CN104352446A - Levetiracetam sustained release pellets and preparation method thereof - Google Patents
Levetiracetam sustained release pellets and preparation method thereof Download PDFInfo
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- CN104352446A CN104352446A CN201410670492.5A CN201410670492A CN104352446A CN 104352446 A CN104352446 A CN 104352446A CN 201410670492 A CN201410670492 A CN 201410670492A CN 104352446 A CN104352446 A CN 104352446A
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Abstract
The invention provides levetiracetam sustained release pellets. The levetiracetam sustained release pellets comprise medicine-containing pellets and coating layers, wherein the medicine-containing pellets are coated by the coating layers; the medicine-containing pellets comprise 250mg of levetiracetam, 70mg of hollow pellet cores, 60-110mg of filling agent, 18-68mg of lubricating agent and 2-10mg of adhesive; the coating layers comprise 45-225mg of Eudragit NE30D and 7-68mg of talcum powder. A preparation method of the levetiracetam sustained release pellets comprises the following processes: 1. material preparation; 2. mixing; 3. preparation of the adhesive; 4. preparation of the pellets; 5. preparation of a coating agent; 6. coating; 7. filling; 8. aluminium-plastic packaging and preparation of finished products. The levetiracetam sustained release pellets used for treating epilepsy and the preparation method have the beneficial effects that as the two kinds of advanced technologies, namely novel sustained release preparations and pellet preparations, are adopted, the levetiracetam sustained release pellets have stable treatment effects and higher 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 levetiracetam slow release pellet and preparation method thereof.
Background technology
" epilepsy " or " epilepsy " that epilepsy (epilepsy) is namely commonly called as, is the electric discharge of cerebral neuron paroxysmal abnormality, causes a kind of chronic disease of of short duration cerebral disorder.According to the sick data display of Chinese cri dernier cri, the overall prevalence of domestic epilepsy is 7.0 ‰, and annual morbidity is have the activeness epilepsy prevalence of outbreak to be 4.6 ‰ in 28.8/10 ten thousand, 1 year.
be divided into according to clinical episodes type:
1, general tonic-clonic seizure (grand mal): sudden loss of consciousness, then first tetanic rear clonic spasm, normal companion screams, purplish complexion, urinary incontinence, tongue bites, spit out white foams or blood foam, platycoria, after continuing tens of second or several minutes, convulsion stops naturally, fall into a comatose state, after waking up, have the giddy of short time, irritated, tired, can not recall episode process, if outbreak is constant, the person that do not lie in a comatose condition claims grand mal persistent state always, normal threat to life.
2, petit mal (petit mal): sudden ergasia is interrupted, and loss of consciousness, can accompany myoclonus or automatism, second more than the several seconds to ten of once showing effect, electroencephalogram occurs that 3 times/second slow or sharp slow waves of sour jujube are comprehensive.
3. simple partial seizure: a certain local or side limbs tetanic, Myoclonic seizures, or paraesthesia outbreak, last of short duration, Clear consciousness, if can accompany loss of consciousness outbreak scope extends to other limbs or whole body during along motor region, claims jackson seizures (Jack), after outbreak, suffering limb can have temporary paralysis, claims Todd paralysis.
4, complex partial seizures (psychomotor attack): psychosensory, psychomotor activity and Combination outbreak, there are disturbance of consciousness in various degree and significantly thinking more, consciousness, emotion and Psychomotor disorders, can have fugue, the automatism performances such as sleep-walking, sometimes in hallucination, can hurt sb.'s feelings under the domination of vain hope, the violent behavior such as self inflicted injury.
5, autonomic seizures (diencephalon): can headache-type be had, abdominal pain type, acroesthesia type, type of fainting or cardiovascular outbreak.
6, be essential epilepsy without clear and definite cause of disease person, be secondary to intracranial tumor, wound, infect, parasitic disease, cerebrovascular, general metabolism disease waits causer to be secondary epilepsy.
the medicine for the treatment of epilepsy in the market has a lot, and most drug belongs to tranquilizer, and effect is unstable, bioavailability is low, only play the effect of respite, cannot fundamentally cure, and side effects of pharmaceutical drugs are comparatively large, can damage human nerve.
Summary of the invention
the object of this invention is to provide a kind of levetiracetam slow release pellet being used for the treatment of epilepsy and preparation method thereof.
object of the present invention is achieved through the following technical solutions: a kind of levetiracetam slow release pellet, comprise pastille micropill, coatings, pastille micropill wraps up by described coatings, described pastille micropill comprises: 250mg levetiracetam, 70mg celphere, 60-110mg filler, 18-68mg lubricant, 2-10mg binding agent, and described coatings comprises: 45-225mg is strange NE30D, 7-68mg Pulvis Talci especially.
the best in quality proportioning of described pastille micropill Raw is: 250mg levetiracetam, 70mg celphere, 70mg filler, 20mg lubricant, 10mg binding agent.
the best in quality proportioning of described coatings Raw is: 45mg is strange NE30D, 7mg Pulvis Talci especially.
described filler is microcrystalline Cellulose.
described lubricant is Pulvis Talci.
described binding agent is hypromellose.
sodium lauryl sulphate or Polyethylene Glycol trace is also comprised in described coatings.
the preparation method of described a kind of levetiracetam slow release pellet, comprises following operation:
step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize levetiracetam, crosses 100 mesh sieves;
step 2: mixing: take levetiracetam according to above-mentioned quality proportioning, microcrystalline Cellulose put into three-dimensional mixer mixing 30 minutes, make fine drug powder, take out for subsequent use;
step 3: the preparation of binding agent: take appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is mixed with the binding agent that concentration is 2%, for subsequent use;
step 4: pill: the charging spout mixed fine drug powder being put into centrifugal pellet processing machine, binding agent puts into feed tank, and celphere is put in pot, opens machine, adjustment parameter, start hydrojet, start for powder, after fine drug powder has all spread when ball core has during damp, Pulvis Talci is added in charging spout, continue for powder, after Pulvis Talci has all spread, discharging; Then use vulcanization bed drying machine to dry, first use cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature is at 50-55 degree Celsius, and use 14,24 mesh sieve after drying, the pastille micropill getting 14-24 order size is for subsequent use;
step 5: the preparation of coating materials: take especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined in purified water and stir evenly dissolving, add after especially strange NE30D stirs evenly again, limit is stirred and is just added Pulvis Talci, stirs for subsequent use after 10 minutes;
step 6: coating: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating materials is put into feed tank, stir constantly, open machine, adjustment parameter, starts coating, to be coated dose be finished after, start to heat up and keep temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, loads pastille micropill in 0# capsule;
step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
beneficial effect of the present invention: the levetiracetam slow release pellet being used for the treatment of epilepsy of the present invention, adopt novel slow releasing preparation and the advanced technology of pellet preparations two kinds, slow release refers to by delaying medicine from the rate of releasing drug this dosage form, reduce the absorption rate that medicine enters body, thus play more stable therapeutic effect; Micropill has medicine and increases at gastrointestinal tract surface distributed area, can reduce zest, improves bioavailability, does not affect by gastric emptying factor simultaneously, and drug absorption in vivo is even, and individual variation is little; The advantages such as two kinds of advanced technology apply the technical advantage more enhancing this medicine simultaneously, compared with oral liquid, have medicine stability good, packaging, transport, and 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 takes the present invention, within 7 days, is a course for the treatment of, and another group matched group takes carbamazepine, every group selection outpatient 100 example, wherein man 25 example, female 70 example, max age 75 years old, minimal ages 35 years old, within 7 days, be a course for the treatment of, clinical manifestation for consciousness stupor, tic of the limbs, spit out white foams, purplish complexion, urinary incontinence, monospasm, psychentonia, 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.
Detailed description of the invention
embodiment 1
a kind of levetiracetam slow release pellet, comprise pastille micropill, coatings, pastille micropill wraps up by described coatings, described pastille micropill comprises: 250mg levetiracetam, 70mg celphere, 60-110mg filler, 18-68mg lubricant, 2-10mg binding agent, and described coatings comprises: 45-225mg is strange NE30D, 7-68mg Pulvis Talci especially.
the best in quality proportioning of described pastille micropill Raw is: 250mg levetiracetam, 70mg celphere, 70mg filler, 20mg lubricant, 10mg binding agent.
the best in quality proportioning of described coatings Raw is: 45mg is strange NE30D, 7mg Pulvis Talci especially.
described filler is microcrystalline Cellulose.
described lubricant is Pulvis Talci.
described binding agent is hypromellose.
sodium lauryl sulphate or Polyethylene Glycol trace is also comprised in described coatings.
embodiment 2
a preparation method for levetiracetam slow release pellet, comprises following operation:
step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize levetiracetam, crosses 100 mesh sieves;
step 2: mixing: take levetiracetam according to above-mentioned quality proportioning, microcrystalline Cellulose put into three-dimensional mixer mixing 30 minutes, make fine drug powder, take out for subsequent use;
step 3: the preparation of binding agent: take appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is mixed with the binding agent that concentration is 2%, for subsequent use;
step 4: pill: the charging spout mixed fine drug powder being put into centrifugal pellet processing machine, binding agent puts into feed tank, and celphere is put in pot, opens machine, adjustment parameter, start hydrojet, start for powder, after fine drug powder has all spread when ball core has during damp, Pulvis Talci is added in charging spout, continue for powder, after Pulvis Talci has all spread, discharging; Then use vulcanization bed drying machine to dry, first use cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature is at 50-55 degree Celsius, and use 14,24 mesh sieve after drying, the pastille micropill getting 14-24 order size is for subsequent use;
step 5: the preparation of coating materials: take especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined in purified water and stir evenly dissolving, add after especially strange NE30D stirs evenly again, limit is stirred and is just added Pulvis Talci, stirs for subsequent use after 10 minutes;
step 6: coating: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating materials is put into feed tank, stir constantly, open machine, adjustment parameter, starts coating, to be coated dose be finished after, start to heat up and keep temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, loads pastille micropill in 0# capsule;
step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
Claims (8)
1. a levetiracetam slow release pellet, comprise pastille micropill, coatings, it is characterized in that: pastille micropill wraps up by described coatings, described pastille micropill comprises: 250mg levetiracetam, 70mg celphere, 60-110mg filler, 18-68mg lubricant, 2-10mg binding agent, and described coatings comprises: 45-225mg is strange NE30D, 7-68mg Pulvis Talci especially.
2. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: the best in quality proportioning of described pastille micropill Raw is: 250mg levetiracetam, 70mg celphere, 70mg filler, 20mg lubricant, 10mg binding agent.
3. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: the best in quality proportioning of described coatings Raw is: 45mg is strange NE30D, 7mg Pulvis Talci especially.
4. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: described filler is microcrystalline Cellulose.
5. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: described lubricant is Pulvis Talci.
6. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: described binding agent is hypromellose.
7. a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: also comprise sodium lauryl sulphate or Polyethylene Glycol trace in described coatings.
8. the preparation method of a kind of levetiracetam slow release pellet according to claim 1, is characterized in that: comprise following operation:
Step 1: get the raw materials ready: by above-mentioned quality proportioning, use pulverizer to pulverize levetiracetam, crosses 100 mesh sieves;
Step 2: mixing: take levetiracetam according to above-mentioned quality proportioning, microcrystalline Cellulose put into three-dimensional mixer mixing 30 minutes, make fine drug powder, take out for subsequent use;
Step 3: the preparation of binding agent: take appropriate hypromellose by above-mentioned quality proportioning, adds appropriate hot water and is mixed with the binding agent that concentration is 2%, for subsequent use;
Step 4: pill: the charging spout mixed fine drug powder being put into centrifugal pellet processing machine, binding agent puts into feed tank, and celphere is put in pot, opens machine, adjustment parameter, start hydrojet, start for powder, after fine drug powder has all spread when ball core has during damp, Pulvis Talci is added in charging spout, continue for powder, after Pulvis Talci has all spread, discharging; Then use vulcanization bed drying machine to dry, first use cool breeze dry, after epidermis parches, open Hot-blast Heating, inlet temperature is at 50-55 degree Celsius, and use 14,24 mesh sieve after drying, the pastille micropill getting 14-24 order size is for subsequent use;
Step 5: the preparation of coating materials: take especially strange NE30D, Pulvis Talci, sodium lauryl sulphate, purified water by above-mentioned quality proportioning, first sodium lauryl sulphate is joined in purified water and stir evenly dissolving, add after especially strange NE30D stirs evenly again, limit is stirred and is just added Pulvis Talci, stirs for subsequent use after 10 minutes;
Step 6: coating: by the pastille micropill of 14-24 order size, put into fluidized-bed coating machine, coating materials is put into feed tank, stir constantly, open machine, adjustment parameter, starts coating, to be coated dose be finished after, start to heat up and keep temperature of charge more than 40 degree, dry 30 minutes, cooling, discharging, closing machine;
Step 7: fill: the pastille micropill after above-mentioned coating is used capsule filling machine, loads pastille micropill in 0# capsule;
Step 8: plastic-aluminum: above-mentioned capsule is used aluminium-plastic bubble plate packing machine, is packaged into aluminium-plastic panel, packed products.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410670492.5A CN104352446A (en) | 2014-11-21 | 2014-11-21 | Levetiracetam sustained release pellets and preparation method thereof |
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| CN201410670492.5A CN104352446A (en) | 2014-11-21 | 2014-11-21 | Levetiracetam sustained release pellets and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105267155A (en) * | 2015-12-07 | 2016-01-27 | 黑龙江省智诚医药科技有限公司 | Cefaclor sustained-release pellet and preparation method thereof |
| CN105267154A (en) * | 2015-12-07 | 2016-01-27 | 黑龙江省智诚医药科技有限公司 | Etodolac sustained-release pellets and preparation method thereof |
| CN105287396A (en) * | 2015-12-07 | 2016-02-03 | 黑龙江省智诚医药科技有限公司 | Acyclovir sustained release pellets and preparation method thereof |
| WO2024021050A1 (en) * | 2022-07-29 | 2024-02-01 | 上海安必生制药技术有限公司 | Levetiracetam sustained-release formulation and preparation method therefor |
-
2014
- 2014-11-21 CN CN201410670492.5A patent/CN104352446A/en active Pending
Non-Patent Citations (1)
| Title |
|---|
| 林丽峰，等: "左乙拉西坦缓释微丸的研究", 《中国现代应用药学》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105267155A (en) * | 2015-12-07 | 2016-01-27 | 黑龙江省智诚医药科技有限公司 | Cefaclor sustained-release pellet and preparation method thereof |
| CN105267154A (en) * | 2015-12-07 | 2016-01-27 | 黑龙江省智诚医药科技有限公司 | Etodolac sustained-release pellets and preparation method thereof |
| CN105287396A (en) * | 2015-12-07 | 2016-02-03 | 黑龙江省智诚医药科技有限公司 | Acyclovir sustained release pellets and preparation method thereof |
| WO2024021050A1 (en) * | 2022-07-29 | 2024-02-01 | 上海安必生制药技术有限公司 | Levetiracetam sustained-release formulation and preparation method therefor |
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Application publication date: 20150218 |