Resumen
<div notation="docdba" type="abstract" xml:base="/api/emi/section/39ae1ddc-68d7-41ec-b80b-0f84ed1085f6/image" xml:lang="en"><p>FIELD: medicine, pharmacy. SUBSTANCE: invention relates to pharmaceutical composition made as granule that comprises antifungal compound itraconazole or superconazole. Granules comprise inert core of size from 50 to 600 mcm and coating layer. Coating involves a single layer prepared by spraying on indicated inert core of solution involving itraconazole or superconazole, hydrophilic polymer and nonionic surface-active substance. Coating layer is applied at the constant rate for all process. Indicated coating layer is subjected for a single drying stage at 45 C being application of coating layer and its drying are carried out into the same apparatus that provides the improvement of chemical and physical integrity of granules. Pharmaceutical composition provides the improved solubility of indicated antifungal compounds and their enhanced bioavailability. EFFECT: improved preparing method, reduced price and time of process. 7 cl, 1 ex</p></div>
Reivindicaciones
1. An oral pharmaceutical composition in the form of a pellet, comprising a compound having antifungal activity as active principle, an inert core and a coating including said active principle, characterized in that said inert core has a particle size comprised between 50 and 600 µm, and in that said coating comprises a single layer obtained by spraying, on said inert core, a solution comprising a compound having antifungal activity, a hydrophilic polymer and a non-ionic surfactant. 2. An oral pharmaceutical composition as claimed in claim 1, characterized in that said inert core has a particle size comprised between 500 and 600 µm. 3. An oral pharmaceutical composition as claimed in claim 1, characterized in that said compound having antifungal activity is selected between Itraconazole and Saperconazole. 4. An oral pharmaceutical composition as claimed in claim 1, characterized in that said hydrophilic polymer is selected among the group comprising hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), polyvinyl pyrrolidone (PVP) and methacrylates. 5. An oral pharmaceutical composition as claimed in claim 1, characterized in that said non-ionic surfactant can be selected from propylene glycol esters, glycerol esters, (mono-di-tri-)acetylated sorbitan, (mono, di-tri)acetylated saccharose, polyoxyethylene sorbitan esters of fatty acids, polyoxyethylene alkyl ethers of fatty chain, polyoxyethylene-polyoxypropylene copolymers. 6. An oral pharmaceutical composition as claimed in any of the previous claims, characterized in that the proportions of hydrophilic polymer, non-ionic surfactant, active principle and inert core in the final pellet are, respectively: hydrophilic polymer (25%-60%), preferably (27%-55%), non-ionic surfactant (1%-15%), preferably (3%-10%), antifungal compound (19%-30%), preferably (20%-25%), and inert core (10%-45%), preferably (15%-43%). 7. An oral pharmaceutical composition as claimed in any of the previous claims, characterized in that the weight to weight ratio between the antifungal compound and hydrophilic polymer is [(1:1)-(1:3)], and between the antifungal compound and the surfactant is [(1.5:1)-(29:1)] 8. A method for obtaining an oral pharmaceutical composition as claimed in any of the preceding claims, characterized in that the following steps are performed: a/ a coating, comprising a single layer, of the inert cores having a size between 50 and 600 µm, by means of the spraying of a solution composed by the antifungal agent, the hydrophilic polymer and the non-ionic surfactant, at a constant coating speed throughout the whole process; and b/ a single drying step of said coating in the same apparatus.
