EP0340677A2
Expired / Lapsed
EP
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Gabapentin monohydrate and a process for producing the same
Assignee: Warner Lambert Co LLC
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Filing: 1989-04-28
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Granted: —
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Expires: 2009-04-28
Abstract
Abstract A novel crystalline form of gabapentin and a novel processes for the small and large scale preparations of the anticonvulsant compound in a highly pure state is disclosed. This novel hydrate is produced by a cost effective process which provides an additional purification stage.
Inventors
- 👤 Donald Eugene Butler
- 👤 Barbara Jean Greenman
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-05 20:04
CPC Classifications
C; C07; C07C; C07C229/00; C07C229/02; C07C229/28; A; A61; A61P; A61P25/00; A61P25/08; C07C2601/00; C07C2601/12; C07C2601/14
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
5 words
Gabapentin monohydrate having the formula
Claim 2
Dependent Claim
5 words
Gabapentin monohydrate having the formula
Claim 3
Dependent Claim
43 words
Gabapentin monohydrate according to claim 1 exhibiting essentially the following X-ray diffraction data: Spacing 'd' Relative Intensities 14.255 99 7.196 99 5.438 4 4.848 99 4.575 7 4.291 7 3.633 99 3.376 21 3.220 9 2.903 28 2.771 23 2.356 7 2.344 12
Claim 4
Dependent Claim
20 words
Gabapentin monohydrate according to Claim 1 and 2 having a bulk density within the range of 0.35 to 0.49 g/cm³.
Claim 5
Dependent Claim
78 words
A process for the preparation of a compound of formula which comprises: (a) pouring a solution of an acid salt of (1-aminomethyl)-cyclohexaneacetic acid in deionized water onto an ion exchange column in the basic form and eluting the column with deionized water; (b) concentrating the eluate producing a slurry; (c) cooling and adding alcohol to the slurry from step (b); (d) cooling and centrifuging the slurry from step (c); and (e) drying the precipitate of the desired product.
Claim 6
Dependent Claim
78 words
A process for the preparation of a compound of formula which comprises: (a) pouring a solution of an acid salt of (1-aminomethyl)-cyclohexaneacetic acid in deionized water onto an ion exchange column in the basic form and eluting the column with deionized water; (b) concentrating the eluate producing a slurry; (c) cooling and adding alcohol to the slurry from step (b); (d) cooling and centrifuging the slurry from step (c); and (e) drying the precipitate of the desired product.
Claim 7
Dependent Claim
18 words
A process according to Claim 4 wherein in step (a) the acid salt is gabapentin hydrochloride hydrate (4:4:1).
Claim 8
Dependent Claim
37 words
A process according to Claim 4 wherein in step (b) the eluate is concentrated in a glass-lined still at 72 - 77 hPa of vacuum at a temperature of from 25°C to 50°C to produce a slurry.
Claim 9
Dependent Claim
29 words
A process according to Claim 4 wherein in step (c) the slurry is cooled to 25° to 45°C for 1 to 3 hours and the alcohol added is 2-propanol.
Claim 10
Dependent Claim
23 words
A process according to Claim 4 wherein in step (d) the slurry is cooled to -10°C to 0°C for 12 to 16 hours.
Claim 11
Dependent Claim
26 words
A process according to Claim 4 wherein in step (e) the precipitate is dried at 29-31 inches of vacuum at 25-35°C for 8 to 24 hours.
Claim 12
Dependent Claim
44 words
A process for the preparation of a compound of formula which comprises: (a) dissolving pure gabapentin monohydrate in methanol; (b) diluting and cooling the solution from step (a) producing a slurry; (c) centrifuging the slurry from step (b) and drying the precipitate formula above.
Claim 13
Dependent Claim
44 words
A process for the preparation of a compound of formula which comprises: (a) dissolving pure gabapentin monohydrate in methanol; (b) diluting and cooling the solution from step (a) producing a slurry; (c) centrifuging the slurry from step (b) and drying the precipitate formula above.
Claim 14
Dependent Claim
10 words
A pharmaceutical composition containing gabapentin monohydrate and pharmaceutically acceptable additives.
Claim 15
Dependent Claim
10 words
A pharmaceutical composition containing gabapentin monohydrate and pharmaceutically acceptable additives.
Claim 16
Dependent Claim
22 words
Use of gabapentin monohydrate for the preparation of pharmaceutical compositions useful in the treatment of epilepsy, faintness atacks, hypokinesia and cranial traumas.
Claim 17
Dependent Claim
22 words
Use of gabapentin monohydrate for the preparation of pharmaceutical compositions useful in the treatment of epilepsy, faintness atacks, hypokinesia and cranial traumas.
References Cited (Backward Citations)
No citation records indexed.
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