CN105395507A - Cyclobenzaprine hydrochloride sustained-release tablet - Google Patents
Cyclobenzaprine hydrochloride sustained-release tablet Download PDFInfo
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- CN105395507A CN105395507A CN201510887298.7A CN201510887298A CN105395507A CN 105395507 A CN105395507 A CN 105395507A CN 201510887298 A CN201510887298 A CN 201510887298A CN 105395507 A CN105395507 A CN 105395507A
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- cyclobenzaprine hydrochloride
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Abstract
The invention provides a preparation method of a cyclobenzaprine hydrochloride sustained-release tablet, and belongs to the technical field of a medicine. The cyclobenzaprine hydrochloride sustained-release tablet disclosed by the invention consists of cyclobenzaprine hydrochloride, a sustained-release material, a pore-foaming agent, a filling agent, a lubricating agent and distilled water. The cyclobenzaprine hydrochloride, as a major ingredient, has effects of relieving muscle spasm as well as accompanied severe pain in skeletal muscle and the like; and the provided sustained-release preparation is safe and effective, stable in quality, low in cost and low in administration efficiency, and the sustained-release preparation is capable of enhancing patient compliance and is capable of stably stopping pain and relieving spasm.
Description
Technical field
The invention belongs to medical art, relate to a kind of preparation method of cyclobenzaprine hydrochloride slow releasing tablet, the invention provides a kind of safe and effective, steady quality, with low cost, administration frequency is few, and patient's compliance strengthens, can the slow releasing preparation of steadily pain relieving spasmolytic.
Background technology
Cyclobenzaprine hydrochloride, chemistry 5-(3-dimethylamino propylene) dibenzo [a, e] cycloheptatriene hydrochlorate by name, structural formula is:
Molecular formula: C
20h
21nHCl
Molecular weight: 311.85
Disease of the musculoskeletal system, clinical more common, relates to many-sided diseases such as skeleton, intervertebral disc, nerve, muscle, joint, soft tissue, causes the reason of musculoskeletal pain also a lot, as inflammation, mechanical injuries, immunology reason, tumor etc.Musculoskeletal pain occurs frequent, simultaneously also according to the difference at invasion and attack position, is classified as cervical pain, the back of the body and back pain, arthralgia etc.Usually long-term, chronic injury is caused to torment to sufferer.
Cyclobenzaprine hydrochloride is developed by Merk company the earliest, 1978, and cyclobenzaprine hydrochloride sheet goes on the market in the U.S., specification is 5mg, 10mg, for alleviating the adjoint muscle spasm of acute painful musculoskeletal disease, being still one of the most frequently used muscle relaxant of the U.S. at present, not yet going on the market at home.Cyclobenzaprine hydrochloride slow releasing agent obtains U.S. FDA approval listing first in August, 2007, this product is a kind of long-acting slow releasing preparation, for unique daily muscle relaxant once of U.S. FDA approval, as having a rest and the auxiliary treatment of physical therapy, for alleviating the Sxs such as acute, that painful muscle skeletal diseases is correlated with muscle spasm and adjoint pain, tenderness and limitation of activity, clinical practice is for many years, safe and effective.
Cyclobenzaprine hydrochloride slow releasing agent preparation method known at present, CN103068375A relates to a kind of tablet sleeve of cyclobenzaprine, be mainly described in CN102065691A and carry out repeatedly coating to form the slow release beadlet of pastille, complex manufacturing, is not suitable for suitability for industrialized production.Present invention process is simple, and working condition easily meets, and is applicable to industrialized great production.
Summary of the invention
The invention provides a kind of safe and effective, steady quality, with low cost, administration frequency is few, and patient's compliance strengthens, can the slow releasing preparation of steadily pain relieving spasmolytic.
The present invention takes inconvenience, shortcoming that bioavailability is low to solve existing cyclobenzaprine hydrochloride preparation, invent cyclobenzaprine hydrochloride slow releasing tablet, reduce medicining times, slow down absorption rate, extend biological half-life, blood drug level is controlled within the scope of effective blood drug concentration, thus reduces side effect, improve the compliance of patient.
Applicant finds, existing cyclobenzaprine hydrochloride is prepared into slow releasing tablet in conjunction with specific adjuvant, has that stability is high, had good sustained release effect and a high advantage of bioavailability.
The application provides a kind of slow releasing tablet of cyclobenzaprine hydrochloride, comprising:
In this application, specific adjuvant is selected to prepare cyclobenzaprine hydrochloride slow releasing tablet.Wherein said slow-release material is the compositions of xanthan gum and hydroxypropyl emthylcellulose, and the two part by weight is 3:1, and porogen is microcrystalline Cellulose, and the ratio of slow-release material and porogen is 3:2, and filler is lactose, and lubricant is selected from magnesium stearate or Pulvis Talci.Experiment proves, not any pharmacy customary adjuvant is all applicable to preparing cyclobenzaprine hydrochloride slow releasing tablet, and the effect of cyclobenzaprine hydrochloride slow releasing tablet in release, stability, pharmacokinetics etc. selecting this specific adjuvant to prepare is better than the cyclobenzaprine hydrochloride slow releasing tablet that other adjuvants prepare far away.
Preferably, the prescription of slow releasing tablet is (by weight):
The present invention has effectively played the effect of slow releasing preparation on pain relieving spasmolytic class medicine, respond well, takes number of times few, once a day, takes rear drug slow and evenly discharges, can held stationary blood drug level, and with low cost, good patient compliance.
Detailed description of the invention
Inventor adopts and screens prescription with the following method, and each prescription is made tablet, makes 1000:
A. take all medicines (except magnesium stearate) in prescription respectively, cross 80 mesh sieves, put into Wet mixed granulating machine, be dry mixed 5-10 minute, add appropriate distilled water wet mixing, shut down discharging when material omits in bulk, granulate with 16 order nylon screens;
B. wet granular is placed in drying tray, thickness, generally at 2-3cm, sends into baking oven, temperature 50-60 DEG C of oven dry, and after drying, granule dries in the air to room temperature, and discharging, with 14 order nylon screen granulate;
C. granule materials puts into three-dimensional motion mixer, adds magnesium stearate, total mixed 10-15 minute, tabletting, packaging.
The preparation of embodiment 1-6 cyclobenzaprine hydrochloride slow releasing tablet
The supplementary material of according to the form below, by above-mentioned preparation method, the cyclobenzaprine hydrochloride slow releasing tablet of obtained six embodiments.
According to dissolution and drug release determination method (with reference to Chinese Pharmacopoeia version in 2015 four general rule characteristic check methods 0931), measure the cyclobenzaprine hydrochloride dissolution of cyclobenzaprine hydrochloride slow releasing tablet in 24 hours obtained by embodiment 1-6.Test result is in table 2.
As known from Table 2, the cyclobenzaprine hydrochloride slow releasing tablet of embodiment 1 discharged slowly and at the uniform velocity in 24 hours, illustrate that the part by weight when slow-release material xanthan gum and hydroxypropyl emthylcellulose is 3:1, and the slow release effect of cyclobenzaprine hydrochloride slow releasing capsule obtained when the ratio of slow-release material and porogen is 3:2 is best.
cyclobenzaprine hydrochloride slow releasing tablet stability test
Factors influencing has been carried out to the outward appearance of the slow releasing tablet of embodiment 1-6, content.
(1) hot test: Example 1-6 sample is laid in culture dish in right amount, the calorstat being placed in 60 DEG C is placed 10 days, in the 0th, 5,10 days this periods, taking sample determination respectively, measurement result is in table 3;
(2) high wet test: sample thief is laid in culture dish in right amount, places 10 days under the condition of 25 DEG C of relative humidity RH70% ± 5%, in the 0th, 5,10 days this periods, and taking sample determination respectively, measurement result is in table 3;
(3) strong illumination test, sample thief is laid in culture dish in right amount, is placed in the condition illumination 10 day of light cupboard at 4500Lx ± 500Lx, and in the 0th, 5,10 days this periods, taking sample determination respectively, measurement result was in table 3.
The amount of porogen is reduced in embodiment 2, the amount of porogen is improve in embodiment 3, embodiment 4-6 changes the ratio of two kinds of slow-release materials, as can be seen from Dissolution Rate Testing and stability test result, no matter be that two kinds of slow-release material ratios there occurs change, or slow-release material and porogen ratio change, and the stability of the cyclobenzaprine hydrochloride slow releasing tablet (embodiment 2-6) prepared all significantly reduces relative to embodiment 1.
Claims (2)
1. a cyclobenzaprine hydrochloride slow releasing tablet, is characterized in that, remembers by ratio of weight and the number of copies, and each constituent content is:
Cyclobenzaprine hydrochloride 5-30 part
Slow-release material 15-60 part
Porogen 10-30 part
Filler 15-50 part
Lubricant 1-5 part
Distilled water is appropriate
Wherein said slow-release material is the compositions of xanthan gum and hydroxypropyl emthylcellulose, the two part by weight is 3:1, and porogen is microcrystalline Cellulose, and the part by weight of slow-release material and porogen is 3:2, filler is lactose, and lubricant is selected from magnesium stearate or Pulvis Talci.
2. according to cyclobenzaprine hydrochloride slow releasing tablet according to claim 1, it is characterized in that, preferably, remember by ratio of weight and the number of copies, prescription is:
Cyclobenzaprine hydrochloride 15 parts
Xanthan gum 22.5 parts
Hydroxypropyl emthylcellulose 7.5
Microcrystalline Cellulose 20 parts
Lactose 25 parts
Magnesium stearate 3 parts
Distilled water is appropriate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510887298.7A CN105395507B (en) | 2015-12-07 | 2015-12-07 | A kind of cyclobenzaprine hydrochloride sustained release tablets |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201510887298.7A CN105395507B (en) | 2015-12-07 | 2015-12-07 | A kind of cyclobenzaprine hydrochloride sustained release tablets |
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| CN105395507A true CN105395507A (en) | 2016-03-16 |
| CN105395507B CN105395507B (en) | 2018-10-23 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107519142A (en) * | 2017-08-24 | 2017-12-29 | 青岛正大海尔制药有限公司 | A kind of cyclobenzaprine hydrochloride sublingual tablet and preparation method thereof |
| CN107998094A (en) * | 2016-10-31 | 2018-05-08 | 顾世海 | A kind of tenofovir disoproxil fumarate sustained release tablets and preparation method thereof |
| CN109316457A (en) * | 2018-11-26 | 2019-02-12 | 正大制药（青岛）有限公司 | A kind of cyclobenzaprine hydrochloride sustained release preparation and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014167440A1 (en) * | 2013-03-26 | 2014-10-16 | Wockhardt Limited | Modified release pharmaceutical compositions of cyclobenzaprine or salts thereof |
| CN104352474A (en) * | 2014-11-21 | 2015-02-18 | 哈尔滨圣吉药业股份有限公司 | Cyclobenzaprine hydrochloride sustained release tablets and preparation method 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 |
-
2015
- 2015-12-07 CN CN201510887298.7A patent/CN105395507B/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014167440A1 (en) * | 2013-03-26 | 2014-10-16 | Wockhardt Limited | Modified release pharmaceutical compositions of cyclobenzaprine or salts thereof |
| CN104352474A (en) * | 2014-11-21 | 2015-02-18 | 哈尔滨圣吉药业股份有限公司 | Cyclobenzaprine hydrochloride sustained release tablets and preparation method 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 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107998094A (en) * | 2016-10-31 | 2018-05-08 | 顾世海 | A kind of tenofovir disoproxil fumarate sustained release tablets and preparation method thereof |
| CN107519142A (en) * | 2017-08-24 | 2017-12-29 | 青岛正大海尔制药有限公司 | A kind of cyclobenzaprine hydrochloride sublingual tablet and preparation method thereof |
| CN107519142B (en) * | 2017-08-24 | 2021-02-26 | 正大制药（青岛）有限公司 | Cyclobenzaprine hydrochloride sublingual tablet and preparation method thereof |
| CN109316457A (en) * | 2018-11-26 | 2019-02-12 | 正大制药（青岛）有限公司 | A kind of cyclobenzaprine hydrochloride sustained release preparation and preparation method thereof |
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| CN105395507B (en) | 2018-10-23 |
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Address after: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Applicant after: Zhengda Pharmaceutical (Qingdao) Co., Ltd. Address before: 266000 3601 Tuen Jie Road, Qingdao economic and Technological Development Zone, Shandong Applicant before: Qingdao Zhengda Haier Pharmaceutical Co., Ltd. |
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