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Claims for Patent: 6,054,482

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Claims for Patent: 6,054,482

Title: Lactam-free amino acids
Abstract:The present invention concerns cyclic amino acids of formula ##STR1## substantially free from the lactam ##STR2## wherein n is an integer of from 4 to 6, a process for the preparation thereof, compositions containing the compounds and methods of using them.
Inventor(s): Augart; Helmut (Waldkirch, DE), Gebhardt; Uwe (Waldkirch, DE), Herrmann; Wolfgang (Merzhausen, DE)
Assignee: Godecke Aktiengesellschaft (Berlin, DE)
Application Number:08/377,618
Patent Claims: 1. A process for the preparation of a compound of Formula VII ##STR17## wherein n is an integer of from 5 containing less than 0.5% by weight of a compound of Formula VIII ##STR18## wherein n is as defined above and less than 20 ppm of an anion of a mineral acid comprising:

(a) hydrolysis of a compound of Formula VII containing a compound of Formula VIII or of a compound of Formula VIII alone with a mixture of equal volumes of a concentrated mineral acid and water to afford an acid addition salt of a compound of Formula VII and

(b) converting the acid addition salt of a compound of Formula VII by ion exchange to a compound of Formula VII containing less than 0.5% by weight of a compound of Formula VIII and less than 20 ppm of an anion of a mineral acid.

2. A process according to claim 1, wherein in step (a) the acid is hydrochloric acid.

3. A process for preparing stable and pure pharmaceutical compositions containing a compound of formula (VII) ##STR19## wherein n is an integer of 5 and pharmaceutically acceptable adjuvants consisting of the steps of

(a) hydrolysis of a compound of formula VII ##STR20## wherein n is as defined above containing a compound of formula VIII ##STR21## wherein n is as defined above or a compound of Formula VIII alone with a mixture of equal volumes of a concentrated mineral acid and water to afford an acid addition salt of a compound of formula VII substantially free of a compound of formula VIII,

(b) converting the acid addition salt of a compound of formula VII by ion exchange to a compound of formula VII containing less than 0.5% by weight of a compound of formula VIII, wherein the proportion of remaining anion of a mineral acid does not exceed 20 ppm,

(c) adding pharmaceutically acceptable adjuvants to form a pharmaceutical composition wherein the adjuvants do not promote the formation of a lactam of formula VIII ensuring that the lactam formation under the storage conditions at 25.degree. C. and an atmospheric humidity of 50% does not increase within a period of time of one year after the production of the pharmaceutical compositions or of the active material by more than 0.2% by weight, referred to the pure active material.

4. A process of claim 3, wherein the pharmaceutically acceptable adjuvants are selected from the group consisting of hydroxypropylmethylcellulose, polyvinylpyrrolidone, crospovidone, poloxamer 407, poloxamer 188, sodium starch glycolate, copolyvidone, maize starch, cyclodextrine, lactose, talc and copolymers of dimethylamino-methacrylic acid and neutral methacrylic acid ester.

5. A process of claim 3, wherein the mineral acid is hydrochloric acid.

6. A process of claim 4, wherein the mineral acid is hydrocholoric acid.

7. A stable and pure pharmaceutical composition in unit dry medicinal dosage form consisting essentially of:

(i) an active ingredient which is gabapentin in the free amino acid, crystalline anhydrous form containing less than 0.5% by weight of its corresponding lactam and less than 20 ppm of an anion of a mineral acid and

(ii) one or more pharmaceutically acceptable adjuvants that do not promote conversion of more than 0.2% by weight of the gabapentin to its corresponding lactam form when stored at 25.degree. C. and an atmospheric humidity of 50% for one year.

8. A pharmaceutical composition according to claim 7, in which the pharmaceutically acceptable aadjuvant is selected from the group consisting of hydroxypropyl-methylcellulose, polyvinylpyrrolidone, crospovidon, poloxamer 407, poloxamer 188, sodium starch glycolate, copolyvidone, maize starch, cyclodextrin, lactose, talc, co-polymers of dimethylamino-methacrylic acid and neutral methacrylic acid ester.

9. A pharmaceutical composition according to claim 7, wherein the dry medicinal dosage form is a tablet.

10. A pharmaceutical composition according to claim 7, wherein the dry medicinal dosage form is a capsule.

11. A pharmaceutical composition according to claim 7,wherein in (i) the mineral acid is hydrochloric acid.
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