CN109260165A - A kind of Stiripentol tablet composition - Google Patents
A kind of Stiripentol tablet composition Download PDFInfo
- Publication number
- CN109260165A CN109260165A CN201811205864.1A CN201811205864A CN109260165A CN 109260165 A CN109260165 A CN 109260165A CN 201811205864 A CN201811205864 A CN 201811205864A CN 109260165 A CN109260165 A CN 109260165A
- Authority
- CN
- China
- Prior art keywords
- stiripentol
- mannitol
- lactose
- tablet composition
- magnesium stearate
- 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.)
- Withdrawn
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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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
- A61K31/36—Compounds containing methylenedioxyphenyl groups, e.g. sesamin
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
Abstract
The present invention relates to a kind of anti-epileptic compositions, belong to technical field of medicine.Stiripentol tablet composition of the present invention in every thousand, contains Stiripentol 250-500g, lauryl sodium sulfate 1.2-1.8g, Macrogol 6000 6-10g, mannitol 10-25g, sodium citrate 12-22g, lactose 30-60g, microcrystalline cellulose 26-48g, magnesium stearate 1.0-1.8g.In technical solution of the present invention, the introducing of mannitol and lauryl sodium sulfate plays unexpected synergistic effect to the dissolution rate raising of Stiripentol tablet, provides a kind of pharmaceutical preparation for meeting clinical requirement.
Description
Technical field
The present invention relates to a kind of anti-epileptic compositions, belong to technical field of medicine.
Background technique
Dravet syndrome, also known as baby's severe myoclonic epilepsy (severe myoclonic epilepsy in
Infarlcy, SMEI), it is a kind of intractable epilepsy syndrome of rare clinical.Dravet syndrome can lead to serious epilepsy
Property encephalopathy, have age of onset is early, mode of onset is complicated, seizure frequency is high, intelligence damage is serious, drug therapy it is efficient it is low,
The representative of the features such as poor prognosis, the high death rate and intractable epilepsy.Its therapeutic modality can choose operative treatment or nerve
The modes such as regulation, it is not known that the clear cause of disease can choose drug therapy.Epilepsy in childhood is developed to child and intellectual aspect has
Very big influence.
Very limited to the treatment means of Dravet syndrome at present, patient needs to receive continual nursing, this meeting
The quality of life generation of patient and its family are seriously affected.Dravet syndrome patient may be because epileptic attack time mistake
It is long, the die by visitation of God of accident or epileptic attack caused by epilepsy and it is dead, the death rate of patient is 15-20% at present.Patient
There is an urgent need to Innovative therapeutic method improves their quality of life with their parent.
Stiripentol (Stiripentol), trade name: Diacomit, chemical name: 4,4- dimethyl-1-[(3,4-
Methylene-dioxy) phenyl] -1-POL is the research and development of Biocodex company for treating the anticonvulsant drug of epilepsy.?
It is treated together with sodium vedproate (valproate) and Clobazam through getting the Green Light in European Union, Canada, the U.S., Japan and other countries
Dravet syndrome patient.
Commercially available Stiripentol is tablet or capsule, there is 250mg, 500mg specification.Belong to the drug of big specification.Due to department
It is not soluble in water for amylalcohol, and bulk pharmaceutical chemicals are easy moisture absorption, bring certain difficulty to the preparation of tablet.On the one hand, due to specification
Greatly, the amount for adding auxiliary material is limited；On the other hand, after solubility is up to standard, during storage, easily moisture absorption causes piece to tablet
Agent drum is split, and related substance increases obviously.
Summary of the invention
Goal of the invention: in view of the deficiencies of the prior art, the present invention provides a kind of Stiripentol tablet compositions that performance is stable
Object.
The technical scheme is that a kind of Stiripentol tablet composition, in every thousand, contain Stiripentol 250-
500g, lauryl sodium sulfate 1.2-1.8g, Macrogol 6000 6-10g, mannitol 10-25g, sodium citrate 12-22g, cream
Sugared 30-60g, microcrystalline cellulose 26-48g, magnesium stearate 1.0-1.8g.
Preferably, Stiripentol tablet composition of the present invention, in every thousand, containing Stiripentol 250-500g, ten
Sodium dialkyl sulfate 1.3-1.6g, Macrogol 6000 7-9g, mannitol 14-23g, sodium citrate 15-20g, lactose 38-
55g, microcrystalline cellulose 30-45g, magnesium stearate 1.2-1.7g.
Preferably, Stiripentol tablet composition of the present invention in every thousand, contains Stiripentol 250g, dodecane
Base sodium sulphate 1.3g, Macrogol 6000 7g, mannitol 15g, sodium citrate 18g, lactose 50g, microcrystalline cellulose 40g, it is stearic
Sour magnesium 1.4g.
Preferably, Stiripentol tablet composition of the present invention in every thousand, contains Stiripentol 500g, dodecane
Base sodium sulphate 1.6g, Macrogol 6000 9g, mannitol 22g, sodium citrate 20g, lactose 52g, microcrystalline cellulose 38g, it is stearic
Sour magnesium 1.5g.
Preferably, Stiripentol tablet composition of the present invention, the polyethylene glycol is using additional.
The preparation method of Stiripentol tablet composition of the present invention, prepares according to the following steps:
First step Stiripentol crosses 120 meshes, other auxiliary materials cross 60 meshes；
The Stiripentol of second step recipe quantity, lauryl sodium sulfate, mannitol, sodium citrate are uniformly mixed, then with recipe quantity
Lactose, microcrystalline cellulose be uniformly mixed；With 45% ethyl alcohol softwood, fluidized bed granulation, 60 DEG C of drying, whole grain；
Particle obtained by third step second step, is added polyethylene glycol, the magnesium stearate of recipe quantity, is uniformly mixed, tabletting.
The utility model has the advantages that the present invention provides a kind of Stiripentol tablet groups that performance is stable by reasonable prescription dispensing
Object is closed, provides high-quality drug for clinic.In technical solution of the present invention, the introducing of mannitol and lauryl sodium sulfate, to department
Unexpected synergistic effect is played for the dissolution rate raising of amylalcohol tablet.Polyethylene glycol is additional to play the steady in a long-term of tablet
Certain effect is arrived.
Embodiment 1. Stiripentol 250g, lauryl sodium sulfate 1.2g, Macrogol 6000 6g, mannitol 10g, Chinese holly
Rafter acid sodium 12g, lactose 60g, microcrystalline cellulose 26g, magnesium stearate 1.0g, by the preparation of preparation method described in technical solution 1000
Piece.
Embodiment 2. Stiripentol 500g, lauryl sodium sulfate 1.8g, Macrogol 6000 10g, mannitol 25g,
Sodium citrate 22g, lactose 30g, microcrystalline cellulose 48g, magnesium stearate 1.8g, prepared by preparation method described in technical solution
1000.
Embodiment 3. Stiripentol 250g, lauryl sodium sulfate 1.3g, Macrogol 6000 7g, mannitol 15g, Chinese holly
Rafter acid sodium 18g, lactose 50g, microcrystalline cellulose 40g, magnesium stearate 1.4g, by the preparation of preparation method described in technical solution 1000
Piece.
Embodiment 4. Stiripentol 500g, lauryl sodium sulfate 1.6g, Macrogol 6000 9g, mannitol 22g, Chinese holly
Rafter acid sodium 20g, lactose 52g, microcrystalline cellulose 38g, magnesium stearate 1.5g, by the preparation of preparation method described in technical solution 1000
Piece.
1. embodiment of reference examples, 3 prescription, does not add mannitol, and corresponding quality is supplemented by lactose.It is specific as follows:
Stiripentol 250g, lauryl sodium sulfate 1.3g, Macrogol 6000 7g, sodium citrate 18g, lactose 65g, crystallite
Cellulose 40g, magnesium stearate 1.4g, the preparation method with reference to described in technical solution prepare 1000.
The prescription of 2. embodiment 4 of reference examples, does not add Macrogol 6000, and corresponding quality is supplemented by lactose, specifically such as
Under.
Stiripentol 500g, lauryl sodium sulfate 1.6g, mannitol 22g, sodium citrate 20g, lactose 61g, crystallite are fine
Element 38g, magnesium stearate 1.5g are tieed up, the preparation method with reference to described in technical solution prepares 1000.
The prescription of 3. embodiment 4 of reference examples, Macrogol 6000 is interior to be added.It is specific as follows:
Stiripentol 500g, lauryl sodium sulfate 1.6g, Macrogol 6000 9g, mannitol 22g, sodium citrate 20g, cream
Sugared 52g, microcrystalline cellulose 38g, magnesium stearate 1.5g prepare 1000 by following preparation methods.
First step Stiripentol crosses 120 meshes, other auxiliary materials cross 60 meshes；
The Stiripentol of second step recipe quantity, lauryl sodium sulfate, mannitol, sodium citrate are uniformly mixed, then with recipe quantity
Lactose, polyethylene glycol, microcrystalline cellulose be uniformly mixed；With 45% ethyl alcohol softwood, fluidized bed granulation, 60 DEG C of drying, whole grain；
Particle obtained by third step second step, is added the magnesium stearate of recipe quantity, is uniformly mixed, tabletting.
Test example 1. distinguishes Example 1-4 and reference examples 1-3 product each 100, observes the appearance of piece, observes situation
It is recorded in table 1.
Table 1
| 1 product of embodiment | 2 product of embodiment | 3 product of embodiment | 4 product of embodiment | 1 product of reference examples | 2 product of reference examples | 3 product of reference examples | |
| Piece appearance | It is smooth | It is smooth | It is smooth | It is smooth | It is smooth | It is smooth | It is smooth |
Test example 2. measures embodiment 1-4 and reference examples 1-3 product the 60th minute according to the Rotating shakers of States Pharmacopoeia specifications respectively
Dissolution rate, and related content of material (high performance liquid chromatography) is measured, determination data is recorded in table 2.
Table 2
| 1 product of embodiment | 2 product of embodiment | 3 product of embodiment | 4 product of embodiment | 1 product of reference examples | 2 product of reference examples | 3 product of reference examples | |
| 60th minute dissolution rate | 87.28 | 89.15 | 89.08 | 90.64 | 76.82 | 89.88 | 89.98 |
| Related substance, % | 0.16 | 0.15 | 0.15 | 0.15 | 0.15 | 0.18 | 0.17 |
Test example 3. distinguishes Example 1-4 and reference examples 1-3 product each 100, aluminum-plastic packaged respectively, is placed in constant temperature and humidity
In case, 25 DEG C, relative humidity 75% is stored 12 months, and the 12nd the end of month took out, and observes appearance, and measure dissolution in the 60th minute
Degree, secretary are recorded in table 3.
Table 3
| 1 product of embodiment | 2 product of embodiment | 3 product of embodiment | 4 product of embodiment | 1 product of reference examples | 2 product of reference examples | 3 product of reference examples | |
| Piece appearance | It is smooth | It is smooth | It is smooth | It is smooth | It is smooth | 24 have point | 14 have point |
| Appearance yield, % | 100 | 100 | 100 | 100 | 100 | 76 | 86 |
| 60th minute dissolution rate | 87.30 | 89.08 | 89.02 | 90.58 | 76.68 | 80.24 | 84.67 |
| Related substance, % | 0.16 | 0.15 | 0.15 | 0.15 | 0.15 | 0.88 | 0.54 |
3 data of table explanation: 1-4 of embodiment of the present invention product is stable during storage.Its dissolution rate and related substance contain
Amount has almost no change at room temperature and under common damp condition.Illustrate technical solution of the present invention, in product quality
Control aspect plays positive effect.
Claims (6)
1. a kind of Stiripentol tablet composition, which is characterized in that in every thousand, contain Stiripentol 250-500g, dodecane
Base sodium sulphate 1.2-1.8g, Macrogol 6000 6-10g, mannitol 10-25g, sodium citrate 12-22g, lactose 30-60g are micro-
Crystalline cellulose 26-48g, magnesium stearate 1.0-1.8g.
2. Stiripentol tablet composition according to claim 1, which is characterized in that in every thousand, contain Stiripentol
250-500g, lauryl sodium sulfate 1.3-1.6g, Macrogol 6000 7-9g, mannitol 14-23g, sodium citrate 15-
20g, lactose 38-55g, microcrystalline cellulose 30-45g, magnesium stearate 1.2-1.7g.
3. Stiripentol tablet composition according to claim 1, which is characterized in that in every thousand, contain Stiripentol
250g, lauryl sodium sulfate 1.3g, Macrogol 6000 7g, mannitol 15g, sodium citrate 18g, lactose 50g, crystallite are fine
Tie up element 40g, magnesium stearate 1.4g.
4. Stiripentol tablet composition according to claim 1, which is characterized in that in every thousand, contain Stiripentol
500g, lauryl sodium sulfate 1.6g, Macrogol 6000 9g, mannitol 22g, sodium citrate 20g, lactose 52g, crystallite are fine
Tie up element 38g, magnesium stearate 1.5g.
5. Stiripentol tablet composition according to claim 1, which is characterized in that the polyethylene glycol is added using outer addition
Enter.
6. the preparation method of Stiripentol tablet composition according to claim 1, which is characterized in that make according to the following steps
It is standby:
First step Stiripentol crosses 120 meshes, other auxiliary materials cross 60 meshes；
The Stiripentol of second step recipe quantity, lauryl sodium sulfate, mannitol, sodium citrate are uniformly mixed, then with recipe quantity
Lactose, microcrystalline cellulose be uniformly mixed；With 45% ethyl alcohol softwood, fluidized bed granulation, 60 DEG C of drying, whole grain；
Particle obtained by third step second step, is added polyethylene glycol, the magnesium stearate of recipe quantity, is uniformly mixed, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811205864.1A CN109260165A (en) | 2018-10-17 | 2018-10-17 | A kind of Stiripentol tablet composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811205864.1A CN109260165A (en) | 2018-10-17 | 2018-10-17 | A kind of Stiripentol tablet composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109260165A true CN109260165A (en) | 2019-01-25 |
Family
ID=65196851
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811205864.1A Withdrawn CN109260165A (en) | 2018-10-17 | 2018-10-17 | A kind of Stiripentol tablet composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN109260165A (en) |
-
2018
- 2018-10-17 CN CN201811205864.1A patent/CN109260165A/en not_active Withdrawn
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20190125 |