Liothyronine → Thyroxine

HRID 1753749

반응식

HRID 1753749 반응식
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]

참가 물질

4

반응물 3

HCID 5920LiothyronineHCID 6251Mannitol4회HCID 23667619Levothyroxine sodium monohydrate2회

생성물 1

HCID 5819Thyroxine

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-5530cc33ca29462eb9d4db37d0b772cd
출처 데이터셋
uspto-grants-2015_10
특허 번호
US09168238B2

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