Vigabatrin API, vigabatrin solid composition and preparation method thereof

Abstract

The present invention provides a vigabatrin API, a preparation method thereof, and a vigabatrin solid composition, and a preparation method thereof. The vigabatrin API has a needle-shaped particle size D90 of 200 to 460 μm. The vigabatrin API is easy to shape, and the vigabatrin solid composition prepared using the vigabatrin API has good dispersibility and minimal variability in loading. The preparation method is simple to operate, has a high yield, and is suitable for industrial production.

Description

Technical Field

[0001] The present invention relates to the field of medicine, and in particular to a vigabatrin bulk drug, a vigabatrin solid composition and a preparation method thereof. Background Art

[0002] The chemical name of vigabatrin is 4-amino-5-hexenoic acid, and its molecular formula is C6H 11 NO2, with a molecular weight of 129.157, is an analog of gamma-aminobutyric acid (GABA). It can specifically and irreversibly bind to GABA aminotransferase, leading to increased GABA concentrations in the brain, thereby exerting an anti-epileptic effect. As an adjunctive therapy, vigabatrin can be used to treat patients who are refractory to other anti-epileptic drugs, particularly those with partial-onset seizures (primarily used to control complex partial-onset seizures). It can also be used for infants with West syndrome (infantile spasms). As an adjunctive therapy, vigabatrin has shown good efficacy. When used alone, it is effective in newly diagnosed patients.

[0003] Currently, vigabatrin is available in only two dosage forms: oral tablets and powder. Existing technologies for preparing vigabatrin APIs suffer from uneven particle size, leading to poor flowability and large variations in fill volume when preparing vigabatrin powders.

[0004] Therefore, the current vigabatrin solid composition and preparation method thereof still need to be studied. Summary of the Invention

[0005] The present invention aims to solve, at least to a certain extent, at least one of the technical problems existing in the prior art. To this end, the present invention provides a vigabatrin bulk drug substance and a preparation method thereof, as well as a vigabatrin solid composition and a preparation method thereof. The vigabatrin bulk drug substance is easy to shape, and the vigabatrin solid composition prepared using the vigabatrin bulk drug substance has good dispersibility and small variation in loading amount. The preparation method is simple to operate, has a high yield, and is suitable for industrial production.

[0006] In one aspect, the present invention provides a vigabatrin API. According to an embodiment of the present invention, the vigabatrin API has a needle-shaped particle size D90 of 200 to 460 μm. The vigabatrin API of the present invention is easy to shape, and a vigabatrin solid composition prepared using the vigabatrin API exhibits good dispersibility and minimal variation in loading.

[0007] It should be noted that the "particle size D90" described herein refers to the particle size at which the cumulative particle size distribution of a sample reaches 90%. Specifically, "particle size D90 of 200-460 μm" means that the average particle size of 90% of the particles is 200-460 μm.

[0008] According to an embodiment of the present invention, the purity of the vigabatrin API is not less than 98%. In some preferred embodiments, the purity of the vigabatrin API is not less than 99%.

[0009] In another aspect of the invention, a method for preparing the aforementioned vigabatrin API is provided. According to an embodiment of the invention, the method comprises: step 1: mixing crude vigabatrin with water, filtering the resulting mixture, and collecting the filtrate; step 2: mixing the filtrate with an alcohol, subjecting the mixture to heat preservation, cooling, and crystallization, and collecting the crystals to obtain the vigabatrin API; wherein, in step 1, the mass ratio of water to crude vigabatrin is (1.8-2.5):1.

[0010] The inventors found that the ratio between water and crude vigabatrin significantly affects the morphology and particle size distribution of the final crystals formed. Furthermore, after a large number of experiments, the inventors found that when the mass ratio of water to crude vigabatrin is (1.8-2.5):1, the morphology of the obtained vigabatrin crystals is needle-shaped, and the particle size distribution is D90=200-460 μm.

[0011] According to an embodiment of the present invention, in step 1, the purity of the crude vigabatrin is 80-88%, thereby facilitating the formation of crystals.

[0012] According to an embodiment of the present invention, in step 2, the alcohol substance is selected from 1-6 hydric alcohols. In some preferred embodiments, the alcohol substance is ethanol or isopropanol.

[0013] According to an embodiment of the present invention, the mass ratio of the alcohol substance to the crude vigabatrin product is (8-12):1. The inventors have discovered that the mass ratio of the alcohol substance to the crude vigabatrin product affects the morphology and particle size distribution of the ultimately formed crystals. Furthermore, through extensive experiments, the inventors have discovered that when the mass ratio of the alcohol substance to the crude vigabatrin product is (8-12):1, the vigabatrin crystals obtained have a needle-like morphology and a particle size distribution of D90 = 200-460 μm.

[0014] According to an embodiment of the present invention, the crystallization is carried out at 0-20° C. This is conducive to the precipitation of vigabatrin crystals, and needle-shaped crystals with a particle size D90 of 200-460 μm can be obtained.

[0015] According to an embodiment of the present invention, the mixing is performed by dropwise adding the filtrate to the alcoholic substance, thereby facilitating the production of needle-shaped crystals with a particle size D90 of 200 to 460 μm, and the obtained vigabatrin API has a high purity.

[0016] According to an embodiment of the present invention, the dropping speed is 10 to 30 mL / min, which helps to obtain needle-shaped crystals with a particle size D90 of 200 to 460 μm.

[0017] In another aspect, the present invention provides a vigabatrin solid composition. According to an embodiment of the present invention, the vigabatrin solid composition comprises: the aforementioned vigabatrin API and a pharmaceutically acceptable excipient. Thus, the vigabatrin solid composition according to the embodiment of the present invention has good dispersibility and minimal variation in loading.

[0018] According to an embodiment of the present invention, the dosage form of the vigabatrin solid composition is selected from tablets or powders.

[0019] According to an embodiment of the present invention, the auxiliary material includes povidone. Povidone has the properties of bonding, thickening, dispersing, film-forming, and complexing, and can be used as a binder in solid compositions.

[0020] In another aspect, the present invention provides a method for preparing the aforementioned solid vigabatrin composition. According to an embodiment of the present invention, the method comprises mixing the vigabatrin drug substance with a pharmaceutically acceptable excipient, granulating, and drying to obtain the solid vigabatrin composition. Thus, the solid vigabatrin composition prepared according to the method of the embodiment of the present invention exhibits good dispersibility and minimal variability in loading. This preparation method is simple to operate, has a high yield, and is suitable for industrial production.

[0021] According to an embodiment of the present invention, the vigabatrin bulk drug is obtained by the above-mentioned method for preparing the vigabatrin bulk drug.

[0022] According to an embodiment of the present invention, the method further comprises: mixing the vigabatrin API, an alcohol, and a pharmaceutically acceptable excipient to obtain a mixture; granulating the mixture to obtain granules; sizing the granules, drying the granules, sieving the dried granules, and collecting the granules to obtain the vigabatrin solid composition. Thus, the prepared vigabatrin solid composition has good dispersibility and minimal variation in loading.

[0023] Additional aspects and advantages of the present invention will be set forth in part in the description which follows and, in part, will be obvious from the description which follows, or may be learned by practice of the present invention. BRIEF DESCRIPTION OF THE DRAWINGS

[0024] The above and / or additional aspects and advantages of the present invention will become apparent and readily understood from the following description of the embodiments with reference to the accompanying drawings, in which:

[0025] Figure 1The figure shows the morphology of the vigabatrin bulk drug prepared according to Example 3 of the present invention;

[0026] Figure 2 The figure shows the morphology of the vigabatrin bulk drug prepared according to Comparative Example 3 of the present invention. DETAILED DESCRIPTION

[0027] Below, the scheme of the present invention will be explained in conjunction with embodiment.It will be understood by those skilled in the art that the following examples are only used to illustrate the present invention and should not be regarded as limiting the scope of the present invention.In the embodiment, if specific technology or conditions are not indicated, the technology or conditions described in the literature in this area or the product instructions are used.The reagents or instruments used are not indicated by the manufacturer, and are all conventional products that can be obtained by commercial purchase.

[0028] Example 1

[0029] In this example, formamido-5-vinyl-2-pyrrolidone was reacted in concentrated hydrochloric acid and acetic acid to obtain crude vigabatrin, as shown in the following reaction formula:

[0030]

[0031] 1.5 g of 3-formamido-5-vinyl-2-pyrrolidone was added to a three-necked flask, followed by a mixture of 20 ml of concentrated hydrochloric acid and 10 ml of glacial acetic acid, and the mixture was heated under reflux for 16 hours. The reaction solution was then evaporated to dryness under reduced pressure, and the residue was dissolved in water and extracted with diethyl ether. The aqueous phase was treated with activated carbon and neutralized with 2M aqueous ammonia. The neutral solution was passed through an Amberlite IR120 column, and the product was eluted with 2M aqueous ammonia. Evaporation under reduced pressure yielded a residual solid, which was recrystallized from aqueous acetone to obtain crude vigabatrin in a yield of 46.9%. The crude product had a purity of 84.68%.

[0032] The obtained crude vigabatrin was used for subsequent experiments.

[0033] Example 2

[0034] In this example, the following method was used to prepare the vigabatrin bulk drug:

[0035] Weigh 10g of crude vigabatrin into 18g of purified water, dissolve at 50°C, and filter. Transfer the filtrate to a three-necked flask, and add 80g of isopropyl alcohol dropwise at a rate of 10ml / min. Maintain the mixture at 50°C for 1 hour, then slowly cool to 10°C and maintain for 2 hours to allow crystallization. Filter, wash, and dry to obtain the vigabatrin API. The vigabatrin product has a particle size (D90) of 201.5μm and a needle-like morphology. Its purity is 98.53%.

[0036] Example 3

[0037] In this example, the following method was used to prepare the vigabatrin bulk drug:

[0038] Weigh 10g of crude vigabatrin, add it to 20g of purified water, dissolve it at 50℃ and filter it. Transfer the filtrate to a three-necked flask, add 40g of isopropanol at a rate of 30ml / min, keep it at 50℃ for 1h, then slowly cool it to 0℃, keep it at this temperature for 2h to crystallize, filter it, wash it and dry it to obtain the vigabatrin raw material product. The particle size D90 of the vigabatrin product is 316.5μm, and the morphology is needle-shaped. The morphology is shown in the figure. Figure 1 As shown. The purity is 98.27%.

[0039] Example 4

[0040] In this example, the following method was used to prepare the vigabatrin bulk drug:

[0041] Weigh 10g of crude vigabatrin into 25g of purified water, dissolve at 50°C, and filter. Transfer the filtrate to a three-necked flask, and add 120g of isopropyl alcohol dropwise at a rate of 20ml / min. Maintain the mixture at 50°C for 1 hour, then slowly cool to 20°C and crystallize for 2 hours. Filter, wash, and dry to obtain the vigabatrin API. The vigabatrin product has a particle size (D90) of 456.8μm and a needle-like morphology. Its purity is 99.88%.

[0042] Example 5

[0043] In this example, the following method was used to prepare the vigabatrin bulk drug:

[0044] Weigh 10g of crude vigabatrin into 20g of purified water, dissolve at 50°C, and filter. Transfer the filtrate to a three-necked flask, and add 100g of ethanol dropwise at a rate of 20ml / min. Maintain the mixture at 50°C for 1 hour, then slowly cool to 10°C and crystallize for 2 hours. Filter, wash, and dry to obtain the vigabatrin API. The vigabatrin product has a particle size (D90) of 278.3μm and a needle-like morphology. Its purity is 99.86%.

[0045] Comparative Example 1

[0046] In this comparative example, the following method was used to prepare the vigabatrin bulk drug:

[0047] Weigh 10g of crude vigabatrin into 16g of purified water, dissolve at 50°C, and filter. Transfer the filtrate to a three-necked flask, and add 80g of isopropyl alcohol dropwise at a rate of 10ml / min. Maintain the mixture at 50°C for 1 hour, then slowly cool to 10°C and maintain for 2 hours to allow crystallization. Filter, wash, and dry to obtain the vigabatrin API. The vigabatrin product has a particle size (D90) of 158.8μm and a needle-like morphology. Its purity is 93.97%.

[0048] This indicates that the mass ratio of water to crude vigabatrin is too low, which will cause the particle size D90 of the vigabatrin API to be too low.

[0049] Comparative Example 2

[0050] In this comparative example, the following method was used to prepare the vigabatrin bulk drug:

[0051] Weigh 10g of crude vigabatrin into 18g of purified water, dissolve at 50°C, and filter. Transfer the filtrate to a three-necked flask, and add 140g of isopropyl alcohol dropwise at a rate of 10ml / min. Maintain the mixture at 50°C for 1 hour, then slowly cool to 10°C and allow crystallization to proceed for 2 hours. Filter, wash, and dry to obtain the vigabatrin API. The vigabatrin product has a particle size (D90) of 329.7μm and a spherical morphology. Its purity is 99.89%.

[0052] This indicates that the mass ratio of alcohol to crude vigabatrin is too high, and needle-shaped vigabatrin API cannot be obtained.

[0053] Comparative Example 3

[0054] In this comparative example, the following method was used to prepare the vigabatrin bulk drug:

[0055] Weigh 10g of crude vigabatrin, add it to 18g of purified water, dissolve it at 50℃ and filter it. Transfer the filtrate to a three-necked flask, add 80g of isopropanol at a rate of 8ml / min, keep it at 50℃ for 1h, then slowly cool it to 10℃, keep it at this temperature for 2h to crystallize, filter it, wash it and dry it to obtain the vigabatrin raw material product. The particle size D90 of the vigabatrin product is 386.4μm, and the morphology is columnar. The morphology is as shown in the figure. Figure 2 As shown. The purity is 97.34%.

[0056] This indicates that the dripping rate of the filtrate is too low and the needle-shaped vigabatrin raw material cannot be obtained.

[0057] Example 6

[0058] The amounts of each raw material of the vigabatrin powder of the present embodiment are as follows:

[0059] Raw materials Quantity per 1000 packs (g) Proportion Vigabatrin raw materials 500 99.01％ Povidone 5 0.99％ Gross weight 505 100％

[0060] The particle size D90 of the vigabatrin raw material used is 201.5 μm, and the vigabatrin is needle-shaped (prepared in Example 2).

[0061] Preparation method of vigabatrin powder:

[0062] (1) Slurry preparation: Weigh 50 g of ethanol, add the prescribed amount of polyvinylpyrrolidone (PVP) and stir until completely dissolved as a binder;

[0063] (2) Granulation: The prescribed amount of vigabatrin API is placed in a wet granulator for wet granulation to obtain wet granules;

[0064] (3) Wet granulation: wet granulation is performed using a 30-mesh filter;

[0065] (4) Drying: Drying is carried out using a fluidized bed.

[0066] (5) Dry granulation: The dried material is dry granulated using a 40-mesh sieve.

[0067] (6) Filling: Fill at 505 mg / bag.

[0068] The bulk density, tap density, angle of repose, and Carr's index of the dry granules obtained in step (5) were tested, and the Hausner ratio was calculated to evaluate the fluidity. The results were: a Hausner ratio of 1.15, an angle of repose of 33.24°, and a Carr's index of 13.4%, indicating good fluidity.

[0069] Ten bags of the sample obtained in step (6) were filled and the weight of each bag was accurately weighed. The amount of each bag was compared with the labeled amount, and the difference in amount was calculated. The results are shown in Table 1.

[0070] In accordance with the requirements of the "Filling Volume Variance" section of the General Rules of Part IV of the 2020 Chinese Pharmacopoeia, the average filling volume or labeled filling volume is between 0.5g and 1.5g, and the filling volume variance limit (for traditional Chinese medicine and chemical medicine) is ±8%. No more than two bags of powders may exceed the filling volume variance limit, and no single bag may exceed 1 times the filling volume variance limit.

[0071] It can be seen from Table 1 that the difference in the filling amount of the powders obtained using the above formula meets the requirements of the [Filling Amount Difference] item in the General Rules of Part IV of the 2020 Edition of the Chinese Pharmacopoeia.

[0072] Table 1 Results of filling quantity difference detection

[0073]

[0074] Example 7

[0075] The amounts of the raw materials of the vigabatrin powder of this embodiment are the same as those in Example 6.

[0076] The particle size D90 of the vigabatrin raw material used is 316.5 μm, and the vigabatrin is needle-shaped (prepared in Example 3).

[0077] The preparation method of vigabatrin powder is the same as that in Example 6.

[0078] The bulk density, tap density, and angle of repose of the dry granules obtained in step (5) were measured, and the Hausner ratio was calculated to evaluate the fluidity. The results were: a Hausner ratio of 1.12, an angle of repose of 31.43°, and a Carr index of 11.0%, indicating good fluidity.

[0079] Ten bags of the sample obtained in step (6) were filled and the weight of each bag was accurately weighed. The amount of each bag was compared with the labeled amount, and the difference in amount was calculated. The results are shown in Table 2.

[0080] In accordance with the requirements of the "Filling Volume Variance" section of the General Rules of Part IV of the 2020 Chinese Pharmacopoeia, the average filling volume or labeled filling volume is between 0.5g and 1.5g, and the filling volume variance limit (for traditional Chinese medicine and chemical medicine) is ±8%. No more than two bags of powders may exceed the filling volume variance limit, and no single bag may exceed 1 times the filling volume variance limit.

[0081] It can be seen from Table 2 that the difference in the filling amount of the powders obtained using the above formula meets the requirements of the general rules of Part IV of the 2020 edition of the Chinese Pharmacopoeia [Filling amount difference].

[0082] Table 2 Results of filling quantity difference detection

[0083]

[0084] Example 8

[0085] The amounts of the raw materials of the vigabatrin powder of this embodiment are the same as those in Example 6.

[0086] The particle size D90 of the vigabatrin raw material used is 456.8 μm, and the vigabatrin is needle-shaped (prepared in Example 4).

[0087] The preparation method of vigabatrin powder is the same as that in Example 6.

[0088] The bulk density, tap density, and angle of repose of the dry granules obtained in step (5) were measured, and the Hausner ratio was calculated to evaluate the fluidity. The results were: a Hausner ratio of 1.13, an angle of repose of 31.89°, and a Carr index of 11.8%, indicating good fluidity.

[0089] Ten bags of the sample obtained in step (6) were filled and the weight of each bag was accurately weighed. The amount of each bag was compared with the labeled amount, and the difference in amount was calculated. The results are shown in Table 3.

[0090] In accordance with the requirements of the "Filling Volume Variance" section of the General Rules of Part IV of the 2020 Chinese Pharmacopoeia, the average filling volume or labeled filling volume is between 0.5g and 1.5g, and the filling volume variance limit (for traditional Chinese medicine and chemical medicine) is ±8%. No more than two bags of powders may exceed the filling volume variance limit, and no single bag may exceed 1 times the filling volume variance limit.

[0091] It can be seen from Table 3 that the difference in the filling amount of the powders obtained using the above formula meets the requirements of the [Filling Amount Difference] item in the General Rules of Part IV of the 2020 Edition of the Chinese Pharmacopoeia.

[0092] Table 3 Results of filling quantity difference detection

[0093]

[0094] Comparative Example 4

[0095] The amounts of the raw materials of the vigabatrin powder of this embodiment are the same as those in Example 6.

[0096] The particle size D90 of the vigabatrin raw material used is 386.4 μm, and the vigabatrin is in columnar form (prepared in Comparative Example 4).

[0097] The preparation method of vigabatrin powder is the same as that in Example 6.

[0098] The bulk density, tap density, and angle of repose of the dry granules obtained in step (5) were measured, and the Hausner ratio was calculated to evaluate the fluidity. The results were: a Hausner ratio of 1.21, an angle of repose of 32.35°, and a Carr index of 17.6%, indicating that the fluidity was considered fair.

[0099] Take 10 bags of the filled test sample obtained in step (6), accurately weigh the weight of the contents of each bag, compare the amount of each bag with the labeled amount, and calculate the difference in amount. The test results are shown in Table 5.

[0100] In accordance with the requirements of the "Filling Volume Variance" section of the General Rules of Part IV of the 2020 Chinese Pharmacopoeia, the average filling volume or labeled filling volume is between 0.5g and 1.5g, and the filling volume variance limit (for traditional Chinese medicine and chemical medicine) is ±8%. No more than two bags of powders may exceed the filling volume variance limit, and no single bag may exceed 1 times the filling volume variance limit.

[0101] It can be seen from Table 4 that the difference in the filling amount of the powders obtained using the above formula does not meet the requirements of the [Filling Amount Difference] item in the General Rules of Part IV of the 2020 Edition of the Chinese Pharmacopoeia.

[0102] Table 4 Results of filling quantity difference detection

[0103]

[0104] Comparative Example 5

[0105] The amounts of the raw materials of the vigabatrin powder of this embodiment are the same as those in Example 6.

[0106] The particle size D90 of the vigabatrin raw material used is 173.4 μm, and the vigabatrin is needle-shaped (prepared in Comparative Example 1).

[0107] The preparation method of vigabatrin powder is the same as that in Example 6.

[0108] The bulk density, tap density, and angle of repose of the dry granules obtained in step (5) were measured, and the Hausner ratio was calculated to evaluate the fluidity. The results were: a Hausner ratio of 1.18, an angle of repose of 33.23°, and a Carr index of 15.5%, indicating that the fluidity was considered fair.

[0109] Take 10 bags of the filled test sample obtained in step (6), accurately weigh the weight of the contents of each bag, compare the amount of each bag with the labeled amount, and calculate the difference in amount. The test results are shown in Table 6.

[0110] In accordance with the requirements of the "Filling Volume Variance" section of the General Rules of Part IV of the 2020 Chinese Pharmacopoeia, the average filling volume or labeled filling volume is between 0.5g and 1.5g, and the filling volume variance limit (for traditional Chinese medicine and chemical medicine) is ±8%. No more than two bags of powders may exceed the filling volume variance limit, and no single bag may exceed 1 times the filling volume variance limit.

[0111] It can be seen from Table 5 that the difference in the filling amount of the powders obtained using the above formula does not meet the requirements of the [Filling Amount Difference] item in the General Rules of Part IV of the 2020 Edition of the Chinese Pharmacopoeia.

[0112] Table 5 Results of filling quantity difference detection

[0113]

[0114] In the description of this specification, the reference terms "one embodiment", "some embodiments", "example", "specific example", or "some examples" mean that the specific features, structures, materials or characteristics described in conjunction with the embodiment or example are included in at least one embodiment or example of the present invention. In this specification, the schematic representations of the above terms do not necessarily refer to the same embodiment or example. Moreover, the specific features, structures, materials or characteristics described can be combined in any one or more embodiments or examples in a suitable manner. In addition, those skilled in the art can combine and combine different embodiments or examples described in this specification and features of different embodiments or examples without contradiction.

[0115] Although the embodiments of the present invention have been shown and described above, it will be understood that the above embodiments are illustrative and are not to be construed as limitations on the present invention. A person skilled in the art may change, modify, replace and modify the above embodiments within the scope of the present invention.

Claims

1. A vigabatrin bulk drug, characterized in that: The particle size D90 of the vigabatrin raw material is 200-460 μm and is needle-shaped.

2. The vigabatrin bulk drug according to claim 1, wherein The purity of the vigabatrin raw material is not less than 98%.

3. The vigabatrin bulk drug according to claim 1, wherein The purity of the vigabatrin raw material is not less than 99%.

4. A method for preparing the vigabatrin bulk drug according to any one of claims 1 to 3, characterized in that: include: Step 1: Mix the crude vigabatrin with water, filter the resulting mixture, and collect the filtrate; Step 2: mixing the filtrate with an alcoholic substance, preserving the temperature, cooling the mixture, and crystallizing the mixture, collecting the crystals to obtain the vigabatrin raw material; Wherein, in the step 1, the mass ratio of the water to the crude vigabatrin is (1.8-2.5):1; In the step 2, the mass ratio of the alcohol substance to the crude vigabatrin is (8-12):1; The mixing is performed by adding the filtrate dropwise to the alcoholic substance; The dropping speed is 10-30 mL / min.

5. The method according to claim 4, characterized in that In the step 1, the purity of the crude vigabatrin is 80-88%.

6. The method according to claim 4, characterized in that In the step 2, the alcohol substance is selected from 1-6 valent alcohols.

7. The method according to claim 4, characterized in that The alcohol substance is ethanol or isopropanol.

8. The method according to claim 4, characterized in that The crystallization is carried out at 0-20°C.

9. A vigabatrin solid composition, characterized in that: include: The vigabatrin bulk drug and pharmaceutically acceptable excipients according to any one of claims 1 to 3.

10. The vigabatrin solid composition according to claim 9, wherein The dosage form of the vigabatrin solid composition is selected from tablets or powders.

11. The vigabatrin solid composition according to claim 9, wherein The auxiliary material includes povidone.

12. A method for preparing the vigabatrin solid composition according to any one of claims 9 to 11, characterized in that: include: The vigabatrin bulk drug and pharmaceutically acceptable excipients are mixed, granulated and dried to obtain the vigabatrin solid composition.

13. The method according to claim 12, characterized in that The vigabatrin bulk drug is obtained by the method for preparing the vigabatrin bulk drug according to any one of claims 4 to 8.

14. The method according to claim 12, characterized in that Further including: Mixing the vigabatrin raw material, alcohol and pharmaceutically acceptable excipients to obtain a mixture; granulating the mixture to obtain granules; The particles are sized, the obtained particles are dried, and the dried particles are sieved and the obtained particles are collected to obtain the vigabatrin solid composition.

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