Claims (1)
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A8 B8 C8 D8 々、申請專利範圍 4A :第9 1 1 22057號專利申請案 中文申請專利範圍替換本·· (請先閱讀背面之注意事項再填寫本頁) 民國94年7月15日修正 1 · 一種製備結晶狀加巴噴丁脫水物形式B之方法，包 含： U)將加巴噴丁單水合物脫水以形成結晶狀加巴噴丁脫 水物形式A，及 (b)將脫水物A置於周圍溫度下以形成結晶狀加巴噴丁 脫水物形式B。 2.如申請專利範圍第1項之方法，其中脫水步驟（a)係 施用真空、乾燥劑或加熱進行。 3·如申請專利範圍第1項之方法，其中加巴噴丁單水 合物是在水活性維持低於約0.8至約0.9的環境下脫水。 4. 如申請專利範圍第2項之方法，其中加熱之溫度爲 約50°C至低於加巴噴丁單水合物熔點之溫度。 5. 如申請專利範圍第1項之方法，其中脫水物形式A 係置於惰性環境或密封容器中。 經濟部智慧財產局員工消費合作社印製 6. 如申請專利範圍第2項之方法，其中加巴噴丁單水 合物係製備自下列步驟，其係包含： U)在水活性數値大於約0.8至約0.9之溶劑或溶劑混合 物中懸浮加巴噴丁； (b)結晶以及用濾器收集加巴噴丁單水合物。 7. 如申請專利範圍第6項之方法，其中溶劑爲水。 8. —種結晶狀加巴噴丁脫水物形式A，其具有以CuKa 本紙張尺度適用中國國家標準（CNS ) A4規格（210 X 297公釐）-1 - 1245033 A8 B8 C8 D8 々、申請專利範圍 輻射線測得之X射線粉末繞射，該粉末繞射包含下列2-Θ 値爲·· 18.8 及 25.1。 (請先聞讀背面之注意事項再填寫本頁) 9. 一種結晶狀加巴噴丁脫水物形式A，其具有以CuKa 輻射線測得之X射線粉末繞射，該粉末繞射包含下列2 - Θ 値：18.8 、 25.1 及 26.1 。 I 〇. —種結晶狀加巴噴丁脫水物形式A，其具有以 CuKa輻射線測得之X射線粉末繞射，該粉末繞射包含下列 2-Θ 値：6.2、12.5、16.1、18.8、19.2、25.1 及 26.1。 II · 一種結晶狀加巴噴丁脫水物形式A，其特徵在於當 參考六甲基苯的甲基在17.3ppm之外部信號時，其固態13C 核磁共振用百萬分之一表示之化學位移爲：22.1、27.0、 33.7、36.2、37.6、41.0、51.0 以及 177.4。 1 2. —種結晶狀加巴噴丁脫水物形式B，其具有使用 CuKa輻射線測量之X射線粉末繞射，該粉末繞射包含下列 2-Θ 値爲：6.0、7.7 及 18.00。 經濟部智慧財產局員工消費合作社印製 Π. —種結晶狀加巴噴丁脫水物形式B，其具有以 CuKa輻射線測得之X射線粉末繞射，該粉末繞射包含下列 2-Θ 値：6.0, 7.7、16.8 及 18.0。 14· 一種結晶狀加巴噴丁脫水物形式B，其具有以 CuKa輻射線測得之X射線粉末繞射，該粉末繞射包含下列 2-Θ 値：6.0、7.7、16.8、18.0、20.6 以及 24.3。 15· —種結晶狀加巴噴丁脫水物形式B，其特徵在於當 參考六甲基苯的甲基在17.3ppm之外部信號時，其固態13C 核磁共振用百萬分之一表示之化學位移爲：23.3、28.5、 -2- 本紙張尺度適用中國國家標準（CNS ) A4说格（210 X 297公釐） 1245033 A8 B8 C8 D8 六、申請專利範圍 3 5.0、36.2、37.1、42.3、48.2 以及 178.3 (請先閱讀背面之注意事項再填寫本頁) 經濟部智慧財產局員工消費合作社印製 -3- 本紙張尺度適用中國國家標準（CNS ) A4規格（210X297公釐）A8 B8 C8 D8 々 、 Patent application scope 4A: No. 9 1 1 22057 Chinese patent application scope replacement ... (Please read the precautions on the back before filling out this page) Amended on July 15, 1994 · A method for preparing crystalline gabapentin dehydrate form B, comprising: U) dehydrating gabapentin monohydrate to form crystalline gabapentin dehydrate form A, and (b) placing dehydrated A at ambient temperature to form a crystalline form Gabapentin Dehydrate Form B. 2. The method of claim 1, wherein the dehydration step (a) is performed by applying a vacuum, a desiccant, or heat. 3. The method of claim 1 in which the gabapentin monohydrate is dehydrated in an environment where water activity is maintained below about 0.8 to about 0.9. 4. The method according to item 2 of the patent application, wherein the heating temperature is about 50 ° C to a temperature lower than the melting point of gabapentin monohydrate. 5. The method according to item 1 of the patent application, wherein the dehydrated form A is placed in an inert environment or in a sealed container. Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs 6. If the method of the scope of patent application is the second, the gabapentin monohydrate is prepared from the following steps, which include: U) The water activity number is greater than about 0.8 to about 0.9 Gabapentin is suspended in a solvent or solvent mixture; (b) crystallizing and collecting gabapentin monohydrate with a filter. 7. The method of claim 6 in which the solvent is water. 8. A kind of crystalline gabapentin dehydrate form A, which has the Chinese standard (CNS) A4 specification (210 X 297 mm) -1-1245033 A8 B8 C8 D8 in CuKa paper size 々, patent application radiation Measured X-ray powder diffraction. The powder diffraction contains the following 2-Θ 2 as 18.8 and 25.1. (Please read the notes on the back before filling this page) 9. A crystalline gabapentin dehydrate form A, which has an X-ray powder diffraction measured by CuKa radiation, the powder diffraction contains the following 2-Θ 値: 18.8, 25.1 and 26.1. I 〇. A crystalline gabapentin dehydrate form A, which has an X-ray powder diffraction measured with CuKa radiation, the powder diffraction contains the following 2-Θ 値: 6.2, 12.5, 16.1, 18.8, 19.2, 25.1 And 26.1. II · A crystalline form of gabapentin dehydrate, characterized in that when reference is made to the external signal of the methyl group of hexamethylbenzene at 17.3 ppm, the chemical shift of solid-state 13C nuclear magnetic resonance expressed in parts per million is: 22.1, 27.0, 33.7, 36.2, 37.6, 41.0, 51.0, and 177.4. 1 2. A crystalline gabapentin dehydrate form B, which has an X-ray powder diffraction measured using CuKa radiation, the powder diffraction containing the following 2-Θ 値: 6.0, 7.7 and 18.00. Printed by the Consumer Cooperative of the Intellectual Property Bureau of the Ministry of Economy Π. A crystalline gabapentin dehydrate form B, which has an X-ray powder diffraction measured with CuKa radiation, the powder diffraction contains the following 2-Θ 値: 6.0, 7.7, 16.8 and 18.0. 14. A crystalline gabapentin dehydrate form B, which has an X-ray powder diffraction measured with CuKa radiation, the powder diffraction containing the following 2-Θ 値: 6.0, 7.7, 16.8, 18.0, 20.6, and 24.3. 15 · —A crystalline gabapentin dehydrate form B, characterized in that when referring to an external signal of the methyl group of hexamethylbenzene at 17.3 ppm, the chemical shift of the solid-state 13C nuclear magnetic resonance expressed in parts per million is: 23.3 , 28.5, -2- This paper size applies to Chinese National Standard (CNS) A4 format (210 X 297 mm) 1245033 A8 B8 C8 D8 VI. Patent application scope 3 5.0, 36.2, 37.1, 42.3, 48.2, and 178.3 (please Please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Intellectual Property Bureau of the Ministry of Economic Affairs -3- This paper size applies to China National Standard (CNS) A4 (210X297 mm)