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APPLICATION OF MAGNESIUM STEARATE IN DRY POWDER FOR INHALATION
专利权人:
КЬЕЗИ ФАРМАЧЕУТИЧИ С.П.А. (IT)
发明人:
КОККОНИ Даниела (IT),ДАЛЬИ АЛЬБЕРИ Массимильяно (IT),БУСКА Андреа (IT),СКЬЯРЕТТИ Франческа (IT)
申请号:
RU2013113965/15
公开号:
RU2013113965A
申请日:
2011.09.16
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. The use of magnesium stearate in dry powder inhalation formulations comprising carrier particles and an active ingredient containing a hydrolysis sensitive group selected from the group consisting of carbonate, carbamate and ester to inhibit or reduce the chemical decomposition of said active ingredient. The use according to claim 1, where the magnesium stearate is present in amounts in the range of 0.05-1.5%, based on the total weight of the carrier. The use of claim 2, wherein the amount is from 0.1 to 1.0 m / m%. 4. The use according to any one of paragraphs. 1-3, where magnesium stearate covers the surface of the carrier particles to an extent of at least 10% .5. The use of claim 4, wherein the degree of coverage is equal to or greater than 20% .6. The use of claim 1, wherein the carrier particles are made from crystalline sugar. The use of claim 6, wherein the sugar is alpha-lactose monohydrate. The use of claim 1, wherein the carrier particles have a diameter of at least 20 microns. The use of claim 8, wherein the mass diameter is from 80 to 500 microns. The use of claim 9, wherein the mass average diameter is from 210 to 355 microns. 11. The use according to claim 1, wherein the active ingredient is selected from classes consisting of antimuscarinic agents, phosphodiesterase-4 inhibitors and steroids for inhalation. A pharmaceutical composition of a dry inhalation powder comprising a) carrier particles, (b) magnesium stearate and (c) an active ingredient of the general formula (II), wherein R and Roba are phenyl optionally substituted with one or more halogen atoms, and X is a physiologically acceptable anion selected from the group consisting of bromide, chloride and trifluoroacetate. 13. The pharmaceutical composition of claim 12, wherein the magnesium stearate is1. Применение стеарата магния в составах сухого порошка для ингаляции, включающих частицы носителя и активный ингредиент, содержащий группу, чувствительную к гидролизу, выбранную из группы, вклю
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