Silica → Azelastine

HRID 1195138Notes

Reaction equation

[CH3:1][N:2]1[CH2:8][CH2:7][CH:6]([N:9]2[N:19]=[C:18]([CH2:20][C:21]3[CH:22]=[CH:23][C:24]([Cl:27])=[CH:25][CH:26]=3)[C:17]3[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=3[C:10]2=[O:11])[CH2:5][CH2:4][CH2:3]1.Cl.O.OC1O[C@H](CO)[C@@H](O[C@@H]2O[C@H](CO)[C@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]1O.[Si](=O)=O>>[CH3:1][N:2]1[CH2:8][CH2:7][CH:6]([N:9]2[N:19]=[C:18]([CH2:20][C:21]3[CH:26]=[CH:25][C:24]([Cl:27])=[CH:23][CH:22]=3)[C:17]3[CH:16]=[CH:15][CH:14]=[CH:13][C:12]=3[C:10]2=[O:11])[CH2:5][CH2:4][CH2:3]1

Participants

Reactant 3

HCID 24261Silica

HCID 54360Azelastine hydrochloride

HCID 62223Lactose monohydrate

Product 1

HCID 2267Azelastine

Procedure

A premix is prepared of 440 g of azelastine-HCl, 360 mg of micro crystalline cellulose and 200 g of talcum. This premix together with 6000 g of lactose monohydrate, 2870 g of microcrystalline cellulose and 100 g of highly disperse silicon dioxide are passed through a sieve and homogenized in a sutable mixer. 30 g of magnesium stearate are sieved into the mixture so obtained and the resulting mixture is homogenized one more time. The mass so obtained is pressed into tablets weighing 100 mg having a diameter of 6 mm and a radius of curvature of 5.5 mm.

Workup

filtration30 g of magnesium stearate are sieved into the mixture
customso obtained
stirringthe resulting mixture is homogenized one more time
customThe mass so obtained

Sources & evidence

ORD record: ord-aaa964cbfa0b49a386e02b2e143deafb
Source dataset: uspto-grants-1992_05
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US05110814

Reaction notes

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