CN1586485A - Cefaclor oral disintegration tablet - Google Patents
Cefaclor oral disintegration tablet Download PDFInfo
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- CN1586485A CN1586485A CNA2004100627480A CN200410062748A CN1586485A CN 1586485 A CN1586485 A CN 1586485A CN A2004100627480 A CNA2004100627480 A CN A2004100627480A CN 200410062748 A CN200410062748 A CN 200410062748A CN 1586485 A CN1586485 A CN 1586485A
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- cefaclor
- diluent
- high molecular
- molecular polymer
- pharmaceutical salts
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Abstract
The orally disintegrated cefaclor tablet consists of cefaclor or its salt in effective dosage, polymer, diluent, disintegrating agent, effervescent agent, lubricant and corrective. Its cefaclor or cefaclor salt is coated with polymer to form microcapsule grain. When it is taken, no or little water is needed and the orally disintegrated cefaclor tablet will disintegrate inside oral cavity in 5-60 sec before being swallowed into stomach for acting.
Description
Technical field
The present invention relates to a kind of pharmaceutical preparation, particularly oral cavity disintegration tablet of antibacterials cefaclor or its pharmaceutical salts and preparation method thereof.When the patient took this medicine, water or only need to take medicine with low amounts of water not need not to chew, and disintegrate in 5 seconds to 60 seconds in the oral cavity is borrowed and swallowed power, and medicine is gone into the stomach onset.
Background technology
Oral cavity disintegration tablet is a kind of new oral solid preparation, it provides a kind of new instructions of taking, U.S. FDA and Japanese medicine registration body ratify several oral cavity disintegration tablets listings in recent years respectively, its characteristics are: do not need water only to need to become low amounts of water, need not to chew, medicine places lingual surface, borrows swallowing act to go into the stomach onset rapidly after the disintegrate.This dosage form can make things convenient for part patient medication, and as dysphagia person (especially old man, child), or special environment can not obtain patient's medication of water down.SDA has agreed " oral cavity disintegration tablet " to have put 8 kinds at present in detention as novel form.
Oral cavity disintegration tablet definition: be that a kind of water that do not need in the oral cavity can disintegrate or dissolved tablet.Specification requirement: 1. should be in the oral cavity rapidly disintegrate, no grittiness, good mouthfeel, swallow easily, to the oral mucosa nonirritant.Should stipulate under the character item in the quality standard: disintegrate rapidly, no grittiness, good mouthfeel in the oral cavity; 2. set up suitable disintegration time mensuration method and limit, and be incorporated into standard; 3. to insoluble medicine, should set up suitable dissolution determination method and limit; 4. other should meet general rule requirement under the tablet item.
The characteristics of oral cavity disintegration tablet: 1. absorption is fast, bioavailability is high; 2. instructions of taking does not need water 3. intestinal is residual few, few side effects; 4. avoid the first pass effect of liver sausage,
Cefaclor is a kind of semisynthetic oral cephalosporin, and antibacterial properties is wide than other first generation cephalosporin.Activity to product penicillinase staphylococcus aureus, A group Hemolytic streptococcus, Streptococcus viridans and staphylococcus epidermidis is identical with cefadroxil, and is strong 2～4 times than cefadroxil to not producing enzyme staphylococcus aureus and pneumococcal antibacterial action.Gram negative bacilli is comprised the activity of escherichia coli and Klebsiella Pneumoniae etc. strong than cefalexin, similar with cefadroxil, strong to the activity of proteus mirabilis, Salmonella and Shigella than cefadroxil.Moraxelle catarrhalis and Diplococcus gonorrhoeae are very sensitive to cefaclor.
The cefaclor character is white or off-white color crystalline powder, and bitter in the mouth slightly is dissolved in water (1: 100), and soluble,very slightly is in chloroform, ether, methanol, and the pH value of 2.5% aqueous suspension is 3-4.5, and is stable to gastric acid, meets alkali and decomposes gradually.The dosage form of listing is mainly tablet, capsule, powder suspensoid at present.
Because the cefaclor bitter in the mouth is insoluble in water, therefore be difficult to be formed in buccal tablet or the oral cavity disintegration tablet that keeps certain hour in the oral cavity.
Summary of the invention
The present invention finds, adopts technology of the present invention cefaclor or its pharmaceutical salts can be made oral cavity disintegration tablet, has overcome bitter in the mouth, is insoluble in the defective of water, finds that simultaneously oral cavity disintegration tablet bioavailability of the present invention improves greatly.
Cefaclor oral disintegration tablet of the present invention is made up of active component cefaclor or its pharmaceutical salts and auxiliary element, and described auxiliary element is a pharmaceutic adjuvant, comprises diluent, disintegrating agent, effervescent, lubricant, correctives etc.The present invention also comprises the preparation method of cefaclor or its pharmaceutical salts oral cavity disintegration tablet, it is characterized in that, with active component cefaclor or its pharmaceutical salts and pharmaceutic adjuvant mixing, make cefaclor mouth or its pharmaceutical salts cavity disintegrating tablet according to the routine techniques of preparation oral cavity disintegration tablet.
The key of preparation oral cavity disintegration tablet is to seek proper supplementary material, and strong, the disintegrate of good fluidity, compressibility requires prepared tablet mouthfeel good soon, in addition when guaranteeing pressure.Adjuvant at present commonly used has: Icing Sugar, lactose, microcrystalline Cellulose (MCC), mannitol, be adjuvants such as cross-linking sodium carboxymethyl cellulose (CC-Na), crospolyvinylpyrrolidone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na), low-substituted hydroxypropyl cellulose (L-HPC), citric acid, sodium bicarbonate, magnesium stearate, micropowder silica gel, gelatin, aspartame, mannitol.
The present invention selects therein, serves as preferred with microcrystalline Cellulose (MCC), mannitol, crospolyvinylpyrrolidone (PVPP), citric acid and sodium bicarbonate, magnesium stearate, gelatin, aspartame and mannitol;
Selection of the present invention also is, selection is rolled into micron-sized microcapsule granule with cefaclor or its pharmaceutical salts with polymer and further makes oral cavity disintegration tablet again, the oral cavity disintegration tablet that this cefaclor or its pharmaceutical salts are wrapped up with polymer, it consists of, the micron-sized granule that cefaclor or its pharmaceutical salts are rolled into natural or synthetic high molecular polymer is as active part, in addition preferable absorbent of the present invention, disintegrating agent, effervescent, lubricant, correctives.
For cefaclor or its pharmaceutical salts preparation method with the oral cavity disintegration tablet of polymer parcel, it is characterized in that, earlier cefaclor or its pharmaceutical salts are rolled into micron order microcapsule granule with natural or synthetic high molecular polymer, add diluent, disintegrating agent, effervescent, lubricant then, add correctives again, direct compression promptly.
For cefaclor or its pharmaceutical salts oral cavity disintegration tablet with the polymer parcel, natural or synthetic high molecular polymer wherein is selected from: gelatin;
In addition, aspect the selection of adjuvant,
Diluent is selected from: microcrystalline Cellulose (MCC) and mannitol;
Disintegrating agent is selected from: crospolyvinylpyrrolidone (PVPP);
Effervescent is selected from: citric acid and sodium bicarbonate;
Lubricant is selected from: magnesium stearate;
Correctives is selected from: aspartame and mannitol;
Cefaclor oral disintegration tablet of the present invention, wherein cefaclor or the percentage by weight of its pharmaceutical salts in preparation are 1-99%, all the other are pharmaceutic adjuvant.
Cefaclor oral disintegration tablet of the present invention, every tablet preparation contain cefaclor or its pharmaceutical salts 1-1000mg, and all the other are pharmaceutic adjuvant.
For cefaclor or its pharmaceutical salts oral cavity disintegration tablet with the polymer parcel, wherein the amount of each component accounts for the percentage ratio of gross weight and is:
For cefaclor or its pharmaceutical salts oral cavity disintegration tablet, contain in each sheet with the polymer parcel:
Cefaclor or its pharmaceutical salts 25-100mg
Natural or synthetic high molecular polymer 50-100mg
Diluent 100-200mg
Disintegrating agent 5-10mg
Effervescent 10-20mg
Lubricant 1-3mg
Correctives 1-3mg
Preferably:
Cefaclor or its pharmaceutical salts 62.5mg
Natural or synthetic high molecular polymer 62.5mg
Diluent 145mg
Disintegrating agent 8mg
Effervescent 18mg
Lubricant 2mg
Correctives 2mg
For preferred cefaclor or its pharmaceutical salts oral cavity disintegration tablet, wherein the micron-sized microcapsule granule that is rolled into natural or synthetic high molecular polymer of cefaclor or its pharmaceutical salts prepares by the following method:
[1] diluent is joined method: diluent is NA
2SO
4Solution, its concentration is by the NA in the cohesion bag system
2SO
4Concentration (as being a%) adds 1.5%[and gets (a+1.5) %], the diluent volume is 3 times of cohesion bag system cumulative volume, the diluent temperature is 15 ℃.Used diluent excessive concentration or low excessively can make the agglomerating or dissolving of cohesion capsular adhesion.
After above-mentioned granule is made, add diluent, disintegrating agent, effervescent, lubricant, add correctives again, direct compression promptly.
Cefaclor of the present invention or its pharmaceutical salts oral cavity disintegration tablet are compared with existing dosage form has following advantage: when the patient takes this medicine, water or only need to take medicine with low amounts of water not need not to chew disintegrate in 5 seconds to 60 seconds in the oral cavity, borrow and swallow power, medicine is gone into the stomach onset.Take medicine and save trouble, save the trouble with the water delivery service medicine, treatment in time, and is effective; Make things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment.For the preferred cefaclor oral disintegration tablet of the present invention, also have the following advantages especially: disintegrate is rapid, good mouthfeel.
The specific embodiment:
By the following examples, the invention will be further described.
Embodiment 1:
Take by weighing principal agent cefaclor 2.5g, microcrystalline Cellulose (MCC) 7.2g, mannitol 2.8g, crospolyvinylpyrrolidone (PVPP) 1.6g, low-substituted hydroxypropyl cellulose (L-HPC) 0.8g, citric acid 0.4g, sodium bicarbonate 0.4g, magnesium stearate 0.2g, aspartame 0.15g, flavoring orange essence 0.2g, direct compression promptly get 1000.
By the Orally-disintegrating tablet that this prescription makes, disintegrate is rapid, but flavor is slightly bitter.
Embodiment 2:
Take by weighing gelatin 6.25g, add 125ml distilled water immersion swelling, melt into rubber cement in 60 ℃ of water-baths, add microcrystalline Cellulose 2.0g, after stirring, add cefaclor 6.25g, acetum in 50 ℃ of addings 10% is regulated PH to 3.5～3.8, slowly adds 20% Na under middling speed stirs
2SO
4(about 5ml) must condense capsule, adds the diluent (the diluent temperature is 15 ℃) of 3 times of amounts, makes the capsule sedimentation.NaOH with 20% regulates PH to 8～9, in adding 37% formalin (about 30ml) below 15 ℃ capsule is solidified.Leave standstill, sucking filtration is put the vacuum drying oven drying in 55 ℃, promptly gets microcapsule.Add mannitol 7.3g then, microcrystalline Cellulose (MCC) 4.8g, crospolyvinylpyrrolidone (PVPP) 1.2g, citric acid 1g, sodium bicarbonate 0.8g, magnesium stearate 0.2g, aspartame 0.2g, direct compression promptly get 1000.
According to the oral cavity disintegration tablet that this prescription makes, disintegrate is rapid, good mouthfeel, no bitterness.
Embodiment 3:
Take by weighing gelatin 12.5g, add 250ml distilled water immersion swelling, melt into rubber cement in 60 ℃ of water-baths, add microcrystalline Cellulose 3.6g, after stirring, add cefaclor 10g, acetum in 50 ℃ of addings 10% is regulated PH to 3.5～3.8, the Na of slow adding 20% under stirring fast
2SO
4(10ml) must condense capsule, add the diluent (the diluent temperature is 15 ℃) of 3 times of amounts, make the capsule sedimentation.NaOH with 20% regulates PH to 8～9, in adding 37% formalin (50ml) below 15 ℃ capsule is solidified.Leave standstill, sucking filtration is put the vacuum drying oven drying in 55 ℃, promptly gets microcapsule.Add mannitol 2.15g then, microcrystalline Cellulose (MCC) 3.6g, crospolyvinylpyrrolidone (PVPP) 0.8g, citric acid 0.5g, sodium bicarbonate 0.4g, magnesium stearate 0.2g, aspartame 0.2g, direct compression promptly get 1000.
According to the oral cavity disintegration tablet that this prescription makes, good mouthfeel, no bitterness.
Claims (10)
1. an antibacterial combination that contains cefaclor or its pharmaceutical salts is characterized in that said composition is disintegrate in the oral cavity.
2. the compositions of claim 1, it is characterized in that: said composition is by the cefaclor and the high molecular polymer of medicine effective quantity, diluent, disintegrating agent, effervescent, lubricant, correctives is formed, and wherein cefaclor or its pharmaceutical salts are rolled into microcapsule granule by high molecular polymer.
3. the compositions of claim 2 is characterized in that: described
High molecular polymer is selected from: gelatin
Diluent is selected from: microcrystalline Cellulose, mannitol;
Disintegrating agent is selected from: crospolyvinylpyrrolidone;
Effervescent is selected from: citric acid, sodium bicarbonate;
Lubricant is selected from: magnesium stearate;
Correctives is selected from: aspartame, mannitol.
4. the compositions of claim 2 is characterized in that: be oral cavity disintegration tablet, contain in each sheet:
Cefaclor or its pharmaceutical salts 25-100mg
High molecular polymer 50-100mg
Diluent 100-200mg
Disintegrating agent 5-10mg
Effervescent 10-20mg
Lubricant 1-3mg
Correctives 1-3mg.
5. the compositions of claim 4 is characterized in that: described
High molecular polymer is selected from: gelatin
Diluent is selected from: microcrystalline Cellulose, mannitol;
Disintegrating agent is selected from: crospolyvinylpyrrolidone;
Effervescent is selected from: citric acid, sodium bicarbonate;
Lubricant is selected from: magnesium stearate;
Correctives is selected from: aspartame, mannitol.
6. the compositions of claim 4 is characterized in that: contain in each sheet:
Cefaclor or its pharmaceutical salts 62.5mg
High molecular polymer 62.5mg
Diluent 145mg
Disintegrating agent 8mg
Effervescent 18mg
Lubricant 2mg
Correctives 2mg.
7. the compositions of claim 6 is characterized in that: described
High molecular polymer is selected from: gelatin
Diluent is selected from: microcrystalline Cellulose, mannitol;
Disintegrating agent is selected from: crospolyvinylpyrrolidone;
Effervescent is selected from: citric acid, sodium bicarbonate;
Lubricant is selected from: magnesium stearate;
Correctives is selected from: aspartame, mannitol.
8. the preparation of compositions method of claim 4, it is characterized in that: be rolled into microcapsule granule by high molecular polymer through cefaclor or its pharmaceutical salts, after granule is made, add diluent, disintegrating agent, effervescent, lubricant, add correctives again, direct compression promptly.
9. the preparation method of claim 8, wherein cefaclor or its pharmaceutical salts are rolled into granule through following steps by high molecular polymer: cefaclor and gelatin solution suspendible, through the cohesion capsule, the sedimentation capsule, the crosslinking curing capsule, microcapsule granule.
10. the preparation method of claim 9, process following steps: take by weighing gelatin 6.25g, add 125ml distilled water immersion swelling, melt into rubber cement in 60 ℃ of water-baths, add microcrystalline Cellulose 2.0g, after stirring, add cefaclor or its pharmaceutical salts 6.25g, acetum in 50 ℃ of addings 10% is regulated PH to 3.5～3.8, slowly adds 20% Na under middling speed stirs
2SO
45ml must condense capsule, adds the diluent of 3 times of amounts, makes the capsule sedimentation, and the NaOH with 20% regulates PH to 8～9, makes capsule curing adding 37% formalin 30ml below 15 ℃, leaves standstill, and sucking filtration is put the vacuum drying oven drying in 55 ℃, promptly gets microcapsule granule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100627480A CN1586485A (en) | 2004-07-08 | 2004-07-08 | Cefaclor oral disintegration tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2004100627480A CN1586485A (en) | 2004-07-08 | 2004-07-08 | Cefaclor oral disintegration tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1586485A true CN1586485A (en) | 2005-03-02 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2004100627480A Pending CN1586485A (en) | 2004-07-08 | 2004-07-08 | Cefaclor oral disintegration tablet |
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| Country | Link |
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| CN (1) | CN1586485A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100446759C (en) * | 2006-10-16 | 2008-12-31 | 北京科信必成医药科技发展有限公司 | Gastrodine tablets disintegrating in oral cavity and process for producing same |
| CN101444513B (en) * | 2007-11-27 | 2011-05-11 | 上官清 | Cefaclor orally disintegrating tablet and preparation method thereof |
| CN102357086A (en) * | 2011-11-01 | 2012-02-22 | 上海理工大学 | Cefprozil orally disintegrating tablets |
| CN102973514A (en) * | 2012-10-08 | 2013-03-20 | 李正梅 | Preparation method for cefaclor granule composition |
| CN105287599A (en) * | 2015-10-14 | 2016-02-03 | 康普药业股份有限公司 | Cefradine pharmaceutical composition |
| CN105902490A (en) * | 2016-05-20 | 2016-08-31 | 江苏正大清江制药有限公司 | Cefaclor compound solid preparation and preparation method thereof |
-
2004
- 2004-07-08 CN CNA2004100627480A patent/CN1586485A/en active Pending
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100446759C (en) * | 2006-10-16 | 2008-12-31 | 北京科信必成医药科技发展有限公司 | Gastrodine tablets disintegrating in oral cavity and process for producing same |
| CN101444513B (en) * | 2007-11-27 | 2011-05-11 | 上官清 | Cefaclor orally disintegrating tablet and preparation method thereof |
| CN102357086A (en) * | 2011-11-01 | 2012-02-22 | 上海理工大学 | Cefprozil orally disintegrating tablets |
| CN102973514A (en) * | 2012-10-08 | 2013-03-20 | 李正梅 | Preparation method for cefaclor granule composition |
| CN105287599A (en) * | 2015-10-14 | 2016-02-03 | 康普药业股份有限公司 | Cefradine pharmaceutical composition |
| CN105902490A (en) * | 2016-05-20 | 2016-08-31 | 江苏正大清江制药有限公司 | Cefaclor compound solid preparation and preparation method thereof |
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Addressee: Wang Jinjing Document name: Deemed as a notice of withdrawal |
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