CN106377515A - Flupirtine maleate slow release tablet - Google Patents
Flupirtine maleate slow release tablet Download PDFInfo
- Publication number
- CN106377515A CN106377515A CN201610792689.5A CN201610792689A CN106377515A CN 106377515 A CN106377515 A CN 106377515A CN 201610792689 A CN201610792689 A CN 201610792689A CN 106377515 A CN106377515 A CN 106377515A
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- CN
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- Prior art keywords
- parts
- flupirtine maleate
- flupirtine
- granules
- release
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a flupirtine maleate slow release tablet. The tablet is prepared from, by weight, 20-50 parts of flupirtine maleate quick release particles, 10-20 parts of flupirtine maleate slow release particles, 5-12 parts of sodium carboxymethyl starch, 1-9 parts of aerosil, 2-6 parts of magnesium stearate, 2-8 parts of an antioxidant, and 3-5 parts of microcrystalline cellulose. Problems of heavy side effects caused by initial excessive administration for keeping an effective amount of the plasma concentration and reaching the treatment effect through multi-time administration due to short half life of flupirtine maleate and adverseness to reduction of patients' pains and unable reaching of the treatment effect, caused by insufficient dosage, are solved in the invention.
Description
Technical field
The present invention relates to technical field of pharmaceutical chemistry is and in particular to a kind of flupirtine maleate sustained-release tablet.
Background technology
Flupirtine maleate (FlupirtineMaleate, chemical name：2- amino -6- [(4- luorobenzyl) amino] -3- pyrrole
Pyridine urethanes maleate) it is selective neuronal potassium channel openers, it is a kind of to act on central nervous system
Nonopioid analgesic, does not produce dependence and tolerance.Flupirtine maleate activates G egg on neuron membrane ++ white coupling
K channel, K outflow stablize resting membrane electric potential, cell film activity reduces, thus indirectly inhibiting the activation of nmda receptor.Treatment
The flupirtine maleate of concentration is not combined with α 1, α 2,5HTl, 5HT2, dopamine, Benzodiazepine, opium, maincenter M and n receptor.
Flupirtine maleate Central nervous system mainly has three kinds of effects：Analgesic activity, Muscle relaxation, prevent the unresolved progress of pain
Effect.
Due to the half-life short of flupirtine maleate, common oral preparation need frequent drug administration (daily 3-4 time, every time
100mg), blood concentration fluctuation is larger, easily produces obvious side effect.
Content of the invention
For the deficiencies in the prior art, the invention provides a kind of flupirtine maleate sustained-release tablet, there is good controlling
Treatment acts on.
For realizing object above, the present invention is achieved by the following technical programs：
The invention provides a kind of flupirtine maleate sustained-release tablet is it is characterised in that raw material by following parts by weight
It is prepared from：Flupirtine maleate immediate-release granules：20-50 part, flupirtine maleate slow-releasing granules：10-20 part, CMS
Sodium：5-12 part, superfine silica gel powder：1-9 part, magnesium stearate：2-6 part, antioxidant：2-8 part, microcrystalline cellulose：3-5 part；
Preferably, it is prepared from by the raw material of following parts by weight：Flupirtine maleate immediate-release granules：25-45 part, Malaysia
Sour Flupirtine slow-releasing granules：12-18 part, sodium carboxymethyl starch：6-11 part, superfine silica gel powder：2-8 part, magnesium stearate：4-5 part, anti-
Oxygen agent：3-6 part, microcrystalline cellulose：3-5 part.
Preferably, it is prepared from by the raw material of following parts by weight：Flupirtine maleate immediate-release granules：25 parts, maleic acid
Flupirtine slow-releasing granules：14 parts, sodium carboxymethyl starch：6 parts, superfine silica gel powder：3 parts, magnesium stearate：4 parts, antioxidant：3 parts, micro-
Crystalline cellulose：3 parts.
Preferably, it is prepared from by the raw material of following parts by weight：Flupirtine maleate immediate-release granules：30 parts, maleic acid
Flupirtine slow-releasing granules：12 parts, sodium carboxymethyl starch：10 parts, superfine silica gel powder：5 parts, magnesium stearate：4 parts, antioxidant：3 parts, micro-
Crystalline cellulose：3 parts.
Preferably, described flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-
105 parts, Hydroxypropyl methylcellulose 1-2 part.
Preferably, described flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate
290-310 part, Hydroxypropyl methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate
1.1-1.15 part, talcum powder 1.3-1.7 part.
Beneficial effect of the present invention：
The beneficial effects of the present invention is：(1) the flupirtine maleate sustained release tablets application " quick-release-sustained release pastille of the present invention
Particle is individually pelletized, quick-release-slow-releasing granules mixed pressuring plate in proportion " technique, wherein immediate-release granules can rapid-onset, and be sustained
Particle can be with the valid density of maintaining treatment；(2) overcome because flupirtine maleate relative half-lives are short in prior art, need many
Secondary administration, the blood concentration in order to maintain effective dose reaches therapeutic effect, and the initially excessive of administration initial stage causes more secondary work
With, and underdosage is helpless to mitigate patient suffering it is impossible to reach the problem of therapeutic effect.
Specific embodiment
Purpose, technical scheme and advantage for making the embodiment of the present invention are clearer, below in conjunction with the enforcement of the present invention
Example, is clearly and completely described to the technical scheme in the embodiment of the present invention.Based on the embodiment in the present invention, this area
The every other embodiment that those of ordinary skill is obtained under the premise of not making creative work, broadly falls into present invention protection
Scope.
Embodiment 1：
A kind of flupirtine maleate sustained-release tablet, is prepared from by the raw material of following parts by weight：Flupirtine maleate speed
Release particle：20 parts, flupirtine maleate slow-releasing granules：10 parts, sodium carboxymethyl starch：5 parts, superfine silica gel powder：1 part, magnesium stearate：
2 parts, antioxidant：2 parts, microcrystalline cellulose：3 parts, dibutyl phthalate：2 parts, azodiisobutyronitrile：2 parts, oleic acid diethyl
Alkylolamides：2 parts, aerosil：3 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Embodiment 2：
The invention provides a kind of flupirtine maleate sustained-release tablet, it is prepared from by the raw material of following parts by weight：Horse
Carry out sour Flupirtine immediate-release granules：50 parts, flupirtine maleate slow-releasing granules：20 parts, sodium carboxymethyl starch：12 parts, superfine silica gel powder：
9 parts, magnesium stearate：6 parts, antioxidant：8 parts, microcrystalline cellulose：5 parts, dibutyl phthalate：10 parts, azo two isobutyl
Nitrile：10 parts, oleic acid diethyl amide：8 parts, aerosil：10 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Embodiment 3：
The invention provides a kind of flupirtine maleate sustained-release tablet, it is prepared from by the raw material of following parts by weight：Horse
Carry out sour Flupirtine immediate-release granules：25 parts, flupirtine maleate slow-releasing granules：12 parts, sodium carboxymethyl starch：6 parts, superfine silica gel powder：2
Part, magnesium stearate：4 parts, antioxidant：3 parts, microcrystalline cellulose：3 parts, dibutyl phthalate：3 parts, azodiisobutyronitrile：4
Part, oleic acid diethyl amide：3 parts, aerosil：6 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Embodiment 4：
The invention provides a kind of flupirtine maleate sustained-release tablet, it is prepared from by the raw material of following parts by weight：Horse
Carry out sour Flupirtine immediate-release granules：45 parts, flupirtine maleate slow-releasing granules：18 parts, sodium carboxymethyl starch：11 parts, superfine silica gel powder：
8 parts, magnesium stearate：5 parts, antioxidant：6 parts, microcrystalline cellulose：5 parts, dibutyl phthalate：9 parts, azodiisobutyronitrile：
8 parts, oleic acid diethyl amide：5 parts, aerosil：8 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Embodiment 5：
The invention provides a kind of flupirtine maleate sustained-release tablet, it is prepared from by the raw material of following parts by weight：Horse
Carry out sour Flupirtine immediate-release granules：25 parts, flupirtine maleate slow-releasing granules：14 parts, sodium carboxymethyl starch：6 parts, superfine silica gel powder：3
Part, magnesium stearate：4 parts, antioxidant：3 parts, microcrystalline cellulose：3 parts, dibutyl phthalate：3 parts, azodiisobutyronitrile：4
Part, oleic acid diethyl amide：4 parts, aerosil：6 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Embodiment 6：
The invention provides a kind of flupirtine maleate sustained-release tablet, it is prepared from by the raw material of following parts by weight：Horse
Carry out sour Flupirtine immediate-release granules：30 parts, flupirtine maleate slow-releasing granules：12 parts, sodium carboxymethyl starch：10 parts, superfine silica gel powder：
5 parts, magnesium stearate：4 parts, antioxidant：3 parts, microcrystalline cellulose：3 parts, dibutyl phthalate：4 parts, azodiisobutyronitrile：
6 parts, oleic acid diethyl amide：3 parts, aerosil：6 parts；
Flupirtine maleate immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, hydroxypropyl
Methylcellulose 1-2 part.
Flupirtine maleate slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, hydroxypropyl
Methylcellulose 8-10 part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder
1.3-1.7 part.
Above example only in order to technical scheme to be described, is not intended to limit；Although with reference to the foregoing embodiments
The present invention has been described in detail, it will be understood by those within the art that：It still can be to aforementioned each enforcement
Technical scheme described in example is modified, or carries out equivalent to wherein some technical characteristics；And these modification or
Replace, do not make the essence of appropriate technical solution depart from the spirit and scope of various embodiments of the present invention technical scheme.
Claims (6)
1. a kind of flupirtine maleate sustained-release tablet is it is characterised in that be prepared from by the raw material of following parts by weight：Maleic acid
Flupirtine immediate-release granules：20-50 part, flupirtine maleate slow-releasing granules：10-20 part, sodium carboxymethyl starch：5-12 part, micro mist
Silica gel：1-9 part, magnesium stearate：2-6 part, antioxidant：2-8 part, microcrystalline cellulose：3-5 part.
2. flupirtine maleate sustained-release tablet as claimed in claim 1 is it is characterised in that raw material system by following parts by weight
Standby form：Flupirtine maleate immediate-release granules：25-45 part, flupirtine maleate slow-releasing granules：12-18 part, CMS
Sodium：6-11 part, superfine silica gel powder：2-8 part, magnesium stearate：4-5 part, antioxidant：3-6 part, microcrystalline cellulose：3-5 part.
3. flupirtine maleate sustained-release tablet as claimed in claim 2 is it is characterised in that raw material system by following parts by weight
Standby form：Flupirtine maleate immediate-release granules：25 parts, flupirtine maleate slow-releasing granules：14 parts, sodium carboxymethyl starch：6 parts,
Superfine silica gel powder：3 parts, magnesium stearate：4 parts, antioxidant：3 parts, microcrystalline cellulose：3 parts.
4. flupirtine maleate sustained-release tablet as claimed in claim 2 is it is characterised in that raw material system by following parts by weight
Standby form：Flupirtine maleate immediate-release granules：30 parts, flupirtine maleate slow-releasing granules：12 parts, sodium carboxymethyl starch：10 parts,
Superfine silica gel powder：5 parts, magnesium stearate：4 parts, antioxidant：3 parts, microcrystalline cellulose：3 parts.
5. the preparation method of flupirtine maleate sustained-release tablet as claimed in claim 1 is it is characterised in that described maleic acid fluorine
Pyrrole spit of fland immediate-release granules are made up of following components in parts by weight：Flupirtine maleate 95-105 part, Hydroxypropyl methylcellulose 1-2 part.
6. the preparation method of flupirtine maleate sustained-release tablet as claimed in claim 1 is it is characterised in that described maleic acid
Flupirtine slow-releasing granules are made up of following components in parts by weight：Flupirtine maleate 290-310 part, Hydroxypropyl methylcellulose 8-10
Part, microcrystalline cellulose 25-35 part, Utech NE30D25-35 part, calcium monohydrogen phosphate 1.1-1.15 part, talcum powder 1.3-1.7 part.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610792689.5A CN106377515A (en) | 2016-08-31 | 2016-08-31 | Flupirtine maleate slow release tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610792689.5A CN106377515A (en) | 2016-08-31 | 2016-08-31 | Flupirtine maleate slow release tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106377515A true CN106377515A (en) | 2017-02-08 |
Family
ID=57938199
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610792689.5A Pending CN106377515A (en) | 2016-08-31 | 2016-08-31 | Flupirtine maleate slow release tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN106377515A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109806233A (en) * | 2017-11-21 | 2019-05-28 | 北京泰德制药股份有限公司 | A kind of composition and preparation method thereof containing Flupirtine or its pharmaceutical salts |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102764257A (en) * | 2011-10-21 | 2012-11-07 | 四川百利药业有限责任公司 | Flupirtine maleate sustained release tablet |
-
2016
- 2016-08-31 CN CN201610792689.5A patent/CN106377515A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102764257A (en) * | 2011-10-21 | 2012-11-07 | 四川百利药业有限责任公司 | Flupirtine maleate sustained release tablet |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109806233A (en) * | 2017-11-21 | 2019-05-28 | 北京泰德制药股份有限公司 | A kind of composition and preparation method thereof containing Flupirtine or its pharmaceutical salts |
| CN109806233B (en) * | 2017-11-21 | 2022-05-20 | 北京泰德制药股份有限公司 | Composition containing flupirtine or medicinal salt thereof and preparation method thereof |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20170208 |
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