Aquespheres, their preparation and uses thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

Reexamination Certificate

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C514S059000, C536S045000, C424S489000, C424S490000

Reexamination Certificate

active

06998393

ABSTRACT:
This invention provides method for sustained release delivery of structurally delicate agents such as proteins and peptides. Using a unique emulsion system (Stable polymer aqueous-aqueous emulsion), proteins and peptides can be microencapsulated in polysacchride glassy particles under a condition free of any chemical or physical hazard such as organic solvents, strong interfacial tension, strong shears, elevated temperature, large amount of surfactants, and cross-linking agents. Proteins loaded in these glassy particles showed strong resistance to organic solvents, prolonged activity in hydrated state, and an excellent sustained release profile with minimal burst and incomplete release when being further loaded in degradable polymer microspheres. This invention provides a simple yet effective approach to address all the technical challenges raised in sustained release delivery of proteins.

REFERENCES:
patent: 5716644 (1998-02-01), Zale et al.
patent: 9640071 (1996-10-01), None
Cleland, J. L. et al, “Stable Formulations of Recombinant Human Growth Harmone and Interferon-gamma for Microencapsulation in Biodegradable Microspheres”, Pharmaceutical Research, 1996, 13(10), 1465-1475).
A. Berthold et al “Preparation and characterization of chitosan microspheres as drug carrier for prednisolone sodium phosphate as model antiinflammatory drugs”. Journal of Controlled Release, 1996, 39, 17-25.
U.S. Appl. No. 09/886,555, Jin, Tuo, Li Chen, and Hua Zhu, for Stable Polymer Aqueous/Aqueous Emulsion Sylstem and Uses Thereof (2001). [Exhibit 3].
Langer, R., Folkman, J., “Polymers for the sustained release of proteins and other macromolecules,” Nature 263, 797-800 (1976). [Exhibit 4].
CAS, Results of search on chemical abstracts on the subject of sustained release of proteins based on degradable polymers. (2002). [Exhibit 5].
Weert, M. v., Hennink, W. E., Jiskoot, W., “Protein instability in poly(lactic-co-glycolic acid) microprarticles,” Pharm. Res. 17, 1159-1167 (2000). [Exhibit 6].
Bartus, R. T., Tracy, M.A., Emerich, D.F., Zale, S.E., “Sustained delivery of proteins for novel therapeutic products,” Science 281, 1161-1162 (1998). [Exhibit 7].
Burke, P. A., “Controlled release protein therapeutics: effects of process and formulation on stability,” Handbook of pharmaceutical controlled release technology, Marcel Dekker, 661-692 (2000). [Exhibit 8].
Cleland, J. L., Jones J.S., “Stable formulations of recombinant human growth hormone and interferon-γ for microencapsulation in biodegradable mircospheres,” Pharm. Res. 13, 1464-1475 (1996). [Exhibit 9].
Johnson, O. L., “The stabilization and encapsulation of human growth hormone into biodegradable microspheres,” Pharmaceutical Research 14, 730-735 (1997). [Exhibit 10].
Cunningham, B. C., Mulkerrin, M. G., Wells, J. A., “Dimerization of human growth hormone by zinc,” Science 253, 545-548 (1991). [Exhibit 11].
Sanchez, A., Villamayor, B., Guo, Y., Mclver, J., Alonso, M. J., “Formulation strategies for the stabilization of tetanus toxoid in poly(lactide-co-glycolide) microspheres,” Intern. J. Pharm. 185, 255-266 (1999). [Exhibit 12].
Schwendeman, S. P., Tobio, M., Jaworowicz, M., Alonso, M. J., Langer, R., “New strategies for the microencapsulation of tetanus vaccine,” J. Microencapsulation 15, 299-318 (1998). [Exhibit 13].
Morlock, M., Koll, H., Winter, G., Kissel, T., “Microencapsulation of rh-erythropoietin, using biodegradable poly(D,L-lactide-co-glycolide):protein stability and the effects of stabilizing excipients,” European Journal of Pharmaceutics and Biopharmaceutics 43, 29-36 (1997). [Exhibit 14].
Yoshioka, S., Aso, Y., Kojima, S., “Dependence of the molecular mobility and protein stabilitiy of freeze-dried γ-globulin formulations on the molecular weight of dextran,” Pharmaceutical Research 14, 736-741 (1997). [Exhibit 15].
Weert, M. v. d., Hof, R. v., Weerd, J. v. d., Heeren, M.A., Posthuma, G., Hennink, W. E., Crommelin D. J. A., “Lysozyme distribution and conformation in a biodegradable polymer matrix as determined by FTIR techniques,” J. Controlled Release 68, 31-40 (2000). [Exhibit 16].
Morita, T., Horikiri, Y., Suzuki, T., Yoshino, H., “Preparation of gelatin microparticles by co-lyophilization with poly(ethylene glycol): characterization and application to entrapment into biodegradable microspheres,” International Journal of Pharmaceutics 219, 127-137 (2001). [Exhibit 17].
Maa, Y.-F., Nguyen, P-A., Hsu, S. W., “Spray-drying of air-liquid interface sensitive recombinant human growth hormone,” J. Pharm. Sci., 87, 152-159 (1998). [Exhibit 18].
Morita, T., Horikiri, Y., Yamahara, H., Suzuki, T., Yoshino, H., “Formation and isolation of spherical fine protein microparticles through lyophilization of protein-poly(ethylene glycol) aqueous mixture,” Pharm. Res. 17, 1367-1373 (2000). [Exhibit 19].
Park, T. G., Lee, H.Y., Nam, Y.S., “A new preparation method for protein loaded poly(D,L-lactic-co-glycolic acid) microspheres and protein release mechanism study,” J. Controlled Release 55, 181-191 (1998). [Exhibit 20].
Franssen, O., Hennink, W. E., “A novel preparation method for polymeric microparticles without the use of organic solvents,” Intern. J. Pharm., 168, 1-7 (1998). [Exhibit 21].
Schwendeman, S. P., Cardamone, M., Brandon, M. R., Klibanov, A., Langer, R., “Stability of proteins and their delivery from biodegradable polymer microspheres,” S. C. H. Bernstein, Ed.,Microparticulate Systems for the Delivery of Proteins and Vaccines,(Mercel Dekker, New York, 1996), vol. 77. [Exhibit 22].
Liu, W. R., Langer, R., Klibanov, A. M., “Moisture-induced aggregation of lyophilized proteins in the solid state,” Biotech. Bioeng. 37, 177-184 (1991). [Exhibit 23].
Bittner, B., Morlock, M., Koll, H., Winter, G., Kissel, T., “Recombinant human erythropoietin (rhEPO) loaded poly(lactide-co-glycolide) microspheres: infludence of the encapsulation technique and polymer purity on microsphere characteristics,” Eur. J. Pharm. Biopharm. 45, 295-305 (1998). [Exhibit 24].
Takahata, H., Lavelle, E.C., Coombes, A.G.A., Davis, S.S., “The distribution of protein associated with poly(DL-lactide co-glycolide) microparticles and its degradation in simulated body fluids,” J. Controlled Release 50, 237-246 (1998). [Exhibit 25].

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