CN109381446A - A kind of cyclobenzaprine hydrochloride spansule - Google Patents
A kind of cyclobenzaprine hydrochloride spansule Download PDFInfo
- Publication number
- CN109381446A CN109381446A CN201811412685.5A CN201811412685A CN109381446A CN 109381446 A CN109381446 A CN 109381446A CN 201811412685 A CN201811412685 A CN 201811412685A CN 109381446 A CN109381446 A CN 109381446A
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- CN
- China
- Prior art keywords
- cyclobenzaprine hydrochloride
- slow
- parts
- cyclobenzaprine
- spansule
- 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.)
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Classifications
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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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
Abstract
The present invention relates to a kind of cyclobenzaprine hydrochloride spansule, belong to field of pharmaceutical preparations.The present invention provides a kind of cyclobenzaprine hydrochloride spansule, and it to further include diluent, adhesive, disintegrating agent and lubricant that it includes active ingredient hydrochloric acid cyclobenzaprine and slow-release materials.Mainly screening is optimized to slow-release material in cyclobenzaprine hydrochloride spansule of the invention, by testing a variety of slow-release materials, it finally found that best as the slow release effect of slow-release material using ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer, burst size for 24 hours reaches 100%, and influence factor test, accelerated test and room temperature keep sample for a long time test the equal exhibit stabilization of test result it is fine.Cyclobenzaprine hydrochloride spansule of the invention is a kind of excellent slow release product, very good solution cyclobenzaprine hydrochloride due to Half-life in vivo is shorter and medication frequently to influence patient medication compliance the problem of.
Description
Technical field
The present invention relates to field of pharmaceutical preparations, and in particular to a kind of cyclobenzaprine hydrochloride spansule.
Background technique
Cyclobenzaprine hydrochloride (cyclobenzaprine hydrochloride, 1), (3- dimethylamino is sub- by the entitled 5- of chemistry
Propyl) dibenzo [a, d] cycloheptyl pinene hyhrochloride, it is the muscle relaxant of Merck company, U.S. research and development, in multinational listing,
Trade name Flexeril.
Cyclobenzaprine hydrochloride is central muscle relaxant, and site of action may not be the resistance of neuromere muscle in brain stem
, there is skeletal muscle relaxation effect, cyclobenzaprine hydrochloride also has cholinolytic effect, can alleviate local muscles in disconnected agent after administration
Spasm symptom, while the normal function of muscle is not interfered, muscle epidemic disease contraction caused by Central nervous systemic disease is invalid.Clinic is main
It is used to treat the adjuvant drug of painful part muscle cramp.
The high sensitiveness of muscle in several animal models can be alleviated or be eliminated to cyclobenzaprine hydrochloride.Zooscopy mentions
Show, cyclobenzaprine hydrochloride is unable to direct interference animal muscle nervous function or directly affects skeletal muscle function, mainly makees
For the brain part of central nervous system, and not directly control muscle cramp and the open-minded flesh of relaxation bone.Evidence show hydrochloric acid
Cyclobenzaprine reduces abnormalities muscular movement, reaches flesh pine effect by influencing motor fibre.
However, general formulation is multiple per medication day by day since half-life period is shorter in vivo for cyclobenzaprine hydrochloride, use
Medicine is more frequent, affects the compliance of patient medication, thus develops cyclobenzaprine hydrochloride sustained release preparation and be of great significance.
Summary of the invention
The purpose of the present invention is to provide a kind of cyclobenzaprine hydrochloride sustained release preparation that quality is stable.
To solve this technical problem, technical solution provided by the present application is a kind of cyclobenzaprine hydrochloride spansule, packet
Cyclobenzaprine containing active ingredient hydrochloric acid and slow-release material further include diluent, adhesive, disintegrating agent and lubricant.
The slow-release material includes ethylene-vinyl acetate copolymer, polylactic acid-acrylic copolymer and polymethylacrylic acid
One of ester is a variety of.
Preferably, the slow-release material includes ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer, described
Ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer ratio are 1-5:2-10.
The diluent includes one of starch, Icing Sugar, dextrin, microcrystalline cellulose and lactose or a variety of.
Described adhesive includes one of povidone, gelatin, sucrose, pregelatinized starch and glucose or a variety of.
The disintegrating agent includes one of dried starch, sodium carboxymethyl starch, crospovidone and calcium carboxymethylcellulose
Or it is a variety of.
The lubricant includes one in talcum powder, magnesium stearate, superfine silica gel powder, sldium lauryl sulfate and hydrogenated vegetable oil
Kind is a variety of.
The weight of cyclobenzaprine hydrochloride spansule each component of the present invention are as follows: 2-8 parts of cyclobenzaprine hydrochloride, sustained release
15-22 parts of material, 20-30 parts of diluent, 1-6 parts of adhesive, 12-18 parts and lubricant 0.5-2 parts of disintegrating agent.
Preferably, the weight of cyclobenzaprine hydrochloride spansule each component of the present invention are as follows: cyclobenzaprine hydrochloride 4-6
Part, 18-20 parts of slow-release material, 22-26 parts of diluent, 2-4 parts of adhesive, 14-16 parts and lubricant 1-1.5 parts of disintegrating agent.
Beneficial effects of the present invention:
Mainly screening is optimized to slow-release material in cyclobenzaprine hydrochloride spansule of the invention, by a variety of slow
It releases material to be tested, finally found that using ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer as sustained release material
The slow release effect of material is best, and burst size for 24 hours reaches 100%, and influence factor test, accelerated test and room temperature keep sample for a long time
The test result of test shows that its stability is fine.Cyclobenzaprine hydrochloride spansule of the invention is a kind of excellent sustained release
Product, very good solution cyclobenzaprine hydrochloride are shorter and medication is frequently complied with to influence patient medication due to Half-life in vivo
The problem of property.
Specific embodiment
Present invention will be further explained below with reference to specific examples.It should be understood that these embodiments are merely to illustrate the present invention
Rather than it limits the scope of the invention.In the following examples, the experimental methods for specific conditions are not specified, usually according to conventional strip
Part or according to the normal condition proposed by manufacturer.Unless otherwise stated, otherwise all percentage, ratio, ratio or number is pressed
Poidometer.
Unless otherwise defined, all professional and scientific terms as used herein and meaning familiar to those skilled in the art
Justice is identical.In addition, any method similar to or equal to what is recorded and material can be applied to the method for the present invention.Wen Zhong
The preferred implement methods and materials are for illustrative purposes only.
The preparation of 1 cyclobenzaprine hydrochloride spansule of embodiment
Cyclobenzaprine hydrochloride spansule embodiment is prepared using the conventional method of capsule according to the formula (g/) of table 1
1-7。
1 cyclobenzaprine hydrochloride spansule formula (one) of table
The screening of 2 cyclobenzaprine hydrochloride spansule slow-release material of embodiment
The cyclobenzaprine hydrochloride spansule of embodiment 1-7 is subjected to Dissolution Rate Testing, test method is Rotating shaker, revolving speed
For 50rpm, test solution is water 900mL, and test temperature is 37 ± 0.5 DEG C.The results are shown in Table 2.
The cyclobenzaprine hydrochloride spansule dissolution test result of the different slow-release materials of table 2
According to result above it is found that individually using ethylene-vinyl acetate copolymer, polylactic acid-acrylic copolymer or gathering
When methacrylate is as slow-release material, slow release effect is general, and burst size for 24 hours generally can only achieve 80% or so, uses
Two kinds in ethylene-vinyl acetate copolymer, polylactic acid-acrylic copolymer and polymethacrylates are used as slow-release material
When, slow release effect increases, wherein using ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer as sustained release
The slow release effect of material is best, and burst size for 24 hours reaches 100%, using ethylene-vinyl acetate copolymer, polylactic acid-acrylic acid
Copolymer and polymethacrylates three are also preferable as the effect of slow-release material, but from simplifying prescription and save the cost
Angle considers, using ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer as slow-release material technical solution most
It is good.
The preparation of 3 cyclobenzaprine hydrochloride spansule of embodiment
Select ethylene-vinyl acetate copolymer and polylactic acid-acrylic copolymer as slow-release material, according to matching for table 3
Side (g/) prepares cyclobenzaprine hydrochloride spansule embodiment 8-10 using the conventional method of capsule.
3 cyclobenzaprine hydrochloride spansule formula (two) of table
| Embodiment 8 | Embodiment 9 | Embodiment 10 | |
| Cyclobenzaprine hydrochloride | 0.015 | 0.015 | 0.015 |
| Ethylene-vinyl acetate copolymer | 0.005 | 0.01 | 0.02 |
| Polylactic acid-acrylic copolymer | 0.025 | 0.02 | 0.01 |
| Starch | 0.03 | 0.03 | 0.03 |
| Lactose | 0.03 | 0.03 | 0.03 |
| Povidone | 0.02 | 0.02 | 0.02 |
| Sodium carboxymethyl starch | 0.02 | 0.02 | 0.02 |
| Magnesium stearate | 0.001 | 0.001 | 0.001 |
The test of 4 cyclobenzaprine hydrochloride spansule influence factor of embodiment
The cyclobenzaprine hydrochloride spansule of Example 8-10 is placed in high temperature (40 DEG C), illumination (4500 ± 500Lx), low
Under the conditions of warm (- 18 DEG C), sampled, each inspection target of stability test is detected, as a result such as 4 institute of table respectively at the 5th, 10 day
Show.
4 cyclobenzaprine hydrochloride spansule influence factor test result of table
According to result above it is found that the cyclobenzaprine hydrochloride spansule influence factor test result of the application conforms to
It asks.
5 cyclobenzaprine hydrochloride spansule accelerated test of embodiment
The cyclobenzaprine hydrochloride spansule of Example 8-10 is placed in 40 DEG C, under the conditions of RH75%, respectively at the 0th, 1,
2, March samples, and detects to stability test items inspection target.The results are shown in Table 5.
5 cyclobenzaprine hydrochloride spansule accelerated test result of table
According to result above it is found that the cyclobenzaprine hydrochloride spansule accelerated test result of the application meets the requirements.
6 cyclobenzaprine hydrochloride spansule room temperature of embodiment keeps sample test for a long time
The cyclobenzaprine hydrochloride spansule of Example 8-10 is placed under room temperature, is sampled respectively at the 0th, 3 months,
Stability test items inspection target is detected.The results are shown in Table 6.
6 cyclobenzaprine hydrochloride spansule room temperature of table keeps sample test result for a long time
According to result above, it is found that the cyclobenzaprine hydrochloride spansule room temperature of the application keeps sample for a long time, test result meets
It is required that.
It follows that cyclobenzaprine hydrochloride spansule performance of the invention is stablized.
The foregoing is merely illustrative of the preferred embodiments of the present invention, the substantial technological content model being not intended to limit the invention
It encloses, substantial technological content of the invention is broadly defined in the scope of the claims of application, any technology that other people complete
Entity or method also or a kind of equivalent change, will if identical with defined in the scope of the claims of application
It is considered as being covered by among the scope of the claims.
Claims (10)
1. a kind of cyclobenzaprine hydrochloride spansule, which is characterized in that it includes active ingredient hydrochloric acid cyclobenzaprines and sustained release material
Material, further includes diluent, adhesive, disintegrating agent and lubricant.
2. cyclobenzaprine hydrochloride spansule according to claim 1, which is characterized in that the slow-release material includes ethylene
~acetate ethylene copolymer, polylactic acid~one of acrylic copolymer and polymethacrylates or a variety of.
3. cyclobenzaprine hydrochloride spansule according to claim 2, which is characterized in that the slow-release material includes ethylene
~acetate ethylene copolymer and polylactic acid~acrylic copolymer.
4. cyclobenzaprine hydrochloride spansule according to claim 3, which is characterized in that the ethylene~vinyl acetate is total
Polymers and polylactic acid~acrylic copolymer ratio are 1~5:2~10.
5. cyclobenzaprine hydrochloride spansule according to any one of claims 1 to 4, which is characterized in that the diluent
Including one of starch, Icing Sugar, dextrin, microcrystalline cellulose and lactose or a variety of.
6. cyclobenzaprine hydrochloride spansule according to any one of claims 1 to 4, which is characterized in that described adhesive
Including one of povidone, gelatin, sucrose, pregelatinized starch and glucose or a variety of.
7. cyclobenzaprine hydrochloride spansule according to any one of claims 1 to 4, which is characterized in that the disintegrating agent
Including one of dried starch, sodium carboxymethyl starch, crospovidone and calcium carboxymethylcellulose or a variety of.
8. cyclobenzaprine hydrochloride spansule according to any one of claims 1 to 4, which is characterized in that the lubricant
Including one of talcum powder, magnesium stearate, superfine silica gel powder, sldium lauryl sulfate and hydrogenated vegetable oil or a variety of.
9. cyclobenzaprine hydrochloride spansule according to claim 1, which is characterized in that the weight of each component
Are as follows: 2~8 parts of cyclobenzaprine hydrochloride, 15~22 parts of slow-release material, 20~30 parts of diluent, 1~6 part of adhesive, disintegrating agent 12~
18 parts and 0.5~2 part of lubricant.
10. cyclobenzaprine hydrochloride spansule according to claim 9, which is characterized in that the weight of each component
Are as follows: 4~6 parts of cyclobenzaprine hydrochloride, 18~20 parts of slow-release material, 22~26 parts of diluent, 2~4 parts of adhesive, disintegrating agent 14~
16 parts and 1~1.5 part of lubricant.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811412685.5A CN109381446A (en) | 2018-11-26 | 2018-11-26 | A kind of cyclobenzaprine hydrochloride spansule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201811412685.5A CN109381446A (en) | 2018-11-26 | 2018-11-26 | A kind of cyclobenzaprine hydrochloride spansule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN109381446A true CN109381446A (en) | 2019-02-26 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201811412685.5A Pending CN109381446A (en) | 2018-11-26 | 2018-11-26 | A kind of cyclobenzaprine hydrochloride spansule |
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Citations (7)
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|---|---|---|---|---|
| CN101889975A (en) * | 2010-07-27 | 2010-11-24 | 北京虹湾医药技术有限公司 | Rosuvastatin calcium sustained-release preparation and preparation method thereof |
| WO2013158638A1 (en) * | 2012-04-17 | 2013-10-24 | Mylan, Inc. | Stable dosage forms of skeletal muscle relaxants with extended release coating |
| WO2014167440A1 (en) * | 2013-03-26 | 2014-10-16 | Wockhardt Limited | Modified release pharmaceutical compositions of cyclobenzaprine or salts thereof |
| CN104473908A (en) * | 2014-11-21 | 2015-04-01 | 哈尔滨圣吉药业股份有限公司 | Cyclobenzaprine hydrochloride sustained release pellets and preparation method thereof |
| CN104523655A (en) * | 2014-12-22 | 2015-04-22 | 青岛正大海尔制药有限公司 | Cyclobenzaprine hydrochloride sustained-release capsules |
| US20170056342A1 (en) * | 2015-08-31 | 2017-03-02 | Apotex Technologies Inc. | Extended Release Dosage Form Comprising Cyclobenzaprine Hydrochloride |
| CN106860430A (en) * | 2008-06-20 | 2017-06-20 | 阿代尔制药股份有限公司 | The preparation of the skeletal muscle relaxant dosage forms of control release |
-
2018
- 2018-11-26 CN CN201811412685.5A patent/CN109381446A/en active Pending
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106860430A (en) * | 2008-06-20 | 2017-06-20 | 阿代尔制药股份有限公司 | The preparation of the skeletal muscle relaxant dosage forms of control release |
| CN101889975A (en) * | 2010-07-27 | 2010-11-24 | 北京虹湾医药技术有限公司 | Rosuvastatin calcium sustained-release preparation and preparation method thereof |
| WO2013158638A1 (en) * | 2012-04-17 | 2013-10-24 | Mylan, Inc. | Stable dosage forms of skeletal muscle relaxants with extended release coating |
| WO2014167440A1 (en) * | 2013-03-26 | 2014-10-16 | Wockhardt Limited | Modified release pharmaceutical compositions of cyclobenzaprine or salts thereof |
| CN104473908A (en) * | 2014-11-21 | 2015-04-01 | 哈尔滨圣吉药业股份有限公司 | Cyclobenzaprine hydrochloride sustained release pellets and preparation method thereof |
| CN104523655A (en) * | 2014-12-22 | 2015-04-22 | 青岛正大海尔制药有限公司 | Cyclobenzaprine hydrochloride sustained-release capsules |
| US20170056342A1 (en) * | 2015-08-31 | 2017-03-02 | Apotex Technologies Inc. | Extended Release Dosage Form Comprising Cyclobenzaprine Hydrochloride |
Non-Patent Citations (1)
| Title |
|---|
| 于佳: "盐酸环苯扎林缓释微丸的制备及体外释放度考察", 《中国药房》 * |
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
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Application publication date: 20190226 |