CN110934843A - Frovatriptan succinate tablet and preparation method thereof - Google Patents
Frovatriptan succinate tablet and preparation method thereof Download PDFInfo
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- CN110934843A CN110934843A CN201911264663.3A CN201911264663A CN110934843A CN 110934843 A CN110934843 A CN 110934843A CN 201911264663 A CN201911264663 A CN 201911264663A CN 110934843 A CN110934843 A CN 110934843A
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- enteric
- succinate
- furotriptan
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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
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- 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
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- 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
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
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- 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
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Pain & Pain Management (AREA)
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- General Chemical & Material Sciences (AREA)
Abstract
The invention discloses a furotriptan succinate enteric-coated tablet and a preparation method thereof. The invention can improve the bioavailability of the furotriptan succinate and reduce the stimulation of the medicament to gastric mucosa, and has simple preparation process, stable quality of the obtained product and suitability for large-scale production.
Description
Technical Field
The invention relates to a western medicine preparation technology, in particular to a furotriptan succinate enteric-coated tablet, and also relates to a preparation method of the enteric-coated tablet, belonging to the technical field of medicines.
Background
Migraine is a common chronic neurovascular disease, the most common primary headache type in clinic, the disease is mostly caused in children and adolescence, the peak of the disease occurs in middle and young age, women are common, the prevalence rate is 5% -10% in people, and the genetic background is common. Migraine is primarily caused by dysfunction of the central nervous system, while vascular changes are secondary, with migraine attacks accompanied by numerous neuromediator disturbances in the blood and cerebrospinal fluid. The recent attention paid to the theory of trigeminal vasoreflexion is the combination of nerves, blood vessels and neuromediators, which are integrated into the trigeminal vascular system. This hypothesis suggests that by stimulating certain specific areas in the brain, a series of reactions cause cranial vasodilation and carotid vasodilation, resulting in headache. In this process, 5-HT released by platelets enhances the sensitivity of vascular receptors and plays an important role in pain production. This hypothesis better explains some of the clinical manifestations of migraine, providing a reasonable explanation for the use of drugs acting on both the central and peripheral nervous systems for the treatment of migraine.
Frovatriptan succinate is an isolated cerebral vasoconstrictor, and the activity of Frovatriptan succinate as a vasoconstrictor was observed on isolated arterial vessels and compared with sumatriptan. In the middle cerebral artery of the human brain, furotriptan succinate is a partial agonist (relative to 5-HT) and has at least a 5-fold effect as compared to sumatriptan. Furotriptan succinate is a full agonist for the human basal artery, with about 8.3 times the effect of sumatriptan. Furotriptan succinate had 23 and 3 times greater effect on rabbit basal arteries and cat middle cerebral arteries than sumatriptan, respectively.
Enteric formulations are those which release no or little drug in a defined acidic medium, but release most or all of the drug in a phosphate buffered solution at ph6.8 for the required period of time. The enteric-coated tablet is one of enteric-coated preparations, can prevent the drug from being damaged by enzymes in the stomach or gastric acid, prevent the drug from stimulating the gastric mucosa, provide the effect of delaying release, transfer the drug mainly absorbed by the small intestine to the part as much as possible at the highest concentration, and is favorable for improving the bioavailability.
Disclosure of Invention
In order to overcome the defects of the prior art and research and develop an enteric-coated tablet with stable quality and simple preparation process, the invention provides the furotriptan succinate enteric-coated tablet through screening of auxiliary materials and process optimization by a large number of tests, and the enteric-coated tablet has stable quality, high bioavailability and simple preparation process.
In order to achieve the purpose, the invention adopts the technical scheme that:
a furotriptan succinate enteric-coated tablet comprises furotriptan succinate, a filler, a disintegrant, an enteric material, a plasticizer and a lubricant, and is characterized in that the furotriptan succinate enteric-coated tablet comprises the following components in percentage by weight:
15-25% of furotriptan succinate
40 to 50 percent of filling agent
5 to 10 percent of disintegrating agent
Enteric material 15-25%
3 to 8 percent of plasticizer
3-8% of lubricant.
Preferably, the content of each component is as follows according to weight percentage:
frovatriptan succinate 20%
45 percent of filler
7 percent of disintegrating agent
Enteric-coated material 20%
Plasticizer 5%
3% of lubricant.
Wherein the filler is microcrystalline cellulose; the disintegrant is croscarmellose sodium; the enteric material is one or more of phthalic acid cellulose acetate, hydroxypropyl methyl cellulose titanate or acrylic resin II; the plasticizer is trioctyl citrate; the lubricant is magnesium stearate.
Wherein, the enteric material is preferably cellulose acetate phthalate and hydroxypropyl methyl cellulose titanate; preferably, the weight ratio of the cellulose acetate phthalate to the hydroxypropyl methylcellulose titanate is 2: 1.
The furotriptan succinate enteric-coated tablet can be prepared by the following method:
(1) uniformly mixing the furotriptan succinate, the filler and the disintegrant according to the weight percentage, granulating by taking absolute ethyl alcohol as a bonding agent and a sieve with 50-100 meshes, drying and tabletting to obtain a furotriptan succinate tablet core;
(2) dissolving the enteric material, the plasticizer and the lubricant by 80 percent ethanol to prepare enteric coating liquid;
(3) and (3) uniformly spraying the prepared enteric coating solution in the step (2) on the surface of the furatriptan succinate tablet core prepared in the step (1), and drying to obtain the furatriptan succinate enteric-coated tablet.
The furotriptan succinate enteric-coated tablet provided by the invention has the following beneficial effects:
(1) the quality is stable, the stimulation of the medicine to gastric mucosa can be reduced, the enteric effect is ideal, and the bioavailability is improved;
(2) the selected auxiliary materials are common, the preparation process is simple, the obtained product has stable quality, and the method is suitable for large-scale production.
Detailed Description
The following further describes the embodiments of the present invention with reference to examples, but these examples are only illustrative and do not limit the scope of the present invention. It will be understood by those skilled in the art that various changes in form and details may be made therein without departing from the spirit and scope of the invention, and that such changes and modifications may be made without departing from the spirit and scope of the invention.
A preparation method of furotriptan succinate enteric-coated tablets comprises the following steps:
(1) uniformly mixing the furotriptan succinate, the filler and the disintegrant according to the weight percentage, granulating by taking absolute ethyl alcohol as a bonding agent and a sieve with 50-100 meshes, drying and tabletting to obtain a furotriptan succinate tablet core;
(2) dissolving the enteric material, the plasticizer and the lubricant by 80 percent ethanol to prepare enteric coating liquid;
(3) and (3) uniformly spraying the prepared enteric coating solution in the step (2) on the surface of the furatriptan succinate tablet core prepared in the step (1), and drying to obtain the furatriptan succinate enteric-coated tablet.
Examples 1-6 preparation of Furotriptan succinate enteric-coated tablets
Preparing the furotriptan succinate enteric-coated tablet according to the preparation method and the raw and auxiliary materials in the following formula. Where "/" indicates unused.
Test example 1 dissolution rate measurement of Frovatriptan succinate enteric-coated tablets obtained in examples 1 to 6
According to the guidance principle of slow-release, controlled-release and delayed-release preparations of 9013 in 2015 th four-part general rule, a proper amount (about 100 mg) of furaltriptan succinate enteric-coated tablets prepared in examples 1-6 are respectively and precisely weighed by using artificial gastric juice with pH1.2 and artificial intestinal juice medium with pH6.8, and the dissolution rate is measured according to 0931 in 2015 th four-part general rule in china pharmacopoeia. The results are shown in tables 1 and 2.
As can be seen from Table 1, the furotriptan succinate enteric-coated tablets prepared in examples 1 to 6 are slowly dissolved out in artificial gastric juice with a pH of 1.2, and only 10.3% of the dissolution is carried out in 4 hours at most, so that the furotriptan succinate enteric-coated tablets have better acid resistance; wherein the dissolution of the furotriptan succinate enteric-coated tablet of example 4 is minimum in 4h, which shows that the furotriptan succinate enteric-coated tablet prepared by using cellulose acetate phthalate and hydroxypropyl methyl cellulose titanate as enteric-coated materials has the best acid resistance.
As can be seen from Table 2, the Frovatriptan succinate enteric-coated tablets prepared in examples 1-6 are rapidly released in the artificial intestinal juice with pH of 6.8, and can achieve the purpose of quick release; the dissolution rate of the furotriptan succinate enteric-coated tablet in example 4 is highest at 60min, which shows that the furotriptan succinate enteric-coated tablet prepared by using cellulose acetate phthalate and hydroxypropyl methyl cellulose titanate as enteric-coated materials has the best release effect in the intestinal tract.
EXAMPLE 7-11 preparation of Furotriptan succinate enteric-coated tablet
Preparing the furotriptan succinate enteric-coated tablet according to the preparation method and the raw and auxiliary materials in the following formula.
TEST EXAMPLE 2 dissolution test of Furotriptan succinate enteric-coated tablets obtained in examples 7-11
The measurement method was the same as in test example 1, and the measurement results are shown in tables 3 and 4.
As can be seen from table 3, the furotriptan succinate enteric-coated tablet of example 8 dissolves most slowly in artificial gastric juice at ph1.2, which indicates that when the weight ratio of the enteric-coated material cellulose acetate phthalate to hydroxypropyl methylcellulose titanate is 2:1, the prepared furotriptan succinate enteric-coated tablet has the best acid resistance.
As can be seen from Table 4, the furotriptan succinate enteric-coated tablet in example 8 is released rapidly in artificial intestinal juice with pH of 6.8, and has the highest dissolution rate within 60min, which indicates that when the weight ratio of the enteric-coated material cellulose acetate phthalate to hydroxypropyl methyl cellulose titanate is 2:1, the prepared furotriptan succinate enteric-coated tablet has the best release effect in intestinal tract.
From the above, it is known that when cellulose acetate phthalate and hydroxypropyl methyl cellulose titanate are used as the enteric material, and the weight ratio of the two is 2:1, the prepared furotriptan succinate enteric-coated tablet has good acid resistance in gastric juice, high dissolution rate in intestinal juice, and the best effect.
Claims (3)
1. A furotriptan succinate enteric-coated tablet consists of a furotriptan succinate tablet core and an enteric coating layer coated outside the furotriptan succinate tablet core, wherein the tablet core comprises furotriptan succinate, a filler and a disintegrant, and the enteric coating layer comprises an enteric material, a plasticizer and a lubricant, and is characterized in that the furotriptan succinate enteric-coated tablet comprises the following components in percentage by weight:
frovatriptan succinate 20%
45 percent of filler
7 percent of disintegrating agent
Enteric-coated material 20%
Plasticizer 5%
3% of lubricant.
2. Furotriptan succinate enteric tablet according to claim 1, characterized in that the filler is microcrystalline cellulose; the disintegrant is croscarmellose sodium; the enteric material is phthalic acid cellulose acetate and hydroxypropyl methyl cellulose titanate, and the weight ratio is 2: 1; the plasticizer is trioctyl citrate; the lubricant is magnesium stearate.
3. A process for preparing furotriptan succinate enteric-coated tablet of claim 1, comprising the steps of:
(1) uniformly mixing the furotriptan succinate, the filler and the disintegrant according to the weight percentage, granulating by taking absolute ethyl alcohol as a bonding agent and a sieve with 50-100 meshes, drying and tabletting to obtain a furotriptan succinate tablet core;
(2) dissolving the enteric material, the plasticizer and the lubricant by 80 percent ethanol to prepare enteric coating liquid;
(3) and (3) uniformly spraying the prepared enteric coating solution in the step (2) on the surface of the furatriptan succinate tablet core prepared in the step (1), and drying to obtain the furatriptan succinate enteric-coated tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201911264663.3A CN110934843A (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 |
|---|---|---|---|
| CN201911264663.3A CN110934843A (en) | 2019-12-11 | 2019-12-11 | Frovatriptan succinate tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN110934843A true CN110934843A (en) | 2020-03-31 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201911264663.3A Withdrawn CN110934843A (en) | 2019-12-11 | 2019-12-11 | Frovatriptan succinate tablet and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102688221A (en) * | 2012-04-27 | 2012-09-26 | 陕西科技大学 | Method for preparing aceclofenac enteric microcapsules |
| CN103142545A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Enteric capsule of etoposide |
| CN104490802A (en) * | 2014-12-04 | 2015-04-08 | 武汉信嘉和诚药物化学有限公司 | Salidroside enteric-coated tablets and preparation method thereof |
| 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 |
-
2019
- 2019-12-11 CN CN201911264663.3A patent/CN110934843A/en not_active Withdrawn
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102688221A (en) * | 2012-04-27 | 2012-09-26 | 陕西科技大学 | Method for preparing aceclofenac enteric microcapsules |
| CN103142545A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Enteric capsule of etoposide |
| CN104490802A (en) * | 2014-12-04 | 2015-04-08 | 武汉信嘉和诚药物化学有限公司 | Salidroside enteric-coated tablets and preparation method thereof |
| 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 |
Non-Patent Citations (3)
| Title |
|---|
| 《中国家庭养生保健书库》编委会，: "《健康养胃必知的生活细节大全》", 31 August 2015, 中国医药科技出版社， * |
| 刘晓霞，: ""琥珀酸呋罗曲坦薄膜衣片的制备及体外溶出行为考察"", 《中国药房》 * |
| 王世宇，: "《药用辅料学》", 30 April 2019, 中国中医药出版社， * |
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Application publication date: 20200331 |