CN1634114A - Clindamycin phosphate orally disintegrating tablet - Google Patents
Clindamycin phosphate orally disintegrating tablet Download PDFInfo
- Publication number
- CN1634114A CN1634114A CN 200410079330 CN200410079330A CN1634114A CN 1634114 A CN1634114 A CN 1634114A CN 200410079330 CN200410079330 CN 200410079330 CN 200410079330 A CN200410079330 A CN 200410079330A CN 1634114 A CN1634114 A CN 1634114A
- Authority
- CN
- China
- Prior art keywords
- oral cavity
- clindamycin phosphate
- disintegration tablet
- cavity disintegration
- sodium
- 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
Links
Abstract
The invention relates to an orally disintegrating tablet of clindamycin phosphate and its preparing process, wherein the orally disintegrating tablet comprises clindamycin phosphate of physiological effective dose and pharmaceutically acceptable carrying agent suitable for preparing orally disintegrating tablet, the pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet include macromolecular material, bulking agent, crumbling agent, effervescent agent, lubricating agent, flavoring agent and other pharmaceutically acceptable carrying agents suitable for preparing orally disintegrating tablet.
Description
Technical field:
The present invention relates to field of medicaments, particularly oral cavity disintegration tablet of clindamycin phosphate 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 pharmaceutical dosage forms, English " Orally disintegratingtables " by name.U.S. FDA has been ratified this dosage form listing, and reason is: make things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment.
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.
Clindamycin phosphate is a lincomycin series antibiotics, and compare this product antibacterial action with lincomycin strong 4～8 times, good absorbing, bone concentration height and anaerobic infection had good curative effect.This product mainly has very strong antibacterial activity to gram positive coccus and anaerobe, comprises gram positive coccus: staphylococcus aureus, staphylococcus epidermidis, streptococcus (except the phosphorus streptococcus), streptococcus pneumoniae, Micrococcus etc.; Anaerobe: Clostridium, Bacteroides, bacillus fusiformis genus, propionibacterium, Eubacterium, anaerobic cocci etc.The clinical microbial following various infectious disease of Grain-positive that are used for: (1) tonsillitis, suppurative otitis media, sinusitis etc.(2) acute bronchitis, acute episode of chronic bronchitis, pneumonia, pulmonary abscess and concurrent infection of bronchiectasis etc.(3) skin and soft tissue infection: furuncle, carbuncle, abscess, cellulitis, wound, burn and post-operative infection etc.(4) urinary system infection: acute urethritis, acute pyelonephritis, prostatitis etc.(5) other: osteomyelitis, septicemia, peritonitis and oral cavity infection etc.And be used for the microbial various infectious disease of anaerobism: (1) empyema, pulmonary abscess, anaerobe pneumonia.(2) skin and soft tissue infection, septicemia.(3) infect in the abdomen: peritonitis, intra-abdominal abscess.(4) female pelvic cavity and genital infection: endometritis, non-gonococcus property fallopian tube and ovarian abscess, pelvicellulitis and gynecilogical operation postoperative infection etc.
The oral formulations of existing clindamycin phosphate comprises tablet, capsule etc., all to use water delivery service, and, clindamycin phosphate has the bitterness of strong row and has GI irritation, the invention provides a kind of clindamycin phosphate orally disintegrating tablet, this tablet get by direct compression, and advantage is patient when taking this medicine, not water or only need take medicine with low amounts of water, need not to chew, disintegrate in 5 seconds to 60 seconds in the oral cavity is borrowed and is swallowed power, and medicine is gone into the stomach onset, no bitterness, nonirritant is treated patient timely and effectively, saves trouble.
Summary of the invention:
The present invention makes oral cavity disintegration tablet with clindamycin phosphate, has technically overcome bitter taste of drug, and disintegrate has rapidly improved bioavailability of medicament greatly in the oral cavity.
Clindamycin phosphate orally disintegrating tablet of the present invention is made up of active component clindamycin phosphate and auxiliary element.Every contains active component 0.1-0.2g, is preferably 0.15g (in clindamycin phosphate), and all the other are auxiliary element.Auxiliary element is the medicine acceptable carrier that is fit to make oral cavity disintegration tablet, mainly comprises macromolecular material, filler, disintegrating agent, effervescent, lubricant, correctives etc.Feature of the present invention also is to adopt packaging technique and preconditioning technique to prepare the clindamycin phosphate microcapsule, and then makes oral cavity disintegration tablet.
Oral cavity disintegration tablet require disintegrate rapidly, no husky large sense, good mouthfeel, swallow easily, to the oral mucosa nonirritant, so having relatively high expectations adjuvant.Adjuvant commonly used has: acrylic resin, ethyl cellulose, gelatin, cellulose, acrylate copolymer, ethylene copolymer, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, handle agar, citric acid, sodium bicarbonate, mannitol, Camphora, lactose, erythrol, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, xylitol, mannitol, protein sugar, stevioside, sucrose, sorbitol, vitamin C, sodium sulfite, sodium sulfite, pyrosulfite, sodium thiosulfate, different VC, thiourea, cysteine, methionine, thiacetic acid., thioglycerol, butylated hydroxyarisol, two fourth cresols, PG, tocopherol, lecithin, sodium lauryl sulphate, Pulvis Talci, magnesium stearate, micropowder silica gel, Opadry
II, ethanol, water, gelatin, aspartame, Fructus Citri tangerinae essence, adjuvants such as Herba Menthae essence.
Select adjuvant significant to oral cavity disintegration tablet, preferred adjuvant can make disintegrate rapidly, no husky large sense, good mouthfeel, swallow easily, to the oral mucosa nonirritant, the present invention selects adjuvant, serves as preferred with microcrystalline Cellulose (MCC), mannitol, crospolyvinylpyrrolidone (PVPP), low-substituted hydroxypropyl cellulose (L-HPC), citric acid, sodium bicarbonate, magnesium stearate, micropowder silica gel, gelatin, acrylic resin, aspartame, flavoring orange essence, Herba Menthae essence.
Oral cavity disintegration tablet of the present invention preferably consists of:
Clindamycin phosphate 40-60%
Macromolecular material 1-10%
Filler 10-50%
Disintegrating agent 2-15%
Effervescent 1-15%
Correctives 0.5-5%
Lubricant 0.1-3%
Wherein macromolecular material is used to wrap up clindamycin phosphate, to cover bitterness, described macromolecular material is selected from: gelatin, acrylic resin, ethyl cellulose, and filler is selected from: microcrystalline Cellulose, lactose, mannitol, disintegrating agent is selected from: low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, effervescent is selected from: citric acid, sodium bicarbonate, correctives are selected from, aspartame, Fructus Citri tangerinae essence, Herba Menthae essence, and lubricant is selected from: magnesium stearate, micropowder silica gel.
Particularly preferred prescription consists of: be made up of following prescription for 1000, every contains active component 0.15g (in clindamycin phosphate)
Clindamycin phosphate 150g
Acrylic resin 15g
Mannitol 49g
Microcrystalline Cellulose 56g
Low-replacement hydroxypropyl cellulose 12g
Sodium bicarbonate 5g
Citric acid 6g
Micropowder silica gel 2g
Magnesium stearate 3g
Aspartame 2g
Can adopt fluidized bed coating, medicine is rolled into microcapsule, preparation method as following microcapsule: IV150g is dissolved in 95% ethanol with macromolecule coating material acrylic resin, by fluid bed above-mentioned solution slowly is sprayed on medicine (1500g) surface, and medicine is wrapped up.Make microcapsule.
The microcapsule that above method makes with can make oral cavity disintegration tablet of the present invention by direct compression process after other adjuvant mixes.
Oral cavity disintegration tablet of the present invention, employing be the technical method preparation of pharmaceutics routine, as using direct compression process, wet method system granule is pressed disc method again.
Clindamycin phosphate orally disintegrating tablet of the present invention, especially the oral cavity disintegration tablet that particularly preferred prescription is formed is compared with existing dosage form has plurality of advantages: when the patient takes this medicine, water or only need to take medicine not with low amounts of water, 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 particularly preferred clindamycin phosphate orally disintegrating tablet of the present invention, also have the following advantages especially: disintegrate is rapid, no grittiness, and no bitterness, good mouthfeel absorbs rapidly nonirritant, bioavailability height.
The specific embodiment:
By the following examples, the invention will be further described.
Embodiment 1:
It is as follows to write out a prescription:
Clindamycin phosphate 150g
Mannitol 67g
Microcrystalline Cellulose 46g
Cross-linking sodium carboxymethyl cellulose (CCN
z) 12g
Sodium bicarbonate 8g
Citric acid 10g
Magnesium stearate 2g
Micropowder silica gel 1g
Aspartame 2g
Flavoring orange essence 2g
Make 1000 altogether
Preparation method: after clindamycin phosphate, aspartame, flavoring orange essence and mannitol crossed 80 mesh sieves respectively, mix homogeneously.Take by weighing microcrystalline Cellulose, crospolyvinylpyrrolidone, sodium bicarbonate, citric acid, magnesium stearate by recipe quantity again and cross 80 mesh sieves, mix homogeneously respectively.Two kinds of powder mixes are sieved, make its mix homogeneously, promptly with suitable pressure tabletting.The oral cavity disintegration tablet smooth in appearance that makes is glossy, disintegrate disintegrate rapidly in 45s rapidly, and slice, thin piece hardness test 2.5～3.0kg, stripping quantity is 90.72% in the inherent 37 ℃ of water of dissolution test 30min.
Embodiment 2:
Adopt the direct compression method
It is as follows to write out a prescription:
Clindamycin phosphate 150g
Mannitol 59g
Microcrystalline Cellulose 54g
Low-replacement hydroxypropyl cellulose 6g
Crospolyvinylpyrrolidone 12g
Sodium bicarbonate 5g
Citric acid 6g
Magnesium stearate 2g
Micropowder silica gel 1g
Aspartame 3g
Herba Menthae essence 2g
Make 1000 altogether
Preparation method: take by weighing after recipe quantity clindamycin phosphate, aspartame, Herba Menthae essence, mannitol crosses 80 mesh sieves respectively mix homogeneously.Again respectively with other microcrystalline cellulose excipients, low-as to replace hydroxypropyl cellulose, crospolyvinylpyrrolidone, sodium bicarbonate, citric acid, magnesium stearate, micropowder silica gel to cross mixing behind 80 mesh sieves.The drug powder and the adjuvant powder mixing that will contain clindamycin phosphate sieve, with suitable pressure tabletting promptly.The oral cavity disintegration tablet smooth in appearance that makes is glossy, disintegrate disintegrate in 40s rapidly, and slice, thin piece hardness 2.5～3.0kg, dissolution test 30min stripping quantity in 37 ℃ of aqueous mediums is 91.38%.
Embodiment 3:
With gelatin, mannitol and aspartame is correctives, and the proportioning of gelatin/mannitol/Aspartane is 0.5: 1: 0.1.With sodium bicarbonate and citric acid is effervescent.It is as follows to write out a prescription:
Clindamycin phosphate 150g
Mannitol 30g
Microcrystalline Cellulose 75g
Crospolyvinylpyrrolidone 9g
Sodium bicarbonate 8g
Citric acid 8g
Gelatin 15g
Magnesium stearate 2g
Aspartame 3g
Prepare 1000 altogether
Preparation method: clindamycin phosphate and gelatin, mannitol and aspartame are crossed 60 mesh sieves respectively, gelatin is dissolved in an amount of distilled water, heating makes its dissolving.Under agitation clindamycin phosphate, mannitol and aspartame are added, put 70～80 ℃ of stirring evaporates to dryness in the water-bath, crushing screening.After other adjuvant crossed 80 mesh sieves respectively, mix.The drug powder and the adjuvant powder mix homogeneously that will contain clindamycin phosphate.With suitable pressure direct compression promptly.The oral cavity disintegration tablet disintegrate that makes disintegrate rapidly in 60s does not rapidly have husky large sense, good mouthfeel.Slice, thin piece hardness is at 2.5～3.0kg, and dissolution test 30min stripping quantity in 37 ℃ of water is 88.79%.
Embodiment 4:
Clindamycin phosphate 150g
Mannitol 65g
Microcrystalline Cellulose 63g
Low-replacement hydroxypropyl cellulose 7g
Crospolyvinylpyrrolidone 8g
Magnesium stearate 2g
Micropowder silica gel 1g
Aspartame 2g
Flavoring orange essence 2g
Make 1000 altogether
Preparation method: clindamycin phosphate, mannitol, aspartame flavoring orange essence are crossed 80 mesh sieves, mix homogeneously respectively.Again respectively with other microcrystalline cellulose excipients, low-as to replace hydroxypropyl cellulose, crospolyvinylpyrrolidone, magnesium stearate, micropowder silica gel to cross mixing behind 80 mesh sieves.The drug powder and the adjuvant powder mixing that will contain clindamycin phosphate sieve, with suitable pressure tabletting promptly.The oral cavity disintegration tablet smooth in appearance that makes is glossy, and disintegrate is disintegrate after surpassing 60s more slowly, and slice, thin piece hardness 2.5～3.0kg, dissolution test 30min stripping quantity in 37 ℃ of aqueous mediums is 85.72%.
Embodiment 5:
Adopt spray thing seasoning to prepare clindamycin phosphate orally disintegrating tablet.Concrete grammar is as follows: 1. the preparation of microcapsule
With high molecular weight acrylic resin II80g, acrylic resin III70g is dissolved in 3000g 95% ethanol, will be dispersed in the above-mentioned solution that contains macromolecular material, after being uniformly dispersed through micronized medicine clindamycin phosphate (1500g).Start spray thing drying machine, medicinal liquid is sprayed into quantity of steam (0.6Mpa) 25kg/h, compressed air (0.6Mpa) 0.4m
3/ min.Make the pastille microcapsule.
2. tabletting promptly gets clindamycin phosphate orally disintegrating tablet with the clindamycin phosphate and other adjuvant mixing direct compressions that make.It is as follows to write out a prescription:
Clindamycin phosphate microcapsule 165g
Mannitol 49g
Microcrystalline Cellulose 56g
Low-replacement hydroxypropyl cellulose 12g
Sodium bicarbonate 5g
Citric acid 6g
Micropowder silica gel 2g
Magnesium stearate 3g
Aspartame 2g
Make 1000 altogether
Preparation method: the microcapsule of pastille clindamycin phosphate is crossed 60 mesh sieves.After mannitol, aspartame crossed 80 mesh sieves respectively, with clindamycin phosphate microcapsule mix homogeneously.Again with other microcrystalline cellulose excipients, low-as to replace hydroxypropyl cellulose, sodium bicarbonate, citric acid, magnesium stearate, micropowder silica gel to cross 80 mesh sieves respectively, with the mannitol that contains the clarithromycin microcapsule, aspartame powder mixes, sieve, promptly with suitable pressure tabletting.The clindamycin phosphate orally disintegrating tablet smooth in appearance that makes is glossy, good mouthfeel, and slice, thin piece hardness is 2.5～3.0kg, disintegrate is rapid, all disintegrates in 60s.Dissolution test, the 30min stripping quantity in water is 81.58%.
Claims (8)
1, a kind of oral cavity disintegration tablet of clindamycin phosphate is characterized in that, by the clindamycin phosphate of physiology effective dose and the medicine acceptable carrier that is fit to make oral cavity disintegration tablet form.
2, the oral cavity disintegration tablet of claim 1 is characterized in that, the described medicine acceptable carrier that is fit to make oral cavity disintegration tablet is macromolecular material, filler, disintegrating agent, effervescent, lubricant and correctives.
3, the oral cavity disintegration tablet of claim 2 is characterized in that, described medicine acceptable carrier is selected from: gelatin, acrylic resin, ethyl cellulose, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, microcrystalline Cellulose, low-substituted hydroxypropyl cellulose, handle agar, citric acid, sodium bicarbonate, mannitol, Camphora, lactose, erythrol, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, xylitol, mannitol, protein sugar, stevioside, sucrose, sorbitol, vitamin C, sodium sulfite, sodium sulfite, pyrosulfite, sodium thiosulfate, different VC, thiourea, cysteine, methionine, thiacetic acid., thioglycerol, butylated hydroxyarisol, two fourth cresols, PG, tocopherol, lecithin, sodium lauryl sulphate, Pulvis Talci, magnesium stearate, micropowder silica gel, Opadry
II, ethanol, water, aspartame, Fructus Citri tangerinae essence, Herba Menthae essence.
4, the oral cavity disintegration tablet of claim 2 is characterized in that, it consists of:
Clindamycin phosphate 40-60%
Macromolecular material 1-10%
Filler 10-50%
Disintegrating agent 2-15%
Effervescent 1-15%
Correctives 0.5-5%
Lubricant 0.1-3%
5, the oral cavity disintegration tablet of claim 4, it is characterized in that described macromolecular material is selected from: gelatin, acrylic resin, ethyl cellulose, filler is selected from: microcrystalline Cellulose, lactose, mannitol, disintegrating agent is selected from: low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch sodium, effervescent is selected from: citric acid, sodium bicarbonate, correctives are selected from aspartame, Fructus Citri tangerinae essence, Herba Menthae essence, and lubricant is selected from: magnesium stearate, micropowder silica gel.
6, the oral cavity disintegration tablet of claim 4 is characterized in that, form by following prescription for 1000,
Clindamycin phosphate 150g
Acrylic resin 15g
Mannitol 49g
Microcrystalline Cellulose 56g
Low-replacement hydroxypropyl cellulose 12g
Sodium bicarbonate 5g
Citric acid 6g
Micropowder silica gel 2g
Magnesium stearate 3g
Aspartame 2g
7, the preparation method of the oral cavity disintegration tablet of claim 4 is characterized in that, medicine is rolled into microcapsule with macromolecular material, microcapsule and filler, disintegrating agent, effervescent, correctives, mix lubricant, tabletting.
8, the preparation method of claim 7, it is characterized in that the preparation process following steps of microcapsule: IV150g is dissolved in 95% ethanol with macromolecule coating material acrylic resin, by fluid bed above-mentioned solution slowly is sprayed on the 1500g medical surfaces, with the medicine parcel, make microcapsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410079330 CN1634114A (en) | 2004-10-01 | 2004-10-01 | Clindamycin phosphate orally disintegrating tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410079330 CN1634114A (en) | 2004-10-01 | 2004-10-01 | Clindamycin phosphate orally disintegrating tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1634114A true CN1634114A (en) | 2005-07-06 |
Family
ID=34847099
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200410079330 Pending CN1634114A (en) | 2004-10-01 | 2004-10-01 | Clindamycin phosphate orally disintegrating tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1634114A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186661A (en) * | 2017-12-15 | 2018-06-22 | 哈尔滨珍宝制药有限公司 | A kind of pharmaceutical composition comprising Clindamycin Hydrochloride and preparation method thereof |
-
2004
- 2004-10-01 CN CN 200410079330 patent/CN1634114A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108186661A (en) * | 2017-12-15 | 2018-06-22 | 哈尔滨珍宝制药有限公司 | A kind of pharmaceutical composition comprising Clindamycin Hydrochloride and preparation method thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1174745C (en) | Use of coating as taste masking agent for oral preparation | |
| CN1186098C (en) | Tablets quickly disintegrated in the oral cavity | |
| KR101047042B1 (en) | Oral preparations with improved bioavailability | |
| CN1494434A (en) | Utilization of spray-dried powder containing sugar alcohol | |
| JP4443119B2 (en) | Solid formulation comprising modafinil | |
| KR100979328B1 (en) | Coated particulate cefuroxime axetil compositions | |
| CN1225017A (en) | Quickly disintegrable compression-molded materials and process for producing the same | |
| CN1181237A (en) | Solid pharmaceutical preparation | |
| CN1366878A (en) | Texture screening granules containing active components | |
| CN1482903A (en) | Nateglinide-containing preparation | |
| CN102548542A (en) | Tablet that disintegrates rapidly in the mouth and that contains two or more types of particles | |
| KR20080083071A (en) | Pharmaceutical preparation containing nateglinide | |
| WO2008032767A1 (en) | Orally disintegrating tablet and process for production thereof | |
| CN1883456A (en) | Flavor-hidden pharmaceutical granule, preparation method and use thereof | |
| CN1853631A (en) | Fast disintegrant containing paroxetine | |
| CN1742957A (en) | Sangju effervescent tablet for treating common cold | |
| CN1893956A (en) | Doxycycline metal complex in a solid dosage form | |
| CN1391896A (en) | Quinoline keto derivatives medicinal composition and its preparing method | |
| JP5134802B2 (en) | Method for preventing reduction of bromhexine hydrochloride content | |
| CN1943586A (en) | Oral disintegrating tablet using roxithromycin and ambroxol hydrochloride as active component and its preparing method and use | |
| CN1903183A (en) | Dispersion tablets of telbivudine and its prepn. method | |
| CN100339084C (en) | Fosfocina calcium disperser, and its prepn. method | |
| CN1823800A (en) | Oral composition containing spiramycin capabile of masking bitter taster | |
| CN1943561A (en) | Oral disintegration tablet of prulifloxacin and its preparing method | |
| CN1634013A (en) | Zinc gluconate oral disintegrating tablet and its preparation process |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |