CN104352472A - Guanfacine hydrochloride sustained release tablets and preparation method thereof - Google Patents
Guanfacine hydrochloride sustained release tablets and preparation method thereof Download PDFInfo
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- CN104352472A CN104352472A CN201410671047.0A CN201410671047A CN104352472A CN 104352472 A CN104352472 A CN 104352472A CN 201410671047 A CN201410671047 A CN 201410671047A CN 104352472 A CN104352472 A CN 104352472A
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- guanfacine hydrochloride
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Abstract
The invention provides guanfacine hydrochloride sustained release tablets. The guanfacine hydrochloride sustained release tablets are prepared from 1 part of guanfacine hydrochloride, 75-80 parts of sustained release skeleton material and 5-10 parts of lubricating agent by weight. A preparation method of the guanfacine hydrochloride sustained release tablets comprises the steps of material preparing, blending, granulating, blending, tabletting and aluminium-plastic packaging. The guanfacine hydrochloride sustained release tablets have novel dosage forms, are steady in medicine release, have good controllability, have obvious technological advantages compared with tablets on the market, have the effect of improving the bioavailability, and have the advantages of good medicine stability, convenience in packaging, transportation and storage, and the like. The preparation method is simple and practicable and is suitable for industrial production.
Description
Technical field
the invention belongs to chemical medicine slow releasing preparation field, be specifically related to a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof.
Background technology
hyperkinetic syndrome, is also called attention deficit hyperactivity disorder (ADHD), is neural and Mental development obstacle disease in modal children and youth period, with absent minded, easily divert one's attention, move more, impulsive behavior be principal character.In China, ADHD is generally 3%-10% at the total prevalence rate of school age population, and boy is obviously more than girl.
the sickness rate of whole world ADHD is 1.7-16%, and the sickness rate of disease in school age children is 3%-5%, and the direct and indirect costs of the annual ADHD of the U.S. reaches 218.7 hundred million dollars.Whole world ADHD market scale ranks the 9th in central nervous system disease market, and increase progressively with the annual rate of growth of 8% every year, child accounts for 17% of China's population, and the sickness rate of this disease is higher, and be modal children ' s spirit obstacle, therefore PATIENT POPULATION is rather huge.Secondly, the time of this disease continuity is long, can from child until grow up.
guanfacine Hydrochloride, researched and developed by Shire company, first selectivity-adrenoreceptor agonists in global range, 1980 in Switzerland's Initial Public Offering, the listing of U.S. FDA in 1986 approval Guanfacine Hydrochloride is used for the treatment of hyperpietic, the slow releasing tablet of Guanfacine Hydrochloride in 2009 obtain U.S. FDA approval be used for the treatment of 6-17 year child and teenager attention-deficient and hyperkinetic syndrome.At present, this kind is not yet gone on the market in China.
Summary of the invention
the object of this invention is to provide a kind of Guanfacine Hydrochloride slow releasing tablet for child and teenager attention-deficient and hyperkinetic syndrome and preparation method thereof.
object of the present invention is achieved through the following technical solutions: a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, be made up of Guanfacine Hydrochloride, sustained-release matrix material, lubricant, wherein, by weight, Guanfacine Hydrochloride 1 part, sustained-release matrix material 75-80 part, lubricant 5-10 part.
described a kind of Guanfacine Hydrochloride slow releasing tablet, by optimum weight number, Guanfacine Hydrochloride 1 part, sustained-release matrix material 80 parts, lubricant 5 parts.
described sustained-release matrix material is hypromellose.
described hypromellose is 75hd15000cr hypromellose.
described lubricant is one or both combinations in magnesium stearate, Pulvis Talci, silicon dioxide.
a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, the concrete steps of its preparation method are:
step 1, to get the raw materials ready: use pulverizer to pulverize Guanfacine Hydrochloride, cross 100 mesh sieves, for subsequent use;
step 2: always mix: by weight, take Guanfacine Hydrochloride, hypromellose put into three-dimensional mixer mixing 30 minutes, take out for subsequent use;
step 3: granulate: mixed supplementary material fine powder is put into wet granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, starts to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging, uses oscillating granulator, granulate with 18 order nylon screens, use fluid bed dryer is dried, and first uses cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses the swing collator granulate of 16 order nylon screen after drying, for subsequent use;
step 4: always mix: by the granule made, puts into three-dimension type mixer, adds lubricant, and total mixed 30 minutes, discharging was for subsequent use;
step 5: tabletting: use 35 to rush high-speed rotary tabletting machine;
step 6: aluminum-plastic packaged: plain sheet is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, obtained finished product.
described a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, it is characterized in that: in described step 3, method of granulating also can be: mixed supplementary material fine powder is put into fluidised bed granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, after goods fluid is in good condition, open spraying, adjustment inlet temperature, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation, spraying is stopped after granular size is moderate, open Hot-blast Heating, inlet temperature is 50-55 degree Celsius, the swing collator granulate of 16 order nylon screen is used after drying, for subsequent use.
beneficial effect of the present invention: the receptors bind of Guanfacine Hydrochloride energy directly and in prefrontal cortex, and the postsynaptic, the excitement of receptor just may produce and strengthen working memory, reduces degree of diverting one's attention, improves attention adjustment, improves Behavior inhibition power and strengthen the effects such as impulsion control.Guanfacine Hydrochloride is not controlled substance, without known abuse or dependency, and Guanfacine Hydrochloride slow releasing tablet of the present invention, dosage form is novel, the release of medicine is steady, controllability good, has obvious technical advantage, improve bioavailability compared with the tablet that goes on the market, there is medicine stability good, packaging, transport, the advantages such as storage is convenient, its preparation method is simple, is applicable to commercial production.
the present invention is through two groups of clinical verifications, wherein one group is that treatment group uses the present invention, and every day uses once, within 7 days, is a course for the treatment of, another group contrast uses existing lansoprazole tablet, every group selection outpatient 90 example, wherein man 45 example, female 45 example, measure 40 years old large age, minimal ages 6 years old, every day uses once, within 7 days, is a course for the treatment of, clinical manifestation is attention deficit, hyperactivity, behavior is got excited, learning difficulty, nervous system development is abnormal, conduct disorder, adult ADHD, table one is for taking the contrasting data after the course for the treatment of:
table 1 is taken front and back and is compared (unit: people) two groups of courses for the treatment of
there were significant differences for treatment group and matched group, thus can find out that the present invention's application clinically has significant curative effect.
clinical advantage:
1, non-analeptic, no dependence:
central stimulants, mostly is controlled drug, often has potential drug dependence risk, easily recurs after drug withdrawal.Guanfacine is optionally adrenoreceptor agonists, does not belong to central nervous excitation agent, while treatment, without dependent form and additive, safer.
2, selectivity is high, rapid-action, and side effect is little:
intuniv is one optionally maincenter alpha2A adrenoceptor agonists, and the affinity of it and alpha2A is high, be the 15-20 of alpha2B and alpha2C receptor affinity doubly; Compared with tomoxetine, this product selectivity is higher, rapid-action, and energy quick control symptom, is applicable to patients during acute stage and uses; Compared with methylphenidate, this product no dependence, side effect is slight, better tolerance, and child and teenager use safer.
to sum up, Intuniv selectivity is high, rapid-action, and untoward reaction mostly is slight scope, and toleration is high, safer, does not affect growth promoter, without additive, greatly improve the compliance of patient, improves cure rate.
Detailed description of the invention
embodiment 1
a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, is made up of Guanfacine Hydrochloride, sustained-release matrix material, lubricant, wherein, by weight, and Guanfacine Hydrochloride 1 part, sustained-release matrix material 75-80 part, lubricant 5-10 part.
by optimum weight number, Guanfacine Hydrochloride 1 part, sustained-release matrix material 80 parts, lubricant 5 parts.
described sustained-release matrix material is hypromellose.
described hypromellose is 75hd15000cr hypromellose.
described lubricant is one or both combinations in magnesium stearate, Pulvis Talci, silicon dioxide.
embodiment 2
a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, the concrete steps of its preparation method are:
step 1, to get the raw materials ready: use pulverizer to pulverize Guanfacine Hydrochloride, cross 100 mesh sieves, for subsequent use;
step 2: always mix: by weight, take Guanfacine Hydrochloride, hypromellose put into three-dimensional mixer mixing 30 minutes, take out for subsequent use;
step 3: granulate: mixed supplementary material fine powder is put into wet granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, starts to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging, uses oscillating granulator, granulate with 18 order nylon screens, use fluid bed dryer is dried, and first uses cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses the swing collator granulate of 16 order nylon screen after drying, for subsequent use;
step 4: always mix: by the granule made, puts into three-dimension type mixer, adds lubricant, and total mixed 30 minutes, discharging was for subsequent use;
step 5: tabletting: use 35 to rush high-speed rotary tabletting machine;
step 6: aluminum-plastic packaged: plain sheet is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, obtained finished product.
described a kind of Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, it is characterized in that: in described step 3, method of granulating also can be: mixed supplementary material fine powder is put into fluidised bed granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, after goods fluid is in good condition, open spraying, adjustment inlet temperature, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation, spraying is stopped after granular size is moderate, open Hot-blast Heating, inlet temperature is 50-55 degree Celsius, the swing collator granulate of 16 order nylon screen is used after drying, for subsequent use.
Claims (7)
1. Guanfacine Hydrochloride slow releasing tablet and preparation method thereof, is characterized in that: be made up of Guanfacine Hydrochloride, sustained-release matrix material, lubricant, wherein, by weight, and Guanfacine Hydrochloride 1 part, sustained-release matrix material 75-80 part, lubricant 5-10 part.
2. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 1 and preparation method thereof, is characterized in that: by optimum weight number, Guanfacine Hydrochloride 1 part, sustained-release matrix material 80 parts, lubricant 5 parts.
3. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 1 and preparation method thereof, is characterized in that: described sustained-release matrix material is hypromellose.
4. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 3 and preparation method thereof, is characterized in that: described hypromellose is 75hd15000cr hypromellose.
5. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 1 and preparation method thereof, is characterized in that: described lubricant is one or both combinations in magnesium stearate, Pulvis Talci, silicon dioxide.
6. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 1-3 and preparation method thereof, is characterized in that: the concrete steps of its preparation method are:
Step 1, to get the raw materials ready: use pulverizer to pulverize Guanfacine Hydrochloride, cross 100 mesh sieves, for subsequent use;
Step 2: always mix: by weight, take Guanfacine Hydrochloride, hypromellose put into three-dimensional mixer mixing 30 minutes, take out for subsequent use;
Step 3: granulate: mixed supplementary material fine powder is put into wet granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, starts to add wetting agent, open simultaneously and shear fly cutter, 2-5 minute, discharging, uses oscillating granulator, granulate with 18 order nylon screens, use fluid bed dryer is dried, and first uses cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature, at 50-55 degree Celsius, uses the swing collator granulate of 16 order nylon screen after drying, for subsequent use;
Step 4: always mix: by the granule made, puts into three-dimension type mixer, adds lubricant, and total mixed 30 minutes, discharging was for subsequent use;
Step 5: tabletting: use 35 to rush high-speed rotary tabletting machine;
Step 6: aluminum-plastic packaged: plain sheet is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, obtained finished product.
7. a kind of Guanfacine Hydrochloride slow releasing tablet according to claim 6 and preparation method thereof, it is characterized in that: in described step 3, method of granulating also can be: mixed supplementary material fine powder is put into fluidised bed granulator, use pure water as binding agent, binding agent is put into feed tank, open machine, adjustment parameter, after goods fluid is in good condition, open spraying, adjustment inlet temperature, liquid supply speed, air inducing frequency, atomizing pressure, Real Time Observation, spraying is stopped after granular size is moderate, open Hot-blast Heating, inlet temperature is 50-55 degree Celsius, the swing collator granulate of 16 order nylon screen is used after drying, for subsequent use.
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| CN201410671047.0A CN104352472A (en) | 2014-11-21 | 2014-11-21 | Guanfacine hydrochloride sustained release tablets and preparation method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287422A (en) * | 2015-12-07 | 2016-02-03 | 黑龙江省智诚医药科技有限公司 | Alfuzosin hydrochloride sustained release tablets and preparation method thereof |
| CN111346067A (en) * | 2020-03-11 | 2020-06-30 | 广东科泰鼎润药业科技有限公司 | Controlled release preparation of guanfacine and preparation method thereof |
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| US20110217373A1 (en) * | 2010-01-29 | 2011-09-08 | Kumaravel Vivek | Extended release pharmaceutical compositions of guanfacine hydrochloride |
| CN103655503A (en) * | 2013-11-25 | 2014-03-26 | 北京润德康医药技术有限公司 | Merariveron sustained-release tablet and preparation method thereof |
| WO2014151797A1 (en) * | 2013-03-15 | 2014-09-25 | Mylan, Inc. | Extended release formulations resistant to alcohol dose dumping |
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2014
- 2014-11-21 CN CN201410671047.0A patent/CN104352472A/en active Pending
Patent Citations (3)
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|---|---|---|---|---|
| US20110217373A1 (en) * | 2010-01-29 | 2011-09-08 | Kumaravel Vivek | Extended release pharmaceutical compositions of guanfacine hydrochloride |
| WO2014151797A1 (en) * | 2013-03-15 | 2014-09-25 | Mylan, Inc. | Extended release formulations resistant to alcohol dose dumping |
| CN103655503A (en) * | 2013-11-25 | 2014-03-26 | 北京润德康医药技术有限公司 | Merariveron sustained-release tablet and preparation method thereof |
Non-Patent Citations (1)
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| 无: ""赫达药用辅料产品手册"", 《百度文库，HTTP://WENKU.BAIDU.COM/LINK?URL=TKIDF-UBF334P3I3JVNU2ZHQSPHI7HJYM_NHACV2MX2M6IVHDEWFWYP5HOEODBSJZV7NQ2FSO1QYSVLZTGGG_YFSWVBNCC9QI0YINXIUYVW》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105287422A (en) * | 2015-12-07 | 2016-02-03 | 黑龙江省智诚医药科技有限公司 | Alfuzosin hydrochloride sustained release tablets and preparation method thereof |
| CN111346067A (en) * | 2020-03-11 | 2020-06-30 | 广东科泰鼎润药业科技有限公司 | Controlled release preparation of guanfacine and preparation method thereof |
| CN111346067B (en) * | 2020-03-11 | 2022-05-17 | 广东科泰鼎润药业科技有限公司 | Controlled release preparation of guanfacine and preparation method thereof |
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