Dipyridamole inhalation preparation and preparation method thereof
A technology for dry powder inhalers and inhaled drugs, which can be used in anti-inflammatory agents, pharmaceutical formulations, antiviral agents, etc., and can solve the problems of unseen inhaled drugs
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Embodiment 1
[0038] Micronize dipyridamole with a flow energy mill according to the table below, and micronize 5g of anhydrous lactose with a flow energy mill to an average particle size of 70±5μm. After mixing, pass through a 200-mesh sieve for 3 times and then pack in 1000 capsules For No. 3 capsules, the active ingredients in each capsule are shown in the table below.
[0039] Example number active ingredient Dose (µg / capsule) D90 particle size (µm) Dosage of anhydrous lactose (µg / tablet) 1-1 Dipyridamole 10 3.9 1000 1-2 Dipyridamole 50 4.4 1000 1-3 Dipyridamole 100 4.5 1000 1-4 Dipyridamole 500 5.4 1000 1-5 Dipyridamole 1000 9.0 1000
[0040] If necessary, the anhydrous lactose can be replaced by one or more of α-lactose monohydrate, β-anhydrous lactose, amorphous spray-dried lactose, and crystallized dried lactose.
Embodiment 2
[0042] Example number active ingredient 1 Dose (µg / capsule) D90 particle size (µm) active ingredient 2 Dose (µg / capsule) D90 particle size (µm) Dosage of anhydrous lactose (µg / tablet) 2-1 Dipyridamole 50 5.4 fluticasone propionate 100 3.3 1000 2-2 Dipyridamole 50 4.5 fluticasone furoate 50 4.5 1000 2-3 Dipyridamole 100 3.9 Budesonide 200 5.0 1000 2-4 Dipyridamole 100 6.1 mometasone furoate 100 3.5 1000
[0043] According to the table, dipyridamole was micronized with a flow energy mill, and 5 g of lactose monohydrate was micronized with a flow energy mill to an average particle size of 42 μm. The three were mixed, passed through a 200-mesh sieve for 3 times, and then distributed in 1000 capsules of 3 See the table for the active ingredients in each capsule.
[0044] The preparation of aerosol, the active ingredient used is the weight of 1000 dosage units, HFA-134a is 1,1,1,2-tetrafluoroethane, HFA-22...
Embodiment 3
[0046] active ingredient
[0047] Ethanol 10g
[0048] HFA-134a 490g
[0049] Example number active ingredient 1 Dose (µg / spray) Total amount (mg) 3-1 Dipyridamole 100 100 3-2 Dipyridamole 200 500 3-3 Dipyridamole 500 1000 3-4 Dipyridamole 500 2000
[0050] Preparation process: add 1 unit weight of the active ingredient in the table to the prescribed amount of ethanol, stir, fill in divided doses, seal the dose valve system, and then pressurize and inject HFA-134a respectively to obtain the product.
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