CN105520915A - Fenoprofen sustained-release tablets and preparation method thereof - Google Patents

Fenoprofen sustained-release tablets and preparation method thereof Download PDF

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Publication number
CN105520915A
CN105520915A CN201410516666.2A CN201410516666A CN105520915A CN 105520915 A CN105520915 A CN 105520915A CN 201410516666 A CN201410516666 A CN 201410516666A CN 105520915 A CN105520915 A CN 105520915A
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CN
China
Prior art keywords
fenoprofen
preparation
calcium
tablet
sustained release
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.)
Pending
Application number
CN201410516666.2A
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Chinese (zh)
Inventor
曾培安
周群
吴健民
贺莲
张静
刘娟
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kamp Pharmaceuticals Co Ltd
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Kamp Pharmaceuticals Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Kamp Pharmaceuticals Co Ltd filed Critical Kamp Pharmaceuticals Co Ltd
Priority to CN201410516666.2A priority Critical patent/CN105520915A/en
Publication of CN105520915A publication Critical patent/CN105520915A/en
Pending legal-status Critical Current

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Abstract

The invention relates to fenoprofen sustained-release tablets and a preparation method thereof. The fenoprofen sustained-release tablets prepared by the method comprise fenoprofen calcium serving as the main medicine and pharmaceutic adjuvant, wherein the pharmaceutic adjuvant includes acid environment modifier, sustained-release materials, binder and lubricant. The fenoprofen sustained-release tablets prepared by the method has the advantages that the side effects of the fenoprofen sustained-release tablets are reduced, the safety of the fenoprofen sustained-release tablets is increased, the fenoprofen sustained-release tablets are good in stability, fast in dissolution and good in releasing rate, administration frequency is reduced, and the compliance of a patient is increased. The preparation method is simple, suitable for industrial production and promising in market prospect.

Description

A kind of fenoprofen sustained release tablet of calcium and preparation method thereof
Technical field
The present invention relates to biomedical product field, particularly a kind of fenoprofen sustained release tablet of calcium and preparation method thereof.
Background technology
Fenoprofen calcium is a kind of anti-inflammatory analgesic.This product is white crystalline powder; Odorless, tasteless.Dissolve in ethanol, slightly soluble in methanol, soluble,very slightly in water, almost insoluble in chloroform.Be applicable to various arthritis, comprise rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gouty arthritis and other soft tissue pains.Also for other pain as dysmenorrhea, toothache, damage and traumatic pain etc.This product is also phenylpropionic acid derivative, is NSAID (non-steroidal anti-inflammatory drug); Reduced the synthesis of prostaglandin by the suppression to epoxidase, therefore alleviate the sensitivity of tissue hyperemia, swelling, the reduction peripheral nerve pain sensation.It plays refrigeration function by hypothalamus center of body temperature regulation.Absorbed following oral administration is fast, and absorb when roughly the same taking with food, milk and slow down, 1 ~ 2 hour blood drug level peaking after single administration 600mg, concentration is 50mg/ml, and protein binding rate is 99%.T1/2 is 3 hours, discharges in 90% in 24 hours from urine.Mainly discharge with glucuronide form.About 2% discharges from feces.This product is because the half-life is short, medication frequent and stimulate gastrointestinal therefore be suitable for making slow releasing preparation to solve above deficiency.
Summary of the invention
The present invention aims to provide a kind of fenoprofen sustained release tablet of calcium and preparation method thereof, thus the solution fenoprofen calcium conventional formulation half-life is short, medication problem frequently.
For achieving the above object, a kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, technical scheme is:
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that this slow releasing tablet is made up of principal agent fenoprofen calcium and pharmaceutic adjuvant, and pharmaceutic adjuvant comprises sour environment regulator, slow controlled-release material, binding agent, lubricant.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that each weight percentages of components of this slow releasing tablet is counted:
Fenoprofen calcium 10-99% sour environment regulator 1%-10%
Slow controlled-release material 10-65% lubricant 1%-5% binding agent 1-10%.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that the preparation method of this slow releasing tablet is:
1) above-mentioned supplementary material is crossed 100 sieves for subsequent use;
2) take fenoprofen calcium by prescription, mix with the sour environment regulator controlled-release material that eases up, cross 50-100 mesh sieve, mixing, adds binding agent soft material;
3) by step 2) gained soft material crosses 10-30 screen cloth and granulates, with 10-30 mesh sieve granulate after dry;
4) add mix lubricant even, rush in row tabletting with 11mm, adjustment tableting pressure and sheet weight, be pressed into tablet.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that the sour environment regulator of this slow releasing tablet is acrylic acid number resin salt hydrochlorate.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that the slow controlled-release material of this slow releasing tablet is one or more in hydroxypropyl cellulose, hydroxypropyl emthylcellulose, polyacrylic resin II, ethyl cellulose, sodium carboxymethyl cellulose.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that the lubricant of this slow releasing tablet is one or both in magnesium stearate, micropowder silica gel.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that the binding agent of this slow releasing tablet is 60-95% alcoholic solution or 5-8% starch slurry.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that this preparation method step 2) cross 65 mesh sieve 3 times.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that this preparation method step 3) baking temperature is 55-70 DEG C.
A kind of fenoprofen sustained release tablet of calcium of the present invention and preparation method thereof, is characterized in that this preparation method step 4) gained tablet hardness is 5kg/cm 2, sheet is heavily 0.6g.
Beneficial effect of the present invention has:
1. reduce the side effect of preparation, improve the safety of preparation;
2. medicine stability is good, and release conforms with the regulations, and reduces administration frequency, increases the compliance of patient;
3. simple for process, be applicable to industrialized great production.
accompanying drawing illustrates:
Fig. 1 is: fenoprofen calcium dissolution of sustained-release tablets curve chart.
Detailed description of the invention
Following embodiment only for further illustrating technical solution of the present invention, does not limit the present invention in any form.
embodiment 1
The following film-making of prescription 1000 of fenoprofen calcium:
Name of material Consumption (g) Ratio (%)
Fenoprofen calcium 300 50
Acrylic acid Number resin salt hydrochlorate 30 5
Hydroxypropyl cellulose 60 10
Hydroxypropyl emthylcellulose 120 20
60% alcoholic solution In right amount -
Polyacrylic resin II 36 6
Magnesium stearate 12 2
Preparation method: above-mentioned supplementary material is crossed 100 mesh sieves for subsequent use, take fenoprofen calcium by prescription, starch mixes, cross 65 mesh sieve 3 times, mixing, then add the hydroxypropyl emthylcellulose mixing of recipe quantity, add 60% alcoholic solution soft material, cross 20 eye mesh screens and granulate, after 55 DEG C of dryings, use 24 mesh sieve granulate.Add magnesium stearate mix homogeneously, rush in row tabletting with 11mm, adjustment tableting pressure and sheet weight, be pressed into slice, thin piece hardness and be about 5kg/cm 2, sheet is heavily about the tablet of 0.6g.Fenoprofen calcium tablet is gone out by above formula preparation.
embodiment 2
The following film-making of prescription 1000 of fenoprofen calcium:
Name of material Consumption (g) Ratio (%)
Fenoprofen calcium 180 30
Acrylic acid Number resin salt hydrochlorate 30 5
Hydroxypropyl cellulose 120 20
Hydroxypropyl emthylcellulose 150 25
75% alcoholic solution In right amount -
Polyacrylic resin II 48 8
Micropowder silica gel 12 2
Preparation method: above-mentioned supplementary material is crossed 100 mesh sieves for subsequent use, take fenoprofen calcium by prescription, starch mixes, cross 65 mesh sieve 3 times, mixing, then add the hydroxypropyl emthylcellulose mixing of recipe quantity, add 75% alcoholic solution soft material, cross 20 eye mesh screens and granulate, after 60 DEG C of dryings, use 24 mesh sieve granulate.Add micropowder silica gel mix homogeneously, rush in row tabletting with 11mm, adjustment tableting pressure and sheet weight, be pressed into slice, thin piece hardness and be about 5kg/cm 2, sheet is heavily about the tablet of 0.6g.Fenoprofen calcium tablet is gone out by above formula preparation.
embodiment 3
The following film-making of prescription 1000 of fenoprofen calcium:
Name of material Consumption (g) Ratio (%)
Fenoprofen calcium 300 50
Acrylic acid Number resin salt hydrochlorate 30 5
Ethyl cellulose 60 10
Hydroxypropyl emthylcellulose 120 20
Sodium carboxymethyl cellulose 60 10
95% alcoholic solution In right amount -
Polyacrylic resin II 18 3
Magnesium stearate 12 2
Preparation method: above-mentioned supplementary material is crossed 100 mesh sieves for subsequent use, fenoprofen calcium is taken by prescription, sodium carboxymethyl cellulose mixes, cross 65 mesh sieve 3 times, mixing, then the hydroxypropyl emthylcellulose mixing adding recipe quantity, add 95% alcoholic solution soft material, cross 20 eye mesh screens to granulate, after 65 DEG C of dryings, use 24 mesh sieve granulate.Add magnesium stearate mix homogeneously, rush in row tabletting with 11mm, adjustment tableting pressure and sheet weight, be pressed into slice, thin piece hardness and be about 5kg/cm 2, sheet is heavily about the tablet of 0.6g.Fenoprofen calcium tablet is gone out by above formula preparation.
embodiment 4
The following film-making of prescription 1000 of fenoprofen calcium:
Name of material Consumption (g) Ratio (%)
Fenoprofen calcium 180 30
Acrylic acid Number resin salt hydrochlorate 30 5
Hydroxypropyl cellulose 120 20
Hydroxypropyl emthylcellulose 150 25
8% starch slurry In right amount -
Sodium carboxymethyl cellulose 60 10
Polyacrylic resin II 48 8
Micropowder silica gel 12 2
Preparation method: above-mentioned supplementary material is crossed 100 mesh sieves for subsequent use, fenoprofen calcium is taken by prescription, sodium carboxymethyl cellulose mixes, cross 65 mesh sieve 3 times, mixing, then the hydroxypropyl emthylcellulose mixing adding recipe quantity, add 8% starch slurry soft material, cross 20 eye mesh screens to granulate, after 70 DEG C of dryings, use 24 mesh sieve granulate.Add magnesium stearate mix homogeneously, rush in row tabletting with 11mm, adjustment tableting pressure and sheet weight, be pressed into slice, thin piece hardness and be about 5kg/cm 2, sheet is heavily about the tablet of 0.6g.Fenoprofen calcium tablet is gone out by above formula preparation.
Embodiment 1-4 release changes experimental data in time:
Time Embodiment 1 Embodiment 2 Embodiment 3 Embodiment 4
0 0 0 0 0
2 10.43 5.21 7.36 8.97
4 25.52 19.37 15.98 17.76
6 45.75 38.34 42.89 35.88
8 70.47 60.24 55.56 65.65
10 88.42 78.87 72.87 75.66
12 98.68 89.69 85.07 93.96

Claims (10)

1. fenoprofen sustained release tablet of calcium and preparation method thereof, is characterized in that this slow releasing tablet is made up of principal agent fenoprofen calcium and pharmaceutic adjuvant, and pharmaceutic adjuvant comprises sour environment regulator, slow controlled-release material, binding agent, lubricant.
2. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that each weight percentages of components of this slow releasing tablet is counted:
Fenoprofen calcium 10-99% sour environment regulator 1%-10%
Slow controlled-release material 10-65% lubricant 1%-5% binding agent 1-10%.
3. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that the preparation method of this slow releasing tablet is:
1) above-mentioned supplementary material is crossed 100 sieves for subsequent use;
2) take fenoprofen calcium by prescription, mix with the sour environment regulator controlled-release material that eases up, cross 50-100 mesh sieve, mixing, adds binding agent soft material;
3) by step 2) gained soft material crosses 10-30 screen cloth and granulates, with 10-30 mesh sieve granulate after dry, dry, granulate;
4) add mix lubricant even, carry out tabletting with 11mm punch die, adjustment tableting pressure and sheet weight, be pressed into tablet.
4. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that the sour environment regulator of this slow releasing tablet is acrylic acid number resin salt hydrochlorate.
5. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that the slow controlled-release material of this slow releasing tablet is one or more in hydroxypropyl cellulose, hydroxypropyl emthylcellulose, polyacrylic resin II, ethyl cellulose, sodium carboxymethyl cellulose.
6. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that the lubricant of this slow releasing tablet is one or both in magnesium stearate, micropowder silica gel.
7. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 1, is characterized in that the binding agent of this slow releasing tablet is 60-95% alcoholic solution or 5-8% starch slurry.
8. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 3, is characterized in that this preparation method step 2) cross 65 mesh sieve 3 times.
9. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 3, is characterized in that this preparation method step 3) baking temperature is 55-70 DEG C.
10. a kind of fenoprofen sustained release tablet of calcium and preparation method thereof according to claim 3, is characterized in that this preparation method step 4) gained tablet hardness is 5kg/cm 2, sheet is heavily 0.6g.
CN201410516666.2A 2014-09-30 2014-09-30 Fenoprofen sustained-release tablets and preparation method thereof Pending CN105520915A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201410516666.2A CN105520915A (en) 2014-09-30 2014-09-30 Fenoprofen sustained-release tablets and preparation method thereof

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201410516666.2A CN105520915A (en) 2014-09-30 2014-09-30 Fenoprofen sustained-release tablets and preparation method thereof

Publications (1)

Publication Number Publication Date
CN105520915A true CN105520915A (en) 2016-04-27

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Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1352938A (en) * 2000-11-14 2002-06-12 北京万全阳光医药科技有限公司 Slowly releasing bupropion hydrochloride tablet

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1352938A (en) * 2000-11-14 2002-06-12 北京万全阳光医药科技有限公司 Slowly releasing bupropion hydrochloride tablet

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
李娟等: "非诺洛芬钙缓释片的研制及释药性质研究", 《中国药科大学学报》 *
赵春顺等: "非诺洛芬钙亲水凝胶缓释骨架片释药机理的研究", 《药学学报》 *
赵春顺等: "非诺洛芬钙缓释片的制备及其人体药动学初步研究", 《中国药学杂志》 *

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Application publication date: 20160427

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