Methylphenidate Hydrochloride → Methylphenidate

HRID 1257955Notes

Reaction equation

HRID 1257955 reaction equation
[CH3:1][O:2][C:3]([CH:5]([CH:12]1[NH:17][CH2:16][CH2:15][CH2:14][CH2:13]1)[C:6]1[CH:7]=[CH:8][CH:9]=[CH:10][CH:11]=1)=[O:4].Cl>O>[CH3:1][O:2][C:3]([CH:5]([CH:12]1[NH:17][CH2:16][CH2:15][CH2:14][CH2:13]1)[C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][CH:7]=1)=[O:4]

Participants

3

Reactant 1

HCID 9280Methylphenidate Hydrochloride

Product 1

HCID 4158Methylphenidate

Reagents, catalysts & solvents 1

HCID 962WaterSolvent

Conditions

Temperature
32 °C

Procedure

Methylphenidate hydrochloride (850 g), talc (24 g) and hydroxypropyl methylcellulose (HPMC, 48.5 g) were dissolved in water (4800 g) to prepare a coating solution. Microcrystalline cellulose CP102 (106-212 μm, Celphere® Asahi Kasei, Japan, 425 g) was loaded in a GPCG-1 (Glatt, Germany) flow coater. While spraying the prepared coating solution by bottom spraying, coating was performed while maintaining the product temperature at 29-35° C. until the coating solution was exhausted. Then, after drying at 50° C., a core material (1330 g) comprising methylphenidate was obtained. The drug content measured by HPLC was about 65.4%. The obtained core material mostly passed through a 300 μm sieve. When analyzed by scanning electron microscopy (SEM), most of the particles had a diameter in the range from 180 to 300 μm.

Workup

  1. customto prepare a coating solution
  2. customThen, after drying at 50° C.
  3. customwas obtained

Sources & evidence

ORD record
ord-e21277735a4a442d979fc6c0e4d5a450
Source dataset
uspto-grants-2013_06
Patent number
US08465768B2

Reaction notes

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