Azilsartan tablet and preparation method thereof

Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an azilsartan tablet and a preparation method thereof. The azilsartan tablet is prepared from the following raw material components in parts by weight: 35 to 45 parts of azilsartan, 72 to 76 parts of silicified microcrystalline cellulose, 10 to 12 parts of low-substituted hydroxypropyl cellulose, 3 to 7 parts of talcum powder and 0.39 to 1.04 parts of carnauba wax. The particle size D90 of the azilsartan is 50 to 80 [mu] m. According to the preparation method, azilsartan with the particle size D90 of 50-80 microns, silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose and talcum powder are firstly pressed into the tablet, and then a coating is formed on the surface of the tablet by adopting carnauba wax, so that the dissolution rate and the dissolution uniformity of the tablet are improved, and the stability of the tablet is also greatly improved.

Description

Technical Field

[0001] The present application relates to the technical field of pharmaceutical preparations, and in particular to an azilsartan tablet and a preparation method thereof. Background Art

[0002] Azilsartan is a non-peptide angiotensin receptor II inhibitor developed by Takeda Pharmaceuticals of Japan. It can selectively block angiotensin II receptor 1 (AT1-R). Currently, there are two forms of acesartan potassium and azilsartan on the market. Azilsartan potassium is a prodrug of azilsartan, which is hydrolyzed in the gastrointestinal tract to become the active metabolite azilsartan. Azilsartan potassium was approved by the FDA for marketing in 2011, and azilsartan was launched in Japan in 2012. Azilsartan, as a new generation of selective AT1 subtype angiotensin II receptor antagonists, has a strong and lasting antihypertensive effect compared with angiotensin converting enzyme inhibitor antihypertensive drugs, and does not cause dry cough. However, the commonly used azilsartan is difficult to have good stability and dissolution uniformity while ensuring a high dissolution rate. Summary of the invention

[0003] In order to improve the dissolution rate of azilsartan while ensuring uniform dissolution and good stability, the present application provides an azilsartan tablet and a preparation method thereof.

[0004] In the first aspect, the present application provides an azilsartan tablet, which adopts the following technical solution: Disclosed is an azilsartan tablet. The raw materials of the tablet include the following components in parts by weight: 35-45 parts of azilsartan, 72-76 parts of silicified microcrystalline cellulose, 10-12 parts of low-substituted hydroxypropyl cellulose, 3-7 parts of talc, and 0.39-1.04 parts of carnauba wax. The particle size D90 of the azilsartan is 50-80 μm.

[0005] By adopting the above technical solution, azilsartan with a particle size D90 of 50-80um, silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and talc are pressed into tablets, and then carnauba wax is used to form a coating on the surface of the tablets. This not only improves the dissolution rate and dissolution uniformity of the tablets, but also greatly improves the stability of the tablets.

[0006] In a specific embodiment, the particle size D90 of the carnauba wax is 200-230 um.

[0007] In a specific embodiment, the particle size D90 of the silicified microcrystalline cellulose is 300-330 um.

[0008] In a specific embodiment, the particle size D90 of the low-substituted hydroxypropyl cellulose is 200-230 um.

[0009] In a specific embodiment, the particle size D90 of the talc is 10-30 um.

[0010] By adopting the above technical solution, the particle sizes of carnauba wax, silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose and talc are further limited, so that the obtained tablets have better dissolution rate and dissolution uniformity.

[0011] In a second aspect, the present application provides a method for preparing an azilsartan tablet, which adopts the following technical scheme. A method for preparing an azilsartan tablet comprises the following steps: Tablet preparation: Azilsartan and low-substituted hydroxypropyl cellulose are mixed and sieved to obtain premix A; premix A and silicified microcrystalline cellulose are mixed and sieved to obtain premix B; premix B is mixed with talcum powder, pressed into tablets, and azilsartan tablets are obtained; surface treatment: the azilsartan tablets are first preheated, then carnauba wax is sieved, slowly and continuously poured into the azilsartan tablets, mixed and rubbed with the azilsartan tablets, and cooled to obtain azilsartan tablets.

[0012] By adopting the above technical scheme, azilsartan, low-substituted hydroxypropyl cellulose, silicified microcrystalline cellulose and talc are first mixed and tableted to obtain azilsartan tablets, and then the azilsartan tablets are coated with carnauba wax to obtain azilsartan tablets with high dissolution rate, uniform dissolution and good stability.

[0013] In a specific embodiment, the tableting step is: mixing azilsartan and low-substituted hydroxypropyl cellulose and passing the mixture through a 60-mesh sieve to obtain premix A; mixing premix A and silicified microcrystalline cellulose and passing the mixture through a 40-mesh sieve to obtain premix B; mixing premix B with talc and pressing the mixture into tablets to obtain azilsartan tablets.

[0014] In a specific embodiment, the surface treatment step is: first preheating the azilsartan tablets at 40°C, then passing the carnauba wax through a 60-mesh sieve, slowly and continuously pouring it into the azilsartan tablets, stopping heating, mixing and rubbing the carnauba wax and the azilsartan tablets for 25-35 minutes, and cooling to obtain azilsartan tablets.

[0015] By adopting the above technical solution, the preheating temperature and the mixing friction time are further limited, so that the carnauba wax can better coat the azilsartan tablets.

[0016] In summary, the present application includes at least one of the following beneficial technical effects: 1. In the present application, azilsartan with a particle size D90 of 50-80 um, silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and talc are pressed into tablets, and then carnauba wax is used to form a coating on the surface of the tablets, which not only improves the dissolution rate and dissolution uniformity of the tablets, but also greatly improves the stability of the tablets; 2. The particle sizes of carnauba wax, silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose and talc are further limited in the present application, so that the obtained tablets have a good dissolution rate and dissolution uniformity; 3. The method of the present application firstly mixes azilsartan, low-substituted hydroxypropyl cellulose, silicified microcrystalline cellulose and talc and compresses them into tablets to obtain azilsartan tablets, and then coats the azilsartan tablets with carnauba wax to obtain azilsartan tablets with high dissolution rate, good dissolution uniformity and good stability. BRIEF DESCRIPTION OF THE DRAWINGS

[0017] Figure 1 It is a dissolution curve diagram used in this application to reflect the drug in Examples 1-3 and the control example in a phosphate medium with a pH of 6.8.

[0018] Figure 2 It is a dissolution curve diagram used in this application to reflect the drug in Comparative Examples 1-2, Comparative Examples 4-5 and the control example in a phosphate medium with a pH of 6.8. DETAILED DESCRIPTION

[0019] The present application is further described in detail below in conjunction with embodiments.

[0020] All raw materials in the examples are commercially available. Example

[0021] Example 1 Embodiment 1 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 50um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.65 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0022] Example 2 Embodiment 2 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.65 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0023] Example 3 Embodiment 3 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 80um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.65 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0024] Example 4 Embodiment 4 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.39 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0025] Example 5 Embodiment 5 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 1.04 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour it into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0026] Example 6 Embodiment 6 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 35g of azilsartan and 10g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 72g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 3g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.39 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0027] Example 7 Embodiment 7 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 45g of azilsartan and 12g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 76g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 7g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 1.04 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour it into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0028] Comparative Example Comparative Example 1 Comparative Example 1 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 45um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.65 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0029] Comparative Example 2 Comparative Example 2 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 90um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.65 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0030] Comparative Example 3 Comparative Example 3 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 0.26 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0031] Comparative Example 4 Comparative Example 4 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40g of azilsartan and 11g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain premix A; premix A is mixed evenly with 74g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain premix B; premix B is mixed evenly with 5g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130mg; wherein the particle size D90 of azilsartan is 65um; the particle size D90 of silicified microcrystalline cellulose is 320um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220um; and the particle size D90 of talc is 20um; Surface treatment: First, add the azilsartan tablets into the coating equipment, set the heating temperature to 45°C, and the air volume to 1000m 3 / h, speed 4 rpm, preheat to 40°C, then pass 1.17 g of carnauba wax through a 60-mesh sieve, slowly and continuously pour into the azilsartan tablets, stop heating, increase the speed to 6 rpm, continue mixing and rubbing for 30 minutes, and after cooling to room temperature, obtain azilsartan tablets.

[0032] Comparative Example 5 Comparative Example 5 provides a method for preparing an azilsartan tablet, comprising the following steps: Tablet preparation: 40 g of azilsartan and 11 g of low-substituted hydroxypropyl cellulose are mixed evenly, and the mixture is passed through a 60-mesh sieve through a swing granulator to obtain a premix A; premix A is mixed evenly with 74 g of silicified microcrystalline cellulose, and the mixture is passed through a 40-mesh sieve through a swing granulator to obtain a premix B; premix B is mixed evenly with 5 g of talc, and the mixture is compressed through a rotary tablet press to obtain azilsartan tablets with a tablet weight of about 130 mg; wherein the particle size D90 of azilsartan is 65 um; the particle size D90 of silicified microcrystalline cellulose is 320 um; the particle size D90 of low-substituted hydroxypropyl cellulose is 220 um; and the particle size D90 of talc is 20 um.

[0033] Comparison Example The control example is Azilsartan original drug

[0034] Performance test Dissolution performance: The dissolution of the drugs in each example and comparative example in a phosphate buffer medium with a pH of 6.8 was tested by a paddle method, with a medium volume of 900 mL, a water bath temperature of 37 ± 0.5 ° C, and a stirring paddle speed of 50 r / min to obtain a dissolution curve. For details, see Figure 1 and Figure 2 .

[0035] Stability: The drugs in the embodiments and comparative examples were subjected to accelerated tests and high humidity tests, and were placed for 30 consecutive days to examine the changes in related substances in each sample. The accelerated test conditions were: temperature of 40°C ± 2°C, relative humidity of 75% ± 5%; the high humidity test conditions were: temperature of 25°C ± 2°C, relative humidity of 90% ± 5%.

[0036] Table 1 Drug dissolution performance test results Table 2 Drug stability test results Combined with Table 1, Figure 1 , Examples 1-3 and the control example. The dissolution curves of the drugs in Examples 1-3 in a phosphate buffer medium at pH 6.8 are similar to those of the control example. Therefore, the azilsartan tablets of the present invention use azilsartan with a particle size D90 of 50 to 80 um, and are pressed into tablets using silicified microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and talc. Finally, carnauba wax is used to form a coating on the surface of the tablets, which can improve the dissolution performance of the tablets.

[0037] Combined with Table 1, Figure 1-2, Example 1 and Comparative Examples 1-2. It can be seen that in Comparative Example 1, azilsartan is too finely ground. Although its solubility is high, it is too high compared with the original drug. The similarity factor F2 value is lower than 50, and there is a greater risk of in vivo bioequivalence. When the particle size of azilsartan in Comparative Example 2 is too large, its solubility is low. Therefore, the particle size of azilsartan is preferably 50-80um.

[0038] Combined with Table 1, Figure 1-2 , Example 1 and Comparative Example 4, it can be seen that when the dosage of the carnauba wax coating is 0.9%, it will hinder the dissolution and cause the dissolution to be slow. Therefore, when the dosage of the carnauba wax is too large, it will affect the dissolution of the tablet.

[0039] Combined with Table 1, Figure 1 , Comparing Example 5 with the control example, it can be seen that when the carnauba wax coating is not used, the dissolution uniformity is poor and the RSD is large. From the dissolution phenomenon, the applicant found that the coated drug slipped to the center of the bottom of the dissolution cup as soon as it was put into the tablet, and the drug without the coating became sticky due to dissolution and adhered to other positions at the bottom of the cup, causing some to dissolve faster and some to dissolve slower, resulting in differences in uniformity.

[0040] Combined with Table 2, Examples 1-3, Comparative Example 5 and the control example, it can be seen that under accelerated test conditions for 30 days, the 30-day related substances and the increase in the drug in Examples 1-3 are all less than 0.5%, while the 30-day related substances and the increase in the drug in Comparative Examples 5-6 are all above 0.5%; under high humidity test conditions for 30 days, the 30-day related substances and the increase in the drug in Examples 1-3 are all less than 0.5%, while the 30-day related substances and the increase in the drug in Comparative Examples 5-6 are all above 0.5%; It can be seen that the use of Brazilian palm wax to coat azilsartan in the present application has a significant barrier protection effect, thereby improving the stability of the obtained azilsartan tablets.

[0041] Combining Table 2, Example 3 and Comparative Example 4, it can be seen that when using carnauba wax to coat azilsartan, if the dosage is too low, the coating effect is poor, thereby affecting the stability of the obtained azilsartan tablets.

[0042] This specific embodiment is merely an explanation of the present application and is not a limitation of the present application. After reading this specification, those skilled in the art may make modifications to the present embodiment without any creative contribution as needed, but such modifications are protected by the patent law as long as they are within the scope of the claims of the present application.

Claims

1. An azilsartan tablet, characterized in that: The raw materials of the tablets include the following components in parts by weight: 35-45 parts of azilsartan, 72-76 parts of silicified microcrystalline cellulose, 10-12 parts of low-substituted hydroxypropyl cellulose, 3-7 parts of talc, and 0.39-1.04 parts of carnauba wax; the particle size D90 of the azilsartan is 50-80 um.

2. An azilsartan tablet according to claim 1, characterized in that: The particle size D90 of the carnauba wax is 200-230 um.

3. An azilsartan tablet according to claim 1, characterized in that: The particle size D90 of the silicified microcrystalline cellulose is 300-330 um.

4. An azilsartan tablet according to claim 1, characterized in that: The particle size D90 of the low-substituted hydroxypropyl cellulose is 200-230 um.

5. An azilsartan tablet according to claim 1, characterized in that: The particle size D90 of the talcum powder is 10-30 um.

6. A method for preparing the azilsartan tablet according to any one of claims 1 to 5, characterized in that: The following steps are involved: Tablet preparation: Azilsartan and low-substituted hydroxypropyl cellulose are mixed and sieved to obtain premix A; premix A and silicified microcrystalline cellulose are mixed and sieved to obtain premix B; premix B is mixed with talc and pressed into tablets to obtain azilsartan tablets; Surface treatment: first preheat the azilsartan tablets, then sieve the carnauba wax, slowly and continuously pour it into the azilsartan tablets, mix and rub with the azilsartan tablets, cool, and obtain azilsartan tablets.

7. The method for preparing an azilsartan tablet according to claim 6, characterized in that: The tableting steps are: mixing azilsartan and low-substituted hydroxypropyl cellulose and passing the mixture through a 60-mesh sieve to obtain a premix A; mixing the premix A and silicified microcrystalline cellulose and passing the mixture through a 40-mesh sieve to obtain a premix B; mixing the premix B with talcum powder and pressing the mixture into tablets to obtain azilsartan tablets.

8. The method for preparing an azilsartan tablet according to claim 6, characterized in that: The surface treatment step is: first preheating the azilsartan tablets at 40° C., then passing the carnauba wax through a 60-mesh sieve, slowly and continuously pouring it into the azilsartan tablets, stopping heating, mixing and rubbing the carnauba wax and the azilsartan tablets for 25-35 minutes, and cooling to obtain the azilsartan tablets.

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