CN110882226A - Frovatriptan succinate tablet and preparation method thereof - Google Patents
Frovatriptan succinate tablet and preparation method thereof Download PDFInfo
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- CN110882226A CN110882226A CN201911264647.4A CN201911264647A CN110882226A CN 110882226 A CN110882226 A CN 110882226A CN 201911264647 A CN201911264647 A CN 201911264647A CN 110882226 A CN110882226 A CN 110882226A
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- tablet
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- release
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
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
Technical Field
The invention relates to a medicine sustained-release tablet containing furotriptan succinate, belonging to the technical field of medicines. The tablet provided by the invention is safe and effective, has lasting drug effect, stable quality, low cost, convenient administration and strong patient compliance, and can treat migraine.
Background
Furotriptan succinate, Chinese cultural name: r- (+) -3-methylamino-6-carboxamide-1, 2,3, 4-tetrahydrocarbazole monosuccinate monohydrate, the structural formula is as follows:
the molecular formula is as follows: C14H17N 3O. C4H6O 4. H2O
Molecular weight: 379.4
Frovatriptan was developed by Elan Pharm acutiallene, Ireland, and was approved by the U.S. FDA in 11 months of 2001 for marketing in its succinate (1: 1) form for acute treatment of migraine with or without aura, under the trade name Frova. The product is not currently registered in China for sale.
Frovatriptan is a novel anti-migraine drug, and belongs to a selective 5-HT1B/1D receptor agonist. The medicine overcomes the defects of low oral bioavailability, short half-life period and high recurrence rate of the first generation 5-HT1B/1D receptor agonist, is an effective treatment medicine for adult moderate or severe migraine attack, has obvious curative effect on preventing menstrual migraine and less side effect than other medicines, and can be expected to have good market prospect in China, so that the industrial development of furotriptan has great significance.
The applicant screens the skeleton slow-release material through a large number of experiments, and in the screening process, the proportion of ethyl cellulose and methyl cellulose of the slow-release coating material is found to be 2: and 3, the sustained release effect on the furaltriptan succinate is unexpected, and on the basis, the experimental design is continuously optimized, so that the furaltriptan succinate sustained release tablet with the sustained release effect reaching 24 hours is obtained.
Disclosure of Invention
The invention aims to provide a furotriptan succinate sustained-release tablet with sustained-release effect reaching 24 hours, which is used for treating migraine with or without aura. Can be taken once a day, can keep effective blood concentration for a long time, and has the advantages of low administration frequency and less side effect.
The tablet core is a matrix tablet and comprises the following components in parts by weight:
frovatriptan succinate 200-300 parts
9000 portions of 6000-lactose-
3000 portions of microcrystalline cellulose 2000-
100 parts of silicon dioxide
50-75 parts of sodium carboxymethyl starch
Magnesium stearate 100-150 parts
The coating layer comprises the following coating liquid components in parts by weight:
200 portions and 300 portions of slow-release coating material
Purified water 1200-1800 parts
The slow-release coating material in the coating layer is ethyl cellulose: the methylcellulose is 2: 3.
the preparation method comprises the following steps: (1) preparation of a tablet core: weighing the main drug furotriptan succinate according to the prescription of the tablet core, and sieving the furotriptan succinate with a 80-mesh sieve for later use; weighing microcrystalline cellulose, lactose, silicon dioxide and carboxymethyl starch sodium according to the prescription amount for later use; mixing the main drug with microcrystalline cellulose, silicon dioxide and carboxymethyl starch sodium; mixing the mixture with lactose; adding magnesium stearate in a prescription amount and mixing uniformly; adjusting the weight of the tablet, and tabletting to obtain a tablet core; (2) coating: weighing a prescription amount of water in a preparation container, and starting a stirrer; weighing a formula amount of slow-release coating material, slowly adding into the preparation container to obtain a uniform suspension coating solution; and (3) putting the tablet cores into a coating pan, adjusting the rotating speed of the coating pan, and performing film coating until the weight of the tablet cores is increased by about 2.0-4.0%.
Detailed Description
Example 1
The tablet core is a matrix tablet and comprises the following components in parts by weight:
frovatriptan succinate 250 parts
7500 parts of lactose
2500 parts of microcrystalline cellulose
120 parts of silicon dioxide
60 parts of sodium carboxymethyl starch
120 parts of magnesium stearate
The coating layer comprises the following coating liquid components in parts by weight:
ethyl cellulose 120 parts
180 portions of methyl cellulose
1500 parts of purified water.
The preparation method comprises the following steps: (1) preparation of a tablet core: weighing the main drug furotriptan succinate according to the prescription of the tablet core, and sieving the furotriptan succinate with a 80-mesh sieve for later use; weighing microcrystalline cellulose, lactose, silicon dioxide and carboxymethyl starch sodium according to the prescription amount for later use; mixing the main drug with microcrystalline cellulose, silicon dioxide and carboxymethyl starch sodium; mixing the mixture with lactose; adding magnesium stearate in a prescription amount and mixing uniformly; adjusting the weight of the tablet, and tabletting to obtain a tablet core; (2) coating: weighing a prescription amount of water in a preparation container, and starting a stirrer; weighing a formula amount of slow-release coating material, slowly adding into the preparation container to obtain a uniform suspension coating solution; and (3) putting the tablet cores into a coating pan, adjusting the rotating speed of the coating pan appropriately, and performing film coating until the weight of the tablet cores is increased by 2.0%.
Example 2
The tablet core is a matrix tablet and comprises the following components in parts by weight:
frovatriptan succinate 250 parts
Lactose 7000 parts
2200 parts of microcrystalline cellulose
110 parts of silicon dioxide
55 parts of sodium carboxymethyl starch
110 parts of magnesium stearate
The coating layer comprises the following coating liquid components in parts by weight:
ethyl cellulose 300 parts
1500 parts of purified water.
The preparation method comprises the following steps: (1) preparation of a tablet core: weighing the main drug furotriptan succinate according to the prescription of the tablet core, and sieving the furotriptan succinate with a 80-mesh sieve for later use; weighing microcrystalline cellulose, lactose, silicon dioxide and carboxymethyl starch sodium according to the prescription amount for later use; mixing the main drug with microcrystalline cellulose, silicon dioxide and carboxymethyl starch sodium; mixing the mixture with lactose; adding magnesium stearate in a prescription amount and mixing uniformly; adjusting the weight of the tablet, and tabletting to obtain a tablet core; (2) coating: weighing a prescription amount of water in a preparation container, and starting a stirrer; weighing a formula amount of slow-release coating material, slowly adding into the preparation container to obtain a uniform suspension coating solution; and (3) putting the tablet cores into a coating pan, adjusting the rotating speed of the coating pan, and performing film coating until the weight of the tablet cores is increased by 3.0%.
Example 3
The tablet core is a matrix tablet and comprises the following components in parts by weight:
frovatriptan succinate 250 parts
8000 parts of lactose
2800 parts of microcrystalline cellulose
140 parts of silicon dioxide
70 portions of sodium carboxymethyl starch
140 parts of magnesium stearate
The coating layer comprises the following coating liquid components in parts by weight:
300 portions of methyl cellulose
1500 parts of purified water.
The preparation method comprises the following steps: (1) preparation of a tablet core: weighing the main drug furotriptan succinate according to the prescription of the tablet core, and sieving the furotriptan succinate with a 80-mesh sieve for later use; weighing microcrystalline cellulose, lactose, silicon dioxide and carboxymethyl starch sodium according to the prescription amount for later use; mixing the main drug with microcrystalline cellulose, silicon dioxide and carboxymethyl starch sodium; mixing the mixture with lactose; adding magnesium stearate in a prescription amount and mixing uniformly; adjusting the weight of the tablet, and tabletting to obtain a tablet core; (2) coating: weighing a prescription amount of water in a preparation container, and starting a stirrer; weighing a formula amount of slow-release coating material, slowly adding into the preparation container to obtain a uniform suspension coating solution; : and (3) putting the tablet cores into a coating pan, adjusting the rotating speed of the coating pan appropriately, and performing film coating until the weight of the tablet cores is increased by 4.0%.
Average cumulative release (%), determined by the cup method according to the Chinese pharmacopoeia 2015 edition
The results show that the slow-release coating materials are ethyl cellulose and methyl cellulose, and the weight ratio of ethyl cellulose: the methylcellulose is 2: 3, the best slow release effect is achieved.
Claims (3)
1. A sustained release tablet comprises a tablet core and a coating, wherein the tablet core is a framework tablet and comprises the following components by weight:
frovatriptan succinate 200-300 parts
9000 portions of 6000-lactose-
3000 portions of microcrystalline cellulose 2000-
100 parts of silicon dioxide
50-75 parts of sodium carboxymethyl starch
Magnesium stearate 100-150 parts
The coating layer comprises the following coating liquid components in parts by weight:
200 portions and 300 portions of slow-release coating material
Purified water 1200 + 1800 parts.
2. The extended release tablet of claim 1, wherein the extended release coating material is ethyl cellulose and methyl cellulose, and the ratio of ethyl cellulose: the methylcellulose is 2: 3.
3. the sustained-release tablet of claim 1, wherein the preparation method comprises the steps of: (1) preparation of a tablet core: weighing the main drug furotriptan succinate according to the prescription of the tablet core, and sieving the furotriptan succinate with a 80-mesh sieve for later use; weighing microcrystalline cellulose, lactose, silicon dioxide and carboxymethyl starch sodium according to the prescription amount for later use; mixing the main drug with microcrystalline cellulose, silicon dioxide and carboxymethyl starch sodium; mixing the mixture with lactose; adding magnesium stearate in a prescription amount and mixing uniformly; adjusting the weight of the tablet, and tabletting to obtain a tablet core; (2) coating: weighing a prescription amount of water in a preparation container, and starting a stirrer; weighing a formula amount of slow-release coating material, slowly adding into the preparation container to obtain a uniform suspension coating solution; and (3) putting the tablet cores into a coating pan, adjusting the rotating speed of the coating pan, and performing film coating until the weight of the tablet cores is increased by about 2.0-4.0%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911264647.4A CN110882226A (en) | 2019-12-11 | 2019-12-11 | Frovatriptan succinate tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911264647.4A CN110882226A (en) | 2019-12-11 | 2019-12-11 | Frovatriptan succinate tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN110882226A true CN110882226A (en) | 2020-03-17 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201911264647.4A Withdrawn CN110882226A (en) | 2019-12-11 | 2019-12-11 | Frovatriptan succinate tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN110882226A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111544394A (en) * | 2020-05-08 | 2020-08-18 | 正大制药（青岛）有限公司 | Frovatriptan succinate particle for treating migraine |
| CN116211817A (en) * | 2023-02-21 | 2023-06-06 | 正大制药（青岛）有限公司 | Fusartriptan succinate tablet and preparation process thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6306436B1 (en) * | 2000-04-28 | 2001-10-23 | Teva Pharmaceuticals Usa, Inc. | Stabilized, acid-free formulation for sustained release of bupropion hydrochloride |
| CN104758268A (en) * | 2015-04-22 | 2015-07-08 | 青岛正大海尔制药有限公司 | Frovatriptan succinate tablet and preparation method thereof |
| CN104800184A (en) * | 2015-04-22 | 2015-07-29 | 青岛正大海尔制药有限公司 | Slow-release tablet comprising succinate frovatriptan |
-
2019
- 2019-12-11 CN CN201911264647.4A patent/CN110882226A/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6306436B1 (en) * | 2000-04-28 | 2001-10-23 | Teva Pharmaceuticals Usa, Inc. | Stabilized, acid-free formulation for sustained release of bupropion hydrochloride |
| CN104758268A (en) * | 2015-04-22 | 2015-07-08 | 青岛正大海尔制药有限公司 | Frovatriptan succinate tablet and preparation method thereof |
| CN104800184A (en) * | 2015-04-22 | 2015-07-29 | 青岛正大海尔制药有限公司 | Slow-release tablet comprising succinate frovatriptan |
Non-Patent Citations (1)
| Title |
|---|
| 郑俊民，: "《药用高分子材料学》", 30 April 1993, 中国医药科技出版社， * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111544394A (en) * | 2020-05-08 | 2020-08-18 | 正大制药（青岛）有限公司 | Frovatriptan succinate particle for treating migraine |
| CN116211817A (en) * | 2023-02-21 | 2023-06-06 | 正大制药（青岛）有限公司 | Fusartriptan succinate tablet and preparation process thereof |
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| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20200317 |
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| WW01 | Invention patent application withdrawn after publication |