CN103211777A - Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof - Google Patents
Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof Download PDFInfo
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- CN103211777A CN103211777A CN2013101076709A CN201310107670A CN103211777A CN 103211777 A CN103211777 A CN 103211777A CN 2013101076709 A CN2013101076709 A CN 2013101076709A CN 201310107670 A CN201310107670 A CN 201310107670A CN 103211777 A CN103211777 A CN 103211777A
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Abstract
The invention belongs to the technical field of medicines, and in particular relates to a preparation method of duloxetine hydrochloride enteric coated drugs. The duloxetine hydrochloride is prepared by wrapping four layers of coating on a blank mini-pill, wherein the four layers of coatings are respectively a drug carrier layer, an isolation layer, a enteric coating layer and a film coating layer.
Description
Technical field
The present invention relates to a kind of micropill medicine with enteric function, what more specifically say is duloxetine hydrochloride enteric coated micropill and preparation method thereof.
Background technology
Duloxetine hydrochloride is to be used for the treatment of diseases such as depression and diabetic neuralgia at present, and is used for the medicine that has satisfactory effect in the treatment to female incontinence.
Its chemical structural formula is
Though this medicine belongs to the less medicine of untoward reaction in similar the comparison in the medicine, but the medication process still shows apparent in view untoward reaction, feel sick with gastrointestinal tract especially and react the most obvious, incidence rate can be up to 23%-28%, and it also is the main cause of patient's therapy discontinued, has limited clinical medicine dose.
Summary of the invention
At above-mentioned situation, the present invention will provide a kind of duloxetine hydrochloride medicine with enteric function, to reach under the prerequisite that guarantees therapeutic effect, address the above problem.
Duloxetine hydrochloride enteric medicine of the present invention is made of jointly acceptable adjunct ingredient in duloxetine hydrochloride and the oral drugs, and wherein duloxetine hydrochloride is 10%-70% of a medicine gross weight.The present invention relates to contain duloxetine hydrochloride enteric coated micropill and preparation method thereof.The duloxetine hydrochloride enteric coated micropill is to be got by 4 layers of coating of blank micropill, and the blank pill pericardium contains microcrystalline Cellulose, sucrose, hydroxypropyl methylcellulose, and 4 layers of coating are respectively drug-loaded layer, sealing coat, enteric layer and film-coat layer.Described compositions is by by weight percentage following material:
Duloxetine hydrochloride 5-20%, insolated layer materials 3-10%, enteric layer material 5%-20%, film-coat layered material 3%-7, binding agent 3%-7%.
In said medicine, also have in right amount in the usual way in the adjunct ingredient with water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3%-15% the polyvidone or the binding agent of hypromellose solution.
Preparation method of the present invention comprises the steps:
The preparation of the step 1 blank pill heart: the blank pill pericardium contains microcrystalline Cellulose and sucrose, mass ratio between them is 4:1-1:4, adding is by water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3%-15% the polyvidone or the binding agent of solution, extrudes spheronization technique and prepares the blank pill heart
The configuration of step 2 drug layer coating solution: take by weighing duloxetine hydrochloride crude drug 15-60g, be distributed to by water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is in the binding agent of 3%-15% polyvidone or hypromellose solution, homogenizer high speed shear 5-30min;
The configuration of step 3 sealing coat coating solution: take by weighing polyvidone or hypromellose water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3%-15% solution, as sealing coat;
Step 4 enteric layer coating solution configuration: take by weighing acrylic resin, hypromellose or hydroxypropyl emthylcellulose titanate esters 10-100g, adding entry, ethanol or ethanol/water mixed liquor disperses, other adds triethyl citrate 1-15g, Pulvis Talci 1-9g, join acrylic resin after the high speed shear, hypromellose or hydroxypropyl emthylcellulose titanate esters are disperseed by water, ethanol or ethanol/water mixed liquor to stir 30-120min in the dispersion of gained;
Step 5 film-coat layer coating solution configuration: take by weighing PEG60001-3g, titanium dioxide 1-3g, Pulvis Talci 1-5g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30-120min;
Step 6 takes by weighing the blank pill heart, spray coating at the bottom of the fluid bed, medicine layer weightening finish 30-60g, sealing coat weightening finish 5-7g, enteric layer weightening finish 25-60g, film-coat layer weightening finish 3-8g;
Step 7 is filled into gained band medicine micropill in the capsule shells, gets the duloxetine hydrochloride enteric coated capsule.
Specific embodiment is as follows
Embodiment 1
Take by weighing microcrystalline Cellulose 400g, sucrose 100g adds water 180g system soft material behind the mix homogeneously, extrude spheronizator and prepare the blank pill heart;
Take by weighing duloxetine hydrochloride crude drug 15g, be distributed to by water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is in the binding agent of 3% hypromellose solution, homogenizer high speed shear 10min;
Take by weighing hypromellose 3g water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3% solution, as sealing coat;
Take by weighing acrylic resin 10g, add entry, ethanol or ethanol/water mixed liquor and disperse, other adds triethyl citrate 2.5g, Pulvis Talci 3g, joining hydroxypropyl emthylcellulose after the high speed shear is disperseed by water, ethanol or ethanol/water mixed liquor to stir 30min in the dispersion of gained;
Take by weighing triethyl citrate 1.5g, titanium dioxide 3g, Pulvis Talci 4g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30-120min;
Take by weighing PEG60003g, titanium dioxide 1g, Pulvis Talci 3g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30min;
Take by weighing blank pill heart 100g, spray coating at the bottom of the fluid bed, medicine layer weightening finish 30g, sealing coat weightening finish 5g, enteric layer weightening finish 25g, film-coat layer weightening finish 3g;
Gained band medicine micropill is filled in the capsule shells, and the hydrochloric duloxetine 30mg of every preparation unit gets the duloxetine hydrochloride enteric coated capsule.
Embodiment 2
Take by weighing microcrystalline Cellulose 300g, sucrose 200g adds water 150g system soft material behind the mix homogeneously, extrude spheronizator and prepare the blank pill heart;
Take by weighing duloxetine hydrochloride crude drug 20g, be distributed to by water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is in the binding agent of 3% hypromellose solution, homogenizer high speed shear 10min;
Take by weighing hypromellose 5g water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3% solution, as sealing coat;
Take by weighing acrylic resin 15g, add entry, ethanol or ethanol/water mixed liquor and disperse, other adds triethyl citrate 3g, Pulvis Talci 5g, joining hydroxypropyl emthylcellulose after the high speed shear is disperseed by water, ethanol or ethanol/water mixed liquor to stir 30min in the dispersion of gained;
Take by weighing triethyl citrate 3g, titanium dioxide 2g, Pulvis Talci 4g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30min;
Take by weighing PEG60002.5g, titanium dioxide 3g, Pulvis Talci 1g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30min;
Take by weighing blank pill heart 100g, spray coating at the bottom of the fluid bed, medicine layer weightening finish 30g, sealing coat weightening finish 5g, enteric layer weightening finish 25g, film-coat layer weightening finish 3g;
Gained band medicine micropill is filled in the capsule shells, and the hydrochloric duloxetine 30mg of every preparation unit gets the duloxetine hydrochloride enteric coated capsule.
Embodiment 3
Take by weighing microcrystalline Cellulose 250g, sucrose 250g adds water 180g system soft material behind the mix homogeneously, extrude spheronizator and prepare the blank pill heart;
Take by weighing duloxetine hydrochloride crude drug 25, be distributed to by water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is in the binding agent of 7% hypromellose solution, homogenizer high speed shear 10min;
Take by weighing hypromellose 10g water, the weight ratio that ethanol or ethanol/water mixed liquor are dissolved into is 3% solution, as sealing coat;
Take by weighing acrylic resin 15g, add entry, ethanol or ethanol/water mixed liquor and disperse, other adds triethyl citrate 2.5g, Pulvis Talci 3g, joining hydroxypropyl emthylcellulose after the high speed shear is disperseed by water, ethanol or ethanol/water mixed liquor to stir 30min in the dispersion of gained;
Take by weighing triethyl citrate 3g, titanium dioxide 2.5g, Pulvis Talci 5g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 120min;
Take by weighing PEG60003g, titanium dioxide 1g, Pulvis Talci 3g joins weight ratio that 100g is dissolved into by water, ethanol or ethanol/water mixed liquor and is in 3%-15% the polyvidone or hypromellose solution, stirs 30min;
Take by weighing blank pill heart 100g, spray coating at the bottom of the fluid bed, medicine layer weightening finish 30g, sealing coat weightening finish 5g, enteric layer weightening finish 25g, film-coat layer weightening finish 3g;
Gained band medicine micropill is filled in the capsule shells, and the hydrochloric duloxetine 30mg of every preparation unit gets the duloxetine hydrochloride enteric coated capsule.
Claims (8)
1. an enteric coated preparation that contains duloxetine hydrochloride is to comprise the blank pill heart and pastille coatings thereof, the isolation coat layer, and the compositions of enteric coat layer and film-coat layer is characterized in that: described compositions is by by weight percentage following material:
Duloxetine hydrochloride 5-20%, insolated layer materials 3-10%, enteric layer material 5%-20%, film-coat layered material 3%-7, binding agent 3%-7%.
2. preparation as claimed in claim 1 is characterized in that described insolated layer materials is a hydroxypropyl methylcellulose, ethyl cellulose, methylcellulose, cellulose acetate, acrylic resin, Opadry, one or more in the Sulisi.
3. preparation as claimed in claim 2 is characterized in that described insolated layer materials is a hydroxypropyl methylcellulose, cellulose acetate, methylcellulose, one or more in the acrylic resin.
4. preparation as claimed in claim 1, it is characterized in that described enteric layer material is an acrylic resin, cellulose acetate-phthalate, hydroxypropyl methyl cellulose phthalate, one or more in polyvinyl alcohol phthalate ester (PVAP), the cellulose acetate benzenetricarboxylic acid ester.
5. preparation as claimed in claim 4 is characterized in that described enteric material is an acrylic resin, hypromellose, one or more in the hydroxypropyl methyl cellulose phthalate.
6. preparation as claimed in claim 1 is characterized in that described film-coat layer material is PEG6000 1%-3%, titanium dioxide 1%-3%, one or more in the Pulvis Talci 1%-5%.
7. preparation as claimed in claim 1 is characterized in that described binding agent is a water, ethanol, dehydrated alcohol, starch slurry, polyvidone, one or more in the hydroxypropyl methylcellulose.
8. as any described duloxetine hydrochloride enteric medicine of claim 1 to 7, it is characterized in that described medicine is the enteric-coated pellet capsule agent, the duloxetine hydrochloride content in each preparation unit is 20mg-60mg.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN2013101076709A CN103211777A (en) | 2013-03-31 | 2013-03-31 | Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof |
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| CN2013101076709A CN103211777A (en) | 2013-03-31 | 2013-03-31 | Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof |
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| CN103211777A true CN103211777A (en) | 2013-07-24 |
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| CN2013101076709A Pending CN103211777A (en) | 2013-03-31 | 2013-03-31 | Pharmaceutic preparation of duloxetine hydrochloride and preparation method thereof |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104107169A (en) * | 2014-07-12 | 2014-10-22 | 浙江华海药业股份有限公司 | Duloxetine hydrochloride medicinal composition and a preparation method thereof |
| CN105534949A (en) * | 2016-01-06 | 2016-05-04 | 北京修正创新药物研究院有限公司 | Duloxetine hydrochloride enteric mini-pill preparation |
| CN114099462A (en) * | 2021-12-03 | 2022-03-01 | 宁波高新区美诺华医药创新研究院有限公司 | Duloxetine delayed release pharmaceutical composition and preparation method thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1128141A (en) * | 1994-07-18 | 1996-08-07 | 伊莱利利公司 | Duloxetine enteric pellets |
| CN1759829A (en) * | 2004-10-14 | 2006-04-19 | 上海医药工业研究院 | Duloxetine enteric coated tiny pill capsule, and preparation method |
| WO2009004649A2 (en) * | 2007-05-21 | 2009-01-08 | Sun Pharmaceutical Industries Limited | Enteric coated pharmaceutical compositions |
| CN101448493A (en) * | 2006-05-22 | 2009-06-03 | 特瓦制药工业有限公司 | Duloxetine hydrochloride delayed release formulations |
| CN102908331A (en) * | 2011-08-01 | 2013-02-06 | 浙江九洲药物科技有限公司 | Duloxetine hydrochloride enteric capsules and preparation method thereof |
-
2013
- 2013-03-31 CN CN2013101076709A patent/CN103211777A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1128141A (en) * | 1994-07-18 | 1996-08-07 | 伊莱利利公司 | Duloxetine enteric pellets |
| CN1759829A (en) * | 2004-10-14 | 2006-04-19 | 上海医药工业研究院 | Duloxetine enteric coated tiny pill capsule, and preparation method |
| CN101448493A (en) * | 2006-05-22 | 2009-06-03 | 特瓦制药工业有限公司 | Duloxetine hydrochloride delayed release formulations |
| WO2009004649A2 (en) * | 2007-05-21 | 2009-01-08 | Sun Pharmaceutical Industries Limited | Enteric coated pharmaceutical compositions |
| CN102908331A (en) * | 2011-08-01 | 2013-02-06 | 浙江九洲药物科技有限公司 | Duloxetine hydrochloride enteric capsules and preparation method thereof |
Non-Patent Citations (1)
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| 胡容峰: "《工业药剂学》", 31 July 2010, 北京：中国医药科技出版社 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104107169A (en) * | 2014-07-12 | 2014-10-22 | 浙江华海药业股份有限公司 | Duloxetine hydrochloride medicinal composition and a preparation method thereof |
| CN105534949A (en) * | 2016-01-06 | 2016-05-04 | 北京修正创新药物研究院有限公司 | Duloxetine hydrochloride enteric mini-pill preparation |
| CN114099462A (en) * | 2021-12-03 | 2022-03-01 | 宁波高新区美诺华医药创新研究院有限公司 | Duloxetine delayed release pharmaceutical composition and preparation method thereof |
| CN114099462B (en) * | 2021-12-03 | 2023-11-17 | 宁波高新区美诺华医药创新研究院有限公司 | Duloxetine delayed release pharmaceutical composition and preparation method thereof |
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Application publication date: 20130724 |