CN107982238A - A kind of ranolazine effervescent tablet and preparation method thereof - Google Patents
A kind of ranolazine effervescent tablet and preparation method thereof Download PDFInfo
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- CN107982238A CN107982238A CN201711283941.0A CN201711283941A CN107982238A CN 107982238 A CN107982238 A CN 107982238A CN 201711283941 A CN201711283941 A CN 201711283941A CN 107982238 A CN107982238 A CN 107982238A
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- Prior art keywords
- ranolazine
- effervescent tablet
- acid
- powder
- sodium
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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
-
- 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
- A61K9/2009—Inorganic compounds
-
- 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
- A61K9/2068—Compounds of unknown constitution, e.g. material from plants or animals
-
- 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
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
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- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of ranolazine effervescent tablet and preparation method thereof, it is an object of the invention to many patients and a kind of disintegration of medical personnel's offer are fast, absorption is fast, bioavilability is high, convenient to take, enteron aisle remains less, the novel formulation ranolazine effervescent tablet of Small side effects, using ranolazine as raw material, add some particular types and the auxiliary material of ratio, ranolazine effervescent tablet is prepared into according to the technological means illustrated by the present invention, the product of the present invention is sweet and aromatic, it is rapid-action, bioavilability is high, is particularly easy to improve patient's drug compliance.
Description
Technical field
The present invention relates to a kind of ranolazine effervescent 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,
The adverse reactions such as dizzy, headache, constipation and nausea occur in long-term use.
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 people every year
Number up to more than 4 000 ten thousand, therefore ranolazine has very big market development potential.
Effervescent tablet is a kind of quick-effective preparation to grow up, due to its distinctive advantage, is increasingly closed be subject to people
Note.
Effervescent tablet（chewable tablets）Definition：Reacted generation by organic acid in piece and inorganic base in mouth
Bubble, the tablet for promoting tablet to be swallowed again after being disintegrated rapidly.The organic acid being commonly incorporated into has tartaric acid or citric acid；The nothing of addition
Machine alkali has sodium acid carbonate or sodium carbonate；Sucrose, peppermint, flavorant etc. are added to adjust taste, is suitable for child administration, for
Effervescent tablet, which is made, in the difficult medicine of disintegration can be conducive to absorb.Technical requirements：1. mouthfeel, appearance uniform are good；2. foamed time
3. other in 5 minutes the requirement of tablet general rule should should be met.The characteristics of effervescent tablet：1. disintegration is fast, absorbs fast, bioavilability
It is high；2. 3. enteron aisle residual convenient to take is few, Small side effects.
It is mainly the sweet taste fillers such as lactose, sucrose, xylitol in prescription of the present invention, other flavourings increase the mouth of piece
Sense, covers medicine unhappiness smell, and colouring agent makes tablet have pleasing appearance, these are all more advantageous to increase patient medication and comply with
Property.Present invention also offers the preparation method on ranolazine effervescent tablet.
Auxiliary material supply producer is Ka Lekang pharmacy, Degussa pharmacy, Le Jiawen pharmacy, International Specialty Products system used in the present invention
Medicine Co., Ltd and Huainan mountains and rivers pharmaceutical Co. Ltd.
The content of the invention
The object of the present invention is to provide one kind to absorb rapidly, and bioavilability and the blood medicine that can effectively improve ranolazine are dense
Degree, convenient to take, few side effects ranolazine effervescent tablets and preparation method thereof.
Ranolazine effervescent tablet of the present invention also contains auxiliary material in addition to main ingredient, is 1%~15% Reynolds by weight percentage
Piperazine, 85%~95% auxiliary material.Auxiliary material is to be adapted to the available auxiliary material of any type that effervescent tablet is made, they can include filling
Agent, organic acid, inorganic base, flavouring or odor mask, colouring agent, lubricant etc..In each oral formulations unit, contain ranolazine
20mg~250mg, preferred dose are the mg of 25mg~200, and preferred dosage is 50~100mg. since effervescent tablet requirement is in mouth
Clothes are suck in chamber tablet is swallowed after dissolving, is good mouthfeel, nonirritant to oral mucosa.Therefore to supplementary product kind and its performance
Selection is to prepare the key of effervescent tablet.The present invention is by selection, it is determined that is adapted to the pharmaceutic adjuvant of ranolazine effervescent tablet, wherein filling out
Fill agent selection and be used for increasing the weight and volume of effervescent tablet, shaping and divided dose in order to preparation, filler is excellent in the present invention
Select at least one of lactose, sucrose, mannitol, sorbierite, xylitol etc..The selection of the species and dosage of flavouring is for this
Whether preparation has the mouthfeel of fragrant and sweet happy people most important.Filler lactose, sucrose, mannitol, the xylitol etc. of the present invention has concurrently
The important function of flavoring；The organic acid of the present invention includes the important function that tartaric acid, citric acid etc. have flavoring concurrently；The present invention's
Inorganic base sodium acid carbonate, sodium carbonate etc. have the important function of flavoring concurrently；In addition it also add appropriate taste masking and act on stronger flavoring
Agent, the preferred glycyrrhizin of flavouring, disodium glycyrrhizinate, trisodium glycyrrhetinate, vanilla, cherry, grape, orange, lemon, peppermint, grass
At least one in Pueraria lobota, banana, pineapple, peach flavor, maltitol, saccharin sodium, protein sugar, sucrose, Aspartame, stevioside
Kind, further masks the bad strange taste of ranolazine, improves the mouthfeel of effervescent tablet.It can be added in effervescent tablet a certain amount of
Colouring agent, makes tablet have pleasing visual appearance, helps to eliminate the patient's resistance mood be sick of and taken medicine.The colouring agent of the present invention
It is preferred that chlorophyll, caramel, sunset yellow, cocoa pigment, sodium-iron-chlorophyllin, lemon yellow, amaranth, famille rose, indigo, red fresh
At least one of red, orange, light blue, fast blue.
At least one of the preferred superfine silica gel powder of lubricant, magnesium stearate, talcum powder.
The effervescent tablet of the present invention can be prepared with direct powder compression.
Direct powder compression preparation process is：200 mesh ranolazine powder and 100 mesh lactose powders, equal increments, mixing is equal
It is even；Remaining auxiliary material filler, organic acid, inorganic base, flavouring, odor mask, colouring agent and lubricant equal increments are mixed
200 mesh sieves are crossed after uniformly；It is added in ranolazine and lactose mixed-powder, by equal increments method after mixing, direct tablet compressing
.
The effervescent tablet of the present invention, its basic composition include following supplementary material, can be adjusted according to actual needs
With delete.
Form percentage by weight
Ranolazine 15%~55%
Filler 45%~85%
Organic acid 0.1%~15%
Inorganic base 0.1%~15%
Flavouring 0.01%~15%
Colouring agent 0.01%~0.5%
Lubricant 0.6%~5%.
Embodiment
Embodiment l
Ranolazine 250g
Sucrose 550g
Tartaric acid 60g
Sodium acid carbonate 60g
Disodium glycyrrhizinate 60g
Flavoring orange essence 33g
Red scarlet 32g
Talcum powder 55g
1000 are made altogether
Preparation method：By 200 mesh ranolazine powder and 200 mesh lactose powders, equal increments are uniformly mixed；Remaining auxiliary material is filled
Agent, organic acid, inorganic base, flavouring, odor mask, colouring agent and lubricant equal increments cross 200 mesh sieves after mixing；Add
Into ranolazine and lactose mixed-powder, by equal increments method after mixing, direct tablet compressing.
Embodiment 2
Ranolazine 25g
Lactose 510g
75 g of citric acid
Sodium carbonate 75g
Aspartame 7.5g
10 g of glycyrrhizin
Peach flavor 72.5g
Orange 75g
Superfine silica gel powder 75g
1000 are made altogether
Preparation method：With embodiment 1.
Embodiment 3
Ranolazine 100g
Sucrose 515g
Tartaric acid 85g
Sodium acid carbonate 85g
60 g of disodium glycyrrhizinate
Flavoring orange essence 75g
Red scarlet 75g
Talcum powder 65g
1000 are made altogether
Preparation method：With embodiment 1.
Embodiment 4
Ranolazine 50g
Lactose 535g
75 g of citric acid
Sodium carbonate 75g
Aspartame 25g
Glycyrrhizin 15g
Peach flavor 80g
Orange 70g
Superfine silica gel powder 75g
1000 are made altogether
Preparation method：With embodiment 1.
Claims (7)
- A kind of 1. ranolazine effervescent tablet, it is characterised in that：Include the supplementary material of following weight percent proportioning,Ranolazine 15%~55%Filler 30%~45.0%Organic acid 0.1%~5%Inorganic base 0.1%~5%Flavouring 0.01%~5%Colouring agent 0.01%~0.5%Lubricant 0.6%~5%The wherein described ranolazine, is the three classes for the maintaining treatment of platinum sensitivity recurrent BRCA mutation oophoroma adult patients New drug, currently carries out preclinical study.
- 2. at least one of the wherein described filler preferably sucrose, lactose, mannitol, sorbierite, xylitol etc.；Organic acid At least one of preferably citric acid, tartaric acid, citric acid；At least one of the preferred sodium acid carbonate of inorganic base or sodium carbonate； The preferred glycyrrhizin of the flavouring, disodium glycyrrhizinate, trisodium glycyrrhetinate, vanilla, cherry, grape, orange, lemon, peppermint, In careless Pueraria lobota, banana, pineapple, peach flavor, maltitol, saccharin sodium, protein sugar, sucrose, Aspartame, Stevioside at least It is a kind of；The preferred chlorophyll of the colouring agent, caramel, sunset yellow, cocoa pigment, sodium-iron-chlorophyllin, lemon yellow, three-coloured amaranth At least one of red, carmine, indigo, red scarlet, orange, light blue, fast blue；The lubricant is selected from superfine silica gel powder, hard At least one of fatty acid magnesium, talcum powder.
- A kind of 3. ranolazine effervescent tablet according to claim 1, it is characterised in that：By weight percentage, containing Reynolds Piperazine 15%~55%, the percentage by weight of auxiliary material is 45%~85%.
- 4. the ranolazine effervescent tablet every is about 20mg~250mg containing ranolazine fourth.
- A kind of 5. ranolazine effervescent tablet according to claim 1, it is characterised in that：Ranitidine content is preferably 1%~ 15%, the ranolazine effervescent tablet, per unit weight be 1g it is a piece of in containing ranolazine be 20mg~250mg.
- A kind of 6. ranolazine effervescent tablet according to claim 1, it is characterised in that：Ranolazine content is preferably 1%~12%, The ranolazine effervescent tablet, per unit weight be 1g it is a piece of in containing ranolazine be 20mg~250mg.
- A kind of 7. preparation method of ranolazine effervescent tablet, it is characterised in that：This by 200 mesh ranolazine powder and 200 mesh lactose powders, etc. Amount is incremental to be uniformly mixed；By remaining auxiliary material filler, organic acid, inorganic base, flavouring, odor mask, colouring agent and lubricant Equal increments cross 200 mesh sieves after mixing；It is added in ranolazine and lactose mixed-powder, is uniformly mixed by equal increments method Afterwards, direct tablet compressing.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711283941.0A CN107982238A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine effervescent tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711283941.0A CN107982238A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine effervescent tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107982238A true CN107982238A (en) | 2018-05-04 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711283941.0A Pending CN107982238A (en) | 2017-12-07 | 2017-12-07 | A kind of ranolazine effervescent tablet and preparation method thereof |
Country Status (1)
| Country | Link |
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| CN (1) | CN107982238A (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 |
| CN105902512A (en) * | 2016-06-13 | 2016-08-31 | 佛山市腾瑞医药科技有限公司 | Olaparib effervescent tablet and preparation method thereof |
-
2017
- 2017-12-07 CN CN201711283941.0A patent/CN107982238A/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 |
| CN105902512A (en) * | 2016-06-13 | 2016-08-31 | 佛山市腾瑞医药科技有限公司 | Olaparib effervescent tablet and preparation method thereof |
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Application publication date: 20180504 |
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