CN101658501A - Minocycline hydroehloride sustained- release tablets and preparation method thereof - Google Patents
Minocycline hydroehloride sustained- release tablets and preparation method thereof Download PDFInfo
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- CN101658501A CN101658501A CN200810118869A CN200810118869A CN101658501A CN 101658501 A CN101658501 A CN 101658501A CN 200810118869 A CN200810118869 A CN 200810118869A CN 200810118869 A CN200810118869 A CN 200810118869A CN 101658501 A CN101658501 A CN 101658501A
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- cellulose
- minocycline hydrochloride
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- slow releasing
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Abstract
The invention aims to provide minocycline hydroehloride sustained-release tablets with higher stability of medicament release and administrative safety, which are characterized by consisting of minocycline hydroehloride, a slow release material, a filler, a binder, a lubricating agent and a coating material. The minocycline hydroehloride sustained-release tablets have the characteristics of havingconvenient administration, lasting effect and stable curative effect, reducing untoward effect, improving the compliance of patients and the like.
Description
Technical field
The present invention relates to a kind of minocycline hydrochloride sustained release tablet and preparation method thereof, belong to field of medicaments.
Technical background
Minocycline hydrochloride is semi-synthetic Tetracyclines broad ectrum antibiotic, and tool is efficient and long-lasting, and in tetracycline antibiotics, the antibacterial action of this product is the strongest.Antimicrobial spectrum and tetracycline are close.Gram positive bacteria is comprised the staphylococcus aureus, streptococcus etc. of anti-tetracycline and the anti-plucked instrument bacterium of gonorrhea in the gram-negative bacteria all have very strong effect; To the effect of gram negative bacilli generally a little less than; This product also has good inhibitory effect to chlamydia trachomatis and ureaplasma urealyticum.Owing to abuse tetracycline antibiotics, existing most of common Grain-positives and negative bacterium are all to this product drug resistance in recent years.
The mechanism of action of minocycline hydrochloride is to combine with the A position of ribosome 30S subunit, stops the prolongation of peptide chain, thereby suppresses the protein synthesis of antibacterial or other pathogenic microorganisms.Minocycline hydrochloride is a bacteriostatic, but when high concentration, also has bactericidal action.
Minocycline hydrochloride can cause the thyroid of laboratory animal (rat, Canis familiaris L. and monkey) to become black.Rat gives this product and carries out chronic treatment, and the result causes goiter, even thyroid tumor.Minocycline hydrochloride also can cause the thyroid hypertrophy of rat and Canis familiaris L..
In recent years, it is 40,000,000,000 dollars that the average annual growth rate in antibiotic market, the world is about 8%, 1998 year world's anti-infectives market sales revenue, and last year, anti-infectives market sales revenue in the world's was 56,000,000,000 dollars.Tetracyclines accounts for 5%, 2.8 hundred million dollars of sales volumes.The raw material of minocycline hydrochloride is sold and is accounted for 60%, and its preparation sales volume is more than 1,500,000,000 dollars.Because its clinical application range is wide, has a broad antifungal spectrum, effect is strong.Therefore, minocycline hydrochloride has the huge market share, and along with the production domesticization of raw material, cost will descend, the raising that profit margin will be bigger.Therefore developing this product will obtain huge economic benefit, and social benefit.
Minocycline hydrochloride sustained release tablet has following advantage:
1, compare with conventional formulation, the slow releasing preparation rate of releasing drug is steady, near the zero level rate process, can overcome " peak valley " phenomenon that is produced behind the ordinary preparation multiple dose administration.After conventional formulation was taken medicine, drug level rose to maximum rapidly, because metabolism is drained and Degradation, reduced rapidly again then, drug level was controlled between minimum effective drug concentration and the maximum safe concentration relatively more difficult;
2, can make in the body effective blood drug concentration length of holding time, and steadily, utilization ratio of drug can reach 80～90%, and the utilization rate of conventional medicine only is 40～60%;
3, can reduce medicine to the gastrointestinal side effect.Conventional formulation is made controlled release preparation and can be reduced side effect because the disintegrate stripping rapidly in intestinal of oral back is big to GI irritation;
4, the oral obvious fluctuation of having avoided blood drug level of minocycline hydrochloride sustained release tablet has improved bioavailability.Easy to use, adverse reaction reduction, improved patient's compliance.
Summary of the invention
The purpose of this invention is to provide a kind of stability of medicine release and the higher minocycline hydrochloride sustained release tablet of safety of medication, have that convenient drug administration, effect are lasting, stable curative effect, adverse reaction reduction, characteristics such as patient's compliance of having improved.
Minocycline hydrochloride sustained release tablet of the present invention is characterized in that being made up of minocycline hydrochloride, slow-release material, filler, adhesive, lubricant, coating material.
Slow releasing tablet of the present invention, the minocycline hydrochloride effective dose is 10mg～1000mg, is preferably 100mg～400mg.
Slow releasing tablet of the present invention is characterized in that described slow-release material can select for use in hydroxypropyl methylcellulose, Sulisi aqueous dispersion, ethyl cellulose, methylcellulose, cellulose acetate-phthalate, hydroxypropyl cellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl-cellulose, cellulose acetate, cellulose diacetate, Triafol T, glyceryl monostearate, the hydroxy methocel one or more to make.Preferred hydroxypropyl methylcellulose.
Slow releasing tablet of the present invention, it is characterized in that described filler can be selected from one or more in microcrystalline Cellulose, mannitol, low-substituted hydroxypropyl cellulose, polyvinyl alcohol, poly-phthalic acid vinyl acetate, Polyethylene Glycol, sodium alginate, chitosan, sucrose, lactose, starch, dextrin, Icing Sugar, cross linked polyvinyl pyrrolidone, cross-linking sodium carboxymethyl cellulose, pregelatinized Starch, the titanium dioxide, preferred lactose.
Slow releasing tablet of the present invention, it is characterized in that described adhesive can be selected from one or more in water, ethanol, dehydrated alcohol, starch slurry, polyvidone, copolyvidone, crospolyvinylpyrrolidone, hydroxypropyl methylcellulose and/or other cellulose families, preferred polyvidone, copolyvidone.
Slow releasing tablet of the present invention, it is characterized in that described lubricant can select magnesium stearate, micropowder silica gel, Pulvis Talci, hydrogenated vegetable oil, polyethylene glycols for use, month hang in the pure magnesium sulfate one or more, preferred magnesium stearate, micropowder silica gel, Pulvis Talci.
Slow releasing tablet of the present invention is characterized in that described coating material can be selected from ethyl cellulose, starch, methylcellulose, cellulose acetate, cellulose diacetate, Triafol T, acrylic resin, Opadry, Sulisi, preferred Opadry.
Slow releasing tablet of the present invention is characterized in that counting by weight percentage, and it consists of:
Minocycline hydrochloride 5～70%
Slow-release material 0～60%
Filler 0～50%
Adhesive 0～20%
Lubricant 0～6%
The percentage by weight that coating material accounts for slow releasing tablet is:
Coating material 0～40%
The preparation method of described slow releasing tablet of the present invention, it comprises following steps:
(1) plain sheet preparation
(1.1) the preparation of granules minocycline hydrochloride is crossed 80 mesh sieves, and is standby.Take by weighing slow-release material, minocycline hydrochloride, filler and the adhesive of recipe quantity successively; mix homogeneously; add the moderate lubrication agent again; dry granulation behind the mix homogeneously; be circulated to granule between 16 orders～80 orders more than 80%, with 80 now fine powder with moderate lubrication agent mix homogeneously, after mixing with remaining granule again; add the moderate lubrication agent, mix homogeneously.Measure intermediate content.
(1.2) tabletting granule that (1) is made is with shallow circular stamping.Hardness Control is at 7～11KG.
(2) coating adds coating material in the entry under the stirring of propeller blade, is mixed with coating solution, and tablet is put in the coating pan, carries out coating, promptly.
Specific embodiment
Embodiment 1
Prescription
Minocycline hydrochloride 90g
Hydroxypropyl emthylcellulose (K100LV) 80g
Lactose (Flowlac100) 70g
Copolyvidone 20g
Micropowder silica gel 1.3g
Pulvis Talci 3g
Magnesium stearate 3g
Make 1000 altogether
Coating material
Opadry (03B61194) 7.5g
Water 42.5g
Preparation process
(1) plain sheet preparation
(1.1) the preparation of granules minocycline hydrochloride is crossed 80 mesh sieves, and is standby.Take by weighing hydroxypropyl emthylcellulose (K100LV), minocycline hydrochloride, lactose (Flowlac100) and the copolyvidone of recipe quantity successively; mix homogeneously; add an amount of magnesium stearate again; dry granulation behind the mix homogeneously; be circulated to granule between 16 orders～80 orders more than 80%, with 80 now fine powder with recipe quantity micropowder silica gel mix homogeneously, after mixing with remaining granule again; add an amount of magnesium stearate and recipe quantity Pulvis Talci, mix homogeneously.Measure intermediate content.
(1.2) tabletting granule that (1) is made is with the shallow circular stamping of 9mm.Hardness Control is at 7～11KG.
(2) coating adds Opadry (03B61194) in the entry under the stirring of propeller blade, is mixed with coating solution, and tablet is put in the coating pan, carries out coating, promptly.
Embodiment 2
Prescription
Minocycline hydrochloride 45g
Hydroxypropyl emthylcellulose (K100LV) 80g
Lactose (Flowlac100) 70g
Copolyvidone 20g
Micropowder silica gel 1g
Pulvis Talci 2.5g
Magnesium stearate 2.5g
Make 1000 altogether
Coating material
Opadry (03B61194) 7.5g
Water 42.5g
Preparation process
(1) plain sheet preparation
(1.1) the preparation of granules minocycline hydrochloride is crossed 80 mesh sieves, and is standby.Take by weighing hydroxypropyl emthylcellulose (K100LV), minocycline hydrochloride, lactose (Flowlac100) and the copolyvidone of recipe quantity successively; mix homogeneously; add an amount of magnesium stearate again; dry granulation behind the mix homogeneously; be circulated to granule between 16 orders～80 orders more than 80%, with 80 now fine powder with recipe quantity micropowder silica gel mix homogeneously, after mixing with remaining granule again; add an amount of magnesium stearate and recipe quantity Pulvis Talci, mix homogeneously.Measure intermediate content.
(1.2) tabletting granule that (1) is made is with the shallow circular stamping of 8mm.Hardness Control is at 7～11KG.
(2) coating adds Opadry (03B61194) in the entry under the stirring of propeller blade, is mixed with coating solution, and tablet is put in the coating pan, carries out coating, promptly.
Claims (7)
1, a kind of minocycline hydrochloride sustained release tablet is characterized in that being made up of minocycline hydrochloride, slow-release material, filler, adhesive, lubricant, coating material.
2, claim 1 described slow releasing tablet, the minocycline hydrochloride effective dose is 10mg～1000mg, is preferably 100mg～400mg.
3, each described slow releasing tablet among the claim 1-2 is characterized in that:
Described slow-release material can select for use in hydroxypropyl methylcellulose, Sulisi aqueous dispersion, ethyl cellulose, methylcellulose, cellulose acetate-phthalate, hydroxypropyl cellulose, carboxymethyl cellulose, sodium carboxymethyl cellulose, hydroxyethyl-cellulose, cellulose acetate, cellulose diacetate, Triafol T, glyceryl monostearate, the hydroxy methocel one or more to make.Preferred hydroxypropyl methylcellulose.
Described filler can be selected from one or more in microcrystalline Cellulose, mannitol, low-substituted hydroxypropyl cellulose, polyvinyl alcohol, poly-phthalic acid vinyl acetate, Polyethylene Glycol, sodium alginate, chitosan, sucrose, lactose, starch, dextrin, Icing Sugar, cross linked polyvinyl pyrrolidone, cross-linking sodium carboxymethyl cellulose, pregelatinized Starch, the titanium dioxide, preferred lactose.
Described adhesive can be selected from one or more in water, ethanol, dehydrated alcohol, starch slurry, polyvidone, copolyvidone, crospolyvinylpyrrolidone, hydroxypropyl methylcellulose and/or other cellulose families, preferred polyvidone, copolyvidone.
Described lubricant can be selected one or more in magnesium stearate, micropowder silica gel, Pulvis Talci, hydrogenated vegetable oil, polyethylene glycols, month pure magnesium sulfate of extension, preferred magnesium stearate, micropowder silica gel, Pulvis Talci for use.
Described coating material can be selected from ethyl cellulose, starch, methylcellulose, cellulose acetate, cellulose diacetate, Triafol T, acrylic resin, Opadry, Sulisi, preferred Opadry.
4, aforesaid right requires the slow releasing tablet described in the 1-3, it is characterized in that counting by weight percentage, and it consists of:
Minocycline hydrochloride 5～70%
Slow-release material 0～60%
Filler 0～50%
Adhesive 0～20%
Lubricant 0～6%
The percentage by weight that coating material accounts for slow releasing tablet is:
Coating material 0～40%
5, aforesaid right requires the slow releasing tablet described in the 1-4, it is characterized in that calculating by weight, and it consists of:
Minocycline hydrochloride 90g
Hydroxypropyl emthylcellulose (K100LV) 80g
Lactose (Flowlac100) 70g
Copolyvidone 20g
Micropowder silica gel 1.3g
Pulvis Talci 3g
Magnesium stearate 3g
Make 1000 altogether
Coating material
Opadry (03B61194) 7.5g
Water 42.5g
6, aforesaid right requires the slow releasing tablet described in the 1-4, it is characterized in that calculating by weight, and it consists of:
Minocycline hydrochloride 45g
Hydroxypropyl emthylcellulose (K100LV) 80g
Lactose (Flowlac100) 70g
Copolyvidone 20g
Micropowder silica gel 1g
Pulvis Talci 2.5g
Magnesium stearate 2.5g
Make 1000 altogether
Coating material
Opadry (03B61194) 7.5g
Water 42.5g
7, the preparation method of each described slow releasing tablet among the claim 1-6, it comprises following steps:
(1) plain sheet preparation
(1.1) the preparation of granules minocycline hydrochloride is crossed 80 mesh sieves, and is standby.Take by weighing slow-release material, minocycline hydrochloride, filler and the adhesive of recipe quantity successively; mix homogeneously; add the moderate lubrication agent again; mixing all has back dry granulation; be circulated to granule between 16 orders～80 orders more than 80%, with 80 now fine powder with moderate lubrication agent mix homogeneously, after mixing with remaining granule again; add the moderate lubrication agent, mix homogeneously.Measure intermediate content.
(1.2) tabletting granule that (1) is made is with shallow circular stamping.Hardness Control is at 7～11KG.
(2) coating adds coating material in the entry under the stirring of propeller blade, is mixed with coating solution, and tablet is put in the coating pan, carries out coating, promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810118869A CN101658501A (en) | 2008-08-26 | 2008-08-26 | Minocycline hydroehloride sustained- release tablets and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810118869A CN101658501A (en) | 2008-08-26 | 2008-08-26 | Minocycline hydroehloride sustained- release tablets and preparation method thereof |
Publications (1)
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| CN101658501A true CN101658501A (en) | 2010-03-03 |
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|---|---|---|---|
| CN200810118869A Pending CN101658501A (en) | 2008-08-26 | 2008-08-26 | Minocycline hydroehloride sustained- release tablets and preparation method thereof |
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Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101822650A (en) * | 2010-04-28 | 2010-09-08 | 中国科学院上海生命科学研究院湖州营养与健康产业创新中心 | Minocycline hydrochloride sustained release tablet and preparation method thereof |
| CN101940560A (en) * | 2010-09-16 | 2011-01-12 | 孙卫东 | Minocycline hydrochloride sustained-release tablets and method for preparing same with different specifications |
| CN102119931A (en) * | 2011-02-21 | 2011-07-13 | 寿光富康制药有限公司 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
| CN102772384A (en) * | 2012-08-07 | 2012-11-14 | 四川百利药业有限责任公司 | Minocycline hydrochloride sustained release tablet and preparation method thereof |
| US8722650B1 (en) | 2005-06-24 | 2014-05-13 | Medicis Pharmaceutical Corporation | Extended-release minocycline dosage forms |
| CN104606171A (en) * | 2015-02-04 | 2015-05-13 | 上海华源安徽仁济制药有限公司 | Minocycline hydrochloride capsule and preparation method thereof |
| US9192615B2 (en) | 2008-08-06 | 2015-11-24 | Medicis Pharmaceutical Corporation | Method for the treatment of acne and certain dosage forms thereof |
| US9561241B1 (en) | 2011-06-28 | 2017-02-07 | Medicis Pharmaceutical Corporation | Gastroretentive dosage forms for minocycline |
-
2008
- 2008-08-26 CN CN200810118869A patent/CN101658501A/en active Pending
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8722650B1 (en) | 2005-06-24 | 2014-05-13 | Medicis Pharmaceutical Corporation | Extended-release minocycline dosage forms |
| US9192615B2 (en) | 2008-08-06 | 2015-11-24 | Medicis Pharmaceutical Corporation | Method for the treatment of acne and certain dosage forms thereof |
| CN101822650A (en) * | 2010-04-28 | 2010-09-08 | 中国科学院上海生命科学研究院湖州营养与健康产业创新中心 | Minocycline hydrochloride sustained release tablet and preparation method thereof |
| CN101822650B (en) * | 2010-04-28 | 2012-06-20 | 中国科学院上海生命科学研究院湖州营养与健康产业创新中心 | Minocycline hydrochloride sustained release tablet and preparation method thereof |
| CN101940560A (en) * | 2010-09-16 | 2011-01-12 | 孙卫东 | Minocycline hydrochloride sustained-release tablets and method for preparing same with different specifications |
| CN102119931A (en) * | 2011-02-21 | 2011-07-13 | 寿光富康制药有限公司 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
| CN102119931B (en) * | 2011-02-21 | 2013-02-13 | 寿光富康制药有限公司 | Novel metformin hydrochloride slow-releasing tablet and preparation method thereof |
| US9561241B1 (en) | 2011-06-28 | 2017-02-07 | Medicis Pharmaceutical Corporation | Gastroretentive dosage forms for minocycline |
| CN102772384A (en) * | 2012-08-07 | 2012-11-14 | 四川百利药业有限责任公司 | Minocycline hydrochloride sustained release tablet and preparation method thereof |
| CN104606171A (en) * | 2015-02-04 | 2015-05-13 | 上海华源安徽仁济制药有限公司 | Minocycline hydrochloride capsule and preparation method thereof |
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Open date: 20100303 |