Levodopa → Carbidopa-levodopa mixt.

HRID 2242762Notes

Reaction equation

HRID 2242762 reaction equation
[CH:1]1[C:6]([CH2:7][C@H:8]([NH2:12])[C:9]([OH:11])=[O:10])=[CH:5][C:4]([OH:13])=[C:3]([OH:14])[CH:2]=1.[CH3:15][C@@:16]([NH:29][NH2:30])([C:26]([OH:28])=[O:27])[CH2:17][C:18]1[CH:19]=[CH:20][C:21]([OH:25])=[C:22]([OH:24])[CH:23]=1>C(O)C>[CH:1]1[C:6]([CH2:7][C@H:8]([NH2:12])[C:9]([OH:11])=[O:10])=[CH:5][C:4]([OH:13])=[C:3]([OH:14])[CH:2]=1.[CH3:15][C@@:16]([NH:29][NH2:30])([C:26]([OH:28])=[O:27])[CH2:17][C:18]1[CH:19]=[CH:20][C:21]([OH:25])=[C:22]([OH:24])[CH:23]=1

Participants

4

Reactant 2

HCID 6047Levodopa3×HCID 34359Carbidopa2×

Product 1

HCID 104778Carbidopa-levodopa mixt.

Reagents, catalysts & solvents 1

HCID 702EthanolSolvent

Procedure

The formulations in Table 7, containing 200 mg levodopa and 50 mg carbidopa, were prepared as follows. Drug granulate: a solution of 0.75% w/v Klucel LF in ethanol was used as a binding solution for a mixture of 4:1 levodopa:carbidopa. The granulation was carried out in a Zanchetta Rotolab one pot granulator. The granulate was either dried under vacuum in the granulator or air dried at room temperature protected from light. The final composition of the granulate was levodopa 80.5%, Carbidopa 19.9%, Klucel LF 0.6%. A drug granulate containing levodopa was prepared by the same method. Final composition: 99.4% levodopa, 0.6% Klucel LF.

Workup

  1. customwere prepared
  2. customThe granulate was either dried under vacuum in the granulator or air
  3. customdried at room temperature
  4. additionA drug granulate containing levodopa
  5. customwas prepared by the same method

Sources & evidence

ORD record
ord-baa2f355639f43ea9ef35f2ce9177394
Source dataset
uspto-grants-2010_03
Patent number
US07674480B2

Reaction notes

Loading…