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Capsule type tiotropium bromide inhalation powder

A technology for inhaling powder aerosols and tiotropium bromide, which can be used in aerosol delivery, powder delivery, respiratory diseases and other directions, and can solve problems such as complex preparation processes

Active Publication Date: 2007-09-12
NANJING CAVENDISH BIO ENG TECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The tiotropium bromide powder mist preparations prepared by the above two applications all adopt the method of mixing multiple alternating layers, and the preparation process is complicated

Method used

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  • Capsule type tiotropium bromide inhalation powder
  • Capsule type tiotropium bromide inhalation powder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1. Tiotropium bromide capsule type powder spray

[0035] 1. Lactose micronization

[0036]Take 100g of lactose, add 120ml of water, heat to dissolve completely, let cool, filter, slowly add 300ml of isopropanol under stirring, to precipitate crystals, filter, wash the filter layer in 200ml of 95% isopropanol solution, and pass through 200 mesh Sieve, filter, ventilate and dry at 105°C for 5 hours, and pulverize to obtain.

[0037] 2. Preparation of tiotropium bromide powder spray

[0038] ① Weigh 22.5 mg of tiotropium bromide monohydrate, add 10 ml of absolute ethanol, heat to dissolve completely, and set aside.

[0039] ②Weigh 30.0g of lactose micropowder, mix it with the solution of ① above, make a soft material, sieve 120 mesh to make granules, ventilate and dry at 60°C for 3 hours, and sieve the granules with an 80 mesh sieve.

[0040] ③ Determination of tiotropium bromide (C 19 h 20 NO 3 S 2 ) content, adjust the loading so that each capsule conta...

Embodiment 2

[0044] Embodiment 2. Tiotropium bromide capsule type powder spray

[0045] 1. Lactose micronization

[0046] Take 100g of lactose, add 180ml of water, heat to dissolve completely, let cool, filter, slowly add 200ml of isopropanol under stirring, to precipitate crystals, filter, wash the filter layer in 400ml of anhydrous isopropanol, and pass through a 300-mesh sieve , filtered, placed at 105 ℃ ventilated and dried for 5 hours, crushed, that is.

[0047] 2. Preparation of tiotropium bromide powder spray

[0048] ① Weigh 22.5 mg of tiotropium bromide monohydrate, add 10 ml of absolute ethanol, heat to dissolve completely, and set aside.

[0049] ②Weigh 30.0g of lactose micropowder, mix it with the solution of ① above, make a soft material, sieve 140 mesh to make granules, ventilate and dry at 60°C for 3 hours, and sieve granules with a 100 mesh sieve.

[0050] ③ Determination of tiotropium bromide (C 19 h 20 NO 3 S 2 ) content, adjust the loading so that each capsule con...

Embodiment 3

[0054] Embodiment 3. Tiotropium bromide capsule type powder spray

[0055] The preparation method refers to Example 1, except that the granulating sieve is 100 mesh, and the sizing sieve is 60 mesh.

[0056] Investigate the fluidity (angle of repose) and the deposition amount of the effective part of the particles obtained in the above-mentioned Examples 1-3, as well as the results of the powder spray test, see the table below for details.

[0057] Bottom (cm)

[0058] Example 3

[0059] Table 6 Inspection results of powder aerosol contents

[0060] investigation

[0061] investigation

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Abstract

The present invention discloses one kind of tiotropium bromide capsule atomized powder preparation, which includes tiotropium bromide or tiotropium bromide monohydrate in 0.04-1.5 wt% and fine lactose powder of size smaller than 15 microns for adsorbing tiotropium bromide or tiotropium bromide monohydrate. The present invention also provides the preparation process of the atomized powder preparation. The tiotropium bromide capsule atomized powder preparation has simple preparation process, excellent flowability and homogeneously distributed active component.

Description

technical field [0001] The present invention relates to a kind of pharmaceutical preparation, more specifically, the present invention relates to a kind of tiotropium bromide capsule type inhalation powder and a preparation method thereof. Background technique [0002] Tiotropium bromide is an anticholinergic drug with the chemical name: (1R,2R,4S,5S,7S)-7-[2-hydroxy-2,2-di(2-thienyl) bromide Acetoxy]-9,9-dimethyl-3-epoxy-9-azacyclooctane [3.3.1.0. 2.4 ] Nonane monohydrate, its chemical structure is as follows: [0003] [0004] Boehringer Ingelheim and Pfizer launched tiotropium bromide inhalation in the Netherlands and the Philippines in 2002, trade name: Spiriva TM . Tiotropium bromide is a long-acting antimuscarinic drug with similar affinity for muscarinic receptor subtypes M1 to M5. For the respiratory tract, it acts pharmacologically by inhibiting M3 receptors on smooth muscle, thereby dilating the bronchi. Tests have shown that this antagonist is competitive ...

Claims

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Application Information

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IPC IPC(8): A61K31/46A61K9/12A61K9/14A61K47/26A61P11/00
Inventor 许永翔
Owner NANJING CAVENDISH BIO ENG TECH
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