Pharmaceutical formulations for dry powder inhalers

摘要

A powder for use in a dry powder inhaler comprises: i) a fraction of fine particle size constituted by a mixture of physiologically acceptable excipient and an additive; ii) a fraction of coarse particles; and iii) at least one active ingredient. The powder is suitable for efficacious delivery of active ingredients into the low respiratory tract of patients suffering from pulmonary diseases such as asthma. In particular, the invention provides a formulation to be administered as dry powder for inhalation which is freely flowable, can be produced in a simple way, is physically and chemically stable and capable of delivering accurate doses and/or high fine particle fraction of low strength active ingredients by using a high- or medium resistance device.

主权项

1. A powder for use in a dry powder inhaler, the powder comprising:
i) a fraction of fine particle size comprising composite particles prepared by co-micronising a physiologically acceptable excipient and a surface active additive, the fraction having a mean particle size of less than 35 μm; ii) a fraction of coarse particles constituted of a physiologically acceptable carrier having a particle size of at least 90 μm; and iii) at least one active ingredient having a particle size of less than 10 μm; said fine fraction (i) being composed of up to 99% by weight of particles of the excipient and at least 1% by weight of additive and the ratio between the fine excipient particles and the coarse carrier particles being between 1:99 and 40:60% by weight, and wherein the additive partially coats the surfaces of both the excipient and the coarse particles, and wherein the active ingredients are not selected from the group consisting of budesonide, and its epimers, formoterol, TA2005 and its stereoisomers, salts thereof, and combinations thereof.