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(12) Patent Application Publication (10) Pub. No.: US 2003/0060381A1 Meier Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2003/0060381A1 Meier Et Al US 2003OO60381A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2003/0060381A1 Meier et al. (43) Pub. Date: Mar. 27, 2003 (54) DISPERSION COMPRISING A NON-IONIC (30) Foreign Application Priority Data EMULSIFIER Mar. 10, 2000 (DE)..................................... 100 11447.4 (76) Inventors: Christian Meier, Darmstadt (DE); Johanna Eisele, Darmstadt (DE); Publication Classification Michael Schnabel, Biebesheim (DE); Klaus Schultes, Wiesbaden (DE); (51) Int. Cl." ....................................................... A61K 7/50 Stefan Grimm, Worms (DE); (52) U.S. Cl. ............................................ 510/141; 510/153 Hans-Ulrich Petereit, Darmstadt (DE); Thomas Suefke, Erzhausen (DE) (57) ABSTRACT Correspondence Address: The invention relates to a dispersion Suitable for use as OBLON, SPIVAK, MCCLELLAND, MAIER & coating agent and binder for pharmaceutical forms, having NEUSTADT, P.C. a solids content of 10-70% by weight consisting of 1940 DUKE STREET a) from 90 to 99% by weight of a methacrylate copolymer ALEXANDRIA, VA 22314 (US) consisting of at least 90% by weight of (meth)acrylate monomers containing neutral radicals and having a (21) Appl. No.: 09/926,484 glass transition temperature Tg of from -20°C. to +20 C. as determined by the DSC method, and (22) PCT Filed: Feb. 2, 2001 b) 1-10% by weight of a nonionic emulsifier having an (86) PCT No.: PCT/EP01/01108 HLB of from 15.2 to 17.3. Patent Application Publication Mar. 27, 2003. Sheet 1 of 2 US 2003/0060381 A1 E. CD E H 3 & 8 9 % eSeele Patent Application Publication Mar. 27, 2003. Sheet 2 of 2 US 2003/0060381 A1 E. C) H 33 S. % eSeele US 2003/0060381 A1 Mar. 27, 2003 DISPERSION COMPRISING ANON-ONC or no fractions of monomers containing ionic radicals in EMULSIFIER Such a way that, while retaining the Stability of the disper 0001. The invention relates to the field of dispersions and Sion and its particle size distribution, it is possible to use it to their use as coating agents and binders for pharmaceutical to prepare medicament formulations in which phase Sepa forms. ration with the formation of crystal Structures as a result of the emulsifier does not occur. At the same time, there should PRIOR ART be no deleterious alteration to the active Substance release characteristics and other properties-mechanical properties, 0002 The use of so-called neutral methacrylate copoly for example. mers, i.e. methacrylate copolymers consisting predomi nantly of (meth)acrylate monomers with neutral radicals, 0010 This problem has been solved by means of a Such as methyl methacrylate or ethyl methacrylate as coating dispersion Suitable for use as a coating agent and binder for agents and binders for pharmaceutical forms with delayed pharmaceutical forms, having a solids content of 10-70% by active-Substance release has been known for a long time. weight consisting of 0.003 Uses in mixtures with anionic dispersions are 0011) a) from 90 to 99% by weight of a methacrylate described, for example, in EP-A 152038, EP-A 208 213 or copolymer consisting of at least 90% by weight of EPA 617 972. (meth)acrylate monomers containing neutral radicals and having a glass transition temperature Tg of from 0004. The neutral methacrylate copolymers are nowa –25° C. to +20° C. as determined by the DSC method days used preferably as dispersions. Dispersions of this kind (ISO 11357), and are prepared by emulsion polymerization and therefore include as a result of their preparation an emulsifier, which 0012 b) 1-10% by weight of a nonionic emulsifier also brings about the Stability of the resulting dispersion per having an HLB of from 15.7 to 16.2. Se. In the finished pharmaceutical form, moreover, the 0013) Implementation of the Invention emulsifier present influences the active Substance release 0014) Methacrylate Copolymer characteristics. 0.015 The dispersion of the invention comprises 90-99% 0005. As a result of the intended use in pharmaceuticals, by weight, based on the Solids content, of a methacrylate and on account of the fact that owing to the monomer copolymer. composition the copolymers have few if any charges, the 0016. The methacrylate copolymer consists of at least 90, Selection of appropriate emulsifiers is very limited. in particular 95, preferably 97, in particular 99, with par 0006 Göferich and Lee in “The influence of endogenous ticular preference 100% by weight of (meth)acrylate mono Surfactant On the Structure and drug-release properties of mers containing neutral radicals, especially C to C alkyl Eudragit NE30D matrices”, Journal of Controlled Release radicals. 18 (1992), pp. 133-144, describe how an emulsifier of the 0017 Examples of Suitable monomers are methyl meth nonylphenol type present in the dispersion causes problems acrylate, ethyl methacrylate, butyl methacrylate, methyl for the release of active Substance from coated pharmaceu acrylate, ethyl acrylate and butyl acrylate. Preference is tical forms. The authors describe an anisotropic Structure in given to methyl methacrylate, ethyl acrylate and methyl copolymer films obtained from the dispersion. Both in films acrylate. containing active Substance and in films free of active Substance, phase Separation and crystallization of the emul 0018. In small fractions, not more than 10, preferably not sifier occur as a function of the Storage period and the active more than 5, with particular preference not more than 3 or Substance content. These occurrences obviously result in not more than 1% by weight, methacrylate monomers con inconsistencies in the release of the active Substance clen taining anionic radicals, e.g. methacrylic acid, may be buterol. If the emulsifier is removed from freeze-dried present. copolymer by Washing with water, then a uniform-al 0019. The methacrylate copolymer has a glass transition though slowed-release of active Substance is observed in the purified copolymer. temperature Tg of from -25 C. to +20 C., preferably from -10° C. to 0° C., determined by the DSC method (ISO 0007 DE-A 19503 099 describes a process for preparing 11357). aqueous addition-polymer dispersions by the method of 0020. A typical methacrylate copolymer may be com free-radical aqueous emulsion polymerization in the pres posed, for example, of 25-35% by weight methyl methacry ence of a nonionic emulsifier. Suitable nonionic emulsifiers late and from 75 to 65% by weight ethyl acrylate. are those whose cloud point is situated below the polymer ization temperature. A large number of Suitable compounds 0021. In accordance with the invention, the polymers is listed, including nonylphenol emulsifiers. which are neutral per Se-may include Small amounts of methacrylic acid, which although causing virtually no alter 0008 Problem and Solution ation in the water-insolubility of the polymer may never 0009. The problem was seen to be to improve prior art theless influence Swelling and permit pH-dependent control dispersions comprising methacrylate copolymers with Small of the permeability. US 2003/0060381 A1 Mar. 27, 2003 0022. Emulsifiers 0032) Preparation of the Dispersion 0023 The dispersion of the invention contains from 1 to 0033. The novel dispersion is obtained in a manner 10, preferably from 2 to 8, with particular preference from known per se by aqueous emulsion polymerization by the 4 to 6% by weight, based on the Solids content, of a nonionic batch technique or the feed technique, Semi-continuously or emulsifier having an HLB of from 15.7 to 16.2. else continuously (in this respect See, for example, DE 195 0024. Emulsifiers control the course of the emulsion 03 099 A1). polymerization proceSS by permitting the chain-building 0034. The free-radical polymerization of the monomers reaction of the emulsified monomers in the water phase. in the presence of the emulsifier takes place by means of They therefore constitute an auxiliary which is necessary for radical-forming water-Soluble polymerization initiators, it the preparation and which determines the properties of the being possible for radical formation to take place thermally dispersion. They cannot normally be replaced without fun or by way of redox processes. If desired, molecular weight damental changes in relevant properties of the dispersion. regulators are added for the purpose of adjusting the molar 0025. The HLB, introduced by Griffin in 1950, is a masses. Emulsion polymers are commonly prepared in measure of the hydrophilicity of lipophilicity of nonionic concentrations between 10 and 70% by weight. A solids Surfactants. It may be determined experimentally by the content of 30-50% by weight is advantageous. Batchwise phenol titration method of Marszall; cf. "Parfimerie, Kos preparation generally takes place in Stirred tank reactors. metik”, Volume 60, 1979, pp. 444-448; further literature 0035. For the preparation, in the case of a simple batch references are in Römpp, Chemie-Lexikon, 8th ed. 1983, p. preparation, all monomers are charged to a reaction vessel in 1750. See also, for example, U.S. Pat. No. 4,795,643 (Seth). accordance with the desired copolymer composition, 0026. An HLB (hydrophilic/lipophilic balance) can be together with the emulsifier, initiators, regulators and other determined exactly only for nonionic emulsifiers. For auxiliaries and together with water, and are dissolved or anionic emulsifiers, this value may be determined arithmeti dispersed therein. By activating the initiator (increasing the cally but is virtually always above or well above 20. temperature, adding the redox agent), the polymeric chain reaction is initiated and conducted. In the course of this 0027. The HLB values in emulsifiers have a distinct reaction, the known lateX particles, consisting of polymer influence on the crystallization of the emulsifier. Ideally chains, are formed. these values are between 15.7 and 16.2. Above the claimed range, the emulsifiers crystallize out after drying. Emulsifi 0036) Antifoam emulsion and stabilizers may be added to erS having an HLB below the claimed range are unable to the dispersion.
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