologically active proteins and peptides, by dissolving a biocompatible polymer in a organic solvent to form a polymer solution, dispersing biologically active proteins and peptides in the polymer solution, and then solidifying the polymer to form a polymeric matrix to give a stable formulation.
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And the composition of the present invention is for sustained and controlled release of a drug over an extended period of time through parental administration.
Dated 14th day of August 2008 For Intas Biopharmaceuticals Limited

Jayanthi M Executive IPM
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