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Microencapsulation and sustained release of biologically active polypeptidesRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 25 Or More Peptide Repeating Units In Known Peptide Chain StructureMicroencapsulation and sustained release of biologically active polypeptides description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070027085, Microencapsulation and sustained release of biologically active polypeptides. Brief Patent Description - Full Patent Description - Patent Application Claims
RELATED APPLICATIONS [0001] This application is a divisional of U.S. application Ser. No. 10/688,786, filed on Oct. 17, 2003, which claims the benefit of U.S. Provisional Application No. 60/419,388, filed Oct. 17, 2002. The entire teachings of the above applications are incorporated herein by reference. BACKGROUND OF THE INVENTION [0002] Numerous proteins and peptides, collectively referred to herein as polypeptides, exhibit biological activity in vivo, which renders them useful as medicaments in therapy. Many illnesses or conditions which can be treated with a biologically active polypeptide, require administration of a constant or sustained level of medicament to provide the most effective prophylactic and/or therapeutic effects. As such, administration of biologically active polypeptides can require frequent subcutaneous injections, which result in fluctuating levels of medicament and poor patient compliance. [0003] As an alternative, the use of biodegradable materials, such as polymers, encapsulating the medicament can be employed as a sustained delivery system. The use of biodegradable polymers, for example, in the form of microparticles or microcarriers, can provide a sustained release of medicament, by utilizing the inherent biodegradability of the polymer to control the release of the medicament thereby providing a more consistent, sustained level of medicament and improved patient compliance. [0004] However, these sustained release devices can exhibit high initial bursts of medicament and minimal release thereafter, resulting in serum drug levels outside the therapeutic window and/or poor bioavailability of the medicament. In addition, the presence of polymer, physiological temperatures and body response to the sustained release composition can cause the medicament to be altered (e.g., degraded, aggregated) thereby interfering with the desired release profile for the medicament. [0005] Further, methods used to form sustained release compositions can result in loss of activity of the medicament due to the instability of the medicament and the degradative effects of the processing steps. Degradative effects are particularly problematic when the medicament is a polypeptide. [0006] Therefore, a need exists for a means of administering biologically active polypeptides in a sustained fashion wherein the amount of polypeptide delivered is at therapeutic levels, and retains activity and potency for the desired period of release. SUMMARY OF THE INVENTION [0007] The present invention is based upon the unexpected discovery that when a specific combination of excipients, namely a sugar and salting-out salt, are present in a sustained release composition comprising a biocompatible polymer and a biologically active polypeptide that an improved release profile of active agent is achieved. Most notably, sustained release compositions having this specific combination of excipients exhibit an increase of bioavailability of the polypeptide over compositions lacking the specific combination of excipients, thereby resulting in an improved sustained release composition which can deliver therapeutic levels of polypeptide for a desired period. In addition, the sustained release compositions having this specific combination of excipients can exhibit a reduced lag phase which can provide for a smoothing out of the release profile and can contribute to an increase in the amount of agent released. [0008] This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide, a sugar and a salting-out salt. [0009] The method of the invention, for forming a composition for the sustained release of biologically active polypeptide, includes dissolving a biocompatible polymer in a polymer solvent to form a polymer solution, and combining a biologically active polypeptide, sugar and salting-out salt with the polymer solution. The biologically active polypeptide, sugar and salting-out salt can be combined with the polymer solution either alone or in a premixed form. The biologically active polypeptide, sugar and salting-out salt can be combined with the polymer solution either as solids, liquids or suspensions. It is understood that the method of combining the polymer, active and excipients can be performed in any order. [0010] The method of using the sustained release composition of the present invention comprises providing a therapeutically effective blood level of biologically active polypeptide, in a patient for a sustained period by administering to the patient a dose of the sustained release composition described herein. [0011] In a particular embodiment, the sustained release composition has incorporated therein a hormone, particularly an anti-diabetic or glucoregulatory peptide, for example, GLP-1, GLP-2, exendin-3, exendin-4 or agonists, analogs or derivatives thereof and the composition is administered in a therapeutically effective amount to treat a patient suffering from diabetes mellitus, impaired glucose tolerance (IGT), obesity, cardiovascular (CV) disorder or any other disorder that can be treated by one of the above polypeptides or derivatives, analogs or agonists thereof. [0012] The sustained release composition of the invention overcomes the problem of lack of acceptable bioavailability of the incorporated biologically active polypeptide which can occur when the specific combination of sugar and salting-out salt is not present in the sustained release composition. Further, loss of activity of the biologically active polypeptide due to instability and/or chemical interactions between the biologically active polypeptide and other components which are contained in or used in formulating the sustained release composition, can be minimized. [0013] The advantages of the sustained release formulation for biologically active molecule as described herein include increased patient compliance and acceptance by eliminating the need for repetitive administration, increased therapeutic benefit by eliminating fluctuations in active agent concentration in blood levels by providing a desirable release profile, and a potential lowering of the total amount of biologically active polypeptide necessary to provide a therapeutic benefit by reducing these fluctuations. BRIEF DESCRIPTION OF THE DRAWINGS [0014] FIG. 1 a graph of plasma levels (pg/mL) in rats of exendin-4 versus time in days post administration for the selected microparticle formulations. [0015] FIG. 2A is a graph of % Native Exendin-4 versus time in days for the described stability studies. [0016] FIG. 2B is a graph of % Native Exendin-4 versus time in days for the described stability studies. [0017] FIG. 3 is a graph of % Native Exendin-4 versus time in days for the described stability studies. [0018] FIG. 4 is a graph of plasma levels (pg/mL) in rats of exendin-4 versus time in days post administration for the selected microparticle formulations. [0019] FIG. 5 is a graph of plasma levels (pg/mL) in rats of exendin-4 versus time in days post administration for the selected microparticle formulations. [0020] FIG. 6 is a graph of plasma levels (pg/mL) in rats of exendin-4 versus time in days post administration for the selected microparticle formulations. Continue reading about Microencapsulation and sustained release of biologically active polypeptides... 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