CN101181245A - Compound diclofenac natrium capsule - Google Patents
Compound diclofenac natrium capsule Download PDFInfo
- Publication number
- CN101181245A CN101181245A CNA2007101798447A CN200710179844A CN101181245A CN 101181245 A CN101181245 A CN 101181245A CN A2007101798447 A CNA2007101798447 A CN A2007101798447A CN 200710179844 A CN200710179844 A CN 200710179844A CN 101181245 A CN101181245 A CN 101181245A
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- misoprostol
- diclofenac
- sodium
- diclofenac sodium
- tablet
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Abstract
The invention designs a diclofenac sodium capsule, which more particularly consists of diclofenac sodium and misoprostol. At least one of the diclofenac sodium and the misoprostol is prepared into tablet, then the diclofenac sodium is coated with enteric coating, the misoprostol is coated with stomach coating, and the capsule of the invention is obtained by arranging the two into a capsule. The capsule of the invention can achieve the purpose of simultaneous absorption on the different parts, so as to better achieve the purpose of synergistic treatment.
Description
Technical field
The present invention relates to a kind of compound diclofenac natrium new formulation, belong to field of pharmaceutical preparations.
Background technology
Diclofenac sodium is NSAID (non-steroidal anti-inflammatory drug) (NSAID), and its easing pain and diminishing inflammation act as 2-2.5 times of indomethacin, is 26-50 times of aspirin.Be used for the treatment of rheumatism, rheumatoid arthritis, scapulohumeral periarthritis clinically, injure the inflammation that operation etc. causes outward, the heating that flu is caused also has curative effect preferably.Though diclofenac sodium is the lighter NSAID (non-steroidal anti-inflammatory drug) of a kind of toxic and side effects, but also occurred many untoward reaction in clinical practice, main adverse reactions has clinically: gastrointestinal reaction such as upper abdomen discomfort, feel sick, vomiting, occur intestinal bleeding, dizziness, erythra, granulocytopenia etc. when serious.Now clear and definite, the generation of most of untoward reaction is relevant with using dosage.At present, the clinical using dosage of diclofenac sodium is generally daily dose 75mg.
Misoprostol be on natural PGE1 chemical constitution through synthetic, its chemical constitution increases 35 times than parent.Rice institute prostatitis alcohol absorbs fast, and in medication 15 minutes, the blood plasma active metabolite has reached peak value.Misoprostol can directly act on gastrointestinal tract cell, the gastric acid inhibitory secretion, strengthen gastric mucosal barrier, and each phase gestation is obviously strengthened, its bring out miscarriage and hasten parturition main by excited myometrium, the increase of stimulon palace endogenous PG persistence, the altofrequency when causing this normal labor of class, high-amplitude and rhythmic uterine contraction, pregnant thing is discharged, reach the purpose of miscarriage or induced labor.In addition, the misoprostol gastric ulcer that can also be used to prevent nonsteroidal antiinflammatory drug (NSAID) to bring out, gastric perforation etc.
The approval diclofenac sodium and misoprostol kind be an imported medicine, two medicines share, misoprostol can reduce by diclofenac sodium cause to gastrointestinal side effect.The listing kind of approval is a kind of preparation unit with the form administration of making double-layer tablet, because the main side effect of diclofenac sodium is to cause stomach discomfort, as the heart-burn sense, pantothenic acid, ulcer, gastrorrhagia and gastric perforation, therefore when making preparation, preferably diclofenac sodium is made enteric coated preparation, therefore with the effect of minimizing to the discomfort of stomach, and misoprostol mainly is to reduce the discomfort effect of diclofenac sodium to stomach, because of making gastric solubility preparation, and when making the preparation of different parts release, double-layer tablet has the deficiency of itself, can not reach the purpose that discharges medicine simultaneously, need treat earlier that wherein a kind of medicine is in vivo after the position disintegrate, again medicine being transferred to other position disintegrate by body discharges, and misoprostol is rapid-action, and the half-life is short, therefore can not play ideal therapeutic effect.
Summary of the invention
For overcoming above-mentioned deficiency, the object of the present invention is to provide a kind of compound preparation of the new form of medication of forming by diclofenac sodium and misoprostol.Preparation of the present invention is a capsule, in capsule, at least a tablet form of making earlier in two kinds of main component diclofenac sodiums, the misoprostol, another kind can be granule, micropill, powder or tablet form, and then during these the two kinds principal agents of making pharmaceutical preparation are incapsulated.
Among the present invention, diclofenac sodium preparation unit bag is with enteric coating, misoprostol preparation unit bag is with the gastric solubleness clothing, during preparation behind the coating incapsulated, when taking, treat that in body capsule dissolves after, the preparation unit that different parts discharges medicine can arrive stomach and intestinal separately, disintegrate discharges in vivo, plays collaborative effect.
Among the present invention, diclofenac sodium can be made tablet, bag is with enteric coating, and misoprostol is made granule or micropill form, and bag is with the gastric solubleness clothing, and then during the two is incapsulated; Perhaps diclofenac sodium is made granule or micropill, bag is with enteric coating, and misoprostol is made tablet, and bag is with the gastric solubleness clothing, in incapsulating then; Also can be that diclofenac sodium is made tablet, enteric coated, misoprostol be made tablet, and bag is with the gastric solubleness clothing, in the examples of suitable of then the two being packed into.
Preparation unit in the capsule of the present invention is preferably all makes tablet form with diclofenac sodium and misoprostol.
The present invention makes the preparation unit of tablet, and the diameter of tablet is 4-8mm, is preferably 6mm.
A further object of the present invention provides the unitary prescription of tablet in the capsule.The prescription of diclofenac sodium of the present invention and misoprostol microplate is:
The prescription of diclofenac sodium sheet is:
Diclofenac sodium 50g filler 100-150g disintegrating agent 0-15g
Binding agent moderate lubrication agent 1-4g enteric coating powder 10-30g
Make 1000 altogether
The prescription of misoprostol sheet is:
Misoprostol 200mg filler 140-180g disintegrating agent 0-15g
Binding agent moderate lubrication agent 1-5g gastric solubleness coating powder 4-10g
Make 1000 altogether
Wherein said filler can be any one or two kinds of in starch, microcrystalline cellulose, lactose, the dextrin, described disintegrating agent can be any in polyvinylpolypyrrolidone, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose, and described binding agent can be the polyvidone of carboxymethylstarch slurry sodium, the 5%-15% of 5%～15% starch slurry, 2%-15%, in the 2%-10% hydroxypropyl emthylcellulose any; Lubricant can be any in magnesium stearate, the micropowder silica gel, described enteric coating powder can be any in Lac, Cellulose Acetate Phthalate, alginate jelly, polyvinyl alcohol acetic acid phthalic acid ester, acrylic resin, the hydroxypropyl methyl cellulose phthalate, described gastric solubleness adjuvant can be a hydroxypropyl cellulose, hydroxypropyl emthylcellulose, any in polyethylene acetal diethylin acetic acid and dimethylaminoethyl methacrylate-neutral methacrylic acid esters copolymer.
Preferably, prescription of the present invention is:
The diclofenac sodium prescription is:
Diclofenac sodium 50g lactose 80g microcrystalline Cellulose 45g
Polyvinylpolypyrrolidone 8g magnesium stearate 2g 10% polyvidone is an amount of
The ethanol of Cellulose Acetate Phthalate 18g 80% is an amount of
Make 1000
The prescription of misoprostol sheet is
Misoprostol 200mg starch 140g microcrystalline Cellulose 40g
Cross-linking sodium carboxymethyl cellulose 10g magnesium stearate 2g
An amount of gastric solubleness hypromellose of 8% hypromellose coating powder 8g
80% ethanol is an amount of
Make 1000 altogether
Preparation technology's following steps of the present invention:
One, particulate preparation:
Take by weighing principal agent, filler, disintegrating agent, lubricant, mixing is crossed 100 mesh sieves, adds binding agent, makes soft material, the system granule, and drying takes by weighing the packaging material material and adds in the alcoholic solution, and above-mentioned granule is placed coating pan, coating, the drum hot air drying is promptly.
Two, the preparation of micropill
Take by weighing partially filled dose, add binding agent, in the coating pelletizing machine, make celphere, 30-70 ℃ dry 3-8 hour, celphere; Other gets principal agent, filler, disintegrating agent, lubricant, and mixing is crossed 100 mesh sieves, celphere is placed coating pan, rotating speed 30-100rpm, the mixture of adding medicine and adjuvant, the ethanol of spray 70%, blocked operation all adds until medicated powder, after dosing finishes, take out, place pallet,, get plain ball in 50-80 ℃ of drying; Get coating material and add in the alcoholic solution, above-mentioned plain ball is put in the coating pan, spray into coating solution, the drum hot blast drying sprays into coating solution again, the drum hot blast drying, so repeatedly, to the coating about piller weightening finish 2%-15%.
Three, microplate preparation
Get principal agent, filler, mixing is crossed 100 mesh sieves, adds binding agent, granulates, dry, granulate, adds disintegrating agent again, lubricant, and mixing is pressed into the microplate of 4-8mm; Get coating solution and be dissolved in the alcoholic solution, microplate to coating pan, is sprayed coating solution, the drum hot blast drying sprays coating solution again, so repeats, to microplate coating weightening finish 2%-15%.
Four, encapsulated
Have to preparation unit, wherein contain a kind of tablet unit at least, incapsulate, promptly.
The present invention is owing to adopted the diclofenac sodium preparation unit and the misoprostol preparation unit of packing into independent in capsule, and wrap the coating material that discharges with different parts separately, when taking, after treating that capsule dissolves in vivo, the preparation unit of different coatings can discharge medicine at target site separately, play therapeutic effect better, and its administration is with a dosage form administration, not to take diclofenac sodium enteric tablet and misoprostol gastric soluble tablet respectively, can avoid the medication dose mistake that causes because of obscuring.And technology of the present invention is easy, adopts conventional pharmaceutical equipment to finish.Have the dosage form of selling on the market now and take, when bag discharges the coating at positions with two kinds of differences, because the as a whole preparation unit of double-layer tablet, drug release needs earlier at stomach or intestinal position, after treating that gastric soluble tablet or enteric coatel tablets disintegrate discharge, another kind of tablet could begin to discharge medicine, can not reach the purpose that discharges medicine simultaneously so in vivo and the effect that can not well play Synergistic treatment
Specific embodiment
Embodiment 1
One, the preparation of diclofenac sodium microplate
Get diclofenac sodium 50g, lactose 80g, microcrystalline cellulose 45g, mixing, cross 100 mesh sieves, 45% ethanol liquid of the polyvidone with 10% is binding agent, granulation, granulate, drying, add polyvinylpolypyrrolidone 8g, magnesium stearate 2g, mixing is pressed into the microplate of 1000 diameter 6mm; Take by weighing coating material Cellulose Acetate Phthalate 18g, be dissolved in 80% the ethanol, with microplate to coating pan, the spray coating solution, the drum hot air drying is to increasing to about 10% in the sheet, promptly.
Two, the preparation of misoprostol microplate
Get misoprostol 200mg, starch 140g, microcrystalline Cellulose 40g, mixing, cross 100 mesh sieves, the hypromellose with 8% is a binding agent, and granulation, dry, granulate add crosslinked carboxymethyl fecula sodium 10g, magnesium stearate 2g, mixing is pressed 1000 microplates that diameter is 6mm; Other gets gastric solubleness hypromellose coating powder 8g, is dissolved in 80% the ethanol, the misoprostol microplate is put in the coating pan, spray gastric solubleness coating solution, the drum hot air drying, to coating increase weight to sheet heavy about 4%, promptly.
Three, encapsulated
The diclofenac sodium microplate, the misoprostol sheet that suppress are packed in the capsule, promptly.
Embodiment 2
One, the preparation of diclofenac sodium microplate
Get diclofenac sodium 50g, dextrin 100g, microcrystalline cellulose 35g, mixing, cross 100 mesh sieves, the aqueous solution of the carboxymethylstarch slurry sodium with 10% is a binding agent, granulation, granulate, drying, add sodium carboxymethyl cellulose 10g, magnesium stearate 2g, mixing is pressed into the microplate of 1000 diameter 6mm; Take by weighing coating material hydroxypropyl methyl cellulose phthalate 28g, be dissolved in 80% the ethanol, with microplate to coating pan, the spray coating solution, the drum hot air drying is to increasing to about 14% in the sheet, promptly.
Two, the preparation of misoprostol microplate
Get misoprostol 200mg, starch lactose 130g, microcrystalline Cellulose 50g, mixing is crossed 100 mesh sieves, and the starch slurry with 10% is a binding agent, and granulation, dry, granulate add polyvinylpolypyrrolidone 10g, magnesium stearate 2g, mixing is pressed 1000 microplates that diameter is 6mm; Other gets gastric solubleness hydroxypropyl cellulose coating powder 5g, is dissolved in 80% the ethanol, the misoprostol microplate is put in the coating pan, spray gastric solubleness coating solution, the drum hot air drying, to coating increase weight to sheet heavy about 2%, promptly.
Three, encapsulated
The diclofenac sodium microplate, the misoprostol sheet that suppress are packed in the capsule, promptly.
Claims (5)
1. compound diclofenac natrium capsule, contain principal agent diclofenac sodium and misoprostol, it is characterized in that having at least wherein a kind of medicine at first to make tablet and reinstall capsule, wherein said diclofenac sodium bag is with enteric coating, and described misoprostol bag is with the gastric solubleness clothing.
2. compound diclofenac natrium capsule as claimed in claim 1 is characterized in that and diclofenac sodium can be made tablet that misoprostol incapsulates after making granule or pellet; Or diclofenac sodium makes granule or pellet, and misoprostol is made tablet and incapsulated; Perhaps diclofenac sodium and misoprostol incapsulate after all making tablet form separately, and the diclofenac preparation of sodium bag of wherein making is with enteric coating, and the misoprostol preparation bag of making is with the gastric solubleness clothing.
3. compound diclofenac natrium capsule as claimed in claim 2 is characterized in that being preferably just diclofenac sodium and misoprostol and all makes and incapsulate behind the tablet, and the diclofenac sodium sheet is enteric coated, misoprostol sheet bag gastric solubleness clothing.
4. as the described diclofenac natrium capsule of arbitrary claim in the claim 1 to 3, the wherein said tablet diameters of making tablet form is 4-8mm, and when incapsulating, the capsule internal diameter of selection is suitable with the external diameter of tablet.
5. as the described compound diclofenac natrium capsule of arbitrary claim in the claim 1 to 3, it is characterized in that: the prescription of diclofenac sodium sheet is:
Diclofenac sodium 50g filler 100-150g disintegrating agent 0-15g
Binding agent moderate lubrication agent 1-4g enteric coating powder 10-30g
Make 1000 altogether
The prescription of misoprostol sheet is:
Misoprostol 200mg filler 140-180g disintegrating agent 0-15g
Binding agent moderate lubrication agent 1-5g gastric solubleness coating powder 4-10g
Make 1000 altogether
Wherein said filler can be any one or two kinds of in starch, microcrystalline cellulose, lactose, the dextrin, described disintegrating agent can be any in polyvinylpolypyrrolidone, carboxymethyl starch sodium, the cross-linking sodium carboxymethyl cellulose, and described binding agent can be the polyvidone of carboxymethylstarch slurry sodium, the 5%-15% of 5%～15% starch slurry, 2%-15%, in the 2%-10% hydroxypropyl emthylcellulose any; Lubricant can be any in magnesium stearate, the micropowder silica gel, described enteric coating powder can be any in Lac, Cellulose Acetate Phthalate, alginate jelly, polyvinyl alcohol acetic acid phthalic acid ester, acrylic resin, the hydroxypropyl methyl cellulose phthalate, described gastric solubleness adjuvant can be a hydroxypropyl cellulose, hydroxypropyl emthylcellulose, any in polyethylene acetal diethylin acetic acid and dimethylaminoethyl methacrylate-neutral methacrylic acid esters copolymer.
Compound diclofenac natrium capsule as claimed in claim 5 is characterized in that:
The diclofenac sodium prescription is:
Diclofenac sodium 50g lactose 80g microcrystalline Cellulose 45g
Polyvinylpolypyrrolidone 8g magnesium stearate 2g 10% polyvidone is an amount of
The ethanol of Cellulose Acetate Phthalate 18g 80% is an amount of
Make 1000
The prescription of misoprostol sheet is
Misoprostol 200mg starch 140g microcrystalline Cellulose 40g
Cross-linking sodium carboxymethyl cellulose 10g magnesium stearate 2g
An amount of gastric solubleness hypromellose of 8% hypromellose coating powder 8g
80% ethanol is an amount of
Make 1000 altogether
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101798447A CN101181245A (en) | 2007-12-19 | 2007-12-19 | Compound diclofenac natrium capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007101798447A CN101181245A (en) | 2007-12-19 | 2007-12-19 | Compound diclofenac natrium capsule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101181245A true CN101181245A (en) | 2008-05-21 |
Family
ID=39446759
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007101798447A Pending CN101181245A (en) | 2007-12-19 | 2007-12-19 | Compound diclofenac natrium capsule |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101181245A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101439038B (en) * | 2008-08-08 | 2011-04-13 | 李炳阳 | Medicinal preparation composed of non-steroidal anti-inflammatory medicine and misoprostol |
| 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 |
| CN102697746A (en) * | 2012-06-11 | 2012-10-03 | 广州朗圣药业有限公司 | Rapid melting misoprostol vaginal composition as well as preparation method and application of same |
| CN106667900A (en) * | 2017-01-24 | 2017-05-17 | 楚雄医药高等专科学校 | Gel matrix having bioadhesion and favorable biocompatibility, and preparation method and application thereof |
-
2007
- 2007-12-19 CN CNA2007101798447A patent/CN101181245A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101439038B (en) * | 2008-08-08 | 2011-04-13 | 李炳阳 | Medicinal preparation composed of non-steroidal anti-inflammatory medicine and misoprostol |
| 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 |
| CN102697746A (en) * | 2012-06-11 | 2012-10-03 | 广州朗圣药业有限公司 | Rapid melting misoprostol vaginal composition as well as preparation method and application of same |
| CN106667900A (en) * | 2017-01-24 | 2017-05-17 | 楚雄医药高等专科学校 | Gel matrix having bioadhesion and favorable biocompatibility, and preparation method and application thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20080521 |