CN101332196A - Amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof - Google Patents
Amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof Download PDFInfo
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- CN101332196A CN101332196A CNA2007100429017A CN200710042901A CN101332196A CN 101332196 A CN101332196 A CN 101332196A CN A2007100429017 A CNA2007100429017 A CN A2007100429017A CN 200710042901 A CN200710042901 A CN 200710042901A CN 101332196 A CN101332196 A CN 101332196A
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- amoxicillin
- clavulanate potassium
- dispersible tablets
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Abstract
The present invention discloses an amoxicillin/clavulanate potassium dispersible tablet and a preparation method thereof. The present invention contains amoxicillin/clavulanate potassium and auxiliary materials; the weight proportion of the amoxicillin and the clavulanate potassium is 7:1; the auxiliary materials contain a disintegrant, and one or multiple materials selected from crosslinked carboxymethylcellulose sodium, crosslinked polyvinylpyrrolidone, sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, carboxymethylcellulose sodium, carboxymethylcellulose calcium and sodium dodecyl sulfate; calculated by the total weight of the auxiliary materials, the optimally selected carboxymethylcellulose sodium accounts for 10 to 15 parts. The present invention with appropriate selection of auxiliary materials and active medicines for prescription can rapidly disintegrating the dispersible tablet; the dispersible tablet can be totally disintegrated within 3 minutes in 100ml water at 20 DEG minus/plus 1 DEG; the disintegrated particles should all pass through standard II screen for clinical application.
Description
Technical field
The present invention relates to a kind of amoxicillin and clavulanate potassium preparation and preparation method thereof.
Technical background
This product is the compound preparation of amoxicillin and clavulanate potassium.Britain promptly takes the lead in releasing the compound preparation that first beta-lactam inhibitor and semisynthetic penicillin are formed than Qie Mu company as far back as the beginning of the eighties, and commodity are called Augmentin.And obtain " prize of queen's technological achievement " in Britain.The ratio of amoxicillin and clavulanate potassium has 1: 2,1: 4,1: 5,1: 7,1: 10 etc.
Amoxicillin in 1997 and clavulanate potassium compound preparation are 13.5 hundred million dollars in worldwide sales volume, occupy the share of antibiotic market total value 6.6%, occupy first of world's anti-infectives, occupy the 15th of the 20 kinds of leading medicines in the world, become the SmithKline than Qie Mu company's second largest situation of selling well medicine after the cimetidine that continues.
In the compound preparation of amoxicillin/clavulanate potassium (7: 1); the amoxicillin is a penbritin class antibiotic, and clavulanate potassium itself has only faint antibacterial activity, but has the enzyme inhibition of powerful wide spectrum beta-lactam; both share, and can protect the amoxicillin to exempt from the beta-lactam enzyme hydrolysis.The antimicrobial spectrum of this product is identical with the amoxicillin, and enlarges to some extent.To producing enzyme staphylococcus aureus, staphylococcus epidermidis, coagulase negative staphylococcus and the equal tool good action of enterococcus, some intestinal liver Cordycepps antibacterial, hemophilus influenza, moraxelle catarrhalis, bacteroides fragilis etc. that produce beta lactamase also there is better antibacterial activity.
At present, the compound preparation of amoxicillin/clavulanate potassium (7: 1) is oral solid formulation, is one of pharmaceutical dosage form of using always, but conventional tablet and capsule self exist certain shortcoming, meets water disintegrate rapidly.
Chinese Pharmacopoeia 2000 editions has recording of this novel form of dispersible tablet.Compare with ordinary tablet, dispersible tablet requires at 100ml, in 20 ℃ ± 1 ℃ the water, and the whole disintegrates of energy in 3 minutes, the granule after the disintegrate should be all by No. 2 standard screens.Therefore have the advantage that drug release rate is fast, bioavailability is high, untoward reaction is little, in clinical use, both can swallow, can put into water again, take after the disintegrate rapidly, make things convenient for old man, child especially and swallow the patient which is stranded and take as ordinary tablet.Make medicine little simultaneously, reduced medicine the gastrointestinal zest with the gastrointestinal tract mucous concentration that contacts, thus prevent or alleviated feel sick, the generation of side effect such as vomiting.Therefore select a kind of proper supplementary material, amoxicillin/clavulanate potassium (7: 1) preparation is become dispersible tablet,, have great importance for clinical practice.
Summary of the invention
The purpose of this invention is to provide a kind of amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof, to overcome the above-mentioned defective that prior art exists.
Amoxicillin/clavulanate potassium dispersible tablets of the present invention is made of amoxicillin/clavulanate potassium and adjuvant, wherein:
The part by weight of amoxicillin and clavulanate potassium is 7: 1;
Said adjuvant comprises:
(1) disintegrating agent, be selected from cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, the sodium lauryl sulphate one or more, preferred cross-linking sodium carboxymethyl cellulose, gross weight in adjuvant, be 10 parts～15 parts, can reduce the little trichobothrium of tablet surface that tablet that the strong absorptive because of efficient disintegrating agent itself causes produces in production and packaging process.
(2) filler is selected from microcrystalline Cellulose, lactose, sucrose, mannitol, pregelatinized Starch, the calcium hydrogen phosphate one or more, preferably microcrystalline cellulose; In the gross weight of adjuvant, consumption is 10 parts～45 parts.
(3) lubricated antiplastering aid, in order to make tablet that the bright and clean of good tablet weight variation and tablet surface arranged in pressing process, also comprise 1 part～5 parts lubricated antiplastering aid, be selected from magnesium stearate, stearic acid, calcium stearate, Pulvis Talci, colloidal silica, hydrogenated vegetable oil, Polyethylene Glycol, the sodium lauryl sulphate one or more.
(4) spice correctives in order to improve the taste of solution behind the disintegration of tablet, has added 0.5 part～5 parts spice correctives, is selected from aspartame, glycyrrhizin, saccharin sodium, citric acid, vanillin, the powdered flavor one or more.
In the amoxicillin/clavulanate potassium dispersible tablets, the weight content of amoxicillin/clavulanate potassium is 35 parts～60 parts.
The preparation technology of dispersible tablet of the present invention is similar to the preparation technology of ordinary tablet, and is specific as follows:
With amoxicillin and clavulanate potassium proportionally, put in the mixer with disintegrating agent, filler, spice correctives, mix homogeneously adds the lubricated antiplastering aid that sieves through 100 orders again, remix 1～5 minute, discharging; Take a sample then, after the assay was approved, carry out the tabletting preparation, make qualified finished product at the workshop that meets the GMP working condition.These preparations and method for processing all are as well known to those skilled in the art and familiar.
The present invention has selected proper supplementary material and active medicine to carry out compatibility, disintegrating agent penetrates among the tablet hydrone by capillarity or expansion easily, after suction back powder expands, can make said dispersible tablet hasten soon collapse, this dispersible tablet is at 100ml, in 20 ℃ ± 1 ℃ the water, and internal energy whole disintegrates in 3 minutes, granule after the disintegrate should be convenient to clinical practice all by No. 2 standard screens.
The specific embodiment
The invention will be further elaborated by the following examples.Only be used to illustrate the present invention, rather than a kind of any way limits the present invention.
Embodiment 1
Prescription: composition weight or degree
Amoxicillin: clavulanate potassium (7: 1) 460g
Microcrystalline Cellulose 300g
Cross-linking sodium carboxymethyl cellulose 90g
Magnesium stearate 10g
Colloidal silica 9g
Aspartame 1g
Fructus Musae flavor powdered flavor 1g
Preparation method: with the amoxicillin: clavulanate potassium (7: 1) crude drug is put in the mixer with the recipe quantity cross-linking sodium carboxymethyl cellulose that sieves through 80 orders, microcrystalline Cellulose, colloidal silica, aspartame, Fructus Musae flavor powdered flavor, mixed on low speed 15 minutes, shut down the back and add the magnesium stearate of sieving through 100 orders, remix 1 minute, discharging; Take a sample then, after the assay was approved, carry out the tabletting preparation, make qualified amoxicillin: clavulanate potassium (7: 1) dispersible tablet at the workshop that meets the GMP working condition.This dispersible tablet is at 100ml, in 20 ℃ ± 1 ℃ the water, and internal energy whole disintegrates in 3 minutes, the granule after the disintegrate should be all by No. 2 standard screens.
Embodiment 2
Prescription: composition weight or degree
Amoxicillin: clavulanate potassium (7: 1) 460g
Microcrystalline Cellulose 270g
Cross-linking sodium carboxymethyl cellulose 95g
Magnesium stearate 10g
Colloidal silica 9g
Aspartame 1g
Fructus Musae flavor powdered flavor 1g
Preparation method: with the amoxicillin: clavulanate potassium (7: 1) crude drug is put in the mixer with the recipe quantity cross-linking sodium carboxymethyl cellulose that sieves through 80 orders, microcrystalline Cellulose, colloidal silica, aspartame, Fructus Musae flavor powdered flavor, mixed on low speed 15 minutes, shut down the back and add the magnesium stearate of sieving through 100 orders, remix 5 minutes, discharging; Take a sample then, after the assay was approved, carry out the tabletting preparation, make qualified amoxicillin: clavulanate potassium (7: 1) dispersible tablet at the workshop that meets the GMP working condition.
This dispersible tablet is at 100ml, in 20 ℃ ± 1 ℃ the water, and internal energy whole disintegrates in 3 minutes, the granule after the disintegrate should be all by No. 2 standard screens.
Embodiment 3
Prescription: composition weight or degree
Amoxicillin: clavulanate potassium (7: 1) 460g
Microcrystalline Cellulose 320g
Cross-linking sodium carboxymethyl cellulose 110g
Magnesium stearate 10g
Colloidal silica 9g
Aspartame 1g
Fructus Musae flavor powdered flavor 1g
Preparation method: with the amoxicillin: clavulanate potassium (7: 1) crude drug is put in the mixer with the recipe quantity cross-linking sodium carboxymethyl cellulose that sieves through 80 orders, microcrystalline Cellulose, colloidal silica, aspartame, Fructus Musae flavor powdered flavor, mixed on low speed 15 minutes, shut down the back and add the magnesium stearate of sieving through 100 orders, remix 1～5 minute, discharging; Take a sample then, after the assay was approved, carry out the tabletting preparation, make qualified amoxicillin: clavulanate potassium (7: 1) dispersible tablet at the workshop that meets the GMP working condition.
Embodiment 4
Prescription: composition weight or degree
Amoxicillin: clavulanate potassium (7: 1) 460g
Microcrystalline Cellulose 250g
Cross-linking sodium carboxymethyl cellulose 120g
Magnesium stearate 10g
Colloidal silica 9g
Aspartame 1g
Fructus Musae flavor powdered flavor 1g
Preparation method: with the amoxicillin: clavulanate potassium (7: 1) crude drug is put in the mixer with the recipe quantity cross-linking sodium carboxymethyl cellulose that sieves through 80 orders, microcrystalline Cellulose, colloidal silica, aspartame, Fructus Musae flavor powdered flavor, mixed on low speed 15 minutes, shut down the back and add the magnesium stearate of sieving through 100 orders, remix 3 minutes, discharging; Take a sample then, after the assay was approved, carry out the tabletting preparation, make qualified amoxicillin: clavulanate potassium (7: 1) dispersible tablet at the workshop that meets the GMP working condition.
This dispersible tablet is at 100ml, in 20 ℃ ± 1 ℃ the water, and internal energy whole disintegrates in 3 minutes, the granule after the disintegrate should be all by No. 2 standard screens.
Claims (8)
1. amoxicillin/clavulanate potassium dispersible tablets is characterized in that, is made of amoxicillin/clavulanate potassium and adjuvant, and wherein: the part by weight of amoxicillin and clavulanate potassium is 7: 1;
Said adjuvant comprises:
Disintegrating agent, be selected from cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, sodium carboxymethyl cellulose, carboxymethylcellulose calcium, the sodium lauryl sulphate one or more, preferred cross-linking sodium carboxymethyl cellulose, in the gross weight of adjuvant, it is 10 parts～15 parts.
2. amoxicillin/clavulanate potassium dispersible tablets according to claim 1, it is characterized in that, also comprise filler, be selected from microcrystalline Cellulose, lactose, sucrose, mannitol, pregelatinized Starch, the calcium hydrogen phosphate one or more, in the gross weight of disintegrating agent, consumption is 10 parts～45 parts.
3. amoxicillin/clavulanate potassium dispersible tablets according to claim 2 is characterized in that, filler is a microcrystalline Cellulose.
4. amoxicillin/clavulanate potassium dispersible tablets according to claim 3, it is characterized in that, also comprise lubricated antiplastering aid, be selected from magnesium stearate, stearic acid, calcium stearate, Pulvis Talci, colloidal silica, hydrogenated vegetable oil, Polyethylene Glycol, the sodium lauryl sulphate one or more.In the gross weight of lubricated antiplastering aid, consumption is 1 part～5 parts.
5. amoxicillin/clavulanate potassium dispersible tablets according to claim 4 is characterized in that, also comprises the spice correctives, and consumption is 0.5 part～5 parts.
6. amoxicillin/clavulanate potassium dispersible tablets according to claim 5 is characterized in that the spice correctives is selected from one or more in aspartame, glycyrrhizin, saccharin sodium, citric acid, vanillin, the powdered flavor.
7. according to each described amoxicillin/clavulanate potassium dispersible tablets of claim 1～6, it is characterized in that in the amoxicillin/clavulanate potassium dispersible tablets, the weight content of amoxicillin/clavulanate potassium is 35 parts～60 parts.
8. the method for preparing each described amoxicillin/clavulanate potassium dispersible tablets of claim 1～7, it is characterized in that, comprise the steps: proportionally amoxicillin and clavulanate potassium, put in the mixer with disintegrating agent, filler, spice correctives, mix homogeneously, add the lubricated antiplastering aid that sieves through 100 orders again, remix 1～5 minute, discharging.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100429017A CN101332196A (en) | 2007-06-28 | 2007-06-28 | Amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CNA2007100429017A CN101332196A (en) | 2007-06-28 | 2007-06-28 | Amoxicillin/clavulanate potassium dispersible tablets and preparation method thereof |
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| CN101332196A true CN101332196A (en) | 2008-12-31 |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102240285A (en) * | 2011-04-21 | 2011-11-16 | 南京仕必得生物技术有限公司 | Amoxicillin and potassium clavulanate tablet for dogs and cats, and its preparation method and application |
| CN101897701B (en) * | 2009-05-27 | 2012-06-27 | 华北制药股份有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
| CN103768056A (en) * | 2014-01-21 | 2014-05-07 | 东药集团沈阳施德药业有限公司 | Amoxicillin and clavulanate potassium dispersible tablet |
| CN104161734A (en) * | 2014-09-04 | 2014-11-26 | 海口市制药厂有限公司 | Amoxicillin dispersible tablet as well as preparation method and use thereof |
| CN104188963A (en) * | 2014-07-30 | 2014-12-10 | 上海新亚药业闵行有限公司 | Amoxicillin-potassium clavulanate tablet and preparation method thereof |
-
2007
- 2007-06-28 CN CNA2007100429017A patent/CN101332196A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897701B (en) * | 2009-05-27 | 2012-06-27 | 华北制药股份有限公司 | Preparation method of amoxicillin and clavulanate potassium tablets |
| CN102240285A (en) * | 2011-04-21 | 2011-11-16 | 南京仕必得生物技术有限公司 | Amoxicillin and potassium clavulanate tablet for dogs and cats, and its preparation method and application |
| CN103768056A (en) * | 2014-01-21 | 2014-05-07 | 东药集团沈阳施德药业有限公司 | Amoxicillin and clavulanate potassium dispersible tablet |
| CN103768056B (en) * | 2014-01-21 | 2015-01-07 | 东药集团沈阳施德药业有限公司 | Amoxicillin and clavulanate potassium dispersible tablet |
| CN104188963A (en) * | 2014-07-30 | 2014-12-10 | 上海新亚药业闵行有限公司 | Amoxicillin-potassium clavulanate tablet and preparation method thereof |
| CN104161734A (en) * | 2014-09-04 | 2014-11-26 | 海口市制药厂有限公司 | Amoxicillin dispersible tablet as well as preparation method and use thereof |
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Open date: 20081231 |