CN107898764A - A kind of net compositions of Ai Gelie - Google Patents
A kind of net compositions of Ai Gelie Download PDFInfo
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- CN107898764A CN107898764A CN201711315903.9A CN201711315903A CN107898764A CN 107898764 A CN107898764 A CN 107898764A CN 201711315903 A CN201711315903 A CN 201711315903A CN 107898764 A CN107898764 A CN 107898764A
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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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
- A61K9/2009—Inorganic compounds
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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
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to a kind of net tablet compositions of Ai Gelie, belong to technical field of medicine.In the net compositions of unit dose Ai Gelie of the present invention, contain D90For net 5 15mg of 90 150 microns of Ai Gelie, 50 80mg of lactose, 6 12mg of chitosan, 0.8 1.5mg of lauryl sodium sulfate, 6 10mg of beta cyclodextrin, 12 20mg of sodium citrate, 8 15mg of aerosil, 4 8mg of PVP K30,4 8mg of crospovidone, 1 1.5mg of magnesium stearate.The present invention provides a kind of net tablet compositions of the Ai Gelie of stabilization.
Description
Technical field
The present invention relates to a kind of net tablet compositions of Ai Gelie, belong to technical field of medicine.
Background technology
Diabetes are one group of metabolic diseases characterized by hyperglycaemia.Counted according to International Diabetes Federation, 2014 complete
Ball diabetic is up to 3.87 hundred million people, it is contemplated that is up to 5.92 hundred million people within 2035.Type ii diabetes are the most common shape of diabetes
Formula, accounts for the 90% of diabetic.
Diabetes can cause the various tissues of human body, especially eye, kidney, heart, blood vessel, the chronic lesion of nerve, function
Obstacle.Once as diabetic, it is necessary to take medicine throughout one's life.Diabetes not only influence the quality of life of patient, it is also possible to lead
Cause the shortening in service life.
Ai Gelie is net, English name Ertugliflozin, and chemistry is entitled：1,6- dehydrations -1-C- [the chloro- 3- of 4-
[(4- ethoxyl phenenyls) methyl] phenyl] -5-C- (hydroxymethyl)-BETA-L- idoses, mode of being used as medicine is Ai Gelie net-burnt
Glutamic acid compound, Mo Shadong (Merck) and Pfizer (Pfizer) company joint research and development, submit listing in March, 2017 to FDA
Application.Ai Gelie belongs to small dimension preparation only, commercially available to have 5mg and 15mg；Ai Gelie is only not soluble in water, and complicated.Work
Middle discovery, the net piece dissolution rates of Ai Gelie are not to control very well, and it is in positive growth that it, which stores more than 6 months related materials,.
The content of the invention
The object of the present invention is to provide it is a kind of meet standard requirement the net compositions of Ai Gelie, solve preparation dissolution rate and
Related material instability problem.
Technical solution：
The technical scheme is that：
A kind of net compositions of Ai Gelie, in the composition of unit dose, contain D90For the net 5- of 90-150 microns of Ai Gelie
15mg, lactose 50-80mg, chitosan 6-12mg, lauryl sodium sulfate 0.8-1.5mg, beta cyclodextrin 6-10mg, sodium citrate
12-20mg, aerosil 8-15mg, PVP K30 4-8mg, crospovidone 4-8mg, magnesium stearate 1-1.5mg.
Currently preferred technical solution is：In the composition of unit dose, contain D90For 110-140 microns of Ai Gelie
Net 5-15mg, lactose 60-70mg, chitosan 8-10mg, lauryl sodium sulfate 1.0-1.3mg, beta cyclodextrin 7-9mg, citric acid
Sodium 14-18mg, aerosil 10-13mg, PVP K30 4-8mg, crospovidone 4-8mg, magnesium stearate 1-
1.5mg。
Currently preferred technical solution is：In the composition of unit dose, contain D90For the net 5- of 130 microns of Ai Gelie
15mg, lactose 65mg, chitosan 9mg, lauryl sodium sulfate 1.2mg, beta cyclodextrin 8mg, sodium citrate 16mg, gas phase dioxy
SiClx 12mg, PVP K30 5mg, crospovidone 5mg, magnesium stearate 1.2mg.
In technical solution of the present invention, lauryl sodium sulfate, sodium citrate, chitosan, aerosil, beta cyclodextrin
It is to realize the indispensable factor of the object of the invention.Lauryl sodium sulfate, beta cyclodextrin assist to improve dissolution jointly；Citric acid
Sodium, chitosan, aerosil play positive effect for the stabilization of tablet.
The preparation method of the net compositions of Ai Gelie of the present invention, comprises the following steps：
First step Ai Gelie is crushed to the granularity of needs only, other auxiliary materials cross 100 mesh sieves respectively；
Second step weighs that Ai Gelie of the recipe quantity after the first step is handled is net, lauryl sodium sulfate, β rings paste with recipe quantity
Be skillful in mixing 30-60 minutes in conical mixer, then mixed with the aerosil of recipe quantity, then with half recipe quantity
Lactose and the chitosan of half recipe quantity mix, with the PVP K30 wet granulation of 2/3rds recipe quantities, 45 DEG C
Vacuum drying, crosses 80 mesh sieves；
3rd step mixes the sodium citrate of particle obtained by second step and recipe quantity, crospovidone, then with remaining half
The lactose of recipe quantity and the chitosan of half recipe quantity mix, with the PVP K30 wet method of remaining 1/3rd recipe quantities
Granulation, 45 DEG C of vacuum drying, crosses 80 mesh sieves；
4th step adds the magnesium stearate of recipe quantity, mixes, tabletting.
Preparation method of the present invention, to the stabilization of uniformity of dosage units, and stabilization in relation to material has played positive work
With.Raising to dissolution rate plays certain effect.
Useful achievement：
Technical solution of the present invention provides a kind of net tablet compositions of the Ai Gelie of stabilization, and said composition has excellent dissolution rate,
And before the deadline, its related content of material is stable.Current tablet is solved during storage, related material is elevated
Problem.
Preparation method of the present invention, solves the problems, such as that the net tablet content uniformitys of Ai Gelie are exceeded.
1. D of embodiment90For the net 5g of 90 microns of Ai Gelie, lactose 80g, chitosan 6g, lauryl sodium sulfate 0.8g, β
Cyclodextrin 6g, sodium citrate 12g, aerosil 15mg, PVP K30 4g, crospovidone 4g, magnesium stearate 1g,
Preparation method prepares 1000 as described in technical solution.
2. D of embodiment90For the net 15g of 150 microns of Ai Gelie, lactose 80g, chitosan 12g, lauryl sodium sulfate
1.5g, beta cyclodextrin 10g, sodium citrate 20g, aerosil 8g, PVP K30 8g, crospovidone 8g, stearic acid
Magnesium 1.5g, preparation method prepares 1000 as described in technical solution.
3. D of embodiment90For the net 10g of 130 microns of Ai Gelie, lactose 65g, chitosan 9g, lauryl sodium sulfate
1.2g, beta cyclodextrin 8g, sodium citrate 16g, aerosil 12g, PVP K30 5g, crospovidone 5g, stearic acid
Magnesium 1.2g, preparation method prepares 1000 as described in technical solution.
1. embodiment of reference examples, 3 prescription, cuts sodium citrate, chitosan.It is specific as follows：
Prescription：D90For the net 10g of 130 microns of Ai Gelie, lactose 90g, lauryl sodium sulfate 1.2g, beta cyclodextrin 8g, gas phase
Silica 1 2g, PVP K30 5g, crospovidone 5g, magnesium stearate 1.2g, 1000 are prepared by following preparation methods
Piece.
First step Ai Gelie is crushed to D only90For 130 microns, other auxiliary materials cross 100 mesh sieves respectively；
Second step weighs that Ai Gelie of the recipe quantity after the first step is handled is net, lauryl sodium sulfate, β rings paste with recipe quantity
Be skillful in mixing 30-60 minutes in conical mixer, then mixed with the aerosil of recipe quantity, then with half recipe quantity
Lactose mix, with the PVP K30 wet granulation of 2/3rds recipe quantities, 45 DEG C of vacuum drying, cross 80 mesh sieves；
3rd step mixes the crospovidone of particle obtained by second step and recipe quantity, then with remaining half recipe quantity
Lactose mixes, and with the PVP K30 wet granulation of remaining 1/3rd recipe quantities, 45 DEG C of vacuum drying, cross 80 mesh sieves；
4th step adds the magnesium stearate of recipe quantity, mixes, tabletting.
Reference examples 2,3 prescription of embodiment, cut lauryl sodium sulfate and beta cyclodextrin.It is specific as follows：
Prescription：D90For the net 10g of 130 microns of Ai Gelie, lactose 74.2g, chitosan 9g, sodium citrate 16g, gas phase titanium dioxide
Silicon 12g, PVP K30 5g, crospovidone 5g, magnesium stearate 1.2g, 1000, are prepared by following preparation methods
First step Ai Gelie is crushed to D only90For 130 microns, other auxiliary materials cross 100 mesh sieves respectively；
Second step weighs that Ai Gelie of the recipe quantity after the first step is handled is net, is mixed with the aerosil of recipe quantity, then with
The lactose of half recipe quantity and the chitosan of half recipe quantity mix, with the PVP K30 of 2/3rds recipe quantities
Wet granulation, 45 DEG C of vacuum drying, crosses 80 mesh sieves；
3rd step mixes the sodium citrate of particle obtained by second step and recipe quantity, crospovidone, then with remaining half
The lactose of recipe quantity and the chitosan of half recipe quantity mix, with the PVP K30 wet method of remaining 1/3rd recipe quantities
Granulation, 45 DEG C of vacuum drying, crosses 80 mesh sieves；
4th step adds the magnesium stearate of recipe quantity, mixes, tabletting.
Preparation method of the present invention plays positive effect for the stabilization of uniformity of dosage units.
Reference examples 3,3 prescription of embodiment, one-step method pelletizing press sheet.It is specific as follows：
Prescription：D90For the net 10g of 130 microns of Ai Gelie, lactose 65g, chitosan 9g, lauryl sodium sulfate 1.2g, β ring paste
Smart 8g, sodium citrate 16g, aerosil 12g, PVP K30 5g, crospovidone 5g, magnesium stearate 1.2g.Press
Following preparation methods prepare 1000.
First step Ai Gelie is crushed to D only90For 130 microns, other auxiliary materials cross 100 mesh sieves respectively；
Second step weighs that Ai Gelie of the recipe quantity after the first step is handled is net, lauryl sodium sulfate, β rings paste with recipe quantity
Be skillful in mixing 30-60 minutes in conical mixer, then with the aerosil of recipe quantity, lactose, chitosan, sodium citrate,
Crospovidone mixes, and with the PVP K30 wet granulation of recipe quantity, 45 DEG C of vacuum drying, cross 80 mesh sieves；
3rd step adds the magnesium stearate of recipe quantity, mixes, tabletting.
Each 100 of the product of test example 1, respectively Example 1-3 and reference examples 1-3, it is aluminum-plastic packaged, it is placed in constant temperature and humidity
In case, 25 DEG C, relative humidity 65%, stores 12 months and takes out, high performance liquid chromatography measures related material, data record respectively
In table 1.
Table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Reference examples 1 | Reference examples 2 | Reference examples 3 | |
| 0 day related material, % | 0.16 | 0.17 | 0.16 | 0.28 | 0.21 | 0.24 |
| 12nd the end of month related material, % | 0.18 | 0.17 | 0.18 | 0.68 | 0.28 | 0.46 |
1 data of table illustrate that for product of the embodiment of the present invention during storage, related content of material is stable.And reference examples are produced
The related material rise of product especially reference examples 1 and reference examples 3 is obvious.Illustrate that sodium citrate in technical solution of the present invention, shell gather
The addition of sugar, and preparation method of the present invention, positive effect is played for the stabilization in relation to material.
Test example 2, measure by the Rotating shaker of States Pharmacopoeia specifications embodiment 1-3 and reference examples 1-2 products respectively the 60th point
The dissolution rate of clock.Using the hydrochloric acid solution that pH value is 1 as dissolution medium, data record is in table 2.
Table 2
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Reference examples 2 | |
| 60th minute dissolution rate, % | 89.76 | 88.94 | 90.26 | 68.79 |
2 data of table illustrate that the product of 1-3 of the embodiment of the present invention, its accumulation dissolution rate of the 60th minute is more than 85%, meets mark
The requirement of quasi- States Pharmacopoeia specifications, and reference examples 2, since the addition of no lauryl sodium sulfate and beta cyclodextrin, its dissolution rate are serious
It is unqualified, illustrate in technical solution of the present invention, the raising of the addition of lauryl sodium sulfate and beta cyclodextrin to dissolution rate plays
Positive effect.
Claims (4)
1. a kind of net compositions of Ai Gelie, it is characterised in that in the composition of unit dose, contain D90For 90-150 microns of angstrom
Lattice arrange net 5-15mg, lactose 50-80mg, chitosan 6-12mg, lauryl sodium sulfate 0.8-1.5mg, beta cyclodextrin 6-10mg,
Sodium citrate 12-20mg, aerosil 8-15mg, PVP K30 4-8mg, crospovidone 4-8mg, magnesium stearate
1-1.5mg。
2. according to the net compositions of Ai Gelie described in claim 1, it is characterised in that in the composition of unit dose, contain D90For
110-140 microns of Ai Gelie net 5-15mg, lactose 60-70mg, chitosan 8-10mg, lauryl sodium sulfate 1.0-1.3mg,
Beta cyclodextrin 7-9mg, sodium citrate 14-18mg, aerosil 10-13mg, PVP K30 4-8mg, crospovidone
4-8mg, magnesium stearate 1-1.5mg.
3. according to the net compositions of Ai Gelie described in claim 1, it is characterised in that in the composition of unit dose, contain D90For
130 microns of Ai Gelie net 5-15mg, lactose 65mg, chitosan 9mg, lauryl sodium sulfate 1.2mg, beta cyclodextrin 8mg, lemon
Lemon acid sodium 16mg, aerosil 12mg, PVP K30 5mg, crospovidone 5mg, magnesium stearate 1.2mg.
4. the preparation method of the net compositions of Ai Gelie described in claim 1, it is characterised in that comprise the following steps：
First step Ai Gelie is crushed to the granularity of needs only, other auxiliary materials cross 100 mesh sieves respectively；
Second step weighs that Ai Gelie of the recipe quantity after the first step is handled is net, lauryl sodium sulfate, β rings paste with recipe quantity
Be skillful in mixing 30-60 minutes in conical mixer, then mixed with the aerosil of recipe quantity, then with half recipe quantity
Lactose and the chitosan of half recipe quantity mix, with the PVP K30 wet granulation of 2/3rds recipe quantities, 45 DEG C
Vacuum drying, crosses 80 mesh sieves；
3rd step mixes the sodium citrate of particle obtained by second step and recipe quantity, crospovidone, then with remaining half
The lactose of recipe quantity and the chitosan of half recipe quantity mix, with the PVP K30 wet method of remaining 1/3rd recipe quantities
Granulation, 45 DEG C of vacuum drying, crosses 80 mesh sieves；
4th step adds the magnesium stearate of recipe quantity, mixes, tabletting.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711315903.9A CN107898764A (en) | 2017-12-12 | 2017-12-12 | A kind of net compositions of Ai Gelie |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711315903.9A CN107898764A (en) | 2017-12-12 | 2017-12-12 | A kind of net compositions of Ai Gelie |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102149717A (en) * | 2008-08-28 | 2011-08-10 | 辉瑞大药厂 | Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives |
| CN104721207A (en) * | 2014-07-23 | 2015-06-24 | 迪沙药业集团有限公司 | Drug composition |
| CN105646603A (en) * | 2016-03-01 | 2016-06-08 | 孙霖 | Crystal form A of ertugliflozin and preparation method |
-
2017
- 2017-12-12 CN CN201711315903.9A patent/CN107898764A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102149717A (en) * | 2008-08-28 | 2011-08-10 | 辉瑞大药厂 | Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives |
| CN104721207A (en) * | 2014-07-23 | 2015-06-24 | 迪沙药业集团有限公司 | Drug composition |
| CN105646603A (en) * | 2016-03-01 | 2016-06-08 | 孙霖 | Crystal form A of ertugliflozin and preparation method |
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