Multiparticular pharmaceutical form, which contains active products of nucleic acid of mucoadhesive formulation, as well as a procedure for obtaining the pharmaceutical form
LIZIO, Rosario,PETEREIT, Hans-Ulrich,TRUPTI, Dave,GOTTSCHALK, Michael
申请号：
ES05807707
公开号：
ES2569354T3
申请日:
2005.11.05
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
Multiparticular oral pharmaceutical form, containing ball agglomerates with an average diameter in the range of 50 to 2500 μm, which is essentially constituted by a) an internal matrix layer containing nanoparticles comprising an active nucleic acid product, and are housed matrix consisting of a polymer with a mucoadhesive action, the matrix may optionally contain other pharmaceutical auxiliary substances, b) a film-coated external coating, consisting essentially of an anionic polymer or copolymer, which may optionally be formulated with usual auxiliary substances from the pharmaceutical point of view, especially plasticizers, characterized in that the multiparticular pharmacological form is formulated so that the contained ball agglomerates are released in the stomach pH range, the external coating, by the selection of anionic polymer or copolymer , ob In its formulation with auxiliary substances and its layer thickness, it is adjusted so that it dissolves in pH ranges of 4.0 to 8.0 in the intestine in the range of 15 to 60 min, so that the matrix layer that Contains active, mucoadhesive product, is released, can be attached to the intestinal mucosa and release the active product in it, selecting the polymer with mucoadhesive action so that, in a range of +/- 0.5 pH units, referred at the pH value at which the external coating begins to dissolve, it has a mucoadhesive action of at least ηb>； = 150 to 1000 mPa.s and a water absorption of 10 to 750% in 15 minutes, and the fraction of active product of the nanoparticles in the matrix layer amounts to a maximum of 40% by weight of the content in the polymer with mucoadhesive action.Forma farmacéutica oral multiparticular, que contiene aglomerados en bolas con un diámetro medio en el intervalo de 50 a 2500 μm, que está constituida esencialmente por a) una capa matriz interna que contiene nanopartículas que comprenden un producto activo de ácido nucleico, y están alojados una matriz constituida por un polímero con acci
