Drug delivery system and method of making the same
Patent 4897268 Issued on January 30, 1990. Estimated Expiration Date: August 3, 2007. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
A compatible, biodegradable microcapsule delivery system for active ingredients, including hormonally active peptides, proteins, or other bioactive molecules, and a method of making the same. The ingredients are encapsulated in biodegradable copolymer excipients of varying mole ratios and the blend of the microcapsules are administered to an animal. Delivery of the ingredient occurs over a prolonged period of time at a constant rate as a result of the varying break-down rates of the copolymer excipients.
Other References
Sanders et al., Journal of Pharmaceutical Sciences, vol. 73, pp. 1294-1296, Sep. 1984
Redding et al., Proc. Nat'l Acad. Sci U.S.A., vol. 81, pp. 5845-5848, Sep. 1984
Speiser, "Microencapsulation by Coacervation, Spray Encapsulation, and Nanoencapsulation," In Microencapsulation, J. R. Nixon (ed.) Marcel Dekker (1976)
Sanders et al., "Controlled Delivery of an LHRH Analogue from Biodegradable Injectable Microspheres," J. Controlled Release 2: 187 (1985)
Redding et al., "Long-Acting Delivery Systems for Peptides: Inhibition of Rat Prostate Tumors by Controlled Release of [D-trp6 ] Luteinizing Hormone-Releasing Hormone from Injectable Microcapsules," Proc. Nat'l Acad. Sci. (U.S.A.) 81: 5845 (1984)
Sanders et al., "An Injectable Biodegradable Controlled Release Delivery System for Nafarelin Acetate," in LHRH and its Analogues, Labrie, Belanger and Dupont (eds.) pp. 53-62. (1984)
Kent et al., "Microencapsulation of the Peptide Nafarelin Acetate for Controlled Release," in Long-Acting Contraceptive Delivery Systems, Program for Applied Research on Fertility Regulation Series, pp. 169-179 (1983)
Schally, "Current Status of Antagonistic Analogs of LH-RH as a Contraceptive Method in the Female," Research Frontiers in Fertility Regulation (5): 1 (Jul. 1983)
Mason et al., "Hydrolytic Degradation of Poly-DL-(Lactide)," Polym. Sci. Technol. 14: 279 (1981)
Beck et al., "Biodegradable Microsphere Contraceptive System, " Paper Presented at the 4th Int'l Meeting on Fertility Control, Genova, Italy (Mar. 6-8, 1980)
Beck et al., "Long-Acting Steroidal Contraceptive Systems," Research Frontiers in Fertility Regulation (Northwestern University 1: 1 (Jul. 1980)
Lewis et al., "Sustained Release of Antibiotics from Biodegradable Microcapsules," 7th Int'l Symp. on Controlled Release of Bioactive Materials, Ft. Lauderdale, Fla. (Jul. 28-30, 1980)
Beck et al., "New Long-Acting Injectable Microcapsule Contraceptive System," Am. J. Obstet. Gyn. pp. 419-426 (Oct. 1, 1979)
Beck et al., "A New Long-Acting Injectable Microcapsule System for the Administration of Progesterone," Fert. and Steril. 31(5): 545 (1979)
Chang, "Biodegradable Semipermeable Microcapsules Containing Enzymes, Hormones, Vaccines, and other Biologicals," J. Bioeng. 1: 25 (1976)
Yolles et al., "Long Acting Delivery Systems for Narcotic Antagonists II: Release Rate of Naltrexone from Poly(Lactic Acid) Composites," J. Pharm. Sci. 64 (2): 348 (1975)
Sanders et al., "Prolonged Controlled-Release of Nafarelin, Luteinizing Hormone-Releasing Hormone Analogue, from Biodegradable Polymeric Implants: Influence of Composition and Molecular Weight of Polymer," J. Pharm. Sci. 75(4): 356 (1986)
Vickery, "Comparisons of the Potential Utility of LHRH Agonists and Antagonists for Fertility Control," J. Steroid Biochem. 23: 779 (1985)
Schally et al., "Inhibition of Prostate Tumors by Agonistic and Antagonistic Analogs of LH-RH," The Prostate 4: 545 (1983)
Langer, "Controlled Release of Macromolecules," Chemtech pp. 98-105, (Feb. 1982)
Privalova et al., "Macrokinetics of Degradation of Polyglycolide Threads in Aqueous Solutions of Electrolytes," Polymer Sci. U.S.S.R.) 22(8): 2074 (1980)
Pitt et al., "Biodegradable Drug Delivery Systems Based on Aliphatic Polyesters: Application to Contraceptives and Narcotic Antagonists," Naltrexone: Research Monogram 28 (1980)
Wise et al., "Long Term Controlled Delivery of Levonorgestrel in Rats by Means of Small Biodegradable Cylinders," J. Pharm. Pharmac. 32: 399 (1980)
Benagiano et al., "Biodegradable Systems for the Sustained Release of Fertility-Regulating Agents," J. Steroid Biochem. 11: 449 (1979)
Gliding et al., "Biodegradable Polymers for Use in Surgery-Polyglycolic/Poly(Actic Acid) Homo- and Copolymers: I," Polymer 20: 1459 (1979)
Moiseev et al., "The Specificity of Polymer Degradation in the Living Body," J. Polymer Sci: Polymer Symposium 66, pp. 269 (1979)
Pitt et al., "Sustained Drug Delivery Systems II: Factors Affecting Release Rates from Poly(&3xb5;-Caprolactone) and Related Biodegradable Polyesters," J. Pharm. Sci. 68(12): 1534 (1979)
Pitt et al., "Sustained Drug Delivery Systems I: The Permeability of Poly(&3xb5;-Caprolactone), Poly(DL-Lactic acid), and their Copolymers," J. Biomed. Mater. Res. 13: 497-507 (1979)
Wise et al., "Lactic/Glycolic Acid Polymers," in Drug Carriers in Biology and Medicine, Gregoriadis (ed.), Academic Press (1979)
Krishnan et al., "Controlled Release of Bioactive Compounds with Special Reference to Agriculture," Popular Plastics Apr. (1978)
Wise et al., "Results on Biodegradable Cylindrical Subdermal Implants for Fertility Control," Midland Macromolecular Monogram (Polymer Delivery Systems) (1978)
Wise et al., "Sustained Release of Sulphadiazine," J. Pharm. Pharmac. 30: 686 (1978)
Wise et al., "Sustained Delivery of a Narcotic Antagonist From Lactic/Glycolic Acid Copolymer Implants," in Polymeric Delivery Systems, Kostelnik (ed.), Gordon & Breach Science Publishers (1978)
Miller et al., "Degradation Rates of Oral Resorbable Implants (Polylactates and Polyglycolates): Rate Modification with changes in PLA/PGA Copolymer Ratios," J. Biomed. Mater. Res. 11: 711 (1977)
Nelson et al., "Evaluation and Comparisons of Biodegradable Substances as Osteogenic Agents," Oral Surg., Oral Med., Oral Path. 43(6): 836 (1977)
Schindler et al., "Biodegradable Polymers for Sustained Drug Delivery," in Contemporary Topics in Polymer Science, vol. 2, Parce and Schaefgen (eds), Plenum Publishing Corp. (1977)
Anderson et al., "An Injectable Sustained Release Fertility Control System," Contraception 13(3): 375 (1976)
Yolles et al., "Controlled Release of Biologically Active Drugs," Bulletin of the Parenteral Drug Ass'n vol. 30 Nov.-Dec. (1976)
Cutright et al., "Single Dose, Long Duration, Subcutaneous Drug Administration," J. Oral Medicine 30(1): 5 (1975)
Nash et al., "Assessment of the Toxicity of Delivery Systems for Injectable Contraceptives," J. Steroid Biochem. 6: 909 (1975)
Nilsson et al., "Biodegradable Polylactate as a Steroid-Releasing Polymer: Intrauterine Administrations of d-Norgestrel," Am. J. Obstet. Gynecol. 122(1): 90 (1975)
Schwope et al., "Lactic/Glycolic Acid Polymers as Narcotic Antagonist Delivery Systems," Life Sciences 17: 1877 (1975)
Cutright et al., "Degradation Rates of Polymers and Copolymers of Polylactic and Polyglycolic Acids," Oral Surgery 37(1): 142 (1974)
Brady et al., "Resorption Rate, Route of Elimination, and Ultrastructure of the Implant Site of Polylactic Acid in the Abdominal Wall of the Rat," J. Biomed. Mater. Res. 7: 155 (1973)
Jackanicz et al., "Polylactic Acid as a Biodegradable Carrier for Contraceptive Steroids." Contraception 8(3): 227 (1973)
Sinclair, "Slow-Release Pesticide System Polymers of Lactic and Glycolic Acids as Ecologically Beneficial, Cost-Effective Encapsulating Materials," Environ. Sci. & Tech. 7(10): 955 (1973)
Hegyeli, "Use of Organ Cultures to Evaluate Biodegradation of Polymer Implant Materials," J. Biomed. Mater. Res. 7: 205 (1973)
Kulkarni et al., "Biodegradable Poly(Lactic Acid) Polymers," J. Biomed. Mater. Res. 5: 169 (1971)
Luzzi, "Microencapsulation," J. Pharm. Sci. 59(10): 1367 (1970)
Wiley, "Microencapsulation," in Encyclopedia of Chemical Technology, vol. 13, 2d ed., pp. 436-456, New York, (1967)
Ezan et al., "Radioimmunoassay of [D-Trp6 ]-Luteinizing Hormone-Releasing Hormone: Its Application to Animal Pharmacokinetic Studies after Single Injection and Long-Acting Formulation Administration," Regulatory Peptides 14: 155 (1986)
Schwope et al., "Development of Polylactic/Glycolic Acid Delivery Systems for Use in Treatment of Narcotic Addiction," Nat'l Inst. Drug Abuse Monogr. Ser. pp. 13-18, Jan. 1976
Thies, "Development of Injectable Microcapsules for Use in the Treatment of Narcotic Addiction," Nat'l Inst. Drug Abuse Monogr. Ser. pp. 19-20, Jan. 1976
Mason et al., "Hydrolytic Degradation of Poly D1-(Lactide)," Org. Coat. Plast. Chem. 42:436 (1980)
Sanders, L. M. et al.; J. Pharm. Sci., 75: 356-360 (Apr. 1986)
Schally, A. V. et al.; Proc. Nat'l Acad. Sci., U.S.A. 83 8764-8768 (Nov. 1986)
Tice, T. R. et al.; 11th International Symp. on Controlled Release of Bioactive Materials Ft. Lauderdale, Fla. (Jul. 1984)
Schally, A. V. et al.; Proc. Nat'l Acad. Sci. U.S.A. 82: 2498-2502 (Apr. 1985)
Mason-Garcia, M. et al.; Proc. Nat'l Acad. Sci. U.S.A., 82: 1547-1551 (Mar. 1985)
Torres-Aleman, I. et al.; Proc. Nat'l Acad. Sci. U.S.A., 82: 1252-1256 (Feb. 1985)
Asch, R. H. et al.; J. Andrology, 6: 83-88 (1985)
Sanders, L. M. et al.; 10th International Syposium on Controlled Release of Bioactive Materials, San Francisco, Calif., 91-96 (Jul. 1983)
Kent, J. S. et al.; in: Long-Acting Contraceptive Delivery Systems, Program for Applied Research on Fertility Regulation Series on Fertility Regulation, pp. 169-179 (1984)
Vickery, B. H. et al.; in: Long-Acting Contraceptive Delivery Systems, Program for Applied Research on Fertility Regulation Series on Fertility Regulation, pp. 180-189 (1984)
Kent, J. S. et al.; Reproductive Health Care International Symposium, Maui, Hawaii (Oct. 1982)
Sanders, et al.; Reproductive Health Care International Symposium, Maui, Hawaii (Oct. 1982)
Rojas, F. J. et al.; Abstract for the American Fertility Society Annual Meeting, Sep. 27-Oct. 2, 198