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Pharmaceutical composition for dry powder inhalation and preparation method of composition

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 the effects of increasing the proportion of fine particles, improving the stability of heat and humidity, and avoiding irritation and other side effects

Active Publication Date: 2016-03-23
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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  • Pharmaceutical composition for dry powder inhalation and preparation method of composition
  • Pharmaceutical composition for dry powder inhalation and preparation method of composition
  • Pharmaceutical composition for dry powder inhalation and preparation method of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 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;

[0035] 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;

[0036] 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 .

[0037] Use the above dry powde...

Embodiment 2

[0045] 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;

[0046] 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;

[0047] 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. .

[0048] Use the above dry powder for the preparation of fo...

Embodiment 3

[0056] 1. Mix 3.0 g of magnesium stearate for inhalation, 20 g of micronized lactose monohydrate, and 225 g of lactose monohydrate for carrier in a three-dimensional mixer at a speed of 150 rpm for 4 hours, and 0.5 g of micronized glycopyrronium ( Add 1.10 g of micronized indacaterol (equivalent to 1.43 g of indacaterol maleate) to the above powder, and continue mixing for 2 hours using three-dimensional mixing to obtain a respirable dry powder 1;

[0057] 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;

[0058] 3. The carrier is 248g of lactose monohydrate, 0.5g of micronized glycopyrronium bromide (equivalent to 0.63g of glycopyrronium bromi...

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Abstract

The invention provides a pharmaceutical composition for a dry powder inhalation and a preparation method of the composition. The composition comprises a coating agent, lactose monohydrate for a carrier and micronized active pharmaceutical ingredients, wherein the coating agent is inhaled magnesium stearate or a combination of the inhaled magnesium stearate and micronized lactose monohydrate. The pharmaceutical composition for the dry powder inhalation and the preparation method of the composition have the advantages that the inhaled magnesium stearate with specific particle size characteristics or the combination of the inhaled magnesium stearate and the micronized lactose monohydrate serves as the coating agent to be applied to the composition for the dry powder inhalation, stimulus to the lung caused by deposition of magnesium stearate on the lung or other side effects can be avoided, in-vitro determining parameters of the active ingredients can be increased, fine particle proportion of the active ingredients can be increased, and the hydrothermal stability of the product can be improved.

Description

technical field [0001] The invention relates to a pharmaceutical composition and a preparation method thereof, in particular to a pharmaceutical composition for dry powder inhalation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Dry powder inhalers (Drypowder inhalers, DPI), also known as inhalation powder mist (Aerosolofmicropowdersforinspiration), is a new dosage form developed on the basis of quantitative inhalation aerosol (Pressurizedmetered-doseinhaler, pMDI) and the knowledge of powder engineering. It is a drug delivery system that disperses the micronized drug alone or mixed with a carrier, through a special drug delivery device, and through the active inhalation of the patient, so that the drug is dispersed into a mist and enters the respiratory tract to exert local or systemic effects. [0003] The physiological structure of the lung requires that the drug particles of the dry powder inhaler are very f...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K47/26A61K47/12
Inventor 张春雨秦践郑伟李麒麟
Owner SICHUAN HAISCO PHARMA CO LTD
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