A kind of pinaverium bromide tablets and preparation method thereof

Abstract

The present invention provides a kind of pinaverium bromide tablets and preparation method thereof, the pinaverium bromide tablets include the following components in mass percentage: pinaverium bromide 35-41%, magnesium stearate 0.1-0.5%, pregelatinized starch 1.2-2.0%, carnauba wax 1.4-2.6%, micropowder silica gel 2.5-4.4%, modified kaolinite 0.4-0.8%, hexadecanol ester wax 0.2-0.5%, filler 7.5-10.4% parts, adhesive 10.3-11.5%, the remainder is a sustained-release material; the sustained-release material is selected from one or more of polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate, and trimethylaminoethyl methacrylate chloride; the filler is selected from microcrystalline cellulose and / or sodium alginate. The pinaverium bromide tablets of the present invention have a good sustained-release effect, reduce the stimulation to the stomach, improve the stability of the pinaverium bromide tablets, and make the effect of treating relevant gastrointestinal diseases better.

Description

Technical Field

[0001] The invention belongs to the technical field of pharmaceuticals, and in particular relates to a pinaverium bromide tablet and a preparation method thereof. Background Art

[0002] Pinaverium bromide is a commonly used drug for gastrointestinal diseases. It is an antispasmodic agent that acts on the gastrointestinal tract and a calcium ion antagonist that works by inhibiting the influx of calcium ions into intestinal smooth muscle. Pinaverium bromide tablets are mainly used to treat pain related to gastrointestinal dysfunction, abnormal bowel movements, gastrointestinal discomfort, etc. They can also be used as preparations for barium enema. Their main functions are to relieve spasms, treat intestinal motility abnormalities, and biliary dysfunction. They are a type of drug that is widely used clinically. Pinaverium bromide tablets have significant side effects and are prone to cause irritating vomiting during medication. The purpose of this study is to provide a pinaverium bromide tablet with a sustained-release effect to reduce the irritation caused by taking the existing pinaverium bromide tablets on the market. Summary of the invention

[0003] The purpose of the present invention is to provide a pinaverium bromide tablet and a preparation method thereof. The prepared pinaverium bromide tablet has a sustained-release effect, can reduce irritation to the stomach, alleviate the side effects of taking, and at the same time improves the stability of the pinaverium bromide tablet, so that the pinaverium bromide tablet has a better effect on treating related gastrointestinal diseases.

[0004] In order to achieve the above object, the present invention provides the following technical solutions:

[0005] A pinaverium bromide tablet comprises the following components in percentage by mass: 35-41% of pinaverium bromide, 0.1-0.5% of magnesium stearate, 1.2-2.0% of pregelatinized starch, 1.4-2.6% of carnauba wax, 2.5-4.4% of micropowdered silica gel, 0.4-0.8% of modified kaolinite, 0.2-0.5% of hexadecanol wax, 7.5-10.4% of filler, 10.3-11.5% of binder, and the balance is sustained-release material; wherein the sustained-release material is selected from one or more of polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate, and trimethylaminoethyl methacrylate chloride; and the filler is selected from microcrystalline cellulose and / or sodium alginate.

[0006] Furthermore, the sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate in a mass ratio of (1.5-1.7):1:(2.2-2.6):(0.3-0.8).

[0007] Furthermore, the preparation method of the modified kaolinite is: add 45-50 parts by weight of kaolinite into water for dispersion, continue to add 14-18 parts by weight of polyethylene glycol, 2-5 parts of microcrystalline cellulose, 5-9 parts of talc and 4-6 parts of montmorillonite, heat to 55-58°C, stir for 2-3h, centrifuge, dry and crush to obtain the modified kaolinite.

[0008] Furthermore, the polyethylene glycol is selected from one or more of polyethylene glycol 800, polyethylene glycol 1000, and polyethylene glycol 2000.

[0009] Furthermore, the polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 2-5: 1:0.4-0.8.

[0010] Furthermore, the particle size of the kaolinite is 0.2-0.5 microns.

[0011] Furthermore, the adhesive is a 2wt%-4wt% aqueous solution of povidone K30.

[0012] Furthermore, the filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:2-4.

[0013] The present invention also provides a preparation method of the pinaverium bromide tablets, which specifically comprises the following steps: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and crushing machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, and placing in a hot air oven for drying to obtain the pinaverium bromide tablets.

[0014] Furthermore, the temperature in the hot air oven is set at 50-55°C, and the drying time is 30-40 minutes.

[0015] Compared with the prior art, the advantages and beneficial effects of the present invention are as follows: the present invention provides a pinaverium bromide tablet and a preparation method thereof; polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a specific ratio are added to the system of the present invention so that the pinaverium bromide tablet has an excellent sustained-release effect; at the same time, the specific modified kaolinite of the present invention is added to improve the compatibility of the system and to achieve a synergistic effect with the other components, thereby improving the stability and sustained-release effect of the pinaverium bromide tablet; the preparation method of the present invention has a simple process, and the prepared pinaverium bromide tablet has high stability and a good sustained-release effect. DETAILED DESCRIPTION

[0016] The technical solutions in the embodiments of the present invention are described clearly and completely below. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0017] Example 1

[0018] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.3% magnesium stearate, 1.7% pregelatinized starch, 2.2% carnauba wax, 3.1% micropowder silica gel, 0.7% modified kaolinite, 0.4% cetyl alcohol wax, 8.5% filler, 10.6% binder, and the balance is sustained-release material.

[0019] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0020] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talc and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0021] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0022] The particle size of the kaolinite is 0.2-0.5 microns.

[0023] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0024] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0025] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0026] Example 2

[0027] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.1% magnesium stearate, 1.2% pregelatinized starch, 1.4% carnauba wax, 2.5% micropowder silica gel, 0.4% modified kaolinite, 0.2% cetyl alcohol wax, 7.5% filler, 10.3% binder, and the balance is sustained-release material.

[0028] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0029] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talc and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0030] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0031] The particle size of the kaolinite is 0.2-0.5 microns.

[0032] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0033] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0034] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0035] Example 3

[0036] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.5% magnesium stearate, 2.0% pregelatinized starch, 2.6% carnauba wax, 4.4% micropowder silica gel, 0.8% modified kaolinite, 0.5% cetyl alcohol wax, 10.4% filler, 11.5% binder, and the balance is sustained-release material.

[0037] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0038] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talcum powder and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0039] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0040] The particle size of the kaolinite is 0.2-0.5 microns.

[0041] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0042] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0043] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0044] Example 4

[0045] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.1% magnesium stearate, 2.0% pregelatinized starch, 1.4% carnauba wax, 4.4% micropowder silica gel, 0.4% modified kaolinite, 0.5% cetyl alcohol wax, 7.5% filler, 11.5% binder, and the balance is sustained-release material.

[0046] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0047] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talcum powder and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0048] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0049] The particle size of the kaolinite is 0.2-0.5 microns.

[0050] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0051] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0052] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0053] Example 5

[0054] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.2% magnesium stearate, 1.8% pregelatinized starch, 1.6% carnauba wax, 4.2% micropowder silica gel, 0.5% modified kaolinite, 0.4% cetyl alcohol wax, 10.1% filler, 11.2% binder, and the balance is sustained-release material.

[0055] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0056] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talcum powder and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0057] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0058] The particle size of the kaolinite is 0.2-0.5 microns.

[0059] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0060] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0061] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0062] Example 6

[0063] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.3% magnesium stearate, 1.5% pregelatinized starch, 1.7% carnauba wax, 2.9% micropowder silica gel, 0.8% modified kaolinite, 0.2% cetyl alcohol wax, 10.4% filler, 11% binder, and the balance is sustained-release material.

[0064] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.5:1:2.6:0.8.

[0065] The preparation method of the modified kaolinite is as follows: 45 parts by weight of kaolinite is added into water for dispersion, 14 parts by weight of polyethylene glycol, 5 parts of microcrystalline cellulose, 5 parts of talc and 6 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0066] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 2: 1: 0.8.

[0067] The particle size of the kaolinite is 0.2-0.5 microns.

[0068] The adhesive is a 2 wt % polyvidone K30 aqueous solution.

[0069] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:4.

[0070] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 50°C, and drying time for 40 minutes, to obtain pinaverium bromide tablets.

[0071] Example 7

[0072] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.3% magnesium stearate, 1.7% pregelatinized starch, 2.2% carnauba wax, 3.1% micropowder silica gel, 0.7% modified kaolinite, 0.4% cetyl alcohol wax, 8.5% filler, 10.6% binder, and the balance is sustained-release material.

[0073] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate in a mass ratio of 1.7:1:2.4:0.5.

[0074] The preparation method of the modified kaolinite is as follows: 49 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 7 parts of talc and 5 parts of montmorillonite are added, the temperature is raised to 57° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0075] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1: 0.8.

[0076] The particle size of the kaolinite is 0.2-0.5 microns.

[0077] The adhesive is a 3.5 wt % aqueous solution of povidone K30.

[0078] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.4.

[0079] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 50°C, and drying time for 40 minutes, to obtain pinaverium bromide tablets.

[0080] Example 8

[0081] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 37% pinaverium bromide, 0.2% magnesium stearate, 1.6% pregelatinized starch, 2.4% carnauba wax, 3.7% micro powder silica gel, 0.7% modified kaolinite, 0.2% cetyl alcohol wax, 10% filler, 11% binder, and the balance is sustained-release material.

[0082] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.7:1:2.3:0.6.

[0083] The preparation method of the modified kaolinite is as follows: 49 parts by weight of kaolinite is added to water for dispersion, 15 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talc and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0084] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.7.

[0085] The particle size of the kaolinite is 0.2-0.5 microns.

[0086] The adhesive is a 3.4 wt % aqueous solution of povidone K30.

[0087] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:2.8.

[0088] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 30 minutes, to obtain pinaverium bromide tablets.

[0089] Example 9

[0090] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.5% magnesium stearate, 1.2% pregelatinized starch, 2.6% carnauba wax, 2.5% micropowder silica gel, 0.7% modified kaolinite, 0.3% cetyl alcohol wax, 9.9% filler, 11.2% binder, and the balance is sustained-release material.

[0091] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.3:0.7.

[0092] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 3 parts of microcrystalline cellulose, 8 parts of talc and 5 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0093] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 4: 1:0.6.

[0094] The particle size of the kaolinite is 0.2-0.5 microns.

[0095] The adhesive is a 3 wt % aqueous solution of povidone K30.

[0096] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0097] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0098] Example 10

[0099] The present embodiment provides a pinaverium bromide tablet, which includes the following components in percentage by mass: 40% pinaverium bromide, 0.3% magnesium stearate, 1.7% pregelatinized starch, 2.2% carnauba wax, 3.1% micropowder silica gel, 0.7% modified kaolinite, 0.4% cetyl alcohol wax, 8.5% filler, 11.1% binder, and the balance is sustained-release material.

[0100] The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of 1.6:1:2.5:0.6.

[0101] The preparation method of the modified kaolinite is as follows: 48 parts by weight of kaolinite is added to water for dispersion, 16 parts by weight of polyethylene glycol, 5 parts of microcrystalline cellulose, 8 parts of talc and 4 parts of montmorillonite are added, the temperature is raised to 55° C., stirred for 3 hours, centrifuged, dried and crushed to obtain the modified kaolinite.

[0102] The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 5: 1:0.5.

[0103] The particle size of the kaolinite is 0.2-0.5 microns.

[0104] The adhesive is a 3.2 wt % aqueous solution of povidone K30.

[0105] The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:3.

[0106] The preparation method of the pinaverium bromide tablets is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and crushing them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing them in a hot air oven for drying, setting the temperature in the hot air oven to 55°C, and drying time for 35 minutes, to obtain pinaverium bromide tablets.

[0107] Comparative Example 1

[0108] The difference between this comparative example and Example 1 is: a pinaverium bromide tablet, which includes the following components in mass percentage: 40% pinaverium bromide, 0.7% magnesium stearate, 0.5% pregelatinized starch, 1.2% carnauba wax, 2.0% micropowder silica gel, 1.5% modified kaolinite, 0.7% cetyl alcohol wax, 11.5% filler, 9.6% binder, and the balance is sustained-release material.

[0109] Comparative Example 2

[0110] The difference between this comparative example and Example 1 is: a pinaverium bromide tablet, which includes the following components in mass percentage: 40% pinaverium bromide, 0.7% magnesium stearate, 2.8% pregelatinized starch, 2.9% carnauba wax, 4.7% micropowder silica gel, 0.2% modified kaolinite, 0.9% cetyl alcohol wax, 3.6% filler, 5.6% binder, and the balance is sustained-release material.

[0111] Comparative Example 3

[0112] The difference between this comparative example and Example 1 is that the sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate in a mass ratio of 1:1:(1:1.

[0113] Comparative Example 4

[0114] The difference between this comparative example and Example 1 is that the sustained-release material is polyvinyl alcohol (M W 10000), hydroxypropyl methylcellulose K15M, dibutyl sebacate and povidone K30.

[0115] Comparative Example 5

[0116] The difference between this comparative example and Example 1 is that the preparation method of the modified kaolinite is: 50 parts by weight of kaolinite is added to water for dispersion, 12 parts by weight of polyethylene glycol 1000 is added, the temperature is raised to 55° C., stirred for 2-3 hours, centrifuged, dried, and crushed to obtain the modified kaolinite.

[0117] Comparative Example 6

[0118] The difference between this comparative example and Example 1 is that the kaolinite is not modified.

[0119] Comparative Example 7

[0120] The difference between this comparative example and Example 1 is that the polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 1: 1: 1. The particle size of the kaolinite is 0.6-1.2 μm.

[0121] Performance Testing

[0122] 1. With reference to the "Dissolution and Release Determination Method" of the "Chinese Pharmacopoeia 2015 Edition", the dissolution of the pinaverium bromide tablets of Examples 1-10 and Comparative Examples 1-7 and the commercially available pinaverium bromide tablets (Desuter) was determined, and the calculation formula was: (dissolved mass ÷ total amount of drug) × 100%, the dissolution medium was 0.1 mol / L hydrochloric acid solution (0.3% sodium dodecyl sulfate) (simulating the drug release environment in gastric fluid), and each sample was sampled at 1h, 8h, 16h, and 24h. The results are shown in Table 1. In the table, / represents that no detection is performed at this time point.

[0123] Table 1 Dissolution of Pinaverium Bromide Tablets (%)

[0124]

[0125] 2. The pinaverium bromide tablets of Examples 1-10 and Comparative Examples 1-7 were opened and placed at a temperature of 40±2°C for 90 days. Samples were taken on the 0th day, the 30th day, the 60th day and the 90th day, respectively. The content of pinaverium bromide in the pinaverium bromide tablets was determined by HPLC, and the mass percentage of pinaverium bromide in the pinaverium bromide tablets was calculated by the calculation formula (mass of pinaverium bromide ÷ total amount of drug) × 100%. The results are shown in Table 2.

[0126] Table 2 Content of Pinaverium Bromide in Pinaverium Bromide Tablets (%)

[0127]

[0128] The above is a preferred embodiment of the present invention. It should be pointed out that for ordinary technicians in this technical field, several improvements and modifications can be made without departing from the principles of the present invention. These improvements and modifications should also be regarded as the scope of protection of the present invention.

Claims

1. A pinaverium bromide tablet, characterized in that: The pinaverium bromide tablets include the following components in percentage by mass: 35-41% pinaverium bromide, 0.1-0.5% magnesium stearate, 1.2-2.0% pregelatinized starch, 1.4-2.6% carnauba wax, 2.5-4.4% micropowder silica gel, 0.4-0.8% modified kaolinite, 0.2-0.5% cetyl alcohol wax, 7.5-10.4% filler, 10.3-11.5% binder, and the balance is sustained-release material; The sustained-release material is polyacrylic acid resin IV, hydroxypropyl methylcellulose K4M, dibutyl sebacate and trimethylaminoethyl methacrylate chloride in a mass ratio of (1.5-1.7):1:(2.2-2.6):(0.3-0.8); The preparation method of the modified kaolinite is as follows: 45-50 parts by weight of kaolinite is added to water for dispersion, 14-18 parts by weight of polyethylene glycol, 2-5 parts of microcrystalline cellulose, 5-9 parts of talc and 4-6 parts of montmorillonite are added, the temperature is raised to 55-58° C., stirred for 2-3 hours, centrifuged, dried and crushed to obtain the modified kaolinite; The filler is microcrystalline cellulose and sodium alginate in a mass ratio of 1:2-4.

2. A Pinaverium Bromide Tablet according to claim 1, characterized in that, The polyethylene glycol is selected from one or more of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000.

3. A Pinaverium Bromide Tablet according to claim 2, characterized in that, The polyethylene glycol is a compound of polyethylene glycol 800, polyethylene glycol 1000 and polyethylene glycol 2000 in a mass ratio of 2-5:1:0.4-0.

8.

4. A Pinaverium Bromide Tablet according to claim 3, characterized in that, The particle size of the kaolinite is 0.2-0.5 microns.

5. A Pinaverium Bromide Tablet according to claim 1, characterized in that, The adhesive is a 2wt%-4wt% aqueous solution of povidone K30.

6. The method for preparing the Pinaverium Bromide Tablets according to any one of claims 1 to 5, characterized in that: The preparation method is specifically as follows: taking a prescribed amount of pinaverium bromide and other solid raw materials, mixing and grinding them into fine powder in a mixing and grinding machine, and all of them are sieved through a No. 5 sieve; continuing to add the remaining raw materials, mixing and granulating, placing in a hot air oven for drying, and obtaining pinaverium bromide tablets.

7. The method for preparing Pinaverium Bromide Tablets according to claim 6, characterized in that: The temperature in the hot air oven is set to 50-55°C and the drying time is 30-40 minutes.

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