CN105769799A - Moxixacin tablet and preparation method thereof - Google Patents
Moxixacin tablet and preparation method thereof Download PDFInfo
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- CN105769799A CN105769799A CN201410811538.0A CN201410811538A CN105769799A CN 105769799 A CN105769799 A CN 105769799A CN 201410811538 A CN201410811538 A CN 201410811538A CN 105769799 A CN105769799 A CN 105769799A
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- moxifloxacin
- tablet
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- disintegrating agent
- microcrystalline cellulose
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Abstract
The invention provides a moxixacin tablet and a preparation method thereof. The active ingredients of the moxixacin tablet are composed of moxixacin hydrochloride and an accessory material. The tablet is reasonable in prescription and has better dissolving-out performance and stability compared with the prior art. The preparation method is reasonable in design and convenient to operate and can meet requirements of large production.
Description
Technical field
The present invention provides a kind of Moxifloxacin tablet and preparation method thereof, belongs to technical field of medicine.
Background technology
Moxifloxacin hydrochloride is the super broad spectrum quinolone class medicine that Bayer A.G develops, trade name: visit multiple pleasure (Avelox).Moxifloxacin hydrochloride structural formula is as follows:
Moxifloxacin demonstrates in vitro has broad spectrum antibiotic activity to gram positive bacteria, gram-negative bacteria, anaerobe, acid fast bacteria and atypical microorganism such as mycoplasma, chlamydia and legionella.Antibacterial mechanisms is interference II, IV topoisomerase.Topoisomerase be control DNA topological sum DNA replication dna, repair and transcribe in key enzyme.Moxifloxacin activity in vivo is high.Can quickly almost being fully absorbed after moxifloxacin oral, absolute bioavailability amounts to about 91%, reaches during peak 0.5～4 hour.Moxifloxacin administration is not affected by feed, and the half-life reaches 12 hours, without cytochrome P 450 enzymes metabolism, decrease the probability of drug drug interaction, renal metabolism 45%, liver metabolism 52%, the patient of renal function injury and slight hepatic insufficiency is without adjusting dosage.
Application number be 99813124.5 Chinese patent disclose a kind of Moxifloxacin prescription: Moxifloxacin: 60～70%；Lactose: 7.5～16%；Sodium carboxymethyl cellulose: 2～6%；Magnesium stearate 0.5～1.1%；Microcrystalline Cellulose: 12～15%.Its preparation technology: moxifloxacin hydrochloride, microcrystalline Cellulose, lactose use water are granulated, then by this granule with at least one disintegrating agent and at least one mix lubricant, and optionally tabletting and coating.
In order to meet the demand of clinical practice, in addition it is also necessary to the tablet formulation that dissolution is better, stability is higher.
Summary of the invention
It is an object of the invention to provide a kind of Moxifloxacin hydrochloride tablet and preparation method thereof.
The Moxifloxacin tablet of the present invention is made up of effective ingredient moxifloxacin hydrochloride and adjuvant, and described adjuvant includes: microcrystalline Cellulose, mannitol, disintegrating agent and lubricant, does not contain lactose.
Described microcrystalline Cellulose and mannitol are as filler, and their weight ratio is preferably 4～5:1, more preferably 5:1.
The effective ingredient of Moxifloxacin tablet of the present invention and the ratio of adjuvant be:
The effective ingredient of Moxifloxacin tablet of the present invention and the ratio of adjuvant are preferably:
The effective ingredient of Moxifloxacin tablet of the present invention and the ratio of adjuvant be more preferably:
Described disintegrating agent is preferably carboxymethyl starch sodium.
Described lubricant is selected from one or more in magnesium stearate, silicon dioxide, Pulvis Talci and sodium stearyl fumarate.
The preparation method of Moxifloxacin sheet of the present invention comprises the following steps:
1) moxifloxacin hydrochloride and various adjuvant are sieved respectively, weigh by recipe quantity；
2) by the microcrystalline Cellulose in crude drug moxifloxacin hydrochloride and adjuvant, mannitol, and partial disintegration agent mix homogeneously, add water soft material processed, granulates, dry, and granulate is subsequently adding residue disintegrating agent and lubricant, mix homogeneously；
3) tabletting, film coating.
Above-mentioned steps 2) in can be initially charged the disintegrating agent of 20%-40% and granulate, add remaining disintegrating agent after granulate.Preferably, the disintegrating agent being initially charged 30% is granulated, and adds remaining disintegrating agent after granulate.
Coating material used by described film coating, optional any commercially available film-coat coating material, for instance Opadry.
Moxifloxacin tablet of the present invention is used for being administered orally.
The technical advantage of the present invention is mainly reflected in following several respects:
1, prescription is reasonable, and dissolution, stability are superior to prior art；
2, process design is reasonable, easy and simple to handle, can meet the requirement of big production；
3, adjuvant valency used is low is easy to get, and integral production cost is low；
4, in asian population, the incidence rate of lactose intolerance is many compared with European crowd, the filler of the present invention adopts microcrystalline Cellulose and mannitol, compared with the prescription of lactose, microcrystalline Cellulose, sodium carboxymethyl cellulose in prior art, the filler of the present invention avoids lactose intolerance crowd and takes the symptoms such as the diarrhoea, the abdominal distention that produce after lactose.
Detailed description of the invention:
Below by way of example, the invention will be further described, but this is not limitation of the present invention, those skilled in the art's basic thought according to the present invention, it is possible to make various amendment or improvement, but without departing from the basic thought of the present invention, all within the scope of the present invention.
Embodiment 1:
| Composition | Consumption |
| Moxifloxacin hydrochloride | 430mg |
| Microcrystalline Cellulose | 170mg |
| Mannitol | 35mg |
| Carboxymethyl starch sodium | 25mg |
| Magnesium stearate | 3mg |
1) moxifloxacin hydrochloride is sieved, weigh by recipe quantity.
2) microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate are sieved respectively, weigh by recipe quantity.
3) being mixed homogeneously with microcrystalline Cellulose, mannitol and 7.5mg carboxymethyl starch sodium by recipe quantity crude drug, add water soft material processed, granulates, dry, and granulate adds all the other carboxymethyl starch sodium and magnesium stearate, mix homogeneously.
4) tabletting.
5) film coating.Film-coating material adopts commercially available Opadry.
Embodiment 2:
| Composition | Consumption |
| Moxifloxacin hydrochloride | 430mg |
| Microcrystalline Cellulose | 150mg |
| Mannitol | 50mg |
| Carboxymethyl starch sodium | 15mg |
| Sodium stearyl fumarate | 2mg |
1) moxifloxacin hydrochloride is sieved, weigh by recipe quantity.
2) microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, sodium stearyl fumarate are sieved respectively, weigh by recipe quantity.
3) being mixed homogeneously with microcrystalline Cellulose, mannitol and 4.5mg carboxymethyl starch sodium by recipe quantity crude drug, add water soft material processed, granulates, dry, and granulate adds all the other carboxymethyl starch sodium and sodium stearyl fumarate, mix homogeneously.
4) tabletting.
5) film coating.
Embodiment 3:
| Composition | Consumption |
| Moxifloxacin hydrochloride | 430mg |
| Microcrystalline Cellulose | 200mg |
| Mannitol | 20mg |
| Carboxymethyl starch sodium | 35mg |
| Magnesium stearate | 5mg |
1) moxifloxacin hydrochloride is sieved, weigh by recipe quantity.
2) microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate are sieved respectively, weigh by recipe quantity.
3) being mixed homogeneously with microcrystalline Cellulose, mannitol and 7mg carboxymethyl starch sodium by recipe quantity crude drug, add water soft material processed, granulates, dry, and granulate adds all the other carboxymethyl starch sodium and magnesium stearate, mix homogeneously.
4) tabletting.
5) film coating.
Embodiment 4:
| Composition | Consumption |
| Moxifloxacin hydrochloride | 430mg |
| Microcrystalline Cellulose | 160mg |
| Mannitol | 40mg |
| Carboxymethyl starch sodium | 20mg |
| Magnesium stearate | 2mg |
1) moxifloxacin hydrochloride is sieved, weigh by recipe quantity.
2) microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, magnesium stearate are sieved respectively, weigh by recipe quantity.
3) being mixed homogeneously with microcrystalline Cellulose, mannitol and 8mg carboxymethyl starch sodium by recipe quantity crude drug, add water soft material processed, granulates, dry, and granulate adds all the other carboxymethyl starch sodium and magnesium stearate, mix homogeneously.
4) tabletting.
5) film coating.
Embodiment 5:
| Composition | Consumption |
| Moxifloxacin hydrochloride | 430mg |
| Microcrystalline Cellulose | 180mg |
| Mannitol | 30mg |
| Carboxymethyl starch sodium | 30mg |
| Silicon dioxide | 1.5mg |
| Pulvis Talci | 1.5mg |
1) moxifloxacin hydrochloride is sieved, weigh by recipe quantity.
2) microcrystalline Cellulose, mannitol, carboxymethyl starch sodium, silicon dioxide, Pulvis Talci are sieved respectively, weigh by recipe quantity.
3) being mixed homogeneously with microcrystalline Cellulose, mannitol and 9mg carboxymethyl starch sodium by recipe quantity crude drug, add water soft material processed, granulates, dry, and granulate adds all the other carboxymethyl starch sodium and silicon dioxide, Pulvis Talci, mix homogeneously.
4) tabletting.
5) film coating.
The dissolution detection of Moxifloxacin tablet of the present invention:
Application number is the prescription disclosed in the Chinese patent of 99813124.5: Moxifloxacin: 60～70%；Lactose: 7.5～16%；Sodium carboxymethyl cellulose: 2～6%；Magnesium stearate 0.5～1.1%；Microcrystalline Cellulose: 12～15%.Its preparation technology: moxifloxacin hydrochloride, microcrystalline Cellulose, lactose use water are granulated, then by this granule with at least one disintegrating agent and at least one mix lubricant, and optionally tabletting and coating.
In the present invention, it is called " to photo " according to the tablet of Chinese patent 99813124.5 preparation；The tablet prepared according to the present invention is called " Tablets ".
One, Moxifloxacin tablet dissolution detection method of the present invention:
(1) preparation of reference substance solution
Take moxifloxacin hydrochloride reference substance and be about 24mg, accurately weighed, put in 100mL measuring bottle, adding hydrochloric acid solution (9 → 1000) dissolve and be diluted to scale, shake up, precision measures 1mL, put in 10mL measuring bottle, add hydrochloric acid solution (9 → 1000) and be diluted to scale, shake up, as reference substance solution.
(2) test method
Take Moxifloxacin sheet sample of the present invention, according to dissolution method (Chinese Pharmacopoeia two annex XC the second methods of version in 2010), with hydrochloric acid solution (9 → 1000) 900mL for dissolution medium, rotating speed is 50 turns per minute, operate in accordance with the law, through 30 minutes time, take solution 10mL, filter, precision measures filtrate 1mL, puts in 20mL measuring bottle, adds dissolution medium to scale, shake up, as need testing solution.According to ultraviolet visible spectrophotometry (Chinese Pharmacopoeia two annex IV A of version in 2010), measure absorbance at the wavelength place of 324nm.Separately take reference substance solution, be measured in the same method, calculate the stripping quantity of every.
Two, Tablets and photo stripping curve in hydrochloric acid medium is compared:
Tablets preparation method: prepare according to the embodiment of the present invention 1.
Comparison piece preparation method: prepare according to Chinese patent 99813124.5 embodiment 1.
Heretofore described hydrochloric acid (9 → 1000) is meant that: 9 milliliters of concentrated hydrochloric acid are diluted to 1000mL, and now concentration of hydrochloric acid is about 0.1mol/L, is equivalent to pH1.0～1.2, and gastric acid is close.0.1mol/L hydrochloric acid is also referred to as 0.1N hydrochloric acid.
(1) Tablets: hydrochloric acid medium (9 → 1000) 900mL；50 revs/min of stripping curve (n=3) determination test result tables of rotating speed
(2) to photo: hydrochloric acid medium (9 → 1000) 900mL；50 revs/min of stripping curve (n=3) determination test result tables of rotating speed
(3) Tablets compares (hydrochloric acid medium with to photo stripping curve；Rotating speed 50 revs/min)
Conclusion: Tablets, limit is decided to be 30 minutes and is not less than 85%, and dissolution is qualified.Tablets and the comparison to photo stripping curve in hydrochloric acid solution (9 → 1000), Tablets sheet is better than photo.Within 30 minutes, dissolution compares, and Tablets sheet is better than photo.
Claims (10)
1. a Moxifloxacin tablet, is made up of effective ingredient moxifloxacin hydrochloride and adjuvant, and described adjuvant includes: microcrystalline Cellulose, mannitol, disintegrating agent and lubricant, does not contain lactose.
2. Moxifloxacin tablet as claimed in claim 1, it is characterised in that the weight ratio of described microcrystalline Cellulose and mannitol is 4～5:1.
3. Moxifloxacin tablet as claimed in claim 1, it is characterised in that the effective ingredient of described Moxifloxacin tablet and the ratio of adjuvant be:
4. Moxifloxacin tablet as claimed in claim 3, it is characterised in that the effective ingredient of described Moxifloxacin tablet and the ratio of adjuvant be:
5. Moxifloxacin tablet as claimed in claim 4, it is characterised in that the effective ingredient of described Moxifloxacin tablet and the ratio of adjuvant be:
6. Moxifloxacin tablet as described in any one in Claims 1 to 5, it is characterised in that described disintegrating agent is carboxymethyl starch sodium.
7. Moxifloxacin tablet as described in any one in Claims 1 to 5, it is characterised in that one or more in magnesium stearate, silicon dioxide, Pulvis Talci and sodium stearyl fumarate of described lubricant.
8. the preparation method of Moxifloxacin tablet described in claim 1, comprises the following steps:
1) moxifloxacin hydrochloride and various adjuvant are sieved respectively, weigh by recipe quantity；
2) by the microcrystalline Cellulose in crude drug moxifloxacin hydrochloride and adjuvant, mannitol, and partial disintegration agent mix homogeneously, add water soft material processed, granulates, dry, and granulate is subsequently adding residue disintegrating agent and lubricant, mix homogeneously；
3) tabletting, film coating.
9. preparation method as claimed in claim 8, it is characterised in that step 2) in be initially charged the disintegrating agent of 20%-40%, add remaining disintegrating agent after granulate.
10. preparation method as claimed in claim 9, it is characterised in that step 2) in be initially charged 30% disintegrating agent, add remaining disintegrating agent after granulate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410811538.0A CN105769799A (en) | 2014-12-23 | 2014-12-23 | Moxixacin tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410811538.0A CN105769799A (en) | 2014-12-23 | 2014-12-23 | Moxixacin tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN105769799A true CN105769799A (en) | 2016-07-20 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410811538.0A Pending CN105769799A (en) | 2014-12-23 | 2014-12-23 | Moxixacin tablet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106822021A (en) * | 2016-12-23 | 2017-06-13 | 江苏苏南药业实业有限公司 | A kind of moxifloxacin hydrochloride controlled release tablet |
Citations (4)
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|---|---|---|---|---|
| CN102204911A (en) * | 2011-03-25 | 2011-10-05 | 北京赛科药业有限责任公司 | Moxifloxacin hydrochloride pharmaceutical composition and its preparation method |
| CN103191114A (en) * | 2013-04-07 | 2013-07-10 | 安徽天洋药业有限公司 | Moxifloxacin-containing oral drug solid preparation and preparation method thereof |
| CN103301080A (en) * | 2012-03-15 | 2013-09-18 | 成都国为医药科技有限公司 | Moxifloxacin hydrochloride-containing pharmaceutical composition and preparation method thereof |
| CN103768063A (en) * | 2012-10-19 | 2014-05-07 | 深圳信立泰药业股份有限公司 | Moxifloxacin hydrochloride pharmaceutical composition and preparation method thereof |
-
2014
- 2014-12-23 CN CN201410811538.0A patent/CN105769799A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102204911A (en) * | 2011-03-25 | 2011-10-05 | 北京赛科药业有限责任公司 | Moxifloxacin hydrochloride pharmaceutical composition and its preparation method |
| CN103301080A (en) * | 2012-03-15 | 2013-09-18 | 成都国为医药科技有限公司 | Moxifloxacin hydrochloride-containing pharmaceutical composition and preparation method thereof |
| CN103768063A (en) * | 2012-10-19 | 2014-05-07 | 深圳信立泰药业股份有限公司 | Moxifloxacin hydrochloride pharmaceutical composition and preparation method thereof |
| CN103191114A (en) * | 2013-04-07 | 2013-07-10 | 安徽天洋药业有限公司 | Moxifloxacin-containing oral drug solid preparation and preparation method thereof |
Non-Patent Citations (1)
| Title |
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| 凌沛学 主编: "《药物制剂技术》", 31 May 2007, 北京：中国轻工业出版社 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106822021A (en) * | 2016-12-23 | 2017-06-13 | 江苏苏南药业实业有限公司 | A kind of moxifloxacin hydrochloride controlled release tablet |
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Application publication date: 20160720 |