Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1998-08-17
2000-12-05
Azpuru, Carlos A.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424426, 5147723, A61K 950, A61K 4730, A61F 202
Patent
active
06156348&
ABSTRACT:
Methods and compositions are provided for enhancing the bioadhesive properties of polymers used in drug delivery systems. The bioadhesive properties of a polymer are enhanced by incorporating an anhydride oligomer into the polymer to enhance the ability of the polymer to adhere to a tissue surface such as a mucosal membrane. Anhydride oligomers which enhance the bioadhesive properties of a polymer include oligomers synthesized from dicarboxylic acid monomers, preferably those found in Krebs glycolysis cycle, especially fumaric acid. The oligomers can be incorporated within a wide range of polymers including proteins, polysaccharides and synthetic biocompatible polymers. In one embodiment, anhydride oligomers can be incorporated within polymers used to form or coat drug delivery systems, such as microspheres, which contain a drug or diagnostic agent. The oligomers can either be solubilized and blended with the polymer before manufacture or else used as a coating with polymers over existing systems. The polymers, for example in the form of microspheres, have improved ability to adhere to mucosal membranes, and thus can be used to deliver a drug or diagnostic agent via any of a range of mucosal membrane surfaces including those of the gastrointestinal, respiratory, excretory and reproductive tracts.
REFERENCES:
patent: 2675619 (1954-04-01), Cone
patent: 2677700 (1954-05-01), Jackson et al.
patent: 2979578 (1961-04-01), Curtis
patent: 3036118 (1962-05-01), Jackson et al.
patent: 3535307 (1970-10-01), Moss et al.
patent: 3829506 (1974-08-01), Schmolka et al.
patent: 4757128 (1988-07-01), Domb et al.
patent: 4861627 (1989-08-01), Mathiowitz et al.
patent: 4898734 (1990-02-01), Mathiowitz et al.
patent: 4933431 (1990-06-01), Domb et al.
patent: 4938763 (1990-07-01), Dunn et al.
patent: 4976968 (1990-12-01), Steiner
patent: 4997904 (1991-03-01), Domb
patent: 5019400 (1991-05-01), Gombotz et al.
patent: 5173298 (1992-12-01), Meadows
patent: 5175235 (1992-12-01), Domb et al.
patent: 5271961 (1993-12-01), Mathiowitz et al.
patent: 5474768 (1995-12-01), Robinson
patent: 5518730 (1996-05-01), Fuisz
patent: 5518731 (1996-05-01), Meadows
patent: 5611344 (1997-03-01), Bernstein et al.
patent: 5780044 (1998-07-01), Yewey et al.
Beck, et al., "A new long-acting injectable microcapsule system for the administration of progesterone," Fertil. & Steril., 31(5):545-55 (1979).
Benita, et al., "Characterization of Drug-Loaded Poly(d,l-lactide) Microspheres," J. Pharm. Sci., 73(12):1721-24 (1984).
Chickering & Mathiowitz, "Bioadhesive microspheres: I. A novel electrobalance-based method to study adhesive interactions between individual microspheres and intestinal mucosa," J. Control. Release 34:251-62 (1995).
Duchene, et al., "Pharmaceutical and medical aspects of bioadhesive systems for drug administration," Drug Development & Ind. Pharm., 14(2&3):283-318 (1988).
Edelman, et al., "Perivascular and intravenous administration of basic fibroblast growth factor: Vascular and solid organ deposition," Proc. Natl. Acad. Sci., USA 90:1513-17 (1993).
Gurney et al., "Bioadhesive intraoral release systems: design, testing and analysis," Biomaterials, 5:336-340 (1984).
Harada, et al., "Basic fibroblast growth factor improves myocardial function in chronically ischemic porcine hearts," J. Clin. Invest., 94(2):623-30 (1994).
Horowitz, M., "Mucopolysaccharides and glycoproteins of the alimentary tract," Handbook of Physiology (C.F. Code, ed.), pp. 1063-1085 (American Physiological Society 1967).
Labat-Robert & Decaeus, "Glycoproteines du mucus gastrique: structure, fonctions et pathologie," Pathologie Biologie, 24:241 (Paris 1979).
Labhasetwar, et al., "Sotalol Controlled-release systems for arrhythmias: In vitro characterization, in vivo drug disposition, and electrophysiologic effects," J. Pharm. Sci., 83(2):156-164 (1994).
Lehr, et al., "Intestinal transit of bioadhesive microspheres in an in situ loop in the rat--a comparative study with copolymers and blends based on poly(acrylic acid)," J. Controlled Rel., 13:51-62 (1990).
Li & Li, "Use of Enzymes in Elucidation of Structure", The Glycoconjugates (Horowitz, editor), pp. 51-67 (Academic Press 1977).
Mathiowitz, et al., "Novel microcapsules for delivery systems," Reactive Polymers, 6:275-83 (1987).
Mathiowitz, et al., "Morphology of polyanhydride microsphere delivery systems," Scanning Microscopy, 4(2):329-340 (1990).
Mikos, et al., "Interaction of Polymer Microspheres with Mucin Gels as a Means of Characterizing Polymer Retention on Mucus," J. Colloid & Interface Sci., 143(2):366-73 (1991).
Park, et al., "Alternative Approaches to Oral Controlled Drug Delivery: Bioadhesives and In-Situ Systems", Recent Advances in Drug Delivery Systems (Anderson & Kim, eds.) pp. 163-83 (Plenum Press 1983?).
Smart, et al., "An in vitro investigation of mucosa-adhesive materials for use in controlled drug delivery," J. Pharm. & Pharmacol., 36:295-99 (1984).
Spiro, R., "Glycoproteins," Annual Review of Biochemistry, 39:599-638 (Snell, ed. 1970).
Tutwiler, et al., "A Pharmacologic Profile of McN-3495 [N-(1-methyl-2-pyrrolidinylidene)-N-pheny-1-pyrrolidinecarboxyimidamide], a New, Orally Effective Hypoglycemic Agent," Diabetes, 27(8):856-67 (1978) .
Carino Gerardo P.
Hertzog Benjamin A.
Jacob Jules S.
Mathiowitz Edith
Santos Camila A.
Azpuru Carlos A.
Brown University Research Foundation
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