CN104758938B - It is a kind of to treat felodipine tablet of hypertension and preparation method thereof - Google Patents
It is a kind of to treat felodipine tablet of hypertension and preparation method thereof Download PDFInfo
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- CN104758938B CN104758938B CN201510151689.2A CN201510151689A CN104758938B CN 104758938 B CN104758938 B CN 104758938B CN 201510151689 A CN201510151689 A CN 201510151689A CN 104758938 B CN104758938 B CN 104758938B
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Abstract
The invention belongs to technical field of medicine, disclose and a kind of treat felodipine tablet of hypertension and preparation method thereof, the tablet is formed by medicine-containing particle with direct tablet compressing after lubricant mixing, and medicine-containing particle therein contains felodipine, Tween 80, PVPP and filler.Tablet medicine dissolution prepared by the present invention is rapid, and steady quality, preparation method is simple, it is not necessary to complicated preparation equipment, it is easy to industrialized production.
Description
Technical field
The invention belongs to technical field of medicine, in particular to a kind of solid orally ingestible, more particularly to one kind
Tablet containing felodipine and preparation method thereof.
Background technology
Felodipine, chemical name is 2,6- dimethyl -4- (2,3- dichlorophenyl)-Isosorbide-5-Nitrae-dihydro -3,5- pyridine diformazan
Sour methyl ethyl ester, is a kind of selective cerebrocrast, with preferable antihypertensive effect.The Hypotensive Mechanism of felodipine is mainly
By suppressing the interior stream of calcium outside petty action smooth muscle cells, selectivity expansion parteriole, while to the heart in the range of therapeutic dose
Myotility and cardiac conduction on vein smooth muscle and adrenaline blood vessel tension force without influence, therefore are difficult to cause without directly acting on
Postural hypotension.Meanwhile, the cheap, safe of felodipine also becomes one of the most frequently used antihypertensive drugs.
As a member in numerous insoluble drugs, felodipine solubility in water is 0.00058mg/ml, is corresponded to
5mg raw materials need 8621ml water to dissolve, thus it is equally existed that the bioavilability as caused by low solubility is low, drug effect by
To the problem of influence.As can be seen here, improve and control the rate of dissolution and solubility of felodipine to turn into felodipine preparation
Develop the matter of utmost importance faced.Felodipine tablets are the commercially available main formulations of felodipine, commonly use 2.5mg/ pieces, two kinds of 5mg/ pieces
Specification, is recorded in Pharmacopoeia of People's Republic of China.
CN102462663A discloses a kind of depressor felodipine Pharmaceutical composition and preparation method thereof, and said composition is included
Felodipine, dispersant, filler, disintegrant, solubilizer, lubricant and adhesive, method are first by felodipine with disperseing
After agent is micronized together, then felodipine pharmaceutical preparation prepared using dry granulation, it is to avoid the use of water and organic solvent, subtracted
Lack damp and hot process and energy consumption, be easy to the quality control in production process.
CN103006568A discloses a kind of felodipine medicine solid dispersion thing and preparation method thereof, and it is with slightly solubility medicine
Thing felodipine is active component, after active medicine is well mixed according to a certain percentage with macromolecule carrier, is squeezed by hot melt
Go out the solid dispersion thing that method prepares felodipine, wherein, felodipine medicine accounts for the 10 of whole solid dispersion thing gross mass
~40%.
Above-mentioned art methods serve the effect of solubilising, but system to the dissolving of felodipine medicine to a certain extent
Standby complex process, the requirement to production equipment and operation is higher.
The content of the invention
In view of the deficiencies in the prior art, it is an object of the invention to provide a kind of technique is simple, dissolution is rapid, steady quality
Felodipine tablet.
In order to realize the purpose of the present invention, inventor creatively dissolves felodipine in ethanol, addition Tween 80,
PVPP, stirs, using this suspension as adhesive, is pharmaceutically pelletized on acceptable filler, as a result medicine
Thing Fast Stripping.Specifically, the purpose of the present invention is achieved by the following technical solution：
A kind of felodipine tablet for treating hypertension, the tablet by medicine-containing particle and lubricant mix after direct tablet compressing and
Into medicine-containing particle therein contains felodipine, Tween 80, PVPP and filler.
Preferably, felodipine tablet as described above, medicine-containing particle therein is prepared as follows forming：By non-Lip river
Horizon dissolves in ethanol, then adds Tween 80, PVPP, stirs, filled out using this suspension as adhesive
Fill in agent and pelletize, dry and obtain.
It is further preferred that felodipine tablet as described above, wherein felodipine, Tween 80 and PVPP
Quality amount ratio is 1：(0.5~1.5)：(2~4).
Still further preferably, felodipine tablet as described above, filler therein be lactose, microcrystalline cellulose and
One or more in pregelatinized starch.
Still further preferably, felodipine tablet as described above, lubricant therein is magnesium stearate, stearic acid richness
One or more in horse acid sodium and talcum powder.
Present invention also offers the preparation method of above-mentioned felodipine tablet, this method comprises the following steps：By non-Lip river
Flat dissolving in ethanol, is then added Tween 80, PVPP, stirs, pelletized with this suspension on filler, is done
It is dry, obtain medicine-containing particle；Uniform, the tabletting by this medicine-containing particle and mix lubricant.
Compared with prior art, felodipine tablet of the present invention and preparation method thereof has the following advantages that and significantly
Progressive：Drug-eluting is rapid, and steady quality, preparation method is simple, it is not necessary to complicated preparation equipment, it is easy to which industrialization is big raw
Production.
Embodiment
The preparation process and implementation result of the present invention, but the protection of the present invention are now further described by following examples
Scope is not limited to following examples.
Embodiment 1：The preparation of felodipine tablet
Preparation method：
The felodipine of recipe quantity is added in ethanol, is stirred to dissolve, Tween 80, the crosslinking for then adding recipe quantity are poly-
Ketone is tieed up, stirs, is pelletized with this suspension on the mixed powder of lactose and microcrystalline cellulose, 40 DEG C of dryings obtain medicine-containing particle；
This medicine-containing particle is crossed into 20 mesh sieves, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Embodiment 2：The preparation of felodipine tablet
Preparation method：
The felodipine of recipe quantity is added in ethanol, is stirred to dissolve, Tween 80, the crosslinking for then adding recipe quantity are poly-
Ketone is tieed up, stirs, is pelletized with this suspension on the microcrystalline cellulose of recipe quantity, 45 DEG C of dryings obtain medicine-containing particle；By this
Medicine-containing particle crosses 18 mesh sieves, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Embodiment 3：The preparation of felodipine tablet
Preparation method：
By the felodipine of recipe quantity, add in ethanol, be stirred to dissolve, then add Tween 80, the crosslinking of recipe quantity
PVP, stirs, and is pelletized with this suspension on the microcrystalline cellulose of recipe quantity, and 45 DEG C of dryings obtain medicine-containing particle；Will
This medicine-containing particle crosses 18 mesh sieves, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Comparative example 1：The preparation of felodipine tablet
Preparation method：
Felodipine is crossed into 200 mesh sieves, recipe quantity is weighed, Tween 80, PVPP and microcrystalline cellulose with recipe quantity
Element (crossing 160 mesh sieves) is well mixed, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Comparative example 2：The preparation of felodipine tablet
Preparation method：
The felodipine of recipe quantity is crossed into 200 mesh sieves, then mixed with crossing the PVPP of 160 mesh sieves, microcrystalline cellulose
Close uniform, obtain mixed powder；The Tween 80 of recipe quantity is dissolved in ethanol, pelletized in this, as adhesive on the mixed powder, 45 DEG C are done
It is dry, obtain medicine-containing particle；This medicine-containing particle is crossed into 18 mesh sieves, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Comparative example 3：The preparation of felodipine tablet
Preparation method：
The felodipine of recipe quantity is added in ethanol, is stirred to dissolve, Tween 80, the carboxymethyl of recipe quantity is then added
Sodium starch, stirs, and is pelletized with this suspension on the microcrystalline cellulose of recipe quantity, and 45 DEG C of dryings obtain medicine-containing particle；Will
This medicine-containing particle crosses 18 mesh sieves, is then well mixed with the magnesium stearate of recipe quantity, tabletting.
Embodiment 4：The quality testing experiment of Felodipine tablets
Dissolution determination.The Felodipine tablets 10 for taking each embodiment and comparative example to prepare respectively, according to dissolution method
(paddle board method), using pure water solution 900ml as solvent, rotating speed is 50 turns per minute, operates in accordance with the law, during through 5 minutes, takes solution appropriate
Filtration, discards at least 10ml primary filtrates, and precision measures subsequent filtrate in right amount, and solubilization goes out medium and is made in every 1ml containing 2.8 μ g
Solution, is used as need testing solution.Another precision weighs reference substance 28mg, puts in 200ml measuring bottles, plus methanol dissolves and is diluted to quarter
Degree, shakes up, precision measures 2ml, puts in 100ml measuring bottles, solubilization goes out medium to scale, shakes up, and is used as reference substance solution.Essence
It is close to measure each 50 μ l of above two solution, liquid chromatograph is injected, chromatogram is recorded；It is molten with calculated by peak area every by external standard method
Output, limit is respectively the 80% of labelled amount, should meet regulation.
Chromatographic condition and system suitability.Using octadecylsilane chemically bonded silica as filler, with methanol-water-
14.05% sodium perchlorate solution -8.5% (v/v) perchloric acid solution (65:25:8:2) it is mobile phase, Detection wavelength is 238nm,
Column temperature is set as 25 DEG C, adjustment flow velocity makes felodipine peak retention time be about 12 minutes, and number of theoretical plate is based on felodipine peak
Calculation should be not less than 3000, and tailing factor should be not more than 1.5.
Each embodiment Dissolution of Tablet measurement result of table 1
The Felodipine tablets dissolution rate prepared from the results showed that embodiment of the present invention 1-3 of table 1 is rapid, accelerates examination
Front and rear dissolution rate is tested to be basically unchanged；And comparative example 1 uses tablet prepared by the method for supplementary material mixing direct tablet compressing, its medicine is molten
Go out slow；The tablet that comparative example 2 is prepared using the ethanol solution of Tween 80 as adhesive, its dissolution is also relatively slow, and dissolution after acceleration
Degree is decreased obviously；PVPP is replaced with sodium carboxymethyl starch by comparative example 3, and the result of extraction of the tablet as a result prepared is significantly
Decline.
Claims (4)
1. a kind of felodipine tablet for treating hypertension, it is characterised in that the tablet is after medicine-containing particle and lubricant are mixed
Direct tablet compressing is formed, and medicine-containing particle therein is made up of felodipine, Tween 80, PVPP and filler, by such as lower section
Method is prepared from：By felodipine dissolving in ethanol, Tween 80, PVPP are then added, stirs, is suspended with this
Liquid pelletizes on filler as adhesive, dries and obtain；The quality amount ratio of felodipine, Tween 80 and PVPP is
1：（0.5~1.5）：（2~4）.
2. felodipine tablet according to claim 1, it is characterised in that described filler is lactose, microcrystalline cellulose
One or more in element and pregelatinized starch.
3. felodipine tablet according to claim 1, it is characterised in that described lubricant is magnesium stearate, tristearin
One or more in furmaric acid sodium and talcum powder.
4. the preparation method of felodipine tablet according to claim 1, it is characterised in that this method includes following step
Suddenly：By felodipine dissolving in ethanol, Tween 80, PVPP are then added, is stirred, with this suspension in filling
Pelletized in agent, dry, obtain medicine-containing particle；Uniform, the tabletting by this medicine-containing particle and mix lubricant.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510151689.2A CN104758938B (en) | 2015-04-01 | 2015-04-01 | It is a kind of to treat felodipine tablet of hypertension and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510151689.2A CN104758938B (en) | 2015-04-01 | 2015-04-01 | It is a kind of to treat felodipine tablet of hypertension and preparation method thereof |
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| CN104758938B true CN104758938B (en) | 2017-08-29 |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0274176A2 (en) * | 1987-01-09 | 1988-07-13 | ELAN CORPORATION, Plc | Sustained release capsule or tablet formulation |
| 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 |
| CN101744786A (en) * | 2008-12-17 | 2010-06-23 | 南京星银药业有限公司 | Prescription of felodipine sustained-release tablets and preparation method |
-
2015
- 2015-04-01 CN CN201510151689.2A patent/CN104758938B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0274176A2 (en) * | 1987-01-09 | 1988-07-13 | ELAN CORPORATION, Plc | Sustained release capsule or tablet formulation |
| 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 |
| CN101744786A (en) * | 2008-12-17 | 2010-06-23 | 南京星银药业有限公司 | Prescription of felodipine sustained-release tablets and preparation method |
Non-Patent Citations (1)
| Title |
|---|
| COMPARATIVE STUDY ON EFFECT OF DIFERENT TECHNIQUES USED IN THE FORMULATION OF FELODIPINE FAST DISSOLVING TABLETS;RAGHAVENDRA RAO N. G. et al.;《International Journal of Pharmacy and Pharmaceutical Sciences》;20101231;第2卷;152-158页 * |
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Inventor after: Lu Baocai Inventor after: Liu Xiaohong Inventor after: Gao Jianlian Inventor after: Wang Jincai Inventor after: Miao Wenjie Inventor after: Wu Zhiyan Inventor after: Yu Wenfa Inventor before: Jia Hongrui |
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Effective date of registration: 20170803 Address after: 453100 No. 88 health Road, Weihui, Henan, Xinxiang Applicant after: The First Affiliated Hospital of Xinxiang Medical University Address before: 722405 Jisheng pharmaceutical, Caijiapo Economic Development Zone, Baoji, Shaanxi, Qishan Applicant before: Jia Hongrui |
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Effective date of registration: 20190306 Address after: 226400 No. 118 Jianghai West Road, Chenggao Industrial Park, Rudong County, Nantong City, Jiangsu Province Patentee after: Nantong long and Pharmaceutical Co., Ltd. Address before: No. 88, Weihui City, Xinxiang City, Henan Province Patentee before: The First Affiliated Hospital of Xinxiang Medical University |
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