Sucrose → Phentermine

HRID 1484013Notes

Reaction equation

HRID 1484013 reaction equation
[CH3:1][C:2]([NH2:11])([CH2:4][C:5]1[CH:6]=[CH:7][CH:8]=[CH:9][CH:10]=1)[CH3:3].Cl.C(O)[C@H]1O[C@H](O[C@]2(CO)O[C@H](CO)[C@@H](O)[C@@H]2O)[C@H](O)[C@@H](O)[C@@H]1O>O>[CH3:3][C:2]([NH2:11])([CH2:4][C:5]1[CH:6]=[CH:7][CH:8]=[CH:9][CH:10]=1)[CH3:1]

Participants

4

Reactant 2

HCID 5988Sucrose2×HCID 70969Phentermine Hydrochloride

Product 1

HCID 4771Phentermine

Reagents, catalysts & solvents 1

HCID 962WaterSolvent2×

Procedure

Preparation method: 74.7 g of phentermine hydrochloride (corresponding to 60 g of phentermine) that passed through 80-mesh sieve was weighed, 6.0 g of hydropropylmethylcellulose (HPMC) was weighed as binding agent, they were added with 200 ml of water, stirred and dissolved under heating at 40° C.-50° C., and added with water to reach 300 ml, to obtain a drug-containing coating solution. 400 g of sucrose pellet core (0.71-0.85 mm) was placed in a fluidized bed bottom spray coating pan, inlet air temperature was set at 50-70° C., inlet air pressure was 0.35 bar, atomization pressure was 1.0-2.0 bar, solution spray rate was 3-12 g/min (regulated according to fluidization state at any time). The drug-containing coating solution was sprayed in manner of bottom spray on surface of blank pellet cores when the sucrose pellet cores were in fluidization state, after end of drug-loading, the material was further fluidized at 45° C. for 5 min, and then taken out to obtain drug-loaded pellet of phentermine.

Workup

  1. customPreparation method
  2. dissolutiondissolved
  3. temperatureunder heating at 40° C.-50° C.
  4. customto obtain a drug-containing coating solution
  5. customwas set at 50-70° C.
  6. custominlet air pressure was

Sources & evidence

ORD record
ord-afa482e9bf47498591d8466e73010e83
Source dataset
uspto-grants-2016_08
Patent number
US09421188B2

Reaction notes

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