Dry powder inhalation medicine composition and preparation method thereof

A technology of dry powder inhalation and composition, which is applied in the field of medicine, can solve the problems of alveolar irritation and side effects, achieve strong hygroscopicity, increase the proportion of fine particles, and avoid stimulation and other side effects

Inactive Publication Date: 2016-10-05
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, magnesium stearate with a particle size of about 3 μm, like the active ingredient with the same particle size, will enter the alveoli with the patient's inhalation. Ingestion and deposition in the lungs can cause some irritation of the alveoli and other side effects

Method used

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  • Dry powder inhalation medicine composition and preparation method thereof
  • Dry powder inhalation medicine composition and preparation method thereof
  • Dry powder inhalation medicine composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] 1. Mix 0.5 g of magnesium stearate for inhalation with 249 g of lactose monohydrate as a carrier in a three-dimensional mixer at a speed of 150 rpm for 4 hours, and 0.5 g of micronized glycopyrronium bromide (equivalent to 0.63 glycopyrronium bromide) g) adding to the above powder, using three-dimensional mixing to continue mixing for 2 hours to obtain inhalable dry powder 1;

[0025] 2. Add 0.5g of magnesium stearate for inhalation, 249g of lactose monohydrate for carrier, and 0.5g of micronized glycopyrronium bromide (equivalent to 0.63g of glycopyrronium bromide) into a three-dimensional mixer and mix at a speed of 150 rpm After 6 hours, the inhalable dry powder 2 was obtained;

[0026] 3. Add 249 g of lactose monohydrate as carrier and 0.5 g of micronized glycopyrronium bromide (equivalent to 0.63 g of glycopyrronium bromide) into a three-dimensional mixer and mix for 6 hours at a speed of 150 rpm to obtain inhalable dry powder 3 .

[0027] Use the above dry powde...

Embodiment 2

[0035] 1. 1.5 g of magnesium stearate for inhalation and 248 g of lactose monohydrate as carriers were mixed in a three-dimensional mixer for 4 hours at a speed of 150 rpm, and 0.625 g of micronized umeclidinium (equivalent to 0.75 umeclidinium bromide) g) adding to the above powder, using three-dimensional mixing to continue mixing for 2 hours to obtain inhalable dry powder 1;

[0036] 2. Add 1.5g of magnesium stearate for inhalation, 248g of lactose monohydrate for carrier, and 0.625g of micronized umeclidinium (equivalent to 0.75g of umeclidinium bromide) into a three-dimensional mixer and mix at a speed of 150 rpm After 6 hours, the inhalable dry powder 2 was obtained;

[0037] 3. Add 249 g of lactose monohydrate and 0.625 g of micronized umeclidinium bromide (equivalent to 0.75 g of umeclidinium bromide) into a three-dimensional mixer and mix for 6 hours at a speed of 150 rpm to obtain inhalable dry powder 3. .

[0038] Use the above dry powder for the preparation of fo...

Embodiment 3

[0046] 1. Mix 3.0 g of magnesium stearate for inhalation, 24.5 g of micronized lactose monohydrate and 220.5 g of lactose monohydrate for carrier in a three-dimensional mixer at a speed of 150 rpm for 4 hours, and mix 0.5 g of micronized glycopyrronium (equivalent to 0.63g of glycopyrronium bromide), 1.10g of micronized indacaterol (equivalent to 1.43g of indacaterol maleate) were added to the above powder, and three-dimensional mixing was used to continue mixing for 2 hours to obtain inhalable dry powder 1;

[0047] 2. 3.0 g of magnesium stearate for inhalation, 245 g of lactose monohydrate for carrier, 0.5 g of micronized glycopyrronium bromide (equivalent to 0.63 g of glycopyrronium bromide), and 1.10 g of micronized indacaterol (equivalent to Indacaterol maleate 1.43g) was added together in a three-dimensional mixer and mixed for 6 hours at a speed of 150 rpm to obtain inhalable dry powder 2;

[0048] 3. The carrier is 248g of lactose monohydrate, 0.5g of micronized glyco...

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Abstract

The invention provides a dry powder inhalation medicine composition and a preparation method thereof. The composition is prepared from a coating agent with a specific particle size characteristic, lactose monohydrate with a specific particle size characteristic for a carrier and a micronized medicinal active ingredient, wherein the coating agent is an inhaling magnesium stearate or a mixture of the inhaling magnesium stearate and micronized lactose monohydrate; and the medicinal active ingredient is selected from at least one of glycopyrronium bromide, umeclidinium, indacaterol, formoterol, vilanterol, fluticasone and pharmaceutically available salt of the active ingredients. The preparation method comprises the following steps of sufficiently mixing and coating the coating agent and the lactose monohydrate, and uniformly mixing with the micronized medicinal active ingredients.

Description

technical field [0001] The invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a dry powder inhaler pharmaceutical composition and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Dry powder inhalers (DPI), also known as Aerosol of micropowders for inspiration, are developed on the basis of Pressurized metered-dose inhaler (pMDI) and the knowledge of powder engineering A new dosage form developed, which is a kind of drug delivery system that disperses the drug into a mist and enters the respiratory tract through a special drug delivery device after being mixed with a carrier alone or with a carrier, and exerts local or systemic effects. medicine system. [0003] The physiological structure of the lung requires that the drug particles of the dry powder inhaler are very fine. It is generally believed that the ideal drug particle size is 1-5 μm. Particles larger than this ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K47/26A61K47/12
CPCA61K9/0075A61K47/12A61K47/26
Inventor 张春雨秦践王小平
Owner SICHUAN HAISCO PHARMA CO LTD
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