Mannitol → Cetirizine

HRID 1852352

반응식

HRID 1852352 반응식
[CH:1]1[CH:2]=[CH:3][C:4]([CH:7]([N:15]2[CH2:20][CH2:19][N:18]([CH2:21][CH2:22][O:23][CH2:24][C:25]([OH:27])=[O:26])[CH2:17][CH2:16]2)[C:8]2[CH:9]=[CH:10][C:11]([Cl:14])=[CH:12][CH:13]=2)=[CH:5][CH:6]=1.Cl.Cl.C(O)[C@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O.C(O)[C@@H]1O[C@H](O[C@]2(CCl)O[C@H](CCl)[C@@H](O)[C@@H]2O)[C@@H](O)[C@@H](O)[C@H]1Cl>Cl>[CH:1]1[CH:2]=[CH:3][C:4]([CH:7]([N:15]2[CH2:20][CH2:19][N:18]([CH2:21][CH2:22][O:23][CH2:24][C:25]([OH:27])=[O:26])[CH2:17][CH2:16]2)[C:8]2[CH:9]=[CH:10][C:11]([Cl:14])=[CH:12][CH:13]=2)=[CH:5][CH:6]=1

참가 물질

5

반응물 3

HCID 6251MannitolHCID 55182Cetirizine HydrochlorideHCID 70683051(2R,3S,4R,5R,6S)-2-[(2R,3S,4S,5S)-2,5-bis(chloromethyl)-3,4-dihydroxyoxolan-2-yl]oxy-5-chloro-6-(hydroxymethyl)oxane-3,4-diol

생성물 1

HCID 2678Cetirizine

시약·촉매·용매 1

HCID 313Hydrochloric Acid용매

실험 절차

Cetirizine Dihydrochloride ODT, 10 mg: 903.67 g of taste-masked microparticles and 2418.4 g of rapidly-dispersing microgranules (comprising mannitol and crospovidone at a ratio of 95/5) were blended with 400 g of microcrystalline cellulose (Avicel PH101), 200 g of crospovidone, 64 g of strawberry flavor, and 14 g of Sucralose (a sweetener) in a V-blender and compressed into tablets (13 mm in diameter) with an average weight of 650-653 mg and average hardness of 29-31 N and friability of 0.22-0.39% using a rotary tablet press equipped with an external lubrication system to lubricate the die and punch surfaces prior to each compression to demonstrate robustness of the manufacturing (taste-masking and tabletting) process and a dissolution of 100% (meeting target dissolution specifications of not less than about 75% released in 15 minutes in 0.1N HCl).

후처리

  1. customequipped with an external lubrication system

출처 및 근거

ORD 기록
ord-bce1cc2fe47a45839093522b92ebf7df
출처 데이터셋
uspto-grants-2015_02
특허 번호
US08962022B2

연결된 노트

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