CN107998086A - A kind of ranolazine dispersible tablet and preparation method thereof - Google Patents
A kind of ranolazine dispersible tablet and preparation method thereof Download PDFInfo
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- CN107998086A CN107998086A CN201711283386.1A CN201711283386A CN107998086A CN 107998086 A CN107998086 A CN 107998086A CN 201711283386 A CN201711283386 A CN 201711283386A CN 107998086 A CN107998086 A CN 107998086A
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- ranolazine
- dispersible tablet
- tablet according
- dosage
- disintegrant
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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
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a kind of ranolazine Disket, using ranolazine as raw material, adds auxiliary material, is prepared into ranolazine dispersible tablet.Disintegration is fast, it is fast to absorb, bioavilability height；It is convenient to take；Enteron aisle residual is few, few side effects；It is sweet and aromatic, it is particularly easy to improve patient's drug compliance.
Description
Technical field
The present invention relates to a kind of ranolazine novel form, more particularly to be ranolazine dispersible tablet and preparation method thereof.
Background technology
Ranolazine has antianginal and function of resisting myocardial ischemia, its specific mechanism of action is unclear.Researches show that
It can partly suppress fatty acid oxidation, but can also influence the electrical conduction of heart at the same time, cause the QT interval related with dosage to be prolonged
It is long.Ranolazine be only limited to take the antianginal drugs such as long acting nitrate, calcium ion channel blocker and beta 2 receptor retarding agent without
The patient of effect uses.Clinical test shows that the effect that male patient takes ranolazine is better than women, long
Phase, which takes, occurs the adverse reactions such as dizzy, headache, constipation and nausea.
Ranolazine is a kind of new chemical entities compound, is the first treatment chronic angina medicine that FDA ratifies over 10 years
Thing.Different from existing antianginal drug, ranolazine is partial fatty acid oxidation enzyme inhibitor, on heart rate and blood pressure without influence,
Can effectively allevating angina pectoris, and do not change other kinetic parameters of medicine, the quality of life of patient with angina pectoris can be improved.
According to the estimation U.S. of American heart association, about 6,800,000 people are diagnosed with angina pectoris, Chinese patients number every year
Ten thousand up to more than 4 000, therefore ranolazine has very big market development potential.
Dispersible tablet is a kind of quick-effective preparation, due to its distinctive advantage, has been had been to be concerned by more and more people.It can add
Solubilizer；The dissolution rate of ranolazine insoluble drug can be improved, is suitable for taking.Piece is made for the difficult medicine of disintegration can
Be conducive to absorb.The characteristics of piece：1. disintegration is fast, it is fast to absorb, bioavilability height；2. 3. enteron aisle residual convenient to take is few, pair is made
With less.
The content of the invention
The object of the present invention is to provide a kind of ranolazine dispersible tablet and preparation method thereof.
Objects of the present invention are achieved through the following technical solutions.
Ranolazine dispersible tablet of the present invention is made of following component（Percentage by weight）：
| Ranolazine | 15-60% |
| Filler | 10-40% |
| Disintegrant | 5-25% |
| Adhesive | 0.1-6% |
| Solubilizer | 0.1-6% |
| Lubricant | 0.5-5%。 |
It is above the basic prescription of the present invention, suitably can be adjusted and deleted according to being actually needed.
Ranolazine is active ingredient, preferred content scope 15-40%, further preferred scope 15-20%.Thunder in unit formulation
Promise piperazine dosage 100-500mg, preferred dose 100-200mg, preferred dosage is 100,150,200mg.
Due to dispersible tablet requirement can be disintegrated rapidly in water it is dispersed, have that convenient to take, disintegration is rapid, it is fast to absorb and
The features such as bioavilability is high.Therefore the selection to supplementary product kind and its performance is to prepare the key of piece.Inventor is by multiple
Experiment, it is determined that be adapted to the pharmaceutic adjuvant and its dosage of ranolazine dispersible tablet.
Filler selection is used for increasing the weight and volume of piece, shaping and divided dose in order to preparation.Filled out in the present invention
Fill one or more of mixtures of the agent in lactose, sucrose, microcrystalline cellulose, pregelatinized starch, dextrin etc..Amount ranges
It is preferred that 10-40%, particularly preferred 15-35%.
Disintegrant is selected from the pharmaceutic adjuvants such as low-substituted hydroxypropyl cellulose, crospovidone.Dosage preferred 5-25%, it is especially excellent
Select 5-20%.
The selection of the species and dosage of solubilizer is most important for the dissolution of this preparation.The solubilizer of the present invention selects dodecane
One of base sodium sulphate, Macrogol 6000, Macrogol 4000, Tween 80, polysorbate40, sorbester p18, span 40 are wherein several
The mixture of kind, further masks the bad strange taste of ranolazine, improves the mouthfeel of piece.
One or more of mixtures of the lubricant in superfine silica gel powder, magnesium stearate, talcum powder.
Present invention also offers the preparation method of ranolazine dispersible tablet.Ranolazine dispersible tablet of the present invention can directly be pressed with powder
It is prepared by piece method.Direct powder compression preparation process is：By ranolazine and filler（Such as lactose）, it is disintegrant, solubilizer, viscous
After mixture and mix lubricant are uniform, direct powder compression.
Ranolazine dispersible tablet disintegration of the present invention is fast, absorbs fast, bioavilability height；It is convenient to take；Enteron aisle residual is few, and pair is made
With less；It is sweet, without ranolazine off-odor and aromatic, it is particularly easy to improve patient's drug compliance.
Embodiment
Embodiment l
Prescription：
Preparation method：
（1）By ranolazine powder（200 mesh）With cane sugar powder（150 mesh）Equal increments are uniformly mixed, and obtain mixture A；
（2）After remaining auxiliary material is crossed 200 mesh sieves, equal increments are uniformly mixed, and obtain mixture B；
（3）By mixture A and mixture B by equal increments method after mixing, direct tablet compressing.
Embodiment 2
Prescription：
Preparation method：
（1）By ranolazine powder（200 mesh）With lactose powder（150 mesh）Equal increments are uniformly mixed, and obtain mixture A；
（2）After remaining auxiliary material is crossed 200 mesh sieves, equal increments are uniformly mixed, and obtain mixture B；
（3）By mixture A and mixture B by equal increments method after mixing, direct tablet compressing.
Embodiment 3
Prescription：
Preparation method：
（1）By ranolazine powder（200 mesh）With lactose powder（150 mesh）Equal increments are uniformly mixed, and obtain mixture A；
（2）After remaining auxiliary material is crossed 200 mesh sieves, equal increments are uniformly mixed, and obtain mixture B；
（3）By mixture A and mixture B by equal increments method after mixing, direct tablet compressing.
Embodiment 4
Prescription：
Preparation method：
（1）By ranolazine powder（200 mesh）With lactose powder（150 mesh）Equal increments are uniformly mixed, and obtain mixture A；
（2）After remaining auxiliary material is crossed 200 mesh sieves, equal increments are uniformly mixed, and obtain mixture B；
（3）By mixture A and mixture B by equal increments method after mixing, direct tablet compressing.
Invention formulation and technology prepares the study on the stability of sample：
Sample prepared by embodiment 1, embodiment 2, embodiment 3 and embodiment 4 is respectively placed in stability test case, is set
Temperature carries out accelerating within three months to investigate under the conditions of 40 DEG C, relative humidity 75%RH.
Inspection target is used as using disintegration time limited, it was demonstrated that the science for the tablet recipe technique invented.
Ranolazine raw material used in above example is Pfizer's medicine company production；Auxiliary material supply producer is Ka Lekang pharmacy, moral is solid
Match rule medicine, Le Jiawen pharmacy, International Specialty Products pharmaceutical Co. Ltd and Huainan mountains and rivers pharmaceutical Co. Ltd.
Claims (9)
1. a kind of ranolazine dispersible tablet, is made of following weight percent composition：
Ranolazine 15-60%
Filler 10-40%
Disintegrant 5-25%
Adhesive 0.1-6%
Solubilizer 0.1-6%
Lubricant 0.5-5%.
2. ranolazine dispersible tablet according to claim 1, wherein described：
One or more of mixtures of the filler in microcrystalline cellulose, lactose, sucrose, pregelatinized starch, dextrin etc.；
Disintegrant is in low-substituted hydroxypropyl methylcellulose, crospovidone, sodium carboxymethyl starch, Ac-Di-Sol
One of or wherein several mixtures；
Adhesive is selected from povidone, height substitutes one of hydroxypropylcellulose, gelatine size, starch slurry, sodium carboxymethylcellulose or it
In several mixtures；
One or more of mixtures of the lubricant in superfine silica gel powder, magnesium stearate, talcum powder.
3. ranolazine dispersible tablet according to claim 2, wherein the ranolazine content scope 15-60%.
4. ranolazine dispersible tablet according to claim 2, wherein the filler loading scope 10-40%.
5. ranolazine dispersible tablet according to claim 2, wherein the disintegrant dosage 5-25%.
6. ranolazine dispersible tablet according to claim 2, wherein described adhesive dosage 0.5-2%.
7. the ranolazine dispersible tablet according to any claim in claim 3-6, wherein：Ranolazine content scope 15-
60%；Filler loading 10-40%；Disintegrant dosage 5-25%；Binder dosage 0.5-2%, solubilizer dosage 0.5-2%.
8. ranolazine dispersible tablet according to claim 1, wherein the ranolazine unit dose 100-500mg.
9. the preparation method of ranolazine dispersible tablet described in claim 1, using direct powder compression, by ranolazine and filling
Agent, disintegrant, solubilizer, adhesive and mix lubricant it is uniform after, direct powder compression.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711283386.1A CN107998086A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine dispersible tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711283386.1A CN107998086A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine dispersible tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107998086A true CN107998086A (en) | 2018-05-08 |
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ID=62057426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711283386.1A Pending CN107998086A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine dispersible tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107998086A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066253A (en) * | 2007-06-07 | 2007-11-07 | 北京本草天源药物研究院 | Slow releasing ranolazine tablet |
| CN106074406A (en) * | 2016-06-12 | 2016-11-09 | 佛山市腾瑞医药科技有限公司 | A kind of Vonoprazan fumarate dispersible tablet and preparation method thereof |
-
2017
- 2017-12-07 CN CN201711283386.1A patent/CN107998086A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066253A (en) * | 2007-06-07 | 2007-11-07 | 北京本草天源药物研究院 | Slow releasing ranolazine tablet |
| CN106074406A (en) * | 2016-06-12 | 2016-11-09 | 佛山市腾瑞医药科技有限公司 | A kind of Vonoprazan fumarate dispersible tablet and preparation method thereof |
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|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20180508 |
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| WD01 | Invention patent application deemed withdrawn after publication |