Quickly-dissolved finasteride tablet and production method thereof

Abstract

The invention discloses a rapidly-dissolved finasteride tablet and a production method thereof, and relates to the technical field of medicine preparation. According to the invention, finasteride is loaded in carboxylated mesoporous silica, so that drug molecules of finasteride are dispersed from a crystalline state to an amorphous state, the dissolution rate is improved, carboxyl maintains a non-ionized state in a gastric juice environment, stimulation of drugs in a gastric acid environment is reduced, carboxyl is ionized in an intestinal solution, and the dissolution rate of the drugs is increased. The quick release of the medicine can be realized; according to the invention, a modified polymer emulsion is also prepared as a material of a coating solution, by utilizing the characteristics of the coating solution, the tablet is insoluble in a gastric acid environment and dissolved in an intestinal juice environment, the irritation to patients with stomach diseases is reduced, and the intestinal absorption area is relatively large, so that the absorption rate of the medicine is improved, and the bioavailability is improved.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical preparation technology, specifically to a rapidly dissolving finasteride tablet and its production method. Background Technology

[0002] Finasteride, chemical formula C 23 H 36 N2O2 is a 4-azasteroid compound that is a specific inhibitor of the intracellular enzyme type II 5α-reductase in the process of testosterone metabolism into dihydrotestosterone. By inhibiting the conversion of testosterone to dihydrotestosterone, it reduces the size of the prostate, decreases dihydrotestosterone in the blood and prostate, increases urine flow rate, and prevents benign prostatic hyperplasia.

[0003] Finasteride belongs to the BCS class II compounds and is characterized by low solubility and high permeability. When made into tablets, its dissolution and bioavailability are low, which affects human absorption. In addition, finasteride may irritate patients with stomach problems, leading to side effects such as stomach pain and bloating.

[0004] Therefore, the present invention provides a rapidly dissolving finasteride tablet and a method for producing the same, aiming to improve the dissolution and bioavailability of finasteride tablets by optimizing the production method, while reducing gastric irritation. Summary of the Invention

[0005] The purpose of this invention is to provide a rapidly dissolving finasteride tablet and its production method, in order to solve the problems raised in the prior art.

[0006] To achieve the above objectives, the present invention provides the following technical solution: a method for producing rapidly dissolving finasteride tablets, comprising the following steps: Step 1: Mix mesoporous silica-loaded finasteride, microcrystalline cellulose, magnesium stearate, povidone K30, and maltose-cyclodextrin evenly, compress into tablets, and obtain tablet cores; Step 2: Mix the modified polymer emulsion, titanium dioxide, talc powder and water, stir evenly to obtain a coating solution, place the tablet core in a coating pan, heat to 40~45℃, spray the coating solution, remove and dry after coating to obtain finasteride tablets.

[0007] Furthermore, in step 1, the core comprises the following components by weight: 1-2 parts mesoporous silica loaded with finasteride, 50-70 parts microcrystalline cellulose, 1-2 parts magnesium stearate, 6-10 parts povidone K30, and 5-15 parts maltose-cyclodextrin.

[0008] Furthermore, in step 2, the mass ratio of modified polymer emulsion, titanium dioxide, talc powder and water is (8~10):(0.3~0.5):(0.1~0.3):(100~120).

[0009] Furthermore, in step 2, the mass ratio of the tablet core to the coating solution is 10:(2~4).

[0010] Furthermore, in step 2, the drying process conditions are: temperature 40~45℃, time 8~10h.

[0011] Furthermore, the mesoporous silica-supported finasteride is prepared by the following process: Finasteride was mixed with anhydrous ethanol, stirred and dissolved, then carboxylated mesoporous silica was added, the mixture was shaken in a water bath and dried to obtain mesoporous silica-supported finasteride.

[0012] Furthermore, the ratio of finasteride, anhydrous ethanol, and carboxylated mesoporous silica is (0.10~0.12) g : (40~50) mL : (0.10~0.15) g.

[0013] Furthermore, the process conditions for the water bath oscillation are: temperature 35~37℃, oscillation time 10~24h; The drying process conditions are: temperature 55~65℃, time 3~5h.

[0014] In the above technical solution, finasteride belongs to BCS class II compounds, with a stable crystal structure, compact molecular arrangement, and low solubility. When loaded into carboxylated mesoporous silica, the drug molecules cannot be arranged into crystals and are dispersed in an amorphous form, with a solubility much higher than that of the crystalline form. The molecular structure of finasteride contains amide and tertiary amine groups, which can bind with carboxyl groups through hydrogen bonding, stabilizing the amorphous form in the mesoporous silica channels. In addition, the carboxyl groups maintain a non-ionized state in the gastric juice environment, reducing the drug's irritation in the gastric acid environment. In the intestinal solution, the carboxyl groups are ionized, weakening their ability to act as hydrogen bond donors and reducing their binding force with the drug, thus achieving rapid drug release. Microcrystalline cellulose, as a disintegrant, swells upon contact with water, promoting rapid disintegration and dispersion of tablets. It provides adhesion during tableting, enhances the compressibility of the powder, and reduces the risk of tablet cracking. Magnesium stearate, as a lubricant, reduces friction between particles and the tableting machine during tableting, preventing material from adhering to the surface of the tableting machine and improving production efficiency. Povidone K30, as a binder, forms uniform particles with the powder, improving particle flowability and compressibility. It also acts as a cosolvent, forming hydrogen bonds with the drug to improve drug dissolution. The cavity structure of maltose-cyclodextrin prolongs drug stability, and maltose modification further improves overall water solubility, comprehensively enhancing the dissolution effect.

[0015] Furthermore, the preparation process of the modified polymer emulsion is as follows: Step A: Mix anhydrous hydroxypropyl cellulose with glacial acetic acid, heat to dissolve, then add itaconic anhydride, succinic anhydride and anhydrous sodium acetate, heat to react, add deionized water and concentrated hydrochloric acid to terminate the reaction, precipitate out, wash to pH 5.0~5.5, dialyze, dry to obtain double bond esterified product; Step B: Sodium dodecyl sulfate and water are mixed and stirred to dissolve. Then, double bond esterification products, methacrylic acid, methyl methacrylate, and butyl acrylate are added and mixed for pre-emulsification. Then, ammonium persulfate aqueous solution is added and the mixture is subjected to ultrasonic reaction to obtain a modified polymer emulsion.

[0016] Furthermore, in step A, the ratio of anhydrous hydroxypropyl cellulose, glacial acetic acid, itaconic anhydride, succinic anhydride and anhydrous sodium acetate is 10g: (50~100)mL: (4.5~5.5)g: (2.5~3.5)g: (4.5~5.5)g.

[0017] Furthermore, in step A, the process conditions for heating and dissolving are: temperature 65~70℃, time 0.6~1.0h.

[0018] Furthermore, in step A, the process conditions for the heating reaction are: temperature 80~85℃, time 2.8~3.2h; In step A, the drying process conditions are: temperature 80~85℃, time 4~5h.

[0019] Furthermore, in step B, the ratio of sodium dodecyl sulfate, water, double bond esterification product, methacrylic acid, methyl methacrylate, butyl acrylate and ammonium persulfate aqueous solution is (0.24~0.30) g : (30~40) mL : (1.5~2.5) g : (3.0~3.2) mL : (1.5~2.0) mL : (7.5~8.0) mL : (0.22~0.24) mL.

[0020] Furthermore, the mass fraction of the ammonium persulfate aqueous solution is 1.18~1.22%.

[0021] Furthermore, in step B, the pre-emulsification process conditions are: temperature 70~75℃, time 5~7min; In step B, the process conditions for the ultrasonic reaction are: power 280~400W, temperature 70~75℃, and time 40~45min.

[0022] In the above technical solution, itaconic anhydride and succinic anhydride are first used to esterify hydroxypropyl cellulose to generate ester bonds and carboxyl groups, while introducing double bonds to obtain double bond esterification products. These products are then mixed with acrylic monomers for pre-emulsification. Finally, the double bonds of the double bond esterification products are used to participate in the polymerization reaction to obtain modified polymer emulsions. Acrylic polymers are chemically stable and do not react with drugs. Due to the presence of acidic monomers, they are insoluble in gastric acid but soluble in intestinal fluid. In this invention, water is used as the dispersion medium for pre-emulsification to obtain an aqueous polymeric emulsion, avoiding the use of organic solvents. The addition of butyl acrylate gives the emulsion internal plasticizing properties, eliminating the need for additional plasticizers. At the same time, the terminal carboxyl groups are retained, keeping it stable in gastric fluid and enabling rapid dissolution in intestinal fluid.

[0023] Compared with the prior art, the beneficial effects of the present invention are: 1. In this application, finasteride is loaded into carboxylated mesoporous silica, which transforms its molecular state from crystalline arrangement to amorphous dispersion, greatly improving dissolution. The molecular structure of finasteride contains amide and tertiary amine groups, which can bind with carboxyl groups through hydrogen bonding, stabilizing the amorphous state in the mesoporous silica channels. In addition, the carboxyl groups maintain a non-ionized state in the gastric juice environment, reducing the stimulation of the drug in the gastric acid environment. In the intestinal solution, the carboxyl groups are ionized, which can achieve rapid drug release.

[0024] 2. In this application, an aqueous polymeric emulsion is prepared and used as the main component of the coating liquid, avoiding the use of organic solvents. The acrylic polymer is chemically stable, does not react with the drug, and does not affect the drug's stability. Butyl acrylate also acts as a plasticizer, enhancing the toughness of the coating and reducing the risk of cracking. No additional plasticizer is needed, and it also retains carboxyl groups, which keeps it stable in gastric juice and allows for rapid dissolution in intestinal juice.

[0025] 3. Although finasteride is chemically stable in gastric acid, people with sensitive stomachs such as gastritis and gastric ulcers may still experience discomfort such as stomach pain and bloating after taking it. This invention adds a coating to the outer layer of the finasteride tablet core, making it insoluble in gastric acid but soluble in intestinal fluid, reducing irritation to the stomach. It can also reduce the impact of gastric emptying rate and food digestion on drug absorption, and the larger intestinal absorption area helps maintain a stable therapeutic effect, thereby improving bioavailability. Attached Figure Description

[0026] Figure 1 This is a schematic diagram of a rapidly dissolving finasteride tablet according to the present invention; Figure 2 This is a schematic diagram of the tablet core of a rapidly dissolving finasteride tablet according to the present invention. Detailed Implementation

[0027] The technical solutions of the embodiments of the present invention will be clearly and completely described below with reference to the accompanying drawings. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0028] In the following specific implementation, Microcrystalline cellulose, product number CXH016, is sourced from Hebei Changxinghang Biotechnology Co., Ltd. Maltose-cyclodextrin, product number lnb-1261, is sourced from Wuhan Lanabai Pharmaceutical Chemical Co., Ltd. Titanium dioxide, model CP2020, is sourced from Xi'an Tianzheng Pharmaceutical Excipients Co., Ltd. Talc powder, 1250 mesh, sourced from Shaanxi Yangyuanshen Biotechnology Co., Ltd. Carboxylated mesoporous silica, 100nm particle size, MSNs-C, sourced from Nanjing Dongna Biotechnology Co., Ltd. Concentrated hydrochloric acid, with a mass fraction of 38%.

[0029] Example 1: A method for producing rapidly dissolving finasteride tablets, comprising the following steps: (1) Preparation of finasteride supported on mesoporous silica: Finasteride was mixed with anhydrous ethanol and stirred to dissolve. Then, carboxylated mesoporous silica was added, and the mixture was shaken in a water bath and dried to obtain mesoporous silica-supported finasteride. The ratio of finasteride, anhydrous ethanol, and carboxylated mesoporous silica was 0.12 g: 50 mL: 0.15 g. The water bath shaking conditions were: temperature 37 °C, shaking time 24 h; the drying conditions were: temperature 65 °C, time 5 h. (2) Preparation of modified polymer emulsion: Step A: Anhydrous hydroxypropyl cellulose is mixed with glacial acetic acid and heated to dissolve. Itaconic anhydride, succinic anhydride, and anhydrous sodium acetate are then added. The mixture is heated to react, and deionized water and concentrated hydrochloric acid are added to terminate the reaction. A precipitate is formed, washed until the pH reaches 5.0-5.5, dialyzed, and dried to obtain the double bond esterification product. Step B: Sodium dodecyl sulfate and water are mixed and stirred to dissolve. The double bond esterification product, methacrylic acid, methyl methacrylate, and butyl acrylate are then added and mixed for pre-emulsification. Ammonium persulfate aqueous solution is then added, and the mixture is sonicated to obtain a modified polymer emulsion. In Step A, the ratio of anhydrous hydroxypropyl cellulose, glacial acetic acid, itaconic anhydride, succinic anhydride, and anhydrous sodium acetate is 10g:100mL:5.5g:3.5g:5.5g. In Step A, heating... The dissolution process conditions are: temperature 70℃, time 1.0 h; in step A, the heating reaction process conditions are: temperature 85℃, time 3.2 h; in step A, the drying process conditions are: temperature 85℃, time 5 h; in step B, the ratio of sodium dodecyl sulfate, water, double bond esterification product, methacrylic acid, methyl methacrylate, butyl acrylate and ammonium persulfate aqueous solution is 0.30 g: 40 mL: 2.5 g: 3.2 mL: 2.0 mL: 8.0 mL: 0.24 mL; the mass fraction of ammonium persulfate aqueous solution is 1.22%; in step B, the pre-emulsification process conditions are: temperature 75℃, time 7 min; in step B, the ultrasonic reaction process conditions are: power 400 W, temperature 75℃, time 45 min; (3) Preparation of finasteride tablets: Step 1: Mix mesoporous silica-supported finasteride, microcrystalline cellulose, magnesium stearate, povidone K30, and maltose-cyclodextrin evenly, compress into tablets, and obtain tablet cores; Step 2: Mix modified polymer emulsion, titanium dioxide, talc, and water, stir evenly, and obtain a coating solution. Place the tablet cores in a coating pan, heat to 45°C, spray with the coating solution, remove and dry after coating to obtain finasteride tablets; In Step 1, the tablet cores include the following Mass composition: 2 parts mesoporous silica-supported finasteride, 70 parts microcrystalline cellulose, 2 parts magnesium stearate, 10 parts povidone K30, 15 parts maltose-cyclodextrin; In step 2, the mass ratio of modified polymer emulsion, titanium dioxide, talc and water is 10:0.5:0.3:120; In step 2, the mass ratio of core to coating solution is 10:4; In step 2, the drying process conditions are: temperature 45℃, time 10h.

[0030] Example 2: A method for producing rapidly dissolving finasteride tablets, comprising the following steps: (1) Preparation of finasteride supported on mesoporous silica: Finasteride was mixed with anhydrous ethanol and stirred to dissolve. Then, carboxylated mesoporous silica was added, and the mixture was shaken in a water bath and dried to obtain mesoporous silica-supported finasteride. The ratio of finasteride, anhydrous ethanol, and carboxylated mesoporous silica was 0.11 g: 45 mL: 0.13 g. The water bath shaking conditions were: temperature 36℃, shaking time 16 h; and the drying conditions were: temperature 60℃, time 4 h. (2) Preparation of modified polymer emulsion: Step A: Anhydrous hydroxypropyl cellulose is mixed with glacial acetic acid and heated to dissolve. Itaconic anhydride, succinic anhydride, and anhydrous sodium acetate are then added. The mixture is heated to react, and the reaction is terminated by adding deionized water and concentrated hydrochloric acid. A precipitate is formed, washed until the pH reaches 5.0-5.5, dialyzed, and dried to obtain the double bond esterification product. Step B: Sodium dodecyl sulfate and water are mixed and stirred to dissolve. The double bond esterification product, methacrylic acid, methyl methacrylate, and butyl acrylate are then added and mixed for pre-emulsification. An aqueous solution of ammonium persulfate is then added, and the mixture is sonicated to obtain a modified polymer emulsion. In Step A, the ratio of anhydrous hydroxypropyl cellulose, glacial acetic acid, itaconic anhydride, succinic anhydride, and anhydrous sodium acetate is 10g:80mL:5.0g:3.0g:5.0g. In Step A, the mixture is heated to dissolve... The process conditions are as follows: temperature 68℃, time 0.8h; in step A, the heating reaction conditions are: temperature 83℃, time 3.0h; in step A, the drying process conditions are: temperature 83℃, time 4.5h; in step B, the ratio of sodium dodecyl sulfate, water, double bond esterification product, methacrylic acid, methyl methacrylate, butyl acrylate and ammonium persulfate aqueous solution is 0.28g:35mL:2.0g:3.1mL:1.8mL:7.8mL:0.23mL; the mass fraction of ammonium persulfate aqueous solution is 1.20%; in step B, the pre-emulsification process conditions are: temperature 73℃, time 6min; in step B, the ultrasonic reaction process conditions are: power 320W, temperature 73℃, time 43min. (3) Preparation of finasteride tablets: Step 1: Mix finasteride supported on mesoporous silica, microcrystalline cellulose, magnesium stearate, povidone K30, and maltose-cyclodextrin evenly, compress into tablets to obtain tablet cores; Step 2: Mix modified polymer emulsion, titanium dioxide, talc, and water, stir evenly to obtain a coating solution, place the tablet cores in a coating pan, heat to 43°C, spray with the coating solution, remove and dry after coating to obtain finasteride tablets; In Step 1, the tablet cores include the following mass components: 2 parts mesoporous silica supported on finasteride, 60 parts microcrystalline cellulose, 2 parts magnesium stearate, 8 parts povidone K30, and 10 parts maltose-cyclodextrin; In Step 2, the mass ratio of modified polymer emulsion, titanium dioxide, talc, and water is 9:0.4:0.2:110; In Step 2, the mass ratio of tablet cores to coating solution is 10:3; In Step 2, the drying process conditions are: temperature 43°C, time 9 hours.

[0031] Example 3: A method for producing rapidly dissolving finasteride tablets, comprising the following steps: (1) Preparation of finasteride supported on mesoporous silica: Finasteride was mixed with anhydrous ethanol and stirred to dissolve. Then, carboxylated mesoporous silica was added, and the mixture was shaken in a water bath and dried to obtain mesoporous silica-supported finasteride. The ratio of finasteride, anhydrous ethanol, and carboxylated mesoporous silica was 0.10 g: 40 mL: 0.10 g. The water bath shaking conditions were: temperature 35℃, shaking time 10 h; the drying conditions were: temperature 55℃, time 3 h. (2) Preparation of modified polymer emulsion: Step A: Anhydrous hydroxypropyl cellulose is mixed with glacial acetic acid and heated to dissolve. Itaconic anhydride, succinic anhydride, and anhydrous sodium acetate are then added. The mixture is heated to react, and deionized water and concentrated hydrochloric acid are added to terminate the reaction. A precipitate is formed, washed until the pH reaches 5.0-5.5, dialyzed, and dried to obtain the double bond esterification product. Step B: Sodium dodecyl sulfate and water are mixed and stirred to dissolve. The double bond esterification product, methacrylic acid, methyl methacrylate, and butyl acrylate are then added and mixed for pre-emulsification. Ammonium persulfate aqueous solution is then added, and the mixture is sonicated to obtain a modified polymer emulsion. In Step A, the ratio of anhydrous hydroxypropyl cellulose, glacial acetic acid, itaconic anhydride, succinic anhydride, and anhydrous sodium acetate is 10g:50mL:4.5g:2.5g:4.5g. In Step A, the mixture is heated to dissolve... The process conditions for the solution are: temperature 65℃, time 0.6h; in step A, the process conditions for the heating reaction are: temperature 80℃, time 2.8h; in step A, the process conditions for drying are: temperature 80℃, time 4h; in step B, the ratio of sodium dodecyl sulfate, water, double bond esterification product, methacrylic acid, methyl methacrylate, butyl acrylate and ammonium persulfate aqueous solution is 0.24 g: 30 mL: 1.5 g: 3.0 mL: 1.5 mL: 7.5 mL: 0.22 mL; the mass fraction of ammonium persulfate aqueous solution is 1.18%; in step B, the process conditions for pre-emulsification are: temperature 70℃, time 5 min; in step B, the process conditions for ultrasonic reaction are: power 280W, temperature 70℃, time 40 min; (3) Preparation of finasteride tablets: Step 1: Mix finasteride supported on mesoporous silica, microcrystalline cellulose, magnesium stearate, povidone K30, and maltose-cyclodextrin evenly, compress into tablets to obtain tablet cores; Step 2: Mix modified polymer emulsion, titanium dioxide, talc, and water, stir evenly to obtain a coating solution, place the tablet cores in a coating pan, heat to 40°C, spray with the coating solution, remove and dry after coating to obtain finasteride tablets; In Step 1, the tablet cores include the following mass components: 1 part mesoporous silica supported on finasteride, 50 parts microcrystalline cellulose, 1 part magnesium stearate, 6 parts povidone K30, and 5 parts maltose-cyclodextrin; In Step 2, the mass ratio of modified polymer emulsion, titanium dioxide, talc, and water is 8:0.3:0.1:100; In Step 2, the mass ratio of tablet cores to coating solution is 10:2; In Step 2, the drying process conditions are: temperature 40°C, time 8 hours.

[0032] Comparative Example 1: Compared with Example 1, the mesoporous silica-supported finasteride was replaced with finasteride, and the mass composition of the core was adjusted to: 1 part finasteride, 70 parts microcrystalline cellulose, 2 parts magnesium stearate, 10 parts povidone K30, and 15 parts maltose-cyclodextrin. The other conditions remained unchanged and were the same as in Example 1.

[0033] Comparative Example 2: Compared with Example 1, without adding double bond esterification products to the modified polymer emulsion, sodium dodecyl sulfate, methacrylic acid, methyl methacrylate, and butyl acrylate were directly mixed and pre-emulsified (process conditions were the same as in Example 1), and the other conditions remained unchanged, the same as in Example 1.

[0034] Comparative Example 3: Compared with Example 1, the coating solution was not sprayed on the surface of the tablet core, and the tablet core was prepared directly. All other conditions remained the same as in Example 1.

[0035] Comparative Example 4: Compared with Example 1, mesoporous silica-supported finasteride was replaced with finasteride (the same as in Comparative Example 1), and no double bond esterification product was added to the modified polymer emulsion. All other conditions remained the same as in Example 1.

[0036] experiment: Preparation of artificial gastric juice: Take 16.4 mL of 0.1 mol / L dilute hydrochloric acid and 10 g of pepsin, add water and mix, then make up to 1000 mL to obtain artificial gastric juice; Preparation of artificial intestinal fluid: Take 6.8g of potassium dihydrogen phosphate, mix and dissolve it in 500mL of water, add 0.1mol / L sodium hydroxide to adjust the pH to 6.8, then add 10g of trypsin and mix well, and make up to 1000ml to obtain artificial intestinal fluid; Dissolution test: Finasteride tablets from each example and comparative example were divided into two groups and placed in artificial intestinal fluid. The dissolution rate was determined by high performance liquid chromatography at 5 min, 10 min, 15 min and 60 min. Based on the data in the table above, the following conclusions can be drawn: The finasteride tablets obtained in Examples 1-3 and Comparative Examples 1, 2, and 4 all had a solubility of less than 5% in gastric juice within 15 minutes and less than 15% at 60 minutes, indicating extremely low solubility and not effective drug release. However, Comparative Example 3, which did not have a coating solution on the tablet core surface, had a higher solubility in gastric juice than Comparative Examples 1, 2, and 4, indicating that the addition of coating in this application can achieve non-dissolution in gastric juice. As can be seen from the above, the coating material prepared in this application is enteric-coated, which releases almost no drug in gastric juice and does not irritate the stomach. Based on the data in the table above, the following conclusions can be drawn: Compared with Example 1, the dissolution rate of Comparative Example 1 decreased because, in Comparative Example 1, finasteride molecules are arranged in a crystalline state under normal conditions, while in this application, mesoporous silica is used for loading, which transforms it into an amorphous state and improves the dissolution rate. In Comparative Example 2, no double bond esterification products were added to the modified polymer emulsion, and the coating did not contain carboxyl groups. The dissolution rate in intestinal fluid was low, but the dissolution rate at 60 min was higher than that in Comparative Example 1. This is because after the coating dissolves, the release rate of finasteride supported on mesoporous silica is faster than that of finasteride alone. Comparative Example 3, which did not spray coating solution on the tablet core surface and directly prepared the tablet core, had the highest dissolution rate in intestinal fluid. This is because without coating, the carboxyl groups on the drug-loaded mesoporous silica are ionized, which weakens their ability to act as hydrogen bond donors and reduces their binding force with the drug, thus achieving rapid drug release. Compared with Comparative Examples 1 and 2, the dissolution rate of Comparative Example 4 decreased significantly; As can be seen from the above, the drug loading process and the selection of coating solution in the preparation of mesoporous silica in this application can promote the improvement of the dissolution of the prepared tablets.

[0037] It will be apparent to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above, and that the invention can be implemented in other specific forms without departing from its spirit or essential characteristics. Therefore, the embodiments should be considered in all respects as exemplary and non-limiting, and the scope of the invention is defined by the appended claims rather than the foregoing description. Thus, all variations falling within the meaning and scope of equivalents of the claims are intended to be included within the present invention. No reference numerals in the claims should be construed as limiting the scope of the claims.

Claims

1. A method for producing rapidly dissolving finasteride tablets, characterized in that: Includes the following steps: Step 1: Mix mesoporous silica-loaded finasteride, microcrystalline cellulose, magnesium stearate, povidone K30, and maltose-cyclodextrin evenly, compress into tablets, and obtain tablet cores; Step 2: Mix the modified polymer emulsion, titanium dioxide, talc powder and water, stir evenly to obtain a coating solution, place the tablet core in a coating pan, heat to 40~45℃, spray the coating solution, remove and dry after coating to obtain finasteride tablets.

2. The method for producing a rapidly dissolving finasteride tablet according to claim 1, characterized in that: The mesoporous silica-supported finasteride is prepared by the following process: Finasteride was mixed with anhydrous ethanol, stirred and dissolved, then carboxylated mesoporous silica was added, the mixture was shaken in a water bath and dried to obtain mesoporous silica-supported finasteride.

3. The method for producing a rapidly dissolving finasteride tablet according to claim 1, characterized in that: The preparation process of the modified polymer emulsion is as follows: Step A: Mix anhydrous hydroxypropyl cellulose with glacial acetic acid, heat to dissolve, then add itaconic anhydride, succinic anhydride and anhydrous sodium acetate, heat to react, add deionized water and concentrated hydrochloric acid to terminate the reaction, precipitate out, wash to pH 5.0~5.5, dialyze, dry to obtain double bond esterified product; Step B: Sodium dodecyl sulfate and water are mixed and stirred to dissolve. Then, double bond esterification products, methacrylic acid, methyl methacrylate, and butyl acrylate are added and mixed for pre-emulsification. Then, ammonium persulfate aqueous solution is added and the mixture is subjected to ultrasonic reaction to obtain a modified polymer emulsion.

4. The method for producing a rapidly dissolving finasteride tablet according to claim 2, characterized in that: The ratio of finasteride, anhydrous ethanol, and carboxylated mesoporous silica is (0.10~0.12) g : (40~50) mL : (0.10~0.15) g.

5. The method for producing a rapidly dissolving finasteride tablet according to claim 2, characterized in that: The process conditions for water bath oscillation are: temperature 35~37℃, oscillation time 10~24h.

6. The method for producing a rapidly dissolving finasteride tablet according to claim 3, characterized in that: In step A, the ratio of anhydrous hydroxypropyl cellulose, glacial acetic acid, itaconic anhydride, succinic anhydride and anhydrous sodium acetate is 10g: (50~100)mL: (4.5~5.5)g: (2.5~3.5)g: (4.5~5.5)g.

7. The method for producing a rapidly dissolving finasteride tablet according to claim 3, characterized in that: In step B, the ratio of sodium dodecyl sulfate, water, double bond esterification product, methacrylic acid, methyl methacrylate, butyl acrylate and ammonium persulfate aqueous solution is (0.24~0.30) g : (30~40) mL : (1.5~2.5) g : (3.0~3.2) mL : (1.5~2.0) mL : (7.5~8.0) mL : (0.22~0.24) mL.

8. The method for producing a rapidly dissolving finasteride tablet according to claim 1, characterized in that: In step 1, the core comprises the following components by weight: 1-2 parts mesoporous silica loaded with finasteride, 50-70 parts microcrystalline cellulose, 1-2 parts magnesium stearate, 6-10 parts povidone K30, and 5-15 parts maltose-cyclodextrin.

9. The method for producing a rapidly dissolving finasteride tablet according to claim 1, characterized in that: In step 2, the mass ratio of modified polymer emulsion, titanium dioxide, talc powder and water is (8~10):(0.3~0.5):(0.1~0.3):(100~120).

10. A rapidly dissolving finasteride tablet, characterized in that: Obtained by the production method according to any one of claims 1 to 9.

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