CN107982236A - A kind of felodipine sustained-release tablets - Google Patents
A kind of felodipine sustained-release tablets Download PDFInfo
- Publication number
- CN107982236A CN107982236A CN201810012341.9A CN201810012341A CN107982236A CN 107982236 A CN107982236 A CN 107982236A CN 201810012341 A CN201810012341 A CN 201810012341A CN 107982236 A CN107982236 A CN 107982236A
- Authority
- CN
- China
- Prior art keywords
- release tablets
- felodipine
- cellulose
- felodipine sustained
- hydroxypropyl
- 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.)
- Pending
Links
Classifications
-
- 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
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- 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
- A61K9/2095—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
Abstract
The invention belongs to technical field of pharmaceuticals, is related to a kind of felodipine sustained-release tablets, it, which is formulated to form by weight percentage, is：Felodipine 1~5%, hydroxypropyl methyl cellulose 5~20%, hydroxypropyl cellulose 1~10%, hydrophobicity filler 10~40%, hydrophilic filler 40~70%, other pharmaceutic adjuvants 5~20%.The present invention can make the release more constant speed of medicine uniform.
Description
Technical field
The invention belongs to technical field of pharmaceuticals, relates in particular to a kind of felodipine sustained-release tablets.
Background technology
Felodipine, chemical name are (±) -2,6- dimethyl -4- (2,3- dichlorophenyl)-Isosorbide-5-Nitrae-dihydro -3,5- pyridine
Dicarboxylic acid methyl ester ethyl ester, English name FELODIPINE, molecular formula C18H19Cl2NO4, molecular weight 384.25, chemistry
Structural formula is as follows：
For white to pale yellow crystals or crystalline powder；It is odorless, it is tasteless；Meet photo-labile；In acetone, methanol or ethanol
In it is readily soluble, it is almost insoluble in water.
Felodipine is dihydropyridine class calcium channel blocker, has the cardioselective of height, to blood vessel and the heart
Dirty selectivity ratio is 100.Angiosthenia is reduced by reducing peripheral vascular resistance, to myocardial contraction in the range of therapeutic dose
Power and cardiac conduction are without directly effect.Vein smooth muscle and adrenergic antiotasis are adjusted without influence, therefore do not caused straight
Vertical property low blood pressure, has reduction effect to systolic pressure and diastolic pressure.In addition, felodipine is minimum to myocardium negative effects, for a long time
There is positive meaning using the reverse to hypertensive patient's left ventricular hypertrophy and vascular remodeling.
At present, in the market mainly has felodipine ordinary tablet and sustained release tablets, and wherein ordinary tablet needs take medicine for one day 2~3 times,
Medicining times are more, and blood concentration peak valley is than greatly, causing fluctuation of blood pressure big.Sustained release tablets are slow due to releasing the drug, and reduce medication frequency
Rate, blood concentration peak valley is than reducing, and fluctuation of blood pressure is relatively reduced, and patient's compliance is improved.It is but presently commercially available
Sustained release tablets cause decompression not steady enough, reduce felodipine and delay there is release not constant speed or the problem of keep off constant speed
Release the clinical application effect of piece.
The content of the invention
The object of the present invention is to provide a kind of felodipine sustained-release tablets, make the release more constant speed of medicine uniform.
Felodipine sustained-release tablets of the present invention, it is as follows that it is formulated composition by weight percentage：
Wherein, the viscosity of hydroxypropyl cellulose is all higher than 1500mPa.s.
The hydroxypropyl methyl cellulose is HPMC K4M, hydroxypropyl methyl cellulose K15M, hydroxypropyl
One kind in methylcellulose K100M, or two of which and two or more mixtures.
The hydroxypropyl cellulose is one kind in hydroxypropyl cellulose HF, hydroxypropyl cellulose MF, or two kinds mixed
Compound.
The hydrophobicity filler is microcrystalline cellulose, one kind in calcium carbonate, calcium monohydrogen phosphate, or two of which and two
The mixture of the kind above.
The hydrophilic filler is Lactis Anhydrous, sucrose, one kind in mannitol, or two of which and two or more
Mixture.
Other pharmaceutic adjuvants are rilanit special, superfine silica gel powder, propylgallate, sodium stearyl fumarate, poly- dimension
One kind in ketone, or two of which and two or more mixtures.
The preparation process of felodipine sustained-release tablets is：
By felodipine, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydrophobicity filler, hydrophilic filler mistake
After sieve, it is uniformly mixed with other pharmaceutic adjuvants, ethanol solution is wetting agent granulation, drying, adds lubricant whole grain to mix, measure half
The content of finished particle, tabletting, be coated to obtain felodipine sustained-release tablets.
The present invention fills hydroxypropyl methyl cellulose and Klucel EF, hydrophobicity filler, hydrophily
Agent is used cooperatively, it is ensured that and insoluble drug felodipine can discharge completely, and reach constant speed or close to constant speed release medicine effect,
Make the release more constant speed of medicine uniform, effective felodipine blood concentration can be maintained for a long time, effectively controlling of blood pressure exists
Normal level, so as to reduce fluctuation of blood pressure, realizes steady decompression, significantly reduces because fluctuation of blood pressure is to heart, kidney etc.
The damage of organ, improves the compliance of patient medication.
Embodiment
Embodiment 1
Embodiment 2
Embodiment 3
Embodiment 4
Embodiment 5
Embodiment 6
Embodiment 7
Embodiment 8
Embodiment 9
Embodiment 10
Drug release determination
Take 1-10 of the embodiment of the present invention prepare felodipine sustained-release tablets, according to drug release determination method (《Chinese Pharmacopoeia》
Two the first methods of annex XD of version in 2015), 0.4% cetyl trimethylammonium bromide phosphate buffer (pH6.5) is release
Medium, volume 500ml, rotating speed 100r/min, 37 ± 0.5 DEG C of temperature, operates in accordance with the law.In 0.5h, 1h, 2h, 4h, 7h, 12h, 24h
Take solution 5ml to filter, and same volume, mutually synthermal blank dissolution medium is replenished in time, subsequent filtrate is taken, according to high-efficient liquid phase color
Spectrometry (《Chinese Pharmacopoeia》The two annex VD of version in 2015) experiment.Chromatographic condition and system suitability：With octadecyl silicon
Alkane bonded silica gel is filler, and acetonitrile-methanol-phosphate buffer (pH3.0) is mobile phase；Detection wavelength 254nm.In addition it is smart
The close felodipine reference substance that weighs is appropriate, and after ethanol dissolving, along with stating, dissolution medium dilution is quantitative, is measured in the same method, counts respectively
Calculate the release of the different time points of every felodipine sustained-release tablets.
Releasing result is as follows：
By above release result as it can be seen that with market product felodipine sustained-release tablets (trade name：Plendil) ratio, the present invention
The felodipine sustained-release tablets drug release is more uniform, has zero order kinetics feature, and more preferable steady blood pressure, it is suitable to improve patient medication
Ying Xing.
Claims (6)
1. a kind of felodipine sustained-release tablets, it is characterised in that it is as follows that it is formulated composition by weight percentage：
Wherein, the viscosity of hydroxypropyl cellulose is greater than or equal to 1500mPa.s.
2. felodipine sustained-release tablets according to claim 1, it is characterised in that:The hydroxypropyl methyl cellulose is hydroxypropyl
One kind in methylcellulose K4M, hydroxypropyl methyl cellulose K15M, hydroxypropyl methyl cellulose K100M, or two of which with
And two or more mixture.
3. felodipine sustained-release tablets according to claim 1, it is characterised in that:The hydroxypropyl cellulose is hydroxy propyl cellulose
One kind in plain HF, hydroxypropyl cellulose MF, or two kinds of the mixture.
4. felodipine sustained-release tablets according to claim 1, it is characterised in that:The hydrophobicity filler is microcrystalline cellulose
One kind in element, calcium carbonate, calcium monohydrogen phosphate, or two of which and two or more mixtures.
5. felodipine sustained-release tablets according to claim 1, it is characterised in that:The hydrophilic filler for Lactis Anhydrous,
One kind in sucrose, mannitol, or two of which and two or more mixtures.
6. felodipine sustained-release tablets according to claim 1, it is characterised in that:Other pharmaceutic adjuvants are hydrogenated castor
One kind in oil, superfine silica gel powder, propylgallate, sodium stearyl fumarate, povidone, or two of which and two or more
Mixture.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810012341.9A CN107982236A (en) | 2018-01-05 | 2018-01-05 | A kind of felodipine sustained-release tablets |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810012341.9A CN107982236A (en) | 2018-01-05 | 2018-01-05 | A kind of felodipine sustained-release tablets |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107982236A true CN107982236A (en) | 2018-05-04 |
Family
ID=62040818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810012341.9A Pending CN107982236A (en) | 2018-01-05 | 2018-01-05 | A kind of felodipine sustained-release tablets |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107982236A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112245399A (en) * | 2020-10-29 | 2021-01-22 | 西南医科大学 | Dihydromyricetin gastric floating pill and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090285889A1 (en) * | 2008-05-14 | 2009-11-19 | Capricom Pharma Inc. | Modified release formulations of dihydropyridine compounds and methods of making same |
| CN101627976A (en) * | 2008-07-17 | 2010-01-20 | 北京科信必成医药科技发展有限公司 | Felodipine sustained-release preparation and preparation method thereof |
-
2018
- 2018-01-05 CN CN201810012341.9A patent/CN107982236A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090285889A1 (en) * | 2008-05-14 | 2009-11-19 | Capricom Pharma Inc. | Modified release formulations of dihydropyridine compounds and methods of making same |
| CN101627976A (en) * | 2008-07-17 | 2010-01-20 | 北京科信必成医药科技发展有限公司 | Felodipine sustained-release preparation and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| 朱雨秋等: "非洛地平缓释片的研制及其体外释放研究", 《药学实践杂志》 * |
| 谢向阳等: "中心复合设计_效应面法优化非洛地平缓释片处方", 《医药导报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112245399A (en) * | 2020-10-29 | 2021-01-22 | 西南医科大学 | Dihydromyricetin gastric floating pill and preparation method thereof |
| CN112245399B (en) * | 2020-10-29 | 2023-02-28 | 西南医科大学 | Dihydromyricetin gastric floating pill and preparation method thereof |
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| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180504 |