Liothyronine → Thyroxine

HRID 1753750

反応式

HRID 1753750 の反応式
C1C(OC2C(I)=CC(C[C@H](N)C(O)=O)=CC=2I)=CC(I)=C(O)C=1.[CH:24]1[C:25]([CH2:42][C@H:43]([NH2:47])[C:44]([O-:46])=[O:45])=[CH:26][C:27]([I:41])=[C:28]([O:31][C:32]2[CH:33]=[C:34]([I:40])[C:35]([OH:39])=[C:36]([I:38])[CH:37]=2)[C:29]=1[I:30].O.[Na+].C(O)[C@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O>>[CH:26]1[C:25]([CH2:42][C@H:43]([NH2:47])[C:44]([OH:46])=[O:45])=[CH:24][C:29]([I:30])=[C:28]([O:31][C:32]2[CH:37]=[C:36]([I:38])[C:35]([OH:39])=[C:34]([I:40])[CH:33]=2)[C:27]=1[I:41]

参加物

4

反応物 3

HCID 5920LiothyronineHCID 6251Mannitol4 回HCID 23667619Levothyroxine sodium monohydrate2 回

生成物 1

HCID 5819Thyroxine

実験手順

FIG. 2 depicts graphs of liothyronine (T3) impurity over time at 40° C. for compositions containing 100 μg (“mcg”), 200 μg or 500 μg levothyroxine sodium (L), and either 3 mg or 10 mg mannitol (M). FIG. 3 depicts graphs of T3 impurity over time at 25° C. for compositions containing 100 μg, 200 μg or 500 μg levothyroxine sodium, and either 3 mg or 10 mg mannitol. The graphs in FIGS. 2 and 3 for the compositions containing 3 mg mannitol (open symbols) correspond to the results listed in Table 2. The graphs in FIGS. 2 and 3 for the compositions containing 10 mg mannitol (closed symbols) correspond to results of an analysis of the stability of levothyroxine in solid compositions containing 100 μg, 200 μg or 500 μg levothyroxine sodium and 10 mg mannitol. These solid compositions were formed by combining water, the levothyroxine sodium, the mannitol, and 500 μg dibasic sodium phosphate to form liquid mixtures, and then adding sodium hydroxide to provide a pH of about 11.8. Water for injection (USP) was added to each liquid mixture as needed to provide total volumes of 1 mL. The liquid mixtures were lyophilized to provide solid compositions, which were then stored in vials at temperatures of 25° C. or 40° C. The stability of the levothyroxine in the solid compositions over time at different temperatures was determined by measuring the amount of T3, as described above. The results of these measurements for the compositions containing 10 mg mannitol are listed in Table 3, below.

後処理

  1. customat 40° C.
  2. customat 25° C.

出典と根拠

ORDレコード
ord-c84bc55e6f3a4b618da68af6a954cd31
出典データセット
uspto-grants-2015_10
特許番号
US09168239B2

関連ノート

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