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
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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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