Phenobarbital tablet and preparation method thereof

Abstract

The invention discloses a phenobarbital tablet and a preparation method thereof. The phenobarbital tablet is prepared from the following raw materials in parts by mass: 25 to 33 parts of phenobarbital, 65 to 75 parts of lactose, 18 to 20 parts of potato starch, 0.4 to 3.6 parts of croscarmellose sodium and 0.5 to 1.0 part of magnesium stearate. The preparation method comprises the following steps: mixing part of potato starch with water to prepare an adhesive; mixing phenobarbital, the remaining potato starch and lactose, then adding an adhesive, carrying out wet mixing granulation, and then carrying out drying and granule finishing; and finally adding magnesium stearate and croscarmellose sodium, mixing, and tabletting to obtain the phenobarbital tablet. The phenobarbital tablet is prepared by adopting a wet granulation process, the product quality is qualified, the property is stable, the release speed of the tablet is relatively high, the dissolution rate in a water medium in 15 minutes is more than 75%, the dissolution rate in 30 minutes is more than 90%, and the drug has a remarkable curative effect on sedation, hypnosis, convulsion resistance and epilepsy resistance.

Description

Technical Field

[0001] The present invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a phenobarbital tablet and a preparation method thereof. Background Art

[0002] Phenobarbital, chemical name: 5-ethyl-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione, molecular formula C 12 H 12 N2O3, molecular weight 232, and the chemical structural formula is:

[0003] Phenobarbital is a sedative-hypnotic and anticonvulsant drug, and is a typical representative of long-acting barbiturates. The inhibitory effect on the central nervous system increases with the increase of the dose, showing sedation, hypnosis, anticonvulsant and antiepileptic effects. Large doses have obvious inhibitory effects on the cardiovascular system and respiratory system, and overdose can paralyze the medullary respiratory center and cause death. In vitro electrophysiological experiments show that phenobarbital opens the chloride ion channels of nerve cells, hyperpolarizes the cells, and mimics the action of γ-aminobutyric acid (GABA). Phenobarbital at therapeutic concentrations can reduce the excitatory effect of glutamate, enhance the inhibitory effect of γ-aminobutyric acid, inhibit monosynaptic and polysynaptic transmission in the central nervous system, inhibit the high-frequency discharge of pain foci and their spread to the surrounding areas, reduce gastric juice secretion, and lower gastric tension. By inducing glucuronyl transferase to conjugate bilirubin, the concentration of bilirubin can be reduced, and dependence can be produced, including psychological dependence and physical dependence.

[0004] The dosage forms of phenobarbital generally include tablets, injections and suppositories. The dissolution rate of the existing phenobarbital tablets is slow, and the onset of action in the body is slow. Therefore, how to improve the dissolution rate of phenobarbital tablets is a problem to be solved.

[0005] The information disclosed in this background art section is only intended to enhance the overall understanding of the present invention, and should not be regarded as an admission or any form of suggestion that this information constitutes prior art already known to those of ordinary skill in the art. Summary of the Invention

[0006] The purpose of the present invention is to provide a phenobarbital tablet and a preparation method thereof, and the phenobarbital tablet has stable properties, fast release rate and fast onset of action.

[0007] In order to achieve the above purpose, the technical solution provided by a specific embodiment of the present invention is as follows:

[0008] A phenobarbital tablet, comprising the following raw materials in parts by mass: 25-33 parts of phenobarbital, 65-75 parts of lactose, 18-20 parts of potato starch, 0.4-3.6 parts of croscarmellose sodium, and 0.5-1.0 part of magnesium stearate.

[0009] In one or more embodiments of the present invention, the raw materials include the following parts by mass: 30 parts of phenobarbital, 70 parts of lactose, 19.68 parts of potato starch, 0.6 part of croscarmellose sodium, and 0.6 part of magnesium stearate.

[0010] In one or more embodiments of the present invention, the particle size of the phenobarbital is 75 mesh - 90 mesh.

[0011] The technical solution provided by a specific embodiment of the present invention is as follows:

[0012] A method for preparing a phenobarbital tablet, comprising the following steps:

[0013] Prepare the raw materials phenobarbital, lactose, potato starch, croscarmellose sodium, and magnesium stearate;

[0014] Take a part of the potato starch, mix it with water to make an adhesive;

[0015] Mix phenobarbital, the remaining potato starch, and lactose, then add the adhesive, wet-mix and granulate, and then dry and size the granules;

[0016] Finally, add magnesium stearate and croscarmellose sodium, mix, and press tablets to obtain phenobarbital tablets.

[0017] In one or more embodiments of the present invention, the mass of the potato starch used for the adhesive is 8% - 9% of the total mass of the raw material potato starch, and in the adhesive, the mass concentration of the potato starch is 5% - 9%.

[0018] In one or more embodiments of the present invention, the drying operation is: drying at 50°C - 70°C until the moisture content of the granules is 1.5% - 4.0%.

[0019] In one or more embodiments of the present invention, the sizing operation is sizing with a 14 - 18 mesh sieve.

[0020] In one or more embodiments of the present invention, when mixing phenobarbital, the remaining potato starch, and lactose, the rotation speed is 8 rpm - 12 rpm, and the time is 2 min - 5 min;

[0021] When adding the adhesive and wet-mixing and granulating, the rotation speed is 8 rpm - 12 rpm, and the time is 3 min - 6 min;

[0022] When adding magnesium stearate and croscarmellose sodium and mixing, the rotation speed is 8 rpm - 12 rpm, and the time is 10 min - 20 min.

[0023] Compared with the prior art, the present invention prepares phenobarbital tablets by a wet granulation process. The tablets are scored tablets and are composed of the raw material phenobarbital, lactose, potato starch, croscarmellose sodium and magnesium stearate. Among them, lactose and potato starch are fillers, potato starch paste is a binder, magnesium stearate is a lubricant, and croscarmellose sodium is a disintegrant. The granules prepared by this process have good fluidity and compressibility, qualified quality, stable properties, and the tablets have a relatively fast release rate. The dissolution rate in an aqueous medium is greater than 75% in 15 minutes, and the dissolution rate reaches more than 90% in 30 minutes. This drug has a significant curative effect on the treatment of sedation, hypnosis, anti-convulsion and anti-epilepsy. Detailed implementation mode

[0024] In order to enable those skilled in the art to better understand the technical solutions in the present invention, the technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without making creative efforts shall fall within the protection scope of the present invention.

[0025] A specific implementation mode of the present invention provides a phenobarbital tablet, which comprises the following raw materials in parts by mass: 25-33 parts of phenobarbital, 65-75 parts of lactose, 20 parts of potato starch, 0.4-3.6 parts of croscarmellose sodium, and 0.5-1.0 parts of magnesium stearate.

[0026] Specifically, lactose and potato starch as fillers can increase the volume of the tablets, improve the compressibility, contribute to tablet forming and maintaining the shape after tableting. At the same time, potato starch also has a certain disintegrating effect and can promote the disintegration of the tablets. Croscarmellose sodium as a disintegrant can make the tablets quickly disintegrate and release phenobarbital. Magnesium stearate as a lubricant can improve the fluidity of the granules, increase the uniformity of the raw material mixture, improve the uniformity of the tablets, and improve the production efficiency and quality. By selecting the above raw materials, phenobarbital tablets with excellent quality, stable properties and fast release rate can be obtained.

[0027] Furthermore, the preferred amounts of the raw materials are 30 parts of phenobarbital, 70 parts of lactose, 19.68 parts of potato starch, 0.6 parts of croscarmellose sodium, and 0.6 parts of magnesium stearate. The above amounts can make the dissolution rate of the phenobarbital tablets reach the best.

[0028] Another specific implementation mode of the present invention provides a preparation method of a phenobarbital tablet, which comprises steps 1-4.

[0029] Step 1, prepare the raw materials phenobarbital, lactose, potato starch, croscarmellose sodium and magnesium stearate.

[0030] Specifically, referring to the raw material ratio, take the raw materials in corresponding parts by mass for standby.

[0031] Step 2: Take a part of potato starch, mix it with water to make an adhesive.

[0032] Specifically, take a part of potato starch, the dosage of which is 8%-9% of the total mass of the raw material potato starch. First, moisten it with an appropriate amount of purified water, stir evenly, and then pour in boiling water and stir to make an adhesive with a mass concentration of 5%-9%.

[0033] Step 3: Mix phenobarbital, the remaining potato starch and lactose, then add the adhesive, wet-mix and granulate, and then dry and size the granules.

[0034] Specifically, first place phenobarbital, the remaining potato starch and lactose in a wet granulator for premixing for 2 min - 5 min at a rotation speed of 8 rpm - 12 rpm; then add the adhesive, wet-mix and granulate for 3 min - 6 min at a rotation speed of 8 rpm - 12 rpm; dry the wet granules at 50°C - 70°C until the moisture content of the granules is 1.5% - 4.0%; the sizing operation is carried out using a 14-mesh - 18-mesh sieve for sizing.

[0035] Through premixing, phenobarbital, potato starch and lactose can be evenly mixed, and then the adhesive is added so that each raw material can be evenly distributed. By controlling the moisture content of the granules, it helps to improve the fluidity of the granules, improve the tablet pressing quality, and reduce the possibility of the tablets absorbing moisture and deforming.

[0036] Step 4: Finally, add magnesium stearate and croscarmellose sodium, mix them, and press tablets to obtain phenobarbital tablets.

[0037] Specifically, add magnesium stearate and croscarmellose sodium, mix them at a rotation speed of 8 rpm - 12 rpm for 10 min - 20 min to improve the uniformity of the raw material mixing. Finally, add croscarmellose sodium to wrap the granules obtained in Step 3, which helps to improve the disintegration speed of the tablets and enables phenobarbital to dissolve quickly.

[0038] The following further elaborates on the present invention in combination with specific embodiments.

[0039] In the present invention, the sources are as follows: lactose is purchased from Jiangsu Daoning, potato starch is purchased from Roquette, croscarmellose sodium is purchased from DFE Pharma, magnesium stearate is purchased from Anhui Shanhe, the reference preparation is purchased from Fujinaga pharm Co., Ltd., and the specification is 30 mg.

[0040] Example 1

[0041] The phenobarbital tablets in this example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 36 g of cross-linked carboxymethylcellulose sodium.

[0042] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, and then pour in boiling water while stirring continuously to prepare a 7% binder for standby; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch, and lactose in a wet granulator for pre-mixing for 3 minutes, then add the 7% binder to the wet granulator, wet-mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 1.5%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethylcellulose sodium, mix for 15 minutes, and press tablets.

[0043] The cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes in the aqueous medium were measured to be 51.81%, 71.21%, 80.12%, and 84.23% respectively, and the f2 value compared with the reference preparation was 63, which was similar. In the pH 1.2 hydrochloric acid medium, the cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes were 59.36%, 78.71%, 87.30%, and 94.22% respectively, and the f2 value compared with the reference preparation was 66, which was similar.

[0044] Example 2

[0045] The phenobarbital tablets in this example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 12 g of cross-linked carboxymethylcellulose sodium.

[0046] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, and then pour in boiling water while stirring continuously to prepare a 7% binder for standby; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch, and lactose in a wet granulator for pre-mixing for 3 minutes, then add the 7% binder to the wet granulator, wet-mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 2.0%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethylcellulose sodium, mix for 15 minutes, and press tablets.

[0047] The cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes in the aqueous medium were measured to be 47.382%, 78.59%, 90.17%, and 100.33% respectively, and the f2 value compared with the reference preparation was 57, which was similar.

[0048] Example 3

[0049] The phenobarbital tablets in this example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg / pill of phenobarbital): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 6 g of cross-linked carboxymethylcellulose sodium.

[0050] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to make a binder with a concentration of 7%, and set aside; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch, and lactose in a wet granulator for premixing for 3 min, then add the 7% binder to the wet granulator, wet mix and granulate for 4 min, dry the wet granules at 60 °C by fluidized bed drying until the moisture content reaches 4.0%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethylcellulose sodium, mix for 15 min, and press tablets.

[0051] The cumulative dissolution rates at 5 min, 10 min, 15 min, and 30 min in the aqueous medium were measured to be 43.38%, 70.45%, 84.96%, and 98.06% respectively, and the f2 value compared with the reference preparation was 73, which was similar.

[0052] Example 4

[0053] The phenobarbital tablets in this example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg / pill of phenobarbital): 300 g of 75-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 36 g of cross-linked carboxymethylcellulose sodium.

[0054] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to make a binder with a concentration of 7%, and set aside; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch, and lactose in a wet granulator for premixing for 3 min, then add the 7% binder to the wet granulator, wet mix and granulate for 4 min, dry the wet granules at 60 °C by fluidized bed drying until the moisture content reaches 1.5%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethylcellulose sodium, mix for 15 min, and press tablets.

[0055] The dissolution curve in the aqueous medium was measured to be similar to that of the reference preparation, slightly worse than that of Example 1.

[0056] Comparative Example 1

[0057] The phenobarbital tablets in this comparative example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 36 g of sodium carboxymethyl starch.

[0058] Manufacturing method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to make a binder with a concentration of 7%, and set aside; then accurately weigh each raw and auxiliary material according to the mass fraction, place phenobarbital, potato starch, and lactose in a wet granulator for premixing for 3 minutes, then add the 7% binder to the wet granulator, wet mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 1.5%, and screen the granules through a 16-mesh sieve; then add magnesium stearate and sodium carboxymethyl starch, mix for 15 minutes, and compress into tablets.

[0059] The cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes in the aqueous medium were measured to be 48.53%, 70.40%, 79.52%, and 90.49% respectively, and the f2 value compared with the reference preparation was 82, which was similar. In the pH 1.2 hydrochloric acid medium, the cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes were 42.84%, 60.62%, 70.95%, and 83.39% respectively, and the f2 value compared with the reference preparation was 46, which was not similar.

[0060] Comparative Example 2

[0061] The phenobarbital tablets in this comparative example are scored tablets and are made from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 36 g of crospovidone.

[0062] Manufacturing method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to make a binder with a concentration of 7%, and set aside; then accurately weigh each raw and auxiliary material according to the mass fraction, place phenobarbital, potato starch, and lactose in a wet granulator for premixing for 3 minutes, then add the 7% binder to the wet granulator, wet mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 1.5%, and screen the granules through a 16-mesh sieve; then add magnesium stearate and crospovidone, mix for 15 minutes, and compress into tablets.

[0063] The cumulative dissolution rates at 5 min, 10 min, 15 min, and 30 min in an aqueous medium were 63.40%, 80.63%, 85.69%, and 90.49% respectively. The f2 value compared with the reference preparation was 46, indicating dissimilarity. In 0.1 M hydrochloric acid medium at pH 1.2, the cumulative dissolution rates at 5 min, 10 min, 15 min, and 30 min were 73.79%, 88.11%, 92.76%, and 97.75% respectively. The f2 value compared with the reference preparation was 41, indicating dissimilarity.

[0064] Comparative Example 3

[0065] The phenobarbital tablets in this comparative example were scored tablets and were prepared from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 0 g of cross-linked carboxymethylcellulose sodium.

[0066] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, and then pour in boiling water while stirring continuously to prepare a 7% binder for standby. Then accurately weigh each raw and auxiliary material according to the mass fraction. Place phenobarbital, potato starch, and lactose in a wet granulator for premixing for 3 min, then add the 7% binder to the wet granulator and wet-mix and granulate for 4 min. The wet granules are dried at 60 °C until the moisture content reaches 1.5% by fluidized bed drying, sieved through a 16-mesh sieve, and then magnesium stearate is added and mixed for 15 min, followed by tabletting.

[0067] The cumulative dissolution rates at 5 min, 10 min, 15 min, and 30 min in an aqueous medium were measured to be 19.22%, 35.63%, 46.97%, and 66.02% respectively. The f2 value compared with the reference preparation was 25, indicating dissimilarity.

[0068] Comparative Example 4

[0069] The phenobarbital tablets in this example were scored tablets and were prepared from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 80-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 15 g of magnesium stearate, and 1 g of cross-linked carboxymethylcellulose sodium.

[0070] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to prepare a binder with a concentration of 7%, and set it aside; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch and lactose in a wet granulator for premixing for 3 minutes, then add the 7% binder to the wet granulator, wet mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 1.5%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethyl cellulose sodium, mix for 15 minutes, and press tablets.

[0071] The cumulative dissolution rates at 5 minutes, 10 minutes, 15 minutes, and 30 minutes in the aqueous medium were measured to be 21.42%, 49.07%, 61.03%, and 74.37% respectively, and the f2 value compared with the reference preparation was 33, which was not similar.

[0072] Comparative Example 5

[0073] The phenobarbital tablets in this comparative example were scored tablets, and were prepared from the following raw and auxiliary materials by mass (10,000 tablets, 30 mg of phenobarbital per tablet): 300 g of 65-mesh phenobarbital, 700 g of lactose, 180 g of potato starch, 240 g of 7% potato starch paste, 6 g of magnesium stearate, and 36 g of cross-linked carboxymethyl cellulose sodium.

[0074] Preparation method: Weigh an appropriate amount of potato starch, moisten it with purified water, stir evenly, then pour in boiling water and keep stirring to prepare a binder with a concentration of 7%, and set it aside; then accurately weigh each raw and auxiliary material according to the mass parts, place phenobarbital, potato starch and lactose in a wet granulator for premixing for 3 minutes, then add the 7% binder to the wet granulator, wet mix and granulate for 4 minutes, dry the wet granules at 60 °C by fluidized bed drying to 1.5%, screen the granules through a 16-mesh sieve, then add magnesium stearate and cross-linked carboxymethyl cellulose sodium, mix for 15 minutes, and press tablets.

[0075] The dissolution curve in the aqueous medium was measured to be not similar to that of the reference preparation.

[0076] Table 1 Dissolution determination results of Example 1, Comparative Example 1, and Comparative Example 2 in the aqueous medium

[0077] Sample 5 min 10 min 15 min 30 min Comparative Example 1 48.53％ 70.40％ 79.52％ 90.49％ Comparative Example 2 63.40％ 80.63％ 85.69％ 90.49％ Example 1 51.81％ 71.21％ 80.12％ 84.23％ Reference Preparation 46.65％ 69.35％ 81.77％ 93.28％

[0078] Table 2 Dissolution determination results of Example 1, Comparative Example 1, and Comparative Example 2 in pH 1.2 hydrochloric acid medium

[0079]

[0080]

[0081] As can be seen from Table 1 and Table 2, the dissolution curve of the tablets prepared with sodium carboxymethyl starch as the external disintegrant is slower than that of the reference preparation in the pH 1.2 hydrochloric acid solution and is not similar. The dissolution behavior of the tablets prepared with sodium carboxymethyl starch as the disintegrant is slower in the pH 1.2 hydrochloric acid solution than in water, while the dissolution curves of the reference preparation in the pH 1.2 hydrochloric acid solution and in water are basically the same; when crospovidone is used as the disintegrant, the dissolution behavior is significantly faster than that of the reference preparation; when sodium croscarmellose is used as the disintegrant, the dissolution curve is similar to that of the reference preparation. Therefore, sodium croscarmellose is selected as the disintegrant, and the dosage of the disintegrant is optimized and studied.

[0082] Table 3 Dissolution determination results of Example 2, Example 3, Comparative Example 3, and Comparative Example 4 in aqueous medium

[0083] Sample 5 min 10 min 15 min 30 min Comparative Example 3 19.22％ 35.63％ 46.97％ 66.02％ Example 2 47.382％ 78.59％ 90.17％ 100.33％ Example 3 43.38％ 70.45％ 84.96％ 98.06％ Comparative Example 4 21.42％ 49.07％ 61.03％ 74.37％ Reference Preparation 46.65％ 69.35％ 81.77％ 93.28％

[0084] As can be seen from Table 3, the dissolution behavior of the sample without the disintegrant is slower than that of the reference preparation and is not similar; in Example 2, the dosage of sodium croscarmellose accounts for about 1% of the total mass of the raw materials, and the dissolution curve of the sample is similar to that of the reference preparation, but it is slightly faster in the later stage; in Example 3, the dosage of sodium croscarmellose accounts for about 0.5% of the total mass of the raw materials, and the dissolution curve of the sample is similar to that of the reference preparation. Finally, it is determined that the optimal dosage of externally added 0.5% sodium croscarmellose is the optimal dosage.

[0085] The present invention uses lactose and potato starch as fillers, potato starch paste as a binder, magnesium stearate as a lubricant, and sodium croscarmellose as a disintegrant. The granules prepared by the wet granulation process have good fluidity and compressibility, qualified quality, stable properties, the release rate of the tablet is relatively fast, the Tmax (peak time of the drug) is 1.4 ± 0.5 hours, the dissolution rate in the aqueous medium is greater than 75% in 15 minutes, and the dissolution rate reaches more than 90% in 30 minutes. The drug has a significant effect on the treatment of sedation, hypnosis, anti-convulsion and anti-epilepsy.

[0086] For those skilled in the art, it is obvious that the present invention is not limited to the details of the above exemplary embodiments, and the present invention can be implemented in other specific forms without departing from the spirit or basic characteristics of the present invention. Therefore, from any point of view, the embodiments should be regarded as exemplary and non-limiting. The scope of the present invention is defined by the appended claims rather than the above description. Therefore, it is intended to include all changes falling within the meaning and scope of the equivalent elements of the claims in the present invention.

[0087] In addition, it should be understood that although this specification is described in terms of embodiments, not every embodiment contains only one independent technical solution. This narrative style of the specification is only for clarity. Those skilled in the art should regard the specification as a whole, and the technical solutions in each embodiment can also be appropriately combined to form other embodiments that can be understood by those skilled in the art.

Claims

1. A phenobarbital tablet, characterized in that, It comprises the following raw materials in parts by mass: 25 - 33 parts of phenobarbital, 65 - 75 parts of lactose, 18 - 20 parts of potato starch, 0.4 - 3.6 parts of cross-linked carboxymethyl cellulose sodium, and 0.5 - 1.0 part of magnesium stearate.

2. The phenobarbital tablet according to claim 1, characterized in that, It comprises the following raw materials in parts by mass: 30 parts of phenobarbital, 70 parts of lactose, 19.68 parts of potato starch, 0.6 part of cross-linked carboxymethyl cellulose sodium, and 0.6 part of magnesium stearate.

3. The phenobarbital tablet according to claim 1, characterized in that, The particle size of the phenobarbital is 75 mesh - 90 mesh.

4. The preparation method of the phenobarbital tablet according to any one of claims 1-3, characterized in that, It comprises the following steps: Prepare the raw materials of phenobarbital, lactose, potato starch, cross-linked carboxymethyl cellulose sodium and magnesium stearate; Take a part of the potato starch, mix it with water to make an adhesive; Mix the phenobarbital, the remaining potato starch and lactose, then add the adhesive, wet-mix and granulate, and then dry and screen the granules; Finally, add magnesium stearate and cross-linked carboxymethyl cellulose sodium, mix, and press tablets to obtain phenobarbital tablets.

5. The preparation method of the phenobarbital tablets according to claim 4, characterized in that, The mass of the potato starch used for the adhesive is 8% - 9% of the total mass of the raw material potato starch, and in the adhesive, the mass concentration of the potato starch is 5% - 9%.

6. The preparation method of the phenobarbital tablet according to claim 4, characterized in that, The drying operation is: drying at 50°C - 70°C until the moisture content of the granules is 1.5% - 4.0%.

7. The preparation method of the phenobarbital tablet according to claim 4, characterized in that, The screening operation is to screen the granules with a 14-mesh - 18-mesh sieve.

8. The preparation method of the phenobarbital tablet according to claim 4, characterized in that, When mixing the phenobarbital, the remaining potato starch and lactose, the rotation speed is 8 rpm - 12 rpm, and the time is 2 min - 5 min; When adding the adhesive for wet mixing and granulating, the rotation speed is 8 rpm - 12 rpm, and the time is 3 min - 6 min; When adding magnesium stearate and cross-linked carboxymethyl cellulose sodium for mixing, the rotation speed is 8 rpm - 12 rpm, and the time is 10 min - 20 min.

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