Desloratadine dispersible tablet and preparation method thereof

Abstract

The invention relates to a desloratadine dispersible tablet and a preparation method thereof, and a coated tablet and a preparation method thereof. The desloratadine dispersible tablet is prepared from the following components in percentage by weight: 10 to 15 percent of desloratadine, 80 to 89 percent of filler, 0.1 to 2 percent of sodium carboxymethyl starch serving as a disintegrating agent, 0.5 to 4 percent of lubricant and 0.5 to 2 percent of adhesive. The desloratadine dispersible tablet disclosed by the invention is reasonable in prescription and stable in preparation process, achieves a relatively good effect on selection of auxiliary materials and content selection of main drugs and the auxiliary materials, and is relatively low in production cost.

Description

Technical Field

[0001] The invention relates to the pharmaceutical field, and in particular to a desloratadine dispersible tablet and a preparation method thereof. Background Art

[0002] Desloratadine is a non-sedative, long-acting tricyclic antihistamine and an active metabolite of loratadine. It can selectively antagonize peripheral H1 receptors to relieve symptoms related to allergic rhinitis or chronic idiopathic urticaria. The present invention provides a desloratadine dispersible tablet suitable for pharmaceutical use, which has a simple preparation process, a fast dissolution rate, a dissolution rate of more than 90%, a safe and reliable quality, and a preparation method thereof. Summary of the invention

[0003] The present invention provides a novel desloratadine dispersible tablet and a preparation method thereof. The present inventors determine the prescription through prescription screening, and conduct influencing factor tests and in vitro dissolution curve tests, etc., and all indicators are excellent. The preparation of the present invention has a reasonable prescription and a stable preparation process, the production process can be effectively controlled, the cost is low and the quality is high, and it is suitable for large-scale industrial production.

[0004] Specifically, the present invention provides: (1) a desloratadine dispersible tablet, which is composed of the following components: 10-15 wt % of desloratadine, 80-89 wt % of a filler, 0.1-2 wt % of sodium carboxymethyl starch as a disintegrant, 0.5-4 wt % of a lubricant, and 0.5-2 wt % of a binder.

[0005] (2) The desloratadine dispersible tablet according to (1), wherein the content of the sodium carboxymethyl starch is 0.5 wt %.

[0006] (3) The desloratadine dispersible tablet according to (1), wherein the filler is a mixture of lactose and starch, and the weight ratio of the lactose to the starch is less than 1.

[0007] (4) The desloratadine dispersible tablet according to (1), wherein the lubricant is a mixture of silicon dioxide and magnesium stearate, and the weight ratio of the silicon dioxide to the magnesium stearate is 1:1.

[0008] (5) The desloratadine dispersible tablet according to (1), wherein the binder is povidone K30.

[0009] (6) The desloratadine dispersible tablet according to (3), wherein the content of lactose in the desloratadine dispersible tablet is 30-40 wt %, and the content of starch is 45-55 wt %.

[0010] (7) The desloratadine dispersible tablet according to (6), wherein the content of desloratadine is 12.5% ​​by weight, the content of lactose is 35% by weight, the content of starch is 49% by weight, the content of sodium carboxymethyl starch is 0.5% by weight, the content of lubricant is 2% by weight, and the content of binder is 1% by weight.

[0011] (8) The desloratadine dispersible tablet according to (7), wherein the lubricant is a mixture of silicon dioxide and magnesium stearate, and the weight ratio of the silicon dioxide to the magnesium stearate is 1:1.

[0012] (9) A method for preparing the desloratadine dispersible tablet according to any one of (1) to (8), the method comprising: 1) 10-15 parts by weight of desloratadine, 80-89 parts by weight of a filler and 0.1-2 parts by weight of sodium carboxymethyl starch are uniformly mixed, and an aqueous solution of a binder is added to prepare a soft material; 2) sieving the soft material to prepare wet granules, and drying; 3) granulating, adding 0.1-5 parts by weight of lubricant, and mixing evenly; and 4) Tablet pressing.

[0013] (10) The preparation method according to (9), further comprising, before step 1), sieving desloratadine, filler, sodium carboxymethyl starch and lubricant through a 100-mesh sieve. (11) The preparation method according to (9), wherein in step 2), the drying comprises drying the wet granules at 50°C until the granules have a moisture content of 2-4% by weight.

[0014] (12) The preparation method according to (9), wherein the aqueous solution of the adhesive is a 10 wt% aqueous solution of povidone K30. Specific embodiments

[0015] The present invention is further illustrated below through the description of specific implementation modes, but this is not a limitation of the present invention. Those skilled in the art can make various modifications or improvements based on the basic idea of ​​the present invention, but as long as they do not deviate from the basic idea of ​​the present invention, they are all within the scope of the present invention.

[0016] Embodiment 1: Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 5 Lactose 36 Starch 54 Sodium starch glycolate Povidone K30 1 Silica 1 Magnesium stearate 1 1000 pieces Preparation method: (1) The raw and auxiliary materials are crushed and passed through a 100-mesh sieve for later use; (2) Weigh povidone K30 and prepare a 10 wt % aqueous solution; (3) Accurately weigh the raw materials and excipients according to the prescription amount, mix desloratadine with lactose, starch, and sodium carboxymethyl starch uniformly, and add an appropriate amount of 10 wt % povidone K30 aqueous solution to prepare a soft material; (4) The soft material is passed through a 20-mesh sieve to prepare wet granules, and dried at 50°C until the granules have a moisture content of 2 to 4%; (5) The dry granules are sieved through a 20-mesh sieve, and the prescribed amount of magnesium stearate and silicon dioxide are added and mixed evenly; (6) Tableting. Example 2

[0017] Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 5 Lactose 26 Starch 64 Sodium starch glycolate Povidone K30 1 Silica 1 Magnesium stearate 1 1000 pieces Preparation method: The preparation method is the same as above. Example 3

[0018] Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 5 Lactose 64 Starch 24 Sodium starch glycolate Povidone K30 1 Silica 2 Magnesium Stearate 2 1000 pieces Preparation method: The preparation method is the same as above. Example 4

[0019] Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 10 Lactose 59 Starch 24 Sodium starch glycolate Povidone K30 1 Silica 1.5 Magnesium stearate 1.5 1000 pieces Preparation method: The preparation method is the same as above. Example 5

[0020] Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 10 Lactose 29 Starch 54 Sodium starch glycolate Povidone K30 1 Silica 1 Magnesium stearate 1 1000 pieces Preparation method: The preparation method is the same as above.

[0021] Comparative Example 1: Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 20 Lactose 36 Starch 54 Sodium starch glycolate Povidone K30 1 Silica 1 Magnesium stearate 1 Made into 1000 pieces.

[0022] Preparation method: The preparation method is the same as above. Example 6

[0023] Name of raw materials and auxiliary materials Prescription dosage (g) Desloratadine 30 Lactose 29 Starch 54 Sodium starch glycolate Povidone K30 1 Silica 1 Magnesium stearate 1 Made into 1000 pieces.

[0024] Preparation method: The preparation method is the same as above.

[0025] The dissolution curve was measured with pH 3.5 + 0.5% SDS 900ml as the dissolution medium, paddle method, rotation speed of 75 rpm, detection wavelength of 276nm, and the measured dissolution curve is shown in Table 1. The related substances affecting the factors are shown in Table 2

[0026]

[0027] It can be seen from Table 1 and Table 2 that the dissolution of the loratadine dispersible tablets prepared according to the embodiment of the present invention is significantly better than that of the comparative example; from the above results, it can be seen that the influencing factors of the loratadine dispersible tablets prepared according to the present invention are better than those of the comparative example, and the preparation process is simple, which is suitable for large-scale industrial production.

Claims

1. A desloratadine dispersible tablet, which is composed of the following components: 10-15 wt% of desloratadine, 80-89 wt% of a filler, 0.1-2 wt% of sodium carboxymethyl starch as a disintegrant, 0.5-4 wt% of a lubricant, and 0.5-2 wt% of a binder.

2. The desloratadine dispersible tablet according to claim 1, wherein the content of the sodium carboxymethyl starch is 0.5% by weight.

3. The desloratadine dispersible tablet according to claim 1, wherein the filler is a mixture of lactose and starch, and the weight ratio of the lactose to the starch is less than 1.

4. The desloratadine dispersible tablet according to claim 1, wherein the lubricant is a mixture of silicon dioxide and magnesium stearate, and the weight ratio of the silicon dioxide to the magnesium stearate is 1:

1.

5. The desloratadine dispersible tablet according to claim 1, wherein The adhesive is povidone k30.

6. The desloratadine dispersible tablet according to claim 3, wherein the content of lactose in the desloratadine dispersible tablet is 30-40 wt%, and the content of starch is 45-55 wt%.

7. The desloratadine dispersible tablet according to claim 6, wherein the content of desloratadine is 12.5% ​​by weight, the content of lactose is 35% by weight, the content of starch is 49% by weight, the content of sodium carboxymethyl starch is 0.5% by weight, the content of lubricant is 2% by weight, and the content of binder is 1% by weight.

8. The desloratadine dispersible tablet according to claim 7, wherein the lubricant is a mixture of silicon dioxide and magnesium stearate, and the weight ratio of the silicon dioxide to the magnesium stearate is 1:

1.

9. A method for preparing the desloratadine dispersible tablet according to any one of claims 1 to 8, the method comprising: 1) 10-15 parts by weight of desloratadine, 80-89 parts by weight of a filler and 0.1-2 parts by weight of sodium carboxymethyl starch are uniformly mixed, and an aqueous solution of a binder is added to prepare a soft material; 2) sieving the soft material to prepare wet granules, and drying; 3) granulate, add 0.1-5 parts by weight of lubricant, and mix well; 4) Tablet pressing.

10. The preparation method according to claim 9, further comprising, before step 1), passing desloratadine, filler, sodium carboxymethyl starch and lubricant through a 100-mesh sieve respectively.

11. The preparation method according to claim 9, wherein: In step 2), the drying comprises drying the wet granules at 50° C. until the moisture content of the granules is 2-4% by weight.

12. The preparation method according to claim 9, wherein: The aqueous solution of the adhesive is a 10 wt% polyvidone K30 aqueous solution.

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