CN1943561A - Oral disintegration tablet of prulifloxacin and its preparing method - Google Patents
Oral disintegration tablet of prulifloxacin and its preparing method Download PDFInfo
- Publication number
- CN1943561A CN1943561A CNA2006101125300A CN200610112530A CN1943561A CN 1943561 A CN1943561 A CN 1943561A CN A2006101125300 A CNA2006101125300 A CN A2006101125300A CN 200610112530 A CN200610112530 A CN 200610112530A CN 1943561 A CN1943561 A CN 1943561A
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- prulifloxacin
- disintegration tablet
- preparation
- oral cavity
- mixture
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Abstract
The invention relates to a bioequiavailability of prulifloxacin orally disintegrating tablet for treatment of many infection disease such as acute upper respiratory infection, pneumonia, cystitis , prostatitis, edeitis, etc. also the invention relates to preparation process for said tablet.
Description
Technical field
The present invention relates to medicine of a kind of taking convenience and preparation method thereof, what be particularly related to is the treatment that is used for many infectious disease, as the preparation method and the application thereof of the oral disintegration tablet of prulifloxacin of acute upper respiratory tract infection, pneumonia, cystitis, prostatitis, genital infection etc.
Background technology
Prulifloxacin is a third generation fluoroquinolones broad spectrum antibiotic, gram positive bacteria and gram negative bacteria there is broad-spectrum antibacterial action, particularly, can be used for the treatment of systemic infection to strong with the gram negative bacteria antibacterial ability headed by the bacillus pyocyaneus (also claiming Pseudomonas aeruginosa).Prulifloxacin is except the common feature with fluoroquinolones, similar medicine with other is compared has following characteristics: 1, its resisting gram-positive bacteria and Gatifloxacin are close, surpass like product and resist with the gram negative bacteria headed by the bacillus pyocyaneus, as ciprofloxacin, ofloxacin, levofloxacin and Gatifloxacin, effective equally to the drug resistance bacillus pyocyaneus.2, oral absorption is good, does not have savings in vivo, distribution-free in the cerebrospinal fluid, and side effect is little.3, long half time 8-9 hour, medicining times was few.4, rapid-action, peak time is in 0.5-1 hour, and antibacterial action is (because of it can shift, forming higher concentration) by force in cell in bacterial cell.5, almost not having photosensitive toxicity and neurotoxicity, is the highest product of safety in the present Quinolones medicine.
Oral cavity disintegration tablet is a kind of new pharmaceutical dosage forms, English " Orally disintegrating tables " by name.Be that a kind of water that do not need in the oral cavity can disintegrate or dissolved tablet.It can be in the oral cavity rapidly disintegrate, no grittiness, good mouthfeel, swallow easily, to the oral mucosa nonirritant.The distinguishing feature of this dosage form: 1. absorption is fast, bioavailability is high; 2. instructions of taking does not need water, makes things convenient for part crowd medication, as the patient's medication under old man, child, dysphagia or the special environment. 3. intestinal is residual few, few side effects; 4. avoid the first pass effect of liver sausage.
By retrieval, do not see the pertinent literature and the patent report of relevant oral disintegration tablet of prulifloxacin.
Summary of the invention
The purpose of this invention is to provide a kind of disintegrate fast, absorb rapidly, can effectively improve the bioavailability and the blood drug level of prulifloxacin, improve oral disintegration tablet of prulifloxacin of prulifloxacin off-odor, taking convenience, few side effects and preparation method thereof simultaneously.
Oral disintegration tablet of prulifloxacin of the present invention also contains adjuvant except principal agent.Adjuvant is any available adjuvant that is fit to make oral cavity disintegration tablet, and they can comprise filler, disintegrating agent, effervescent, correctives or odor mask, binding agent, lubricant etc.In each oral formulations unit, contain the about 400mg of prulifloxacin 25mg-, preferred dose is the about 300mg of 50mg-, and more preferred dose is 100-200mg (in active substance UFX).
Because oral cavity disintegration tablet requires disintegrate rapidly in the oral cavity, good mouthfeel, to the oral mucosa nonirritant.Therefore the selection to supplementary product kind and performance thereof is the key of preparation oral cavity disintegration tablet.
The present invention is through selecting, found the pharmaceutic adjuvant of suitable oral disintegration tablet of prulifloxacin, wherein filler selects to be used for increasing the weight and volume of oral cavity disintegration tablet, so that the molding of preparation and divided dose, filler preferably is selected from one or more the mixture in lactose, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, the xylitol etc. among the present invention.
The kind of disintegrating agent and the selection of consumption are for can this preparation disintegrate be most important fully at the appointed time.Disintegrating agent of the present invention one of is selected to comprise in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, pregelatinized Starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium or wherein several mixture.
In oral cavity disintegration tablet, can add an amount of effervescent, help the disintegrate of tablet, and an amount of acid can also be regulated taste.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the effervescent that the present invention selects, or alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.
When the percentage by weight of principal agent in preparation is higher, owing to bitterness may occur, therefore can select to add an amount of odor mask so that the patient accepts and takes, odor mask of the present invention comprises one or more the mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, paraffin, the Brazil wax.
The correctives that the present invention uses one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, Mentholum, aspartame, stevioside, the acesulfame-K or wherein several mixture.
The adding of binding agent and lubricant is for the ease of the preparation of preparation and molding.Binding agent is selected from one or more the mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution.Lubricant is selected from one or more the mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci.
Oral cavity disintegration tablet of the present invention can be by freeze-drying or direct powder compression or granulating tabletting process preparation.
Adopt freeze-drying to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, correctives and odor mask (if necessary), prulifloxacin can be mixed with various adjuvants, add the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization, being shaped to the material lyophilizing gets final product.
Adopt direct powder compression to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, lubricant, correctives and odor mask (if necessary), and behind prulifloxacin and various adjuvant mix homogeneously, direct powder compression gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, binding agent, lubricant, correctives and odor mask (if necessary) with prulifloxacin and partial supplementary material mix homogeneously, add binding agent system soft material, granulate, dry, granulate, add the disintegrating agent and the lubricant of surplus, behind the mix homogeneously, tabletting gets final product.
Adopt granulating tabletting process to prepare oral cavity disintegration tablet, adjuvant can be chosen filler, disintegrating agent, effervescent, binding agent, lubricant, correctives and odor mask (if necessary), the main method step is: acid source in the effervescent and alkali source can be separated granulation, or acid source mixed with alkali source, employing contains the dehydrated alcohol binding agent granulates, dry, granulate, the disintegrating agent and the lubricant of adding surplus, behind the mix homogeneously, tabletting gets final product.
The specific embodiment
Come oral disintegration tablet of prulifloxacin of the present invention done further specifying by following example, but be not limited in following example.
Embodiment 1
Prescription:
Prulifloxacin 100g
Polyvinylpolypyrrolidone 55g
Mannitol 45g
Eudragit?L30D 15g
Flavoring orange essence 2.5g
Make 1000 altogether
Preparation method:
Prulifloxacin is added in the Eudragit L30D suspension, add suitable quantity of water, after stirring, add polyvinylpolypyrrolidone, mannitol, flavoring orange essence, the limit edged stirs, and behind the one-tenth suspension, is poured in the suitable mould lyophilization, press seal, packing.
Embodiment 2
Prescription:
Prulifloxacin 150g
Mannitol 70g
Guar gum 16g
Arabic gum 24g
Xylitol 80g
Fructus Citri Limoniae essence 5g
Make 1000 altogether
Preparation method:
Prulifloxacin is joined in guar gum and the arabic gum mixed liquor, after stirring, add mannitol, xylitol, Fructus Citri Limoniae essence, the limit edged is poured in the suitable mould after stirring and making into even suspension, lyophilization, press seal, packing.
Embodiment 3
Prescription:
Prulifloxacin 200g
Pregelatinized Starch 30g
L-HPC 4g
PPVP 12g
Lactose 40g
Mannitol 50g
Honey peach essence 4g
Magnesium stearate 5g
Micropowder silica gel 5g
Make 1000 altogether
Preparation method:
With the prulifloxacin, L-HPC, PPVP, pregelatinized Starch, mannitol, lactose of all crossing 80 mesh sieves according to the equivalent method mix homogeneously that progressively increases, other mixes with above mixture by the honey peach essence of fetching water, add micropowder silica gel, magnesium stearate mix homogeneously, direct powder compression gets final product.
Embodiment 4
Prescription:
Prulifloxacin 200g
Microcrystalline Cellulose 65g
Crospolyvinylpyrrolidone 10g
Sodium bicarbonate 9g
Citric acid 11g
Pulvis Talci 2g
Aspartame 3g
Make 1000 altogether
Preparation method:
Prulifloxacin, microcrystalline Cellulose, sodium bicarbonate, the citric acid mix homogeneously of 80 mesh sieves will all be crossed, other gets crospolyvinylpyrrolidone, aspartame, Pulvis Talci and adopts the equivalent method of progressively increasing to mix with above mixture, behind the mix homogeneously, direct powder compression gets final product.
Embodiment 5
Prescription:
Prulifloxacin 100g
CMS-Na 10g
L-HPC 20g
Mannitol 25g
Microcrystalline Cellulose 80g
Aspartame 3.5g
Fructus Citri Limoniae essence 1.5g
Pulvis Talci 2.5g
4% starch slurry 7.5g
Make 1000 altogether
Preparation method:
With all crossing prulifloxacin, mannitol, aspartame, Fructus Citri Limoniae essence, L-HPC, the part microcrystalline Cellulose of 80 mesh sieves,, granulate with starch slurry system soft material, dry, granulate, microcrystalline Cellulose, CMS-Na, the Pulvis Talci of adding surplus, mix homogeneously, tabletting gets final product.
Embodiment 6
Prescription:
Prulifloxacin 150g
Microcrystalline Cellulose 100g
Xylitol 50g
Stevioside 3.5g
Flavoring orange essence 10.5g
PPVP 16g
PVP-k30 (50% alcoholic solution) is an amount of
Magnesium stearate 7g
Make 1000 altogether
Preparation method:
To all cross prulifloxacin, xylitol, stevioside, flavoring orange essence, the part microcrystalline Cellulose mix homogeneously of 80 mesh sieves,, granulate with PVP-k30 alcohol liquid system soft material, dry, granulate, microcrystalline Cellulose, PPVP, the magnesium stearate of adding surplus, mix homogeneously, tabletting gets final product.
Embodiment 7
Prescription:
Prulifloxacin 150g
Microcrystalline Cellulose 60g
Sucrose 30g
Citric acid 14g
Sodium bicarbonate 20g
Sodium chloride 10g
Acesulfame-K 6g
The PVP-k30 ethanol solution is an amount of
CMS-Na 9g
PEG6000 3g
Make 1000 altogether
Preparation method:
With all crossing prulifloxacin, sucrose, microcrystalline Cellulose, citric acid, the sodium bicarbonate mix homogeneously of 80 mesh sieves,, granulate with PVP-K30 anhydrous alcohol solution system soft material, dry, granulate add acesulfame-K, sodium chloride, CMS-Na, PEG6000, mix homogeneously, tabletting gets final product.
Embodiment 8
Prescription:
Prulifloxacin 100g
Lactose 50g
Mannitol 140g
L-HPC 30g
Sodium carbonate 3g
Sodium bicarbonate 27g
Tartaric acid 25g
Aspartame 9g
Magnesium stearate 3g
Micropowder silica gel 3g
Make 1000 altogether
Preparation method:
With all cross 80 mesh sieves prulifloxacin, lactose, sodium bicarbonate, sodium carbonate, partly measure the L-HPC mix homogeneously approximately, with 50% ethanol liquid system soft material, granulation, drying, granulate; Other gets mannitol, adds tartaric acid, L-HPC, and mix homogeneously with 50% ethanol liquid system soft material, is granulated, and dry, granulate behind two kinds of granule mix homogeneously, add aspartame, magnesium stearate, micropowder silica gel outward, and tabletting behind the mix homogeneously gets final product.
Claims (10)
1. oral disintegration tablet of prulifloxacin, contain Prulifloxacin active composition (or its esters) and be fit to make the excipient substance of oral cavity disintegration tablet, pharmaceutically suitable carrier and the about 400mg prulifloxacin of about 25mg-(in active substance UFX) are contained in every preparation unit.
2. the compositions of claim 1, the content of wherein said prulifloxacin is the about 300mg of about 50mg-(in active substance UFX).
3. the compositions of claim 1, the content of wherein said prulifloxacin is the about 200mg of about 100mg-(in active substance UFX).
4. the described oral cavity disintegration tablet of claim 1 is characterized in that, the described excipient substance that is fit to make oral cavity disintegration tablet comprises one or more in filler, disintegrating agent, effervescent, correctives, odor mask, binding agent or the lubricant etc.
5. the described oral cavity disintegration tablet of claim 3 is characterized in that described filler is selected from one or more the mixture in lactose, microcrystalline Cellulose, sucrose, fructose, mannitol, pregelatinized Starch, sorbitol, the xylitol.Described disintegrating agent is selected from a kind of or wherein several mixture in low-substituted hydroxypropyl cellulose, crospolyvinylpyrrolidone, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, corn starch, pregelatinized Starch, carboxymethylcellulose calcium, the carboxymethyl starch sodium.Acid source is selected from one or more the mixture in citric acid, tartaric acid, four caproic acids, lysine, the arginine in the described effervescent, and alkali source is selected from one or more mixture wherein such as sodium bicarbonate, sodium carbonate, potassium carbonate, potassium bicarbonate.Described odor mask is selected from one or more the described binding agent of mixture in acrylic resin copolymer, Magnesiumaluminumsilicate, gelatin, melon glue, arabic gum, xanthan gum, paraffin, the Brazil wax and is selected from one or more mixture in syrup, starch slurry, carboxymethylcellulose sodium solution, HPMC solution, the povidone solution; Described lubricant is selected from that one or more the described correctives of mixture in micropowder silica gel, magnesium stearate, PEG6000, the Pulvis Talci one of is selected from Rhizoma et radix valerianae, Fructus Pruni pseudocerasi, Fructus Vitis viniferae, Fructus Citri tangerinae, Fructus Citri Limoniae, Herba Menthae, Fructus Fragariae Ananssae, Fructus Musae, Fructus Ananadis comosi, honey peach essence, maltose alcohol, saccharin sodium, protein sugar, sucrose, aspartame, stevioside, the acesulfame-K or wherein several mixture.
6. the preparation method of the oral cavity disintegration tablet of claim 1 is characterized in that, adopts the preparation of freeze-drying or direct powder compression or granulating tabletting process.
7. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the preparation process of freeze-drying is: prulifloxacin and filler, disintegrating agent, correctives and odor mask are added the suitable quantity of water dilution, behind the mix homogeneously, place suitable sheet shape mould, lyophilization is shaped to the material lyophilizing.
8. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the direct powder compression preparation process is: behind prulifloxacin and filler, disintegrating agent, effervescent, lubricant, correctives and odor mask mix homogeneously, direct powder compression.
9. the preparation method of the described oral cavity disintegration tablet of claim 6, wherein the granulating tabletting process preparation process is: with prulifloxacin and partially filled dose, disintegrating agent, correctives and odor mask, add binding agent system soft material, granulate, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
10. the described preparation method of claim 9, it is characterized in that, the step that wherein adds effervescent is, acid source in the effervescent and alkali source are separated granulation, or acid source is mixed with alkali source, adopt to contain the granulation of dehydrated alcohol binding agent, dry, granulate, the disintegrating agent and the lubricant that add surplus, behind the mix homogeneously, tabletting.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101125300A CN1943561A (en) | 2006-08-23 | 2006-08-23 | Oral disintegration tablet of prulifloxacin and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2006101125300A CN1943561A (en) | 2006-08-23 | 2006-08-23 | Oral disintegration tablet of prulifloxacin and its preparing method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1943561A true CN1943561A (en) | 2007-04-11 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2006101125300A Pending CN1943561A (en) | 2006-08-23 | 2006-08-23 | Oral disintegration tablet of prulifloxacin and its preparing method |
Country Status (1)
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| CN (1) | CN1943561A (en) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210657A (en) * | 2010-04-01 | 2011-10-12 | 南京长澳医药科技有限公司 | Prulifloxacin tablets and preparation process thereof |
| CN102895175A (en) * | 2012-06-04 | 2013-01-30 | 四川科伦药业股份有限公司 | Prulifloxacin oral solid composition and preparation method thereof |
| CN104224744A (en) * | 2014-09-28 | 2014-12-24 | 严相顺 | Ciprofloxacin effervescent tablet for control of silkworm bacterial disease |
| CN106572982A (en) * | 2014-06-20 | 2017-04-19 | 梅琳塔治疗公司 | Antimicrobial compositions with effervescent agents |
| CN106687179A (en) * | 2014-06-20 | 2017-05-17 | 梅琳塔治疗公司 | Methods for treating infections |
-
2006
- 2006-08-23 CN CNA2006101125300A patent/CN1943561A/en active Pending
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102210657A (en) * | 2010-04-01 | 2011-10-12 | 南京长澳医药科技有限公司 | Prulifloxacin tablets and preparation process thereof |
| CN102210657B (en) * | 2010-04-01 | 2016-01-20 | 南京长澳医药科技有限公司 | A kind of prulifloxacin tablet and preparation technology thereof |
| CN102895175A (en) * | 2012-06-04 | 2013-01-30 | 四川科伦药业股份有限公司 | Prulifloxacin oral solid composition and preparation method thereof |
| CN102895175B (en) * | 2012-06-04 | 2014-07-02 | 四川科伦药业股份有限公司 | Prulifloxacin oral solid composition and preparation method thereof |
| CN106572982A (en) * | 2014-06-20 | 2017-04-19 | 梅琳塔治疗公司 | Antimicrobial compositions with effervescent agents |
| CN106687179A (en) * | 2014-06-20 | 2017-05-17 | 梅琳塔治疗公司 | Methods for treating infections |
| AU2015276954B2 (en) * | 2014-06-20 | 2020-07-23 | Melinta Subsidiary Corp. | Antimicrobial compositions with effervescent agents |
| CN106572982B (en) * | 2014-06-20 | 2022-06-03 | 梅琳塔有限责任公司 | Antimicrobial compositions with effervescent agents |
| CN106572982B9 (en) * | 2014-06-20 | 2022-07-08 | 梅琳塔有限责任公司 | Antimicrobial compositions with effervescent agents |
| CN114831955A (en) * | 2014-06-20 | 2022-08-02 | 梅琳塔有限责任公司 | Use of a pharmaceutical composition for the manufacture of a medicament for treating, preventing, or reducing the risk of bacterial infection |
| CN114831955B (en) * | 2014-06-20 | 2024-03-12 | 梅琳塔有限责任公司 | Use of a pharmaceutical composition for the preparation of a medicament for the treatment, prevention or reduction of the risk of a bacterial infection |
| CN104224744A (en) * | 2014-09-28 | 2014-12-24 | 严相顺 | Ciprofloxacin effervescent tablet for control of silkworm bacterial disease |
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| DD01 | Delivery of document by public notice |
Addressee: Yan Diedong Document name: Notice of publication of application for patent for invention |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20070411 |