CN105769805A - Cyclobenzaprine hydrochloride tablet - Google Patents
Cyclobenzaprine hydrochloride tablet Download PDFInfo
- Publication number
- CN105769805A CN105769805A CN201610264717.6A CN201610264717A CN105769805A CN 105769805 A CN105769805 A CN 105769805A CN 201610264717 A CN201610264717 A CN 201610264717A CN 105769805 A CN105769805 A CN 105769805A
- Authority
- CN
- China
- Prior art keywords
- cyclobenzaprine hydrochloride
- controlled
- tablet
- plasticizer
- filler
- 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
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
-
- 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
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
Abstract
The invention provides a cyclobenzaprine hydrochloride tablet, and belongs to the technical field of medicines. The cyclobenzaprine hydrochloride tablet is a controlled-release preparation and consists of a tablet-containing core and a coating film layer wrapping the tablet-containing core, wherein the tablet-containing core is prepared from cyclobenzaprine hydrochloride, a filler and sodium chloride; the coating film layer is prepared from a controlled-release material, a plasticizer and a pore-foaming agent. During preparation, the coating film layer wraps the tablet-containing core, so as to prepare the cyclobenzaprine hydrochloride tablet. Cyclobenzaprine hydrochloride serving as a main component has the effects of relieving muscle spasm and accompanying intense pain in skeletal muscle and the like. The tablet can be slowly released at constant speed, so as to fulfill the aims of long-acting effect and enhancement of the treating effect; furthermore, the dosing amount can be reduced when the same pharmacological function is maintained, so as to reduce the side effect caused by the medicine on a patient; meanwhile, the preparation process is simple, and an obtained product is stable in quality and suitable for large-scale production and application.
Description
Technical field
The invention belongs to pharmaceutical technology field, relate to a kind of cyclobenzaprine hydrochloride sheet, the invention provides a kind of safely and effectively, steady quality, with low cost, administration frequency is few, and patient's compliance strengthens, can the controlled release 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: C20H21N·HCl
Molecular weight: 311.85.
Disease of the musculoskeletal system is more common in clinic, relates to many-sided disease such as skeleton, intervertebral disc, nerve, muscle, joint, soft tissue, and the reason causing musculoskeletal pain is also a lot, such as inflammation, mechanical injuries, immunology reason, tumor etc..Musculoskeletal pain occurs frequently, simultaneously also according to the difference at invasion and attack position, to be classified as cervical pain, the back of the body and back pain, arthralgia etc..Sufferer usually cause long-term, chronic injury torment.
Cyclobenzaprine hydrochloride is developed by Merk company the earliest, 1978, and cyclobenzaprine hydrochloride sheet lists in the U.S., specification is 5mg, 10mg, the muscle spasm adjoint for alleviating acute painful musculoskeletal disease, is still one of the most frequently used muscle relaxant of the U.S. at present, not yet lists at home.Cyclobenzaprine hydrochloride controlled release agent obtains U.S. FDA approval listing first in August, 2007, this product is a kind of long-acting controlled release preparation, only one daily muscle relaxant once for U.S. FDA approval, as the auxiliary treatment having a rest with physical therapy, for alleviating the Sxs such as muscle spasm acute, that painful muscle skeletal diseases is relevant and adjoint pain, tenderness and limitation of activity, clinical practice for many years, safely and effectively.
The cyclobenzaprine hydrochloride controlled release agent preparation method being currently known, CN103068375A relates to the tablet sleeve of a kind of cyclobenzaprine, it is mainly the controlled-release beads carrying out repeatedly coating to form pastille, complex manufacturing described in CN102065691A, is not suitable for industrialized production.Present invention process is simple, and working condition easily meets, and is suitable for industrialized great production.
Summary of the invention
Medicine of the present invention slowly, at the uniform velocity discharge, can reach long-acting, to increase curative effect purpose, it is possible to be reduced to dose when maintaining equal drug effect, thus reducing the side effect that drug administration brings to patient, and preparation technology is simple, products obtained therefrom steady quality, it is suitable for large-scale production and application.The invention provides a kind of safely and effectively, steady quality, with low cost, administration frequency is few, and patient's compliance strengthens, can the controlled release preparation of steadily pain relieving spasmolytic.
The present invention is to solve the shortcoming that inconvenience taken by existing cyclobenzaprine hydrochloride preparation, bioavailability is low, invent cyclobenzaprine hydrochloride controlled release tablet, reduce medicining times, slow down absorption rate, extend biological half-life, making blood drug level control within the scope of effective blood drug concentration, thus reducing side effect, improving the compliance of patient.
It has been found that existing, cyclobenzaprine hydrochloride is prepared into controlled release tablet in conjunction with specific adjuvant, there is stability height, controlled-release effect is good and bioavailability is high advantage.
The application provides a kind of cyclobenzaprine hydrochloride sheet, including:
Cyclobenzaprine hydrochloride 5-20 part
Filler 45-65 part
Osmotic pressure active substance 5-10 part
Controlled-release material 15-30 part
Plasticizer 3-6 part
Porogen 2-6 part
Appropriate amount of ethanol.
Preferably prescription is (by weight):
Cyclobenzaprine hydrochloride 15 parts
Filler 55 parts
Osmotic pressure active substance 7 parts
Controlled-release material 27 parts
Plasticizer 4 parts
Porogen 4 parts
Appropriate amount of ethanol.
In this application, specific adjuvant is selected to prepare cyclobenzaprine hydrochloride controlled release tablet.Filler is at least one in starch or microcrystalline Cellulose；Osmotic pressure active substance is at least one in sodium chloride or potassium chloride；Controlled-release material is at least one in cellulose acetate, ethyl cellulose and ethylene propylene base co-polymer；Plasticizer is at least one in diethyl phthalate or triethyl citrate；Porogen is at least one in dextrin or polyvidone.
It is further preferred that described controlled-release material is cellulose acetate and ethylene propylene base co-polymer, the two weight ratio is 1:2；Preferred filler is microcrystalline Cellulose；Preferred osmotic pressure active substance is sodium chloride；Preferred plasticizer is diethyl phthalate；Preferred porogen is dextrin.
The preparation method of cyclobenzaprine hydrochloride sheet comprises the following steps:
(1) take cyclobenzaprine hydrochloride by ratio of weight and the number of copies, filler is mixed homogeneously with osmotic pressure active substance, with 75% ethanol for binding agent, makes soft material, and 20～24 mesh sieves are granulated, and dried tabletting obtains pastille label；
(2) dissolve controlled-release material, plasticizer and porogen with the ethanol of 75%, make controlled release coat liquid；
(3) the controlled release coat liquid prepared uniformly is sprayed at the pastille wicking surface that step (1) prepares, obtains cyclobenzaprine hydrochloride controlled release tablet after drying.
The cyclobenzaprine hydrochloride controlled release tablet that the present invention relates to has the advantages that
(1) drug release is uniform, can reach long-acting, to increase curative effect purpose, it is possible to be reduced to dose when maintaining equal drug effect, thus reducing the side effect that drug administration brings to patient；
(2) selected by, adjuvant is common, and preparation technology is simple, products obtained therefrom steady quality, is suitable for large-scale production and application.
Detailed description of the invention
Inventor adopts and screens prescription with the following method, and each prescription is made tablet, for 15mg specification, makes 1000:
(1) take cyclobenzaprine hydrochloride by ratio of weight and the number of copies, filler is mixed homogeneously with osmotic pressure active substance, with 75% ethanol for binding agent, makes soft material, and 20～24 mesh sieves are granulated, and dried tabletting obtains pastille label；
(2) dissolve controlled-release material, plasticizer and porogen with the ethanol of 75%, make controlled release coat liquid；
(3) the controlled release coat liquid prepared uniformly is sprayed at the pastille wicking surface that step (1) prepares, obtains cyclobenzaprine hydrochloride controlled release tablet after drying.
The preparation of embodiment 1-6 cyclobenzaprine hydrochloride sheet
The supplementary material of according to the form below, is prepared as described above method, prepares the cyclobenzaprine hydrochloride sheet of six embodiments, and wherein "/" represents and do not use.
Table 1 embodiment 1-6
The vitro release of test example 1 embodiment 1-6 gained cyclobenzaprine hydrochloride sheet measures
Release is measured with drug release determination method (with reference to Chinese Pharmacopoeia four general rule characteristic check methods 0931 of version in 2015) according to dissolution, with distilled water for dissolution medium, respectively 1,2,4,6,8,12h sampling, measure absorbance, calculate accumulative releasing degree according to standard curve.Measure the cyclobenzaprine hydrochloride dissolution that the cyclobenzaprine hydrochloride sheet obtained by embodiment 1-6 is interior at 24 hours.Test result is in Table 2.
Table 2 embodiment 1-6 vitro release investigation table (dissolution medium: distilled water)
As it can be seen from table 1 controlled release tablet obtained by embodiment 1～6 can constant speed, uniformly discharge, illustrate to maintain the medicine effective blood drug concentration of long period, reduce medicining times；Wherein the controlled release tablet of embodiment 1 discharged uniformly in 12 hours, can improve bioavailability, illustrated that using cellulose acetate and ethylene propylene base co-polymer is the cyclobenzaprine hydrochloride controlled release tablet best results made by controlled-release material.
The preparation of embodiment 7-11 cyclobenzaprine hydrochloride sheet
The supplementary material of according to the form below, is prepared as described above method, and each embodiment prepares cyclobenzaprine hydrochloride sheet respectively.The cellulose acetate of embodiment 7 and the weight ratio of ethylene propylene base co-polymer are 1:2, the cellulose acetate of embodiment 8 and the weight ratio of ethylene propylene base co-polymer are 1:1, the cellulose acetate of embodiment 9 and the weight ratio of ethylene propylene base co-polymer are 1:3, the cellulose acetate of embodiment 10 and the weight ratio of ethylene propylene base co-polymer are 2:1, and the cellulose acetate of embodiment 11 and the weight ratio of ethylene propylene base co-polymer are 2:3.
Table 3 embodiment 7-11
The external drug release determination of cyclobenzaprine hydrochloride sheet of test example 2 embodiment 7-11 gained
Assay method is with test example 1.Measurement result is in Table 4.
Table 4 embodiment 7-11 vitro release investigation table (dissolution medium: distilled water)
As known from Table 2, the cyclobenzaprine hydrochloride sheet of embodiment 7 in 12 hours at the uniform velocity, slow releasing, the highest the 12nd hour release, illustrate that bioavailability is higher, illustrate that, when the weight ratio of cellulose acetate and ethylene propylene base co-polymer is 1:2, the controlled-release effect of obtained cyclobenzaprine hydrochloride sheet is best.
Claims (5)
1. a cyclobenzaprine hydrochloride sheet, wherein active component is cyclobenzaprine hydrochloride, it is characterized by by pastille label and be wrapped in its outer coatings rete and form, described pastille label includes cyclobenzaprine hydrochloride, filler and osmotic pressure active substance, described coating rete includes controlled-release material, plasticizer and porogen, it is characterized in that, remember by ratio of weight and the number of copies, each constituent content is:
Cyclobenzaprine hydrochloride 5-20 part
Filler 45-65 part
Osmotic pressure active substance 5-10 part
Controlled-release material 15-30 part
Plasticizer 3-6 part
Porogen 2-6 part
Appropriate amount of ethanol.
2. the cyclobenzaprine hydrochloride sheet described in claim 1, it is characterised in that: remembering by ratio of weight and the number of copies, each constituent content is:
Cyclobenzaprine hydrochloride 15 parts
Filler 55 parts
Osmotic pressure active substance 7 parts
Controlled-release material 27 parts
Plasticizer 4 parts
Porogen 4 parts
Appropriate amount of ethanol.
3. the cyclobenzaprine hydrochloride sheet described in claim 2, it is characterised in that: described filler is at least one in starch or microcrystalline Cellulose；Described osmotic pressure active substance is at least one in sodium chloride or potassium chloride；Described controlled-release material is at least one in cellulose acetate, ethyl cellulose and ethylene propylene base co-polymer；Described plasticizer is at least one in diethyl phthalate or triethyl citrate；Described porogen is at least one in dextrin or polyvidone.
4. the cyclobenzaprine hydrochloride sheet described in claim 3, it is characterised in that: described controlled-release material is cellulose acetate and ethylene propylene base co-polymer, and the two weight ratio is 1:2；Preferred filler is microcrystalline Cellulose；Preferred osmotic pressure active substance is sodium chloride；Preferred plasticizer is diethyl phthalate；Preferred porogen is dextrin.
5. the method for preparation cyclobenzaprine hydrochloride sheet described in any one of claim 1-4, comprises the following steps:
(1) take cyclobenzaprine hydrochloride by ratio of weight and the number of copies, filler is mixed homogeneously with osmotic pressure active substance, with 75% ethanol for binding agent, makes soft material, and 20～24 mesh sieves are granulated, and dried tabletting obtains pastille label；
(2) dissolve controlled-release material, plasticizer and porogen with the ethanol of 75%, make controlled release coat liquid；
(3) the controlled release coat liquid prepared uniformly is sprayed at the pastille wicking surface that step (1) prepares, obtains cyclobenzaprine hydrochloride controlled release tablet after drying.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610264717.6A CN105769805A (en) | 2016-04-26 | 2016-04-26 | Cyclobenzaprine hydrochloride tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610264717.6A CN105769805A (en) | 2016-04-26 | 2016-04-26 | Cyclobenzaprine hydrochloride tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105769805A true CN105769805A (en) | 2016-07-20 |
Family
ID=56399432
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610264717.6A Withdrawn CN105769805A (en) | 2016-04-26 | 2016-04-26 | Cyclobenzaprine hydrochloride tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105769805A (en) |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142539A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Alginic sodium diester controlled-release tablet and preparation method thereof |
| CN103142540A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | PGMS (Propylene Glycol Mannate Sulfate) controlled-release tablet and preparation method thereof |
| CN105395512A (en) * | 2015-12-07 | 2016-03-16 | 青岛正大海尔制药有限公司 | Cyclobenzaprine hydrochloride controlled-release tablet |
-
2016
- 2016-04-26 CN CN201610264717.6A patent/CN105769805A/en not_active Withdrawn
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142539A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Alginic sodium diester controlled-release tablet and preparation method thereof |
| CN103142540A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | PGMS (Propylene Glycol Mannate Sulfate) controlled-release tablet and preparation method thereof |
| CN105395512A (en) * | 2015-12-07 | 2016-03-16 | 青岛正大海尔制药有限公司 | Cyclobenzaprine hydrochloride controlled-release tablet |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB02 | Change of applicant information | ||
| CB02 | Change of applicant information |
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. |
|
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20160720 |