Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1996-08-05
2000-05-30
Kulkosky, Peter F.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424 91, A61K 952, B01J 1304, B01J 304
Patent
active
060688572
DESCRIPTION:
BRIEF SUMMARY
The invention relates to the object characterized in the claims, i.e., new microparticles which contain active ingredients and contain at least one gas or a gaseous phase in addition to the active ingredient(s), agents containing these particles (microparticulate systems), their use for ultrasound-controlled in vivo release of active ingredients, for ultrasound-supported cell incorporation of active ingredients (sonoporation), as well as a process for the production of these particles and agents.
There have been microparticulate systems for controlled release of active ingredients for many years. A considerable number of possible shell substances and active ingredients can be used to this end. Also, there is a whole series of different production processes. Summaries on the shell substances and production processes used are found in, e.g.: M. Bornschein, P. Melegari, C. Bismarck, S. Keipert: Mikro- und Nanopartikeln als Arzneistofftragersysteme unter besonderer Berucksichtigung der Herstellungsmethoden [Microparticles and Nanoparticles as Pharmaceutical Carrier Systems with Special Consideration of the Production Methods], Pharmazie [Pharmaceutics] 44 (1989) 585-593 and M. Chasin, R. Langer (eds.): Biodegradable Polymers as Drug Delivery Systems, Marcel Dekker, New York, 1990.
The release of active ingredients from microparticulate systems is based mainly on diffusion or erosion processes [cf. C. Washington: Drug Release from Microdisperse Systems: A Critical Review, Int. J. Pharm. 58 (1990) 1-12 and J. Heller: Bioerodible Systems, in: R. S. Langer, D. L. Wice (eds.): Medical Applications of Controlled Release Vol. 1, CRC Press, Florida, 1984, pp. 69-101].
These principles are, however, associated with the drawback that the time controllability of the release of active ingredients from microdisperse systems in vivo is limited to the speed of the erosion process and/or diffusion process and can no longer be influenced after administration.
The previously known concepts for local control of the release of active ingredients in vivo from microparticulate systems are based almost exclusively either on non-specific concentrations of the microparticulate active ingredient carrier in certain target organs such as the liver and spleen or on measures for ensuring specific alteration of the organ distribution in vivo after administration by the alteration of the surface properties of the microparticulate systems by means of surfactants or specificity-mediating substances such as, e.g., antibodies (cf.: R. H. Muller: Colloidal Carriers for Controlled Drug Delivery--Modification, Characterization and In Vivo Distribution--, Kiel, 1989; S. D. Trobster, U. Muller, J. Kreuter: Modification of the Biodistribution of Poly(methylmethacrylate) Nanoparticles in Rats by Coating with Surfactants, Int. J. Pharm. 61 (1991), 85-100; S. S. Davis, L. Ilium, J. G. Mevie, E. Tomlinson (eds.); Microspheres and Drug Therapy, Elsevier Science Publishers B. V., 1984, and H. Tsuji, S. Osaka, H. Kiwada: Targeting of Liposomes Surface-Modified with Glycyrrhizin to the Liver, Chem. Pharm. Bull. 39 (1991) 1004-1008]. Other than this, however, all these processes offer no other means of actively influencing the site of the release of active ingredients after administration. In addition, it is not possible to influence the extent and the speed of the release of active ingredients after administration.
First attempts to actively influence the site of the release of active ingredients are based on the possibility of using existing or induced pH or temperature differences to induce release [cf: H. Hazemoto, M. Harada, N. Kamatsubara, M. Haga, Y. Kato: PH-Sensitive Liposomes Composed of Phosphatidyl-ethanolamine and Fatty Acid, Chem. Pharm. Bull. 38 (1990) 748-751 and J. N. Weinstein, R. L. Magin, M. B. Gatwin, D. S. Zaharko: Liposomes and Local Hyperthermia, Science 204 (1979) 188-1911. These methods are associated with the drawback, however, that they are either limited to cases where the necessary temperature or pH differences already exist (e.g.
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Fritzsch Thomas
Hauff Peter
Heldmann Dieter
Stahl Harald
Weitschies Werner
Kulkosky Peter F.
Schering Aktiengesellchaft
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