CN101890169A - Moxifloxacin oral preparation and preparation method thereof - Google Patents
Moxifloxacin oral preparation and preparation method thereof Download PDFInfo
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- CN101890169A CN101890169A CN200910212686XA CN200910212686A CN101890169A CN 101890169 A CN101890169 A CN 101890169A CN 200910212686X A CN200910212686X A CN 200910212686XA CN 200910212686 A CN200910212686 A CN 200910212686A CN 101890169 A CN101890169 A CN 101890169A
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Abstract
The invention relates to an oral pharmaceutical preparation containing moxifloxacin, salts and/or hydrates of the moxifloxacin, soluble starch and pregelatinized starch. The preparation is characterized by containing 2.9%-14.5% of soluble starch and 1.4%-6.5% of pregelatinized starch, wherein all percents are calculated on the basis of the weight of the pharmaceutical preparation. The invention also relates to a preparation method of the preparation and an application of the preparation for treating or preventing bacterial infection of people or animals.
Description
Technical field
The present invention relates to oral drug preparation that contains Moxifloxacin, its salt and/or hydrate and soluble starch and pregelatinized Starch and preparation method thereof.
Background technology
Moxifloxacin (moxifloxacin) is a fluoroquinolone antimicrobial drug of new generation, have advantages such as has a broad antifungal spectrum, antibacterial activity is strong, toxicity is little, can be used for preventing or treating human or animal's bacterial infection, as upper respiratory tract and lower respiratory infection and skin and soft tissue infection.The chemical name of Moxifloxacin is: 1-cyclopropyl-7-[(S, S)-2,8-diazonium-bicyclo-[4.3.0] nonanal-8-group]-6-fluoro-1,4-dihydro-8-methoxyl group-4-oxo-3-quinoline carboxylic acid, chemical structural formula is as follows:
Beyer Co., Ltd in Chinese patent (patent No. ZL89104574.0), described contain Moxifloxacin or its salt, microcrystalline Cellulose, corn starch, insoluble poly--(1-vinyl)-2-Pyrrolidone, finely divided silicon dioxide and the pharmaceutical preparation of magnesium stearate.In addition, the oral drug preparation that contains Moxifloxacin or its salt, lactose, microcrystalline Cellulose, sodium carboxymethyl cellulose and magnesium stearate has been described by Bayer AG in another piece Chinese patent (patent No. ZL99813124.5), wherein the weight content of lactose is 2.5%～25%.Emphasize among the patent ZL99813124.5 to make the Moxifloxacin tablet have enough hardness and outstanding releasing properties owing to used lactose in the prescription.
Yet the price of lactose is more expensive, and the cost for preparing the moxifloxacin oral preparation according to the prescription of patent ZL99813124.5 is higher.In order to reduce production costs, we discover, by using a certain amount of soluble starch and pregelatinized Starch, can obtain having the moxifloxacin oral preparation of enough hardness and same outstanding releasing properties equally in prescription.
Summary of the invention
The invention provides a kind of Moxifloxacin preparation of oral administration, said preparation contains Moxifloxacin, at least a no aqueous adhesive, at least a disintegrating agent and at least a lubricant, it is characterized in that said preparation contains 2.9%～14.5% soluble starch and 1.4%～6.5% pregelatinized Starch (all percentage number averages are basic calculation with the weight of pharmaceutical preparation).The present invention also provides the tablet that contains said preparation and the preparation method of capsule.
The salt of the Moxifloxacin that the present invention mentions comprises and the salt example hydrochloric acid salt of sour addition, sulfate, acetate, lactate etc., and with the salt of alkali addition such as the salt of sodium hydroxide, potassium hydroxide etc., and/or its hydrate.The preferred especially Moxifloxacin hydrochlorate of the present invention or its monohydrate.
Pharmaceutical preparation provided by the present invention contains 50～85%, preferred 55～75%, preferred especially 60～70% Moxifloxacin or its salt and/or its hydrate.Based on single dose, pharmaceutical preparation provided by the present invention contains the Moxifloxacin of 50～800mg, preferred 100～600mg, preferred especially 200～400mg (under every kind of situation all based on interior amine salt form).
Pharmaceutical preparation provided by the present invention contains 2.9%～14.5% soluble starch and 1.4%～6.5% pregelatinized Starch, preferred 4.9%～9.0% soluble starch and 2.2%～3.5% pregelatinized Starch.
Pharmaceutical preparation provided by the present invention contains at least a no aqueous adhesive, and this binding agent for example is selected from: microcrystalline Cellulose, mannitol, calcium phosphate etc.The special preferably microcrystalline cellulose of the present invention.
Pharmaceutical preparation provided by the present invention contains at least a disintegrating agent, and this disintegrating agent for example is selected from: sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, carboxymethyl starch are received etc.The preferred especially cross-linking sodium carboxymethyl cellulose of the present invention.
Pharmaceutical preparation provided by the present invention contains at least a lubricant, and this lubricant is selected from fatty acid and salt thereof.The preferred especially magnesium stearate of the present invention.
Particularly preferred pharmaceutical preparation of the present invention contains:
60～70% Moxifloxacin or its salt and/or its hydrate,
4.9%～9.0% soluble starch,
2.2%～3.5% pregelatinized Starch,
11.8%～24.1% microcrystalline Cellulose,
3.6% cross-linking sodium carboxymethyl cellulose and
2.0% magnesium stearate.
Pharmaceutical preparation provided by the present invention is especially preferably used with tablet and Capsule form.
The invention provides following technology and can advantageously prepare moxifloxacin capsule:
(1) Moxifloxacin, its salt and/or its hydrate, soluble starch, pregelatinized Starch and microcrystalline Cellulose are crossed 100 eye mesh screens, carry out mixing in the equivalent method mode of progressively increasing by recipe quantity;
(2) will go up the mixture water system soft material that goes on foot gained, 18 mesh sieves are granulated;
(3) drying, granulate;
(4) granule is added the cross-linking sodium carboxymethyl cellulose and the magnesium stearate of recipe quantity, mix homogeneously detects, qualified back filled capsules, the Moxifloxacin capsule.
It is good to use the obtained Moxifloxacin capsule of above-mentioned supplementary material to have active component load, adjuvant low price, purchase easily, and the medicine stripping is quick and complete, has good stability in storage.
The present invention can randomly carry out coating (as mentioned above, the percetage by weight in the present patent application is a basic calculation with the gross weight of pharmaceutical preparation, and does not comprise the weight of optional coating) to the Moxifloxacin tablet.For coating, can use the coated preparation of pharmaceutical field routine, for example based on the hydroxypropyl emthylcellulose and/or the Polyethylene Glycol of various molecular weight.In addition, this coating can contain conventional pigment, for example titanium dioxide, iron oxide red etc.
The invention provides following technology and can advantageously prepare the Moxifloxacin Film coated tablets:
(1) Moxifloxacin, its salt and/or its hydrate, soluble starch, pregelatinized Starch and microcrystalline Cellulose are crossed 100 eye mesh screens, carry out mixing in the equivalent method mode of progressively increasing by recipe quantity;
(2) will go up the mixture water system soft material that goes on foot gained, 18 mesh sieves are granulated;
(3) drying, granulate;
(4) with the cross-linking sodium carboxymethyl cellulose and the magnesium stearate of dried granule adding recipe quantity, mix homogeneously detects;
(5) detect qualified back tabletting, preparation Moxifloxacin label;
(6) film coating pre-mix dose of adding recipe quantity in 95% alcoholic solution, preparation concentration is 5～12% syrup;
(7) adopt syrup that label is carried out coating, preparation Moxifloxacin Film coated tablets.
Use the made moxifloxacin hydrochloride sheet of above-mentioned supplementary material to have outstanding hardness, active component load is good, adjuvant low price, purchase easily, and the medicine stripping is quick and complete, has good stability in storage.
Pharmaceutical preparation of the present invention is preferred for treating or preventing human or animal's bacterial infection.
Description of drawings
Fig. 1 is the comparison of the tablet and the Moxifloxacin stripping percentage curves figure that patent ZL99813124.5 prepares of the embodiment of the invention 2.
The specific embodiment
Following representative instance is used for illustrating the present invention, within the technical scheme that those skilled in the art all belong to the present invention to simple replacement that the present invention did or improvement etc. and protected.
Embodiment 1:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 20.0mg
Pregelatinized Starch 10.0mg
Microcrystalline Cellulose 160.0mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.8mg
Embodiment 2:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 35.0mg
Pregelatinized Starch 15.0mg
Microcrystalline Cellulose 145.0mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.2mg
Embodiment 3:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 45.0mg
Pregelatinized Starch 45.0mg
Microcrystalline Cellulose 95.0mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.2mg
Embodiment 4:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 100.0mg
Pregelatinized Starch 45.0mg
Microcrystalline Cellulose 50.0mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.1mg
Embodiment 5:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 62.2mg
Pregelatinized Starch 24.2mg
Microcrystalline Cellulose 104.3mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.0mg
Embodiment 6:(tablet is a basic calculation with coating not)
Moxifloxacin hydrochlorate 437.9mg
Soluble starch 30.0mg
Pregelatinized Starch 10.0mg
Microcrystalline Cellulose 150.0mg
Cross-linking sodium carboxymethyl cellulose 25.0mg
Magnesium stearate 13.9mg
The mensuration that embodiment 7:(presses the sample of embodiment 2 preparations and presses the sample stripping curve of patent ZL99813124.5 preparation)
Dissolving-out method: two appendix XC of Chinese Pharmacopoeia version in 2005 method, second method
Change basket rotating speed: 50rpm
Medium temperature: 37 ℃ ± 0.5 ℃
Assay method: ultraviolet visible spectrophotometry (two appendix IV of Chinese Pharmacopoeia version in 2005 A)
Measure wavelength: the maximum absorption wave strong point
Computational methods: external standard method
The contrast solution compound method: it is an amount of to get the Moxifloxacin hydrochlorate reference substance that is dried to constant weight, and accurate the title decides, and is diluted to the solution of about 4 μ g among every 1ml with dissolution medium
Get this product, 6 every batch, as dissolution medium, test according to above-mentioned stripping and assay method with the hydrochloric acid solution of 0.1mol/L.Get an amount of and fluid infusion of solution respectively at 1min, 3min, 5min, 10min, 15min, 30min, 45min, filter, it is an amount of that precision is measured subsequent filtrate, adds the solution that stripping medium 0.1mol/L hydrochloric acid solution is diluted to about 4 μ g among every 1ml, measure absorbance at the 295nm place, calculate dissolution.
Result of the test is seen accompanying drawing 1.
Claims (10)
1. oral Moxifloxacin preparation contains
Moxifloxacin or its salt and/or its hydrate,
At least a no aqueous adhesive,
At least a disintegrating agent and
At least a lubricant,
It is characterized in that said preparation contains 2.9%～14.5% soluble starch and 1.4%～6.5% pregelatinized Starch based on its weight.
2. the oral Moxifloxacin preparation of claim 1 is characterized in that said preparation is Moxifloxacin or its salt and/or its hydrate that 50～800mg is contained on the basis with the single dose.
3. the oral Moxifloxacin preparation of claim 1, it is characterized in that not having aqueous adhesive is microcrystalline Cellulose
4. the oral Moxifloxacin preparation of claim 1 is characterized in that disintegrating agent is a cross-linking sodium carboxymethyl cellulose.
5. the oral Moxifloxacin preparation of claim 1 is characterized in that lubricant is a magnesium stearate.
6. the oral Moxifloxacin preparation of claim 1 is characterized in that it especially preferably contains:
60～70% Moxifloxacin or its salt and/or its hydrate,
4.9%～9.0% soluble starch,
2.2%～3.5% pregelatinized Starch,
11.8%～24.1% microcrystalline Cellulose,
3.6% cross-linking sodium carboxymethyl cellulose and
2.0% magnesium stearate.
7. the oral pharmaceutical moxifloxacin preparation of any one in the claim 1～6 is characterized in that it contains the Moxifloxacin hydrochlorate.
8. the oral pharmaceutical moxifloxacin preparation of any one in the claim 1～7 is characterized in that preferably using with tablet and Capsule form.
9. the oral pharmaceutical moxifloxacin preparation of any one in the claim 1～8, it is characterized in that and to granulate with water-wet behind Moxifloxacin, its salt and/or hydrate, soluble starch, pregelatinized Starch, at least a binding agent mixing, dry, granulate, even with at least a disintegrating agent and at least a mix lubricant again, be pressed into label or direct fill capsule.
10. the oral pharmaceutical moxifloxacin preparation of any one is used for the treatment of or prevents human or animal's bacterial infection in the claim 1～9.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200910212686 CN101890169B (en) | 2009-11-16 | 2009-11-16 | Moxifloxacin oral preparation and preparation method thereof |
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| CN 200910212686 CN101890169B (en) | 2009-11-16 | 2009-11-16 | Moxifloxacin oral preparation and preparation method thereof |
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| CN101890169A true CN101890169A (en) | 2010-11-24 |
| CN101890169B CN101890169B (en) | 2013-09-11 |
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| CN 200910212686 Active CN101890169B (en) | 2009-11-16 | 2009-11-16 | Moxifloxacin oral preparation and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102247314A (en) * | 2011-01-12 | 2011-11-23 | 北京润德康医药技术有限公司 | Oral solid preparation using moxifloxacin as active component |
| CN102600093A (en) * | 2012-04-11 | 2012-07-25 | 南京优科生物医药有限公司 | Moxifloxacin tablet and preparation method thereof |
| CN102908323A (en) * | 2012-10-30 | 2013-02-06 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN106074413A (en) * | 2016-07-20 | 2016-11-09 | 南通雅本化学有限公司 | A kind of pharmaceutical composition containing Moxifloxacin |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ID29089A (en) * | 1998-11-10 | 2001-07-26 | Bayer Ag | MOKSIFLOXASIN PHARMACEUTICAL PROPERTIES |
| CN1672680A (en) * | 2004-03-23 | 2005-09-28 | 深圳市天一时科技开发有限公司 | Stable moxixacin tablet and its prepn process |
-
2009
- 2009-11-16 CN CN 200910212686 patent/CN101890169B/en active Active
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102247314A (en) * | 2011-01-12 | 2011-11-23 | 北京润德康医药技术有限公司 | Oral solid preparation using moxifloxacin as active component |
| CN102600093A (en) * | 2012-04-11 | 2012-07-25 | 南京优科生物医药有限公司 | Moxifloxacin tablet and preparation method thereof |
| CN102600093B (en) * | 2012-04-11 | 2013-06-05 | 南京优科生物医药有限公司 | Moxifloxacin tablet and preparation method thereof |
| CN102908323A (en) * | 2012-10-30 | 2013-02-06 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN102908323B (en) * | 2012-10-30 | 2015-03-04 | 天津红日药业股份有限公司 | Moxifloxacin-containing pharmaceutical composition |
| CN106074413A (en) * | 2016-07-20 | 2016-11-09 | 南通雅本化学有限公司 | A kind of pharmaceutical composition containing Moxifloxacin |
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| Publication number | Publication date |
|---|---|
| CN101890169B (en) | 2013-09-11 |
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Free format text: FORMER OWNER: JIANGSU YABANG SHENGYUAN MEDICINE CO., LTD. JIANGSU YABANG AIPUSEN PHARMACEUTICAL CO., LTD. Effective date: 20150430 |
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Effective date of registration: 20150430 Address after: 213200 No. 198, Hua Cheng Road, Jintan, Jiangsu Patentee after: Changzhou Yabang Pharmaceutical & Chemical Co., Ltd. Address before: 213200 No. 198, Hua Cheng Road, Jintan, Jiangsu Patentee before: Changzhou Yabang Pharmaceutical & Chemical Co., Ltd. Patentee before: Jiangsu Yabang Shengyuan Medicine Co., Ltd. Patentee before: Jiangsu Yabang Aipusen Pharmaceutical Co., Ltd. |