CN1452983A - Delayed-releasing compound diclofenac sodium prepn - Google Patents
Delayed-releasing compound diclofenac sodium prepn Download PDFInfo
- Publication number
- CN1452983A CN1452983A CN 03123921 CN03123921A CN1452983A CN 1452983 A CN1452983 A CN 1452983A CN 03123921 CN03123921 CN 03123921 CN 03123921 A CN03123921 A CN 03123921A CN 1452983 A CN1452983 A CN 1452983A
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- China
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- vitamin
- diclofenac sodium
- slow release
- preparation
- compound
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Abstract
The present invention relates to delayed-releasing compound diclofenac sodium preparation and its preparation process, and is especially the delayed-releasing compound preparation of diclofenac sodium, vitamin B1, vitamin B6 and vitamin B12 and its application in medical treatment.
Description
Technical field:
The present invention relates to a kind of compound slow release preparation and preparation technology thereof, particularly diclofenac sodium and vitamin B
1B
6B
12The compound slow release preparation of forming, and the application of this compound slow release preparation in medical treatment.
Background technology:
Diclofenac sodium is a NSAID (non-steroidal anti-inflammatory drug), the COX (epoxidase) that this product produces because of inflammatory reaction by the inhibition tissue, thus reduced the synthetic of prostaglandin.Local prostaglandin is synthetic to be reduced, and has alleviated pain perception, has played the effect of periphery analgesic.This product still has certain inhibition lipoxygenase and reduces leukotriene, the effect of products such as slow kinases.In addition, prove in zoopery and people's clinical practice: by suppressing the synthetic of hypothalamus thermotaxic centre prostaglandin, this product also has the antipyretic effect.This product is applicable to the acute attack stage of various chronic arthritiss such as alleviating class pathogenic wind-warm arthritis, osteoarthritis, joint of vertebral column inflammation, gouty arthritis, rheumatic arthritis or lasting arthralgia symptom, anosis effect because of the treatment and the control course of disease; Treat non-arthrogenous various soft tissue rheumatism pain, as shoulder pain, the damaging pain of myalgia and motion back etc.; Acute light, moderate pain is as operation back, strain back, primary dysmenorrhea, toothache, headache etc.; Heating to adult and child has refrigeration function.
Vitamin is that a class is kept body homergy and healthy requisite low-molecular-weight organic compound, and they are very little at people's in-vivo content, and most of vitamin can not synthesize in human body, or the synthetic quantity deficiency.Therefore can not satisfy the body needs, body need constantly absorb from the external world.If the vitamin intake is not enough, a series of vitamin deficiency symptoms then can appear.The vitamin B complex material can be used as the auxiliary treatment of diseases such as peripheral neuritis, long-term chronic inflammatory disease, heating.At present clinically, using that non-steroidal drug is analgesic, when antiinflammatory, analgesia, often giving the vitamin B complex material, as auxiliary treatment.The Neurofenac capsule that Merck (Germany) company produces has added a certain amount of vitamin B exactly in diclofenac sodium
1B
6B
12, clinical trial certificate, list is used diclofenac sodium, and Neurofenac has better therapeutic.
But diclofenac sodium is a conventional tablet among the Neurofenac, onset is rapid, acute pain there is fine, very fast control, but it is also fast that conventional tablet is discharged, for the chronic pain after the acute pain control, one day needs multiple dosing with refusing to obey the inconvenience of using, has also increased patient's financial burden to patient.
Summary of the invention:
The invention provides the diclofenac sodium and the vitamin B that only needed single administration in one day
1B
6B
12The compound preparation of forming,
Compound preparation of the present invention contains the diclofenac sodium and the vitamin B of effective dose
1B
6B
12, by diclofenac sodium being made slow-released part again and vitamin B
1B
6B
12Be mixed and made into and be fit to oral preparation.
Compound preparation of the present invention also contains the medicine acceptable carrier, wherein active component diclofenac sodium and vitamin B
1B
6B
12Account for the 1-99% of total formulation weight amount, the medicine acceptable carrier accounts for the 1-99% of total formulation weight amount.The binding agent that described medicine acceptable carrier is a pharmaceutical purpose, filler, lubricant, disintegrating agent and other pharmaceutically acceptable auxiliaries.
Compound preparation of the present invention can be any dosage form that reaches the object of the invention of suitable for oral administration, as: tablet, capsule, granule, liposome, pill etc., preferably tablet, capsule.
Compound preparation of the present invention can contain in every dose, and diclofenac sodium is 10-200mg, vitamin B
1Be 10-200mg, vitamin B
6Be 10-200mg, vitamin B
12Be 0.1-1mg.Described every dose refers to every or every capsules.
When diclofenac sodium is made slow-released part, what use is medicinal slow-release material, slow-release material can use cellulose family, pyrrolidinone compounds, polyalcohols, Sargassum acids, stearic acid, can select their one or more mixed polymer in use, specifically can be but be not limited to following substances: hydroxypropyl methylcellulose (K
4MK
100M), sodium alginate, chitosan, polyvinyl alcohol, stearic acid, glyceryl monostearate, Brazil wax, ethyl cellulose, polymethyl methacrylate etc.
Below be the preparation method of tablet of the present invention:
Diclofenac sodium is mixed with the pharmaceutical purpose composition, thereby obtain preferred the processing and processing characteristics, operable medicinal ingredient comprises binding agent, filler, lubricant, disintegrating agent and other pharmaceutically acceptable auxiliaries.
Preferably, add a certain amount of binder solution, wet granulation with diclofenac sodium and medicinal ingredient mix homogeneously such as the slow-release material that suits, filler, disintegrating agent.The oven dry of gained granule adds the moderate lubrication agent to a certain degree, is pressed into the tablet that is fit to specification and size.
With a certain amount of vitamin B
1B
6B
12With an amount of filler, binding agent, collapse medicinal ingredient mix homogeneously such as connecing agent, lubricant, mix with the Dicolfanac Sodium Sustained Release Tablets agent of above-mentioned compacting again, be pressed into double-layer tablet.Promptly get the described compound sustained-released double-layer tablet of this invention.
This compound sustained-released double-layer tablet, wherein, one deck is the diclofenac sodium slow release layer, its 24 hours slow release that are released in vivo discharges; One deck is a vitamin B
1B
6B
12Often release layer, its intravital release meets conventional tablet and discharges model.
Below be capsular preparation method of the present invention:
By the material and the preparation technology of Dicolfanac Sodium Sustained Release Tablets in the above-mentioned compound sustained-released double-layer tablet, the diclofenac sodium slow release small pieces of compacting 5-6mm.
With a certain amount of vitamin B
1B
6B
12Powder promptly gets the described compound diclofenac natrium slow releasing capsule of this invention with the diclofenac sodium slow release small pieces filled hard capsules of mix homogeneously such as an amount of filler, lubricant with above-mentioned gained.
This compound sustained release capsules wherein, contains a slice diclofenac sodium slow release small pieces in every capsules, diclofenac sodium is that 24 hours slow release discharge in vivo; Vitamin B
1B
6B
12For Powdered, meet conventional capsule in vivo and discharge model.
Diclofenac sodium also can be made into slow-release pill, again with vitamin B
1B
6B
12Powder mixes is even, and filled capsules promptly gets the compound diclofenac natrium slow releasing capsule.
Being prepared as follows of diclofenac sodium slow-release pill is described:
With diclofenac sodium and suitable component, comprise mix homogeneously such as binding agent, filler, through suitably handling, make suitable core piller.Described core piller can be through extruding/round as a ball prepared, and gained core piller is used for further processing.
In addition, technologies such as available inert species nuclear laminating method, powder lamination method, fluid bed suspension coating method, preparation contains the core pellet of active substance, and the gained core pellet is used for further processing.
Use suitable packaging technique, one or more slow-release materials are coated on the above-mentioned core piller, promptly get the diclofenac sodium slow-release micro-pill.Slow-release material can be dispersed or dissolved in the water or in the appropriate organic solvent.Can use one or more following polymers as the sustained release coating layer, but be not limited to following substances: cellulose acetate, ethyl cellulose, hypromellose, Eudragit NE 30D, Eudragit RL 100, Eudragit RS 100 etc.
The sustained release coating layer can contain pharmaceutically useful plasticizer so that obtain the consistency and elasticity of necessary mechanical strength such as slow release layer.Described plasticizer can include, but are not limited to phthalic acid ester, Polyethylene Glycol, spermol or other plasticizers.In this slow release layer, also can comprise additive such as dispersant, coloring agent, antiplastering aid etc.
With a certain amount of vitamin B
1B
6B
12Mix homogeneously such as powder and an amount of filler, lubricant with the diclofenac sodium slow-release pill filled hard capsules of above-mentioned gained, promptly get the described compound diclofenac natrium slow releasing capsule of this invention
This compound sustained release capsules, wherein, diclofenac sodium is a slow-release micro-pill, its being released to 24 hours and slowly discharging in vivo; Vitamin B
1B
6B
12For Powdered, meet conventional capsule in vivo and discharge model.
Compound preparation of the present invention, can reach be administered once in one day can the whole day pain management effect, use the Neurofenac can be more convenient, more to one's profit economically than patient, the Neurofenac preparation of the more common release of side effect simultaneously decreases, and preparation is very stable also.
The specific embodiment:
Further specify the present invention by the following examples.
Embodiment 1
Prescription:
Diclofenac sodium 50g
HPMC?
K15M 35g
EC 15g
Lactose 55g
Microcrystalline Cellulose 80g
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g
10%PVP solution is an amount of
Preparation technology:
With diclofenac sodium 50g, HPMC35g, EC15g, microcrystalline Cellulose 45g, lactose 30g mix homogeneously, to granulate with 10%PVP solution, oven dry adds magnesium stearate, tabletting.
With vitamin B
150g, B
650g, B
120.25g with microcrystalline Cellulose 35g, lactose 20g mix homogeneously, suppress double-layer tablet with the Dicolfanac Sodium Sustained Release Tablets of above-mentioned compacting again, promptly get the fragrant sour sodium slow releasing tablet of salicyic acid chlorine.
Embodiment 2
Prescription:
Diclofenac sodium 50g
HPMC?
K15M 15g
EC 25g
Lactose 15g
Microcrystalline Cellulose 30g
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g
10%PVP solution is an amount of
Preparation technology:
With diclofenac sodium 50g, HPMC 15g, EC 25g, microcrystalline Cellulose 15g mix homogeneously, to granulate with 10%PVP solution, oven dry adds magnesium stearate, with 6mm punch die tabletting.
With vitamin B
150g, B
650g, B
120.25g with microcrystalline Cellulose 15g, lactose 15g mix homogeneously, load hard capsule No. 1 with the diclofenac sodium slow release small pieces of above-mentioned compacting again, promptly get compound sustained release capsules of the present invention.
Embodiment 3
Prescription:
Diclofenac sodium 50g
Lactose 50g
Microcrystalline Cellulose 50g
10%PVP solution is an amount of
Eudragit?NE?30D 16.5g
Pulvis Talci 1.5g
Pure water 80ml
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g
Preparation technology:
Make binding agent with 10%PVP, by extrude/spheronization prepares diclofenac sodium and contains pill core, the oven dry of gained pastille piller is put in the centrifugal coating pelletizing machine, with the Eudragit NE30D coating solution coating of preparation.Promptly get the diclofenac sodium slow-release pill.Again with fragrant sour sodium slow-release pill of the diclofenac of gained and the suitable vitamin B of handling of process
1B
6B
12Mix and load capsule, promptly get compound sustained release capsules of the present invention.
Claims (10)
1, a kind of compound slow release preparation is characterized in that, this compound slow release preparation is by the diclofenac sodium and the vitamin B of slow release
1, vitamin B
6, vitamin B
12, and the medicine acceptable carrier is formed.
2, the compound slow release preparation of claim 1 is characterized in that, in this compound slow release preparation, diclofenac sodium is a slow release, vitamin B
1, vitamin B
6, vitamin B
12For often releasing.
3, the compound slow release preparation of claim 1 is tablet or capsule, contains diclofenac sodium 10-200mg, vitamin B in every dose
110-200mg, vitamin B
610-200mg, vitamin B
120.1-1mg.
4, the compound slow release preparation of claim 3 is double-layer tablet, and one deck is the diclofenac sodium slow release layer, and another layer is a vitamin B
1, vitamin B
6, vitamin B
12Often release layer.
5, the compound slow release preparation of claim 3, wherein diclofenac sodium is the slow release small pieces, vitamin B
1, vitamin B
6, vitamin B
12Be powder, place same capsule.
6, the compound slow release preparation of claim 4, wherein diclofenac sodium is a slow-release pill, vitamin B
1, vitamin B
6, vitamin B
12Be powder, place same capsule.
7, the compound slow release preparation of claim 4-6, wherein the used slow-release material of the diclofenac sodium of slow release is selected from hydroxypropyl emthylcellulose, sodium alginate, chitosan, polyvinyl alcohol, stearic acid, glyceryl monostearate, Brazil wax, ethyl cellulose, polymethyl methacrylate, cellulose acetate, Eudragit NE30D, Eudragit RL100, Eudragit RS100.
8, the compound slow release preparation of claim 3 is tablets, by
Diclofenac sodium 50g
HPMC?
K15M 35g
EC 15g
Lactose 55g
Microcrystalline Cellulose 80g
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g
10%PVP solution is made in right amount, and its preparation method is as follows, and diclofenac sodium 50g, HPMC35g, EC15g, microcrystalline Cellulose 45g, lactose 30g are mixed, and granulates with 10%PVP solution, and oven dry adds magnesium stearate, tabletting.With vitamin B
150g, B
650g, B
120.25g mix with microcrystalline Cellulose 35g, lactose 20g, suppress double-layer tablet with the Dicolfanac Sodium Sustained Release Tablets of above-mentioned compacting again.
9, the compound slow release preparation of claim 3 is capsules, by
Diclofenac sodium 50g
HPMC?
K15M 15g
EC 25g
Lactose 15g
Microcrystalline Cellulose 30g
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g
10%PVP solution is made in right amount, and its preparation method is as follows, and diclofenac sodium 50g, HPMC 15g, EC 25g, microcrystalline Cellulose 15g are mixed, and granulates with 10%PVP solution, and oven dry adds magnesium stearate, tabletting.With vitamin B
150g, B
650g, B
120.25g mix with microcrystalline Cellulose 15g, lactose 15g, load capsule with the diclofenac sodium slow release small pieces of above-mentioned compacting again.
10, the compound slow release preparation of claim 3 is capsules, by
Diclofenac sodium 50g
Lactose 50g
Microcrystalline Cellulose 50g
10%PVP solution is an amount of
Eudragit?NE?30D 16.5g
Pulvis Talci 1.5g
Pure water 80ml
Vitamin B
150g
Vitamin B
650g
Vitamin B
120.25g
Magnesium stearate 1.8g makes; its preparation method is as follows; make binding agent with 10%PVP; by extrude/spheronization prepares diclofenac sodium and contains pill core; the oven dry of gained pastille piller is put in the centrifugal coating pelletizing machine, with the Eudragit NE30D coating solution coating of preparation; promptly get the diclofenac sodium slow-release pill, again with fragrant sour sodium slow-release pill of the diclofenac of gained and vitamin B
1B
6B
12Mix and load capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03123921 CN1452983A (en) | 2003-05-20 | 2003-05-20 | Delayed-releasing compound diclofenac sodium prepn |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03123921 CN1452983A (en) | 2003-05-20 | 2003-05-20 | Delayed-releasing compound diclofenac sodium prepn |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1452983A true CN1452983A (en) | 2003-11-05 |
Family
ID=29260298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03123921 Pending CN1452983A (en) | 2003-05-20 | 2003-05-20 | Delayed-releasing compound diclofenac sodium prepn |
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| Country | Link |
|---|---|
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101453996B (en) * | 2006-04-03 | 2016-05-11 | 伊萨·奥迪迪 | Drug delivery composition |
| 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 |
| CN114302728A (en) * | 2019-08-26 | 2022-04-08 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B12 |
| CN114302713A (en) * | 2019-08-26 | 2022-04-08 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B6 |
| CN114340602A (en) * | 2019-08-26 | 2022-04-12 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B1 |
-
2003
- 2003-05-20 CN CN 03123921 patent/CN1452983A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101453996B (en) * | 2006-04-03 | 2016-05-11 | 伊萨·奥迪迪 | Drug delivery composition |
| 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 |
| CN114302728A (en) * | 2019-08-26 | 2022-04-08 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B12 |
| CN114302713A (en) * | 2019-08-26 | 2022-04-08 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B6 |
| CN114340602A (en) * | 2019-08-26 | 2022-04-12 | 帝斯曼知识产权资产管理有限公司 | Solid oral dosage form comprising naproxen and vitamin B1 |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |