A metronidazole tablet and preparation method thereof

Abstract

The present invention discloses a metronidazole tablet and a preparation method thereof. The metronidazole tablet is prepared from the following components in parts by weight: 55-60 parts of metronidazole, 35-40 parts of a filler, 5-10 parts of sorbitol, 1-5 parts of povidone K30, 5-15 parts of a binder, 0.2-0.5 parts of magnesium stearate, and 2-6 parts of a coating agent. The use of sorbitol and povidone K30 in the excipients of the present invention can improve the brittleness of the tablet, increase its hardness and stability, and make it less prone to breakage during production and storage. In addition, the synergistic effect of sorbitol and povidone K30 can improve the dissolution rate of the tablet, thereby increasing the bioavailability of the drug.

Description

Technical Field

[0001] The invention belongs to the field of medicine, and in particular relates to a metronidazole tablet and a preparation method thereof. Background Art

[0002] Metronidazole is used to treat intestinal and extraintestinal amebiasis (such as amoebic liver abscess and pleural amebiasis). It can also treat vaginal trichomoniasis, balantidiasis, cutaneous leishmaniasis, and Guinea worm infection. Currently, the drug is also widely used to treat anaerobic infections.

[0003] As a widely used anti-infective drug, the market for metronidazole tablets is expected to experience moderate growth as global health needs grow and healthcare services improve. Demand for antimicrobial drugs continues to grow due to the occurrence of various infectious diseases. As an effective antimicrobial drug, metronidazole tablets have significant efficacy in treating anaerobic infections, resulting in stable market demand. However, existing metronidazole tablets have poor hardness, which affects their friability and may have a certain impact on the drug's dissolution rate. Summary of the Invention

[0004] In view of the shortcomings of the existing technology, the primary purpose of the present invention is to provide a metronidazole tablet and a preparation method thereof to solve the problems of poor hardness and poor solubility of existing metronidazole tablets.

[0005] Another object of the present invention is to provide a method for preparing the erythromycin enteric-coated tablets, which is simple and easy to implement and suitable for large-scale industrial production.

[0006] The purpose of the present invention is achieved through the following technical solutions:

[0007] A metronidazole tablet is prepared from the following components in parts by weight: 55-60 parts of metronidazole, 35-40 parts of a filler, 5-10 parts of sorbitol, 1-5 parts of povidone K30, 5-15 parts of a binder, 0.2-0.5 parts of magnesium stearate, and 2-6 parts of a coating agent.

[0008] Preferably, the metronidazole tablets are prepared from the following components in parts by mass: 55-60 parts of metronidazole, 38-40 parts of filler, 8-10 parts of sorbitol, 3-5 parts of povidone K30, 10-15 parts of binder, 0.2-0.5 parts of magnesium stearate and 3-6 parts of coating agent.

[0009] Preferably, the filler is a mixture of corn starch and calcium hydrogen phosphate.

[0010] Preferably, the mass ratio of corn starch to calcium hydrogen phosphate is 1-3:1.

[0011] Preferably, the binder is a 10 wt% aqueous solution of povidone K30.

[0012] Preferably, the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2 to 3:1.

[0013] The preparation method of the metronidazole tablets comprises the following steps:

[0014] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0015] (2) Adding a binder to the dry mix and performing wet granulation, drying and sizing the granules after granulation, and finally adding magnesium stearate and performing tableting;

[0016] (3) The coating agent is prepared into a coating liquid, and the tablets after tableting are coated to obtain metronidazole tablets.

[0017] Preferably, in step (2), the drying temperature is 50-60°C.

[0018] Preferably, in step (2), the drying step is to dry the sample until the moisture content is 1-3%.

[0019] Preferably, in step (3), the concentration of the coating solution is 15-25%.

[0020] Preferably, in step (3), the coating treatment is performed by fluidized bed coating or spray drying coating.

[0021] Compared with the prior art, the present invention has the following beneficial effects:

[0022] The use of sorbitol and povidone K30 in the excipients of the present invention can improve the brittleness of the tablets, increase their hardness and stability, and make them less prone to breakage during production and storage. In addition, the synergistic effect of sorbitol and povidone K30 can improve the dissolution rate of the tablets, thereby increasing the bioavailability of the drug. DETAILED DESCRIPTION

[0023] In order to make the purpose, technical solutions and advantages of the present invention more clearly understood, the present invention is further described in detail below in conjunction with the embodiments. It should be understood that the specific embodiments described herein are only used to explain the present invention and are not intended to limit the present invention.

[0024] Example 1

[0025] A metronidazole tablet is prepared from the following components in parts by mass: 55 parts of metronidazole, 35 parts of a filler, 5 parts of sorbitol, 1 part of povidone K30, 5 parts of a binder, 0.2 parts of magnesium stearate, and 2 parts of a coating agent.

[0026] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 1:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2:1.

[0027] The preparation method of the metronidazole tablets comprises the following steps:

[0028] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0029] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 50°C (dry to a sample moisture content of 1%), shape the granules, and finally add magnesium stearate and perform tableting.

[0030] (3) The coating agent is prepared into a coating solution with a concentration of 15%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0031] Example 2

[0032] A metronidazole tablet is prepared from the following components in parts by weight: 55 parts of metronidazole, 38 parts of a filler, 8 parts of sorbitol, 3 parts of povidone K30, 10 parts of a binder, 0.2 parts of magnesium stearate, and 3 parts of a coating agent.

[0033] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 2:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2:1.

[0034] The preparation method of the metronidazole tablets comprises the following steps:

[0035] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0036] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 55°C (dry to a sample moisture content of 2%), shape the granules, and finally add magnesium stearate and perform tableting.

[0037] (3) The coating agent is prepared into a coating solution with a concentration of 20%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0038] Example 3

[0039] A metronidazole tablet is prepared from the following components in parts by mass: 60 parts of metronidazole, 40 parts of a filler, 10 parts of sorbitol, 5 parts of povidone K30, 15 parts of a binder, 0.5 parts of magnesium stearate, and 6 parts of a coating agent.

[0040] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 1:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2:1.

[0041] The preparation method of the metronidazole tablets comprises the following steps:

[0042] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0043] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 60°C (dry to a sample moisture content of 1%), shape the granules, and finally add magnesium stearate and perform tableting.

[0044] (3) The coating agent is prepared into a coating solution with a concentration of 15%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0045] Example 4

[0046] A metronidazole tablet is prepared from the following components in parts by weight: 58 parts of metronidazole, 35 parts of a filler, 8 parts of sorbitol, 5 parts of povidone K30, 10 parts of a binder, 0.5 parts of magnesium stearate, and 6 parts of a coating agent.

[0047] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 1:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 3:1.

[0048] The preparation method of the metronidazole tablets comprises the following steps:

[0049] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0050] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 60°C (dry to a sample moisture content of 1%), shape the granules, and finally add magnesium stearate and perform tableting.

[0051] (3) The coating agent is prepared into a coating solution with a concentration of 15%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0052] Comparative Example 1

[0053] A metronidazole tablet is prepared from the following components in parts by mass: 55 parts of metronidazole, 38 parts of a filler, 11 parts of sorbitol, 10 parts of a binder, 0.2 parts of magnesium stearate, and 3 parts of a coating agent.

[0054] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 2:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2:1.

[0055] The preparation method of the metronidazole tablets comprises the following steps:

[0056] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0057] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 55°C (dry to a sample moisture content of 2%), shape the granules, and finally add magnesium stearate and perform tableting.

[0058] (3) The coating agent is prepared into a coating solution with a concentration of 20%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0059] Comparative Example 2

[0060] A metronidazole tablet is prepared from the following components in parts by mass: 55 parts of metronidazole, 38 parts of a filler, 11 parts of povidone K30, 10 parts of a binder, 0.2 parts of magnesium stearate, and 3 parts of a coating agent.

[0061] The filler is a mixture of corn starch and calcium hydrogen phosphate in a ratio of 2:1; the binder is a 10wt% aqueous solution of povidone K30; and the coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2:1.

[0062] The preparation method of the metronidazole tablets comprises the following steps:

[0063] (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix;

[0064] (2) Add a binder to the dry mix, add an appropriate amount of water, and perform wet granulation. After granulation, dry at 55°C (dry to a sample moisture content of 2%), shape the granules, and finally add magnesium stearate and perform tableting.

[0065] (3) The coating agent is prepared into a coating solution with a concentration of 20%, and the tablets after tableting are subjected to fluidized bed coating treatment to obtain metronidazole tablets.

[0066] Dissolution testing

[0067] Take the metronidazole tablets prepared in Examples 1 to 4 and Comparative Examples 1 to 2 and test their dissolution properties. The specific steps are as follows:

[0068] According to the Chinese Pharmacopoeia (2010 edition), Part II, Dissolution Methods, Appendix XC, Method 1: 900 mL of hydrochloric acid solution (9→1000) was used as the dissolution medium at 100 rpm. The solution was filtered at 10, 20, 30, 40, and 60 minutes. The filtrate was then analyzed by UV-Vis spectrophotometry according to the Chinese Pharmacopoeia (2010 edition), Part II, Appendix IVA. The test results are shown in Table 1.

[0069] Table 1 Dissolution results

[0070]

[0071] As can be seen from Table 1, the metronidazole tablets prepared using the preparation method of the present invention achieved a dissolution rate of 84% to 88% at 20 minutes. In Comparative Examples 1 and 2, the samples containing sorbitol or povidone K30 alone, while reaching 80% at 20 minutes, were still lower than the dissolution rates of the examples of the present invention. From a long-term perspective, the metronidazole tablets prepared in the examples of the present invention still achieved a higher dissolution rate at 60 minutes than the comparative examples.

[0072] The specific embodiments of the present invention described above do not limit the scope of protection of the present invention. Any other corresponding changes and modifications made based on the technical concept of the present invention should be included in the scope of protection of the claims of the present invention.

Claims

1. A metronidazole tablet, characterized in that The invention is prepared from the following components in parts by weight: 55-60 parts of metronidazole, 35-40 parts of a filler, 5-10 parts of sorbitol, 1-5 parts of povidone K30, 5-15 parts of a binder, 0.2-0.5 parts of magnesium stearate, and 2-6 parts of a coating agent; The filler is a mixture of corn starch and calcium hydrogen phosphate; The mass ratio of the corn starch to calcium hydrogen phosphate is 1-3:1; The coating agent is a mixture of hydroxypropyl methylcellulose and polyvinyl alcohol in a mass ratio of 2 to 3:

1.

2. The metronidazole tablet according to claim 1, wherein The metronidazole tablets are prepared from the following components in parts by mass: 55-60 parts of metronidazole, 38-40 parts of a filler, 8-10 parts of sorbitol, 3-5 parts of povidone K30, 10-15 parts of a binder, 0.2-0.5 parts of magnesium stearate, and 3-6 parts of a coating agent.

3. The metronidazole tablet according to claim 1, wherein The adhesive is a polyvidone K30 aqueous solution with a concentration of 10 wt%.

4. The method for preparing the metronidazole tablets according to any one of claims 1 to 3, wherein The steps include: (1) First, metronidazole, filler, sorbitol and povidone K30 are uniformly mixed according to the mass ratio to obtain a dry mix; (2) Adding a binder to the dry mix and performing wet granulation, drying and sizing the granules after granulation, and finally adding magnesium stearate and performing tableting; (3) The coating agent is prepared into a coating liquid, and the tablets after tableting are coated to obtain metronidazole tablets.

5. The method for preparing metronidazole tablets according to claim 4, wherein The drying temperature in step (2) is 50-60°C.

6. The method for preparing metronidazole tablets according to claim 5, wherein The drying in (2) is to dry the sample until the moisture content is 1-3%; The concentration of the coating solution (3) is 15-25%.

7. The method for preparing metronidazole tablets according to claim 4, wherein: (3) The coating treatment method is fluidized bed coating or spray drying coating.

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