CN1210022C - Dichlofenac sodium slow-releasing preparation and its preparation method - Google Patents
Dichlofenac sodium slow-releasing preparation and its preparation method Download PDFInfo
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- CN1210022C CN1210022C CN 03126777 CN03126777A CN1210022C CN 1210022 C CN1210022 C CN 1210022C CN 03126777 CN03126777 CN 03126777 CN 03126777 A CN03126777 A CN 03126777A CN 1210022 C CN1210022 C CN 1210022C
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- diclofenac sodium
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- releasing preparation
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Abstract
The present invention discloses a diclofenac sodium slow releasing preparation which uses a biologic frame membrane as a carrier. The present invention is prepared from 0.5 to 20 wt% of diclofenac sodium, 70 to 85 wt% of biologic frame membrane, 0.1 to 0.5 wt% of permeation accelerant, and 5 to 15 wt% of enteric coating membrane. The diclofenac sodium slow releasing preparation of the present invention overcomes the defects existing in the existing diclofenac sodium slow releasing preparation. The present invention has the advantages that the slow releasing performance is good, the effective blood drug level can be kept in a human body for a long time, the biocompatibility is good, and the stimulation from the diclofenac sodium for the gastric mucosa is avoided. The present invention also discloses a preparation method of the diclofenac sodium slow releasing preparation. The method does not need shaping equipment, the technology is simple, and the environmental pollution caused by the synthetic process of auxiliary material is avoided.
Description
Technical field
The present invention relates to a kind of slow releasing preparation and preparation method thereof, particularly a kind of is the diclofenac sodium slow releasing preparation and preparation method thereof of carrier with the biological skeleton film.
Background technology
At present, slow releasing preparation all is to be blocker with synthetic or semisynthetic material, for example cellulose family, resinae, chitosan class and wax class, and its controlled release mode comprises framework controlled release, film controlled release and skeleton-film controlled release.Preparation type has tablet, capsule, pill etc., all necessary special modular system of its manufacture process, and complex technical process, the place that needs is big.Do not find as yet that in existing technology the applying biological framework film is the diclofenac sodium slow releasing preparation of preparing carriers, existing diclofenac sodium slow releasing preparation, stimulation to the stomach film is bigger, biocompatibility is poor, sustained release performance is also relatively poor, and manufacture process needs special modular system, complex technical process in addition, the place that needs is big, and the certain pollution that can bring to environment of adjuvant building-up process.
Summary of the invention
The objective of the invention is to overcome the shortcoming that existing diclofenac sodium slow releasing preparation exists, providing a kind of has the good slow release performance, can keep effective blood drug concentration, good biocompatibility for a long time in vivo and has avoided the diclofenac sodium slow releasing preparation of diclofenac sodium to the stimulation of stomach film.
Another object of the present invention is to provide a kind of and do not need modular system, technology is simple and avoided the above-mentioned diclofenac sodium slow releasing preparation of the preparation method of adjuvant environmental pollution that building-up process is brought.
Diclofenac sodium slow releasing preparation of the present invention is to be carrier with the biological skeleton film, consists of:
Diclofenac sodium 0.5～20 weight %
Biological skeleton film 70～85 weight %
Short penetrating agent 0.1～0.5 weight %
Enteric coating film 5～15 weight %
Wherein the biological skeleton film is a seed, especially is edible plant seed, as corn, bean, foxtail millet or Semen Sesami etc.; Short penetrating agent is propylene glycol or ethanol.The enteric coating film is formed by 35～65 weight % acrylic resins, 10～30 weight % plasticizers, 5～15 weight % surfactants, 10～25 weight % antiplastering aid suspension spray coatings.Wherein acrylic resin is acrylic resin I, II or III number; Plasticizer is triethyl citrate, o-benzoic acid diethylester, acetic acid monoglyceride, Oleum Ricini, certain herbaceous plants with big flowers two dibutyl phthalates or oleic acid; Surfactant is Tweens, spans or monovalence ammonium amine soap class; Antiplastering aid is Pulvis Talci or Kaolin.
Diclofenac sodium slow releasing preparation preparation method of the present invention is as follows:
(1) seed medicine carrying
0.5～20 weight % diclofenac sodium dissolve with pH9～11 alkali liquor, add the short penetrating agent of 0.1～0.5 weight % then, mixing, again 70～85 weight % biological skeleton films are added mixing, airtight, be positioned in the supersonic generator the ultrasonic 0.5～1.5bar 60～80 minutes of pressurizeing below 30～90 minutes or 50～80 ℃, take out drying, obtain the medicine carrying seed.
(2) enteric coated
(1) preparation of enteric coating suspension
35～65 weight % acrylic resins, with 500～1000 milliliter of 95% soak with ethanol 5～10 hours, dissolving, add 10～30 weight % plasticizers, 5～15 weight % surfactants, 10～25 weight % antiplastering aids then, stir, mixing filters with 200 mesh sieves.
(2) enteric coated
With the medicine carrying seed with 150～250 milliliters of enteric coating suspensions, spray coating, drying.
Wherein, the used alkali of dissolving diclofenac sodium is NaOH, Na
2CO
3, NaHCO
3Deng.
Spray coating carries out in ebullated bed coating machine, and the working condition of ebullated bed coating machine is 45～65 ℃ of baking temperatures, and atomisation pressure is 0.6～3.0bar, and the wriggling pump speed is 0.5～5 ml/min.Coating is if use turnadle pan coating, and the axle of coating pan becomes 30 degree with level, and Revolution Per Minute 45 changes 45～55 ℃ of baking temperatures, spray velocity 1～3 ml/min.
Diclofenac sodium slow releasing preparation of the present invention, external dissolution test, simulated gastric fluid, the clothing film was insoluble in 2 hours, in simulated intestinal fluid, dissolving in 3 minutes can effectively be kept diclofenac sodium and discharge more than 8 hours, with diclofenac sodium conventional formulation ratio on the market, can suitably control the rate of release of medicine, prolong this medicine keeping of blood valid density in vivo, and overcome the shortcoming that existing diclofenac sodium slow releasing preparation exists, good biocompatibility is avoided the stimulation of diclofenac sodium to the stomach film.The environmental pollution that preparation method does not need modular system in addition, technology is simple and avoided the adjuvant building-up process to be brought.
The specific embodiment
Following embodiment will help those of ordinary skill in the art further to understand the present invention, but not limit the present invention in any form.
Embodiment 1
(1) the corn medicine carrying is dissolved in pH10 Na with dichlorophen sodium 10 grams
2CO
3In the solution, add propylene glycol 0.5 gram, mixing adds that corn 70 grams are airtight to be positioned in the supersonic generator 60 minutes, takes out drying.
(2) enteric coated
(1) preparation of enteric coating suspension
Acrylic resin I30 gram, with 800 milliliter of 95% soak with ethanol 6 hours, dissolving added o-benzoic acid dibutyl ester 3 grams, Oleum Ricini 12 grams then, and liquid paraffin 12 grams, tween 80 12 grams, Pulvis Talci 15 grams stir, and mixing filters.
(2) enteric coated
With the medicine carrying seed with 200 milliliters of enteric coating suspensions, spray coating, drying.
Spray coating carries out in ebullated bed coating machine, and the working condition of ebullated bed coating machine is 50 ℃ of baking temperatures, and atomisation pressure is 1.0bar, and the wriggling pump speed is 2 ml/min.
Embodiment 2
(1) Semen Glycines medicine carrying
Diclofenac sodium 15 grams are dissolved in pH11 NaHCO
3In the solution, add 10 milliliters of ethanol then, mixing adds Semen Glycines 80 grams again and stirs evenly, and is incubated 65 ℃, and pressurization 1.5bar 60 minutes, takes out drying.
(2) enteric coated
(1) preparation of enteric coating suspension
Acrylic resin II50 gram, with 800 milliliter of 95% soak with ethanol 10 hours, dissolving added triethyl citrate 5 grams, certain herbaceous plants with big flowers two dibutyl phthalates 15 grams, oleic acid 8 grams, Kaolin 20 grams, Arlacel-40 15 grams then, stirs, and mixing filters with 200 mesh sieves.
(2) enteric coated
With the carrier seed with 200 milliliters of enteric coating suspensions, spray coating, drying.
The coating turnadle pan coating, the axle of coating pan becomes 30 degree with level, and Revolution Per Minute 45 changes 50 ℃ of baking temperatures, spray velocity 3 ml/min.
Embodiment 3
(1) Semen Sesami medicine carrying
Diclofenac sodium 2 grams are dissolved in the pH9NaOH solution, add Semen Sesami 70 grams and stir evenly, add 10 milliliters of ethanol again, be incubated 65 ℃, pressurization 1.5bar 60 minutes, takes out drying.
(2) enteric coated
(1) preparation of enteric coating suspension
Acrylic resin III30 gram, with 800 milliliter of 95% soak with ethanol 5 hours, dissolving added o-benzoic acid dibutyl ester 3 grams, Oleum Ricini 12 grams, liquid paraffin 12 grams, Pulvis Talci 15 grams, tween 80 12 grams then, stirs, and mixing filters with 200 mesh sieves.
(2) enteric coated
With the carrier seed with 200 milliliters of molten clothing suspensions, spray coating, drying.
The coating turnadle pan coating, the axle of coating pan becomes 30 degree with level, and Revolution Per Minute 45 changes 50 ℃ of baking temperatures, spray velocity 3 ml/min.
Embodiment 4
The release test
Get the diclofenac sodium slow releasing preparation that makes in embodiment 1,2 and 3, be numbered sample 1, sample 2, sample 3, according to release method of testing (two appendix XD second methods of Chinese Pharmacopoeia version in 2000), adopt dissolution method first subtraction unit, getting 0.1mol/L hydrochloric acid solution 900ml is solvent, per minute 100 changes, and turns round 2 hours, immediately sampling.Discard acid solution in the said vesse, add phosphate buffer (pH6.8 ± 0.05) immediately, operation in accordance with the law, after 1,2,4 and 8 hour, get solution 10ml respectively, and replenish the phosphate buffer of uniform temp, equal volume simultaneously, filter, get subsequent filtrate, according to spectrophotography (two appendix IVP of Chinese Pharmacopoeia version in 2000
18), measure trap at the wavelength place of 276min, measurement result is as shown in table 1.
Table 1
| Release medium | Sample time (hour) | Average cumulative discharges percentage ratio (%) | ||
| Sample 1 | Sample 2 | Sample 3 | ||
| 0.1mol/L hydrochloric acid solution | 2 | -0.01 | 0.02 | -0.02 |
| Phosphate buffered solution (pH6.8 ± 0.05) | 1 | 23.29 | 22.88 | 20.88 |
| 2 | 36.50 | 33.69 | 31.66 | |
| 4 | 55.98 | 52.36 | 60.15 | |
| 8 | 88.30 | 86.59 | 90.20 | |
Claims (8)
1, a kind of diclofenac sodium slow releasing preparation is characterized in that with edible plant seed be carrier.
2, diclofenac sodium slow releasing preparation as claimed in claim 1 is characterized in that being prepared according to following steps by following method:
(1) seed medicine carrying
0.5～20 weight % diclofenac sodium dissolve with pH9～11 alkali liquor, add the short penetrating agent of 0.1～0.5 weight % then, mixing, again the edible plant seed of 70～85 weight % is added mixing, airtight, be positioned in the supersonic generator the ultrasonic 0.5～1.5bar 60～80 minutes of pressurizeing below 30～90 minutes or 50～80 ℃, take out drying, obtain the medicine carrying seed;
(2) enteric coated
(1) preparation of enteric coating suspension
35～65 weight % acrylic resins, with 500～1000 milliliter of 95% soak with ethanol 5～10 hours, dissolving added 10～30 weight % plasticizers, 5～15 weight % surfactants, 10～25 weight % antiplastering aids then, stirred, and mixing filters;
(2) enteric coated
With the medicine carrying seed with 150～250 milliliters of enteric coating suspensions, spray coating, drying.
3, diclofenac sodium slow releasing preparation as claimed in claim 2 is characterized in that edible plant seed is corn, bean, foxtail millet or Semen Sesami.
4, diclofenac sodium slow releasing preparation as claimed in claim 2 is characterized in that short penetrating agent is propylene glycol or ethanol.
5, diclofenac sodium slow releasing preparation as claimed in claim 2 is characterized in that the enteric coating film is formed by 35～65 weight % acrylic resins, 10～30 weight % plasticizers, 5～15 weight % surfactants, 10～25 weight % antiplastering aid suspension spray coatings.
6, diclofenac sodium slow releasing preparation as claimed in claim 7 is characterized in that acrylic resin is acrylic resin I, II or III number; Plasticizer is liquid paraffin, triethyl citrate, o-benzoic acid diethylester, acetic acid monoglyceride, Oleum Ricini, certain herbaceous plants with big flowers two dibutyl phthalates or oleic acid; Surfactant is Tweens, spans or monovalence ammonium amine soap class; Antiplastering aid is Pulvis Talci or Kaolin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03126777 CN1210022C (en) | 2003-06-06 | 2003-06-06 | Dichlofenac sodium slow-releasing preparation and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03126777 CN1210022C (en) | 2003-06-06 | 2003-06-06 | Dichlofenac sodium slow-releasing preparation and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1460470A CN1460470A (en) | 2003-12-10 |
| CN1210022C true CN1210022C (en) | 2005-07-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03126777 Expired - Fee Related CN1210022C (en) | 2003-06-06 | 2003-06-06 | Dichlofenac sodium slow-releasing preparation and its preparation method |
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| CN101804030B (en) * | 2009-02-12 | 2012-09-05 | 杭州赛利药物研究所有限公司 | Sodium dichlorophenolate micro-pill pharmaceutical preparation and preparation method thereof |
| CN105709208A (en) * | 2016-01-29 | 2016-06-29 | 陕西科技大学 | Preparation technology of bitter gourd protein enteric-coated tablets |
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2003
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