CN110882226A - A kind of furotriptan succinate tablet and preparation method thereof - Google Patents

Abstract

The invention relates to a furotriptan succinate sustained-release tablet and a preparation method thereof, belonging to the technical field of medicines. The furotriptan succinate sustained-release preparation comprises furotriptan succinate, a sustained-release material, a filler, a lubricant and a 95% ethanol solution. Wherein the main component of the furotriptan succinate is a novel anti-migraine drug, belongs to a selective 5-HT1B/1D receptor agonist, and is approved to be marketed in the United states in 2001. The dosage form reduces administration frequency, improves patient compliance, and can maintain effective blood concentration for a long time.

Description

A kind of furotriptan succinate tablet and preparation method thereof

technical field

The invention relates to a drug sustained-release tablet containing furotriptan succinate, belonging to the technical field of medicine. The invention provides a tablet which is safe and effective, has lasting drug effect, stable quality, low cost, convenient administration, strong patient compliance and can treat migraine.

Background technique

Furotriptan succinate, Chinese chemical name: R-(+)3-methylamino-6-carbonamide-1,2,3,4-tetrahydrocarbazole monosuccinate monohydrate, the structural formula is as follows:

Molecular formula: C14H17N3O·C4H6O4·H2O

Molecular weight: 379.4

Furotriptan was developed by the Irish company Elan Pharm acutieallne, and was approved by the US FDA in November 2001 as its succinate (1:1) for the acute treatment of migraine with or without aura. Frova. At present, the product is not registered and marketed in China.

Furotriptan is a new type of anti-migraine drug, which is a selective 5-HT1B/1D receptor agonist. It overcomes the shortcomings of the first-generation 5-HT1B/1D receptor agonists, such as low oral bioavailability, short half-life, and high recurrence rate. Headache has a significant curative effect and has fewer side effects than other drugs. It is foreseeable that the drug has a good market prospect in China, so the industrial development of furotriptan is of great significance.

The applicant screened the matrix sustained-release materials through a large number of experiments. During the screening process, it was unexpectedly found that when the ratio of ethyl cellulose and methyl cellulose of the sustained-release coating material was 2:3, furotriptan succinate It has an unexpected sustained-release effect. On this basis, the experimental design is continuously optimized, and a sustained-release tablet of furotriptan succinate with a sustained-release effect of up to 24 hours is obtained.

SUMMARY OF THE INVENTION

The object of the present invention is to provide a sustained-release tablet of furotriptan succinate with a sustained-release effect of up to 24 hours for the treatment of migraine with or without aura. It can be administered once a day, can maintain the effective blood drug concentration for a long time, and has the advantages of low frequency of administration and few side effects.

The tablet core is a skeleton tablet, including the following components, and its weight composition is:

Furotriptan succinate 200-300 servings

Lactose 6000-9000 servings

Microcrystalline cellulose 2000-3000 servings

Silica 100-150 parts

50-75 servings of sodium carboxymethyl starch

Magnesium Stearate 100-150 servings

The coating layer composed of the coating liquid of the following components is composed by weight:

Sustained release coating material 200-300 copies

Purified water 1200-1800 parts

The sustained-release coating material in the coating layer is 2:3 ethyl cellulose:methyl cellulose.

The preparation method includes the following steps: (1) Preparation of tablet cores: weigh the main drug furotriptan succinate according to the tablet core recipe, pass through an 80-mesh sieve for use; , sodium carboxymethyl starch, for use; mix the main drug with microcrystalline cellulose, silicon dioxide, sodium carboxymethyl starch; mix the mixture evenly with lactose; add the prescribed amount of magnesium stearate and mix well; adjust the tablet weight, press (2) Coating: Weigh the prescribed amount of water in the preparation container, and start the mixer; Weigh the prescribed amount of slow-release coating material and slowly add it to the above preparation container to obtain a uniform Put the tablet core in the coating pot, adjust the appropriate coating pot rotation speed, and carry out film coating, and the tablet core weight can be increased by about 2.0% to 4.0%.

specific implementation

Example 1

The tablet core is a skeleton tablet, including the following components, and its weight composition is:

Furotriptan Succinate 250 servings

Lactose 7500 servings

Microcrystalline Cellulose 2500 servings

Silica 120 parts

60 parts of sodium carboxymethyl starch

Magnesium Stearate 120 servings

The coating layer composed of the coating liquid of the following components is composed by weight:

120 ethyl cellulose

Methylcellulose 180 servings

Purified water 1500 parts.

The preparation method includes the following steps: (1) Preparation of tablet cores: weigh the main drug furotriptan succinate according to the tablet core recipe, pass through an 80-mesh sieve for use; , sodium carboxymethyl starch, for use; mix the main drug with microcrystalline cellulose, silicon dioxide, sodium carboxymethyl starch; mix the mixture evenly with lactose; add the prescribed amount of magnesium stearate and mix well; adjust the tablet weight, press (2) Coating: Weigh the prescribed amount of water in the preparation container, and start the mixer; Weigh the prescribed amount of slow-release coating material and slowly add it to the above preparation container to obtain a uniform Put the tablet core in the coating pan, adjust the appropriate coating pan rotation speed, perform film coating, and wait for the tablet core to increase by 2.0% in weight.

Example 2

The tablet core is a skeleton tablet, including the following components, and its weight composition is:

Furotriptan Succinate 250 servings

Lactose 7000 servings

Microcrystalline Cellulose 2200 servings

Silica 110 parts

55 parts of sodium carboxymethyl starch

Magnesium Stearate 110 servings

The coating layer composed of the coating liquid of the following components is composed by weight:

300 ethyl cellulose

Purified water 1500 parts.

The preparation method includes the following steps: (1) Preparation of tablet cores: weigh the main drug furotriptan succinate according to the tablet core recipe, pass through an 80-mesh sieve for use; , sodium carboxymethyl starch, for use; mix the main drug with microcrystalline cellulose, silicon dioxide, sodium carboxymethyl starch; mix the mixture evenly with lactose; add the prescribed amount of magnesium stearate and mix well; adjust the tablet weight, press (2) Coating: Weigh the prescribed amount of water in the preparation container, and start the mixer; Weigh the prescribed amount of slow-release coating material and slowly add it to the above preparation container to obtain a uniform Put the tablet core in the coating pan, adjust the appropriate coating pan speed, and carry out film coating, and then the tablet core is ready to increase in weight by 3.0%.

Example 3

The tablet core is a skeleton tablet, including the following components, and its weight composition is:

Furotriptan Succinate 250 servings

Lactose 8000 servings

Microcrystalline Cellulose 2800 servings

Silica 140 parts

70 parts of sodium carboxymethyl starch

Magnesium Stearate 140 servings

The coating layer composed of the coating liquid of the following components is composed by weight:

Methylcellulose 300 servings

Purified water 1500 parts.

The preparation method includes the following steps: (1) Preparation of tablet cores: weigh the main drug furotriptan succinate according to the tablet core recipe, pass through an 80-mesh sieve for use; , sodium carboxymethyl starch, for use; mix the main drug with microcrystalline cellulose, silicon dioxide, sodium carboxymethyl starch; mix the mixture evenly with lactose; add the prescribed amount of magnesium stearate and mix well; adjust the tablet weight, press (2) Coating: Weigh the prescribed amount of water in the preparation container, and start the mixer; Weigh the prescribed amount of slow-release coating material and slowly add it to the above preparation container to obtain a uniform : Put the tablet core in the coating pot, adjust the appropriate rotation speed of the coating pot, carry out film coating, and wait for the tablet core to increase by 4.0% in weight.

According to the Chinese Pharmacopoeia 2015 edition, the average cumulative release rate (%) determined by the cup method

The results show that the sustained-release coating materials are ethyl cellulose and methyl cellulose, and the ethyl cellulose: methyl cellulose ratio of 2:3 has the best sustained-release effect.

Claims (3)

1. a sustained-release tablet, comprising a tablet core and a coating, wherein the tablet core is a matrix tablet, comprising the following components, and its weight composition is: Furotriptan succinate 200-300 servings Lactose 6000-9000 servings Microcrystalline cellulose 2000-3000 servings Silica 100-150 parts 50-75 servings of sodium carboxymethyl starch Magnesium Stearate 100-150 servings The coating layer composed of the coating liquid of the following components is composed by weight: Sustained release coating material 200-300 copies Purified water 1200-1800 copies. 2 . The sustained-release tablet of claim 1 , wherein the sustained-release coating material is ethyl cellulose and methyl cellulose, and the ratio of ethyl cellulose:methyl cellulose is 2:3. 3 . 3 . The sustained-release tablet according to claim 1 , wherein the preparation method comprises the following steps: (1) Preparation of tablet cores: take the main drug furotriptan succinate according to the tablet core recipe quantity, and measure the amount of 80 mesh Sieve for later use; Weigh the microcrystalline cellulose, lactose, silicon dioxide, and sodium carboxymethyl starch in the recipe amount, and set aside for later use; mix the main drug with microcrystalline cellulose, silicon dioxide, and sodium carboxymethyl starch; mix the mixture with lactose evenly; add the prescribed amount of magnesium stearate and mix well; adjust the tablet weight, press the tablet to obtain the tablet core; (2) coating: weigh the prescribed amount of water in the preparation container, start the mixer; weigh the prescribed amount of water Slow-release coating material is slowly added to the above preparation container to obtain a uniform suspension coating liquid; the tablet core is placed in the coating pot, the appropriate rotation speed of the coating pot is adjusted, film coating is performed, and the tablets are prepared The core weight increase is about 2.0% to 4.0%.