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Levetiracetam slow release pellet capsule preparation

A technology of sustained-release pellets and capsules, which is applied in the field of levetiracetam sustained-release pellets and capsule preparations and its preparation, can solve the problems of large individual differences in gastric emptying, achieve improved bioavailability, small individual differences, good fluidity

Inactive Publication Date: 2011-08-17
天津药物研究院药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

By using pellets and sustained-release technology to make levetiracetam into sustained-release capsule preparations, it can not only achieve the effect of stable blood drug concentration and reduce side effects of sustained-release preparations, but also fundamentally solve the problem of tablets being affected by the gastric pyloric sphincter. The problem of large individual differences in gastric emptying

Method used

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  • Levetiracetam slow release pellet capsule preparation
  • Levetiracetam slow release pellet capsule preparation
  • Levetiracetam slow release pellet capsule preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Levetiracetam Extended Release Pellets Capsules Prescription: (Quality)

[0032] Levetiracetam 62%

[0033] Blank ball core (diameter 350 micron-450 micron) 18%

[0034] Hypromellose E5 6.5%

[0035] Ethyl cellulose aqueous dispersion E-7-19040 (solid content) 12%

[0036] Talc 1%

[0037] Colloidal silicon dioxide 0.5%

[0038] Preparation method of levetiracetam sustained-release pellets and capsules:

[0039] Measured according to the prescription, levetiracetam was pulverized through a 100-mesh sieve, and hydroxypropylmethylcellulose E5 was prepared into a 5% solution with purified water to be used as a binder. Add the blank ball core (diameter 350 micron-450 micron) in the sugar-coating machine (diameter 60 centimeters), adjust the rotating speed 20-25 rev / min, elevation angle 10-20 °, make the blank ball core be in motion, then put 5 % hydroxypropylmethylcellulose E5 aqueous solution binder is sprayed in through a spray gun (atomization pressure 0.02 MPa, at...

Embodiment 2

[0051] Levetiracetam Extended Release Pellets Capsules Prescription: (Quality)

[0052] Levetiracetam 62%

[0053] Blank ball core (diameter 350 micron-450 micron) 18%

[0054] Hypromellose E5 6.5%

[0055] EUDRAGIT NE 30D (solid content) 8%

[0056] Talc 5%

[0057] Colloidal silicon dioxide 0.5%

[0058] Preparation method of levetiracetam sustained-release pellets and capsules:

[0059] Measured according to the prescription, levetiracetam was pulverized through a 100-mesh sieve, and hydroxypropylmethylcellulose E5 was prepared into a 5% solution with purified water to be used as a binder. Blank ball core (diameter 350 micron-450 micron) is added in the sugar-coating machine (diameter 60 centimeters), adjust rotating speed 20-25 rev / min, elevation angle 10-20 °, make blank ball core be in motion state, then put 5 % hydroxypropylmethylcellulose E5 aqueous solution binder is sprayed in through a spray gun (atomization pressure 0.02 MPa, atomization distance 10-20 cm) to...

Embodiment 3

[0064] Levetiracetam Extended Release Pellets Capsules Prescription: (Quality)

[0065] Levetiracetam 60%

[0066] Blank ball core (diameter 350 micron-450 micron) 18%

[0067] Povidone K30 8.5%

[0068] Ethyl cellulose aqueous dispersion E-7-19040 (solid content) 12%

[0069] Talc 1%

[0070] Colloidal silicon dioxide 0.5%

[0071] Preparation method of levetiracetam sustained-release pellets and capsules:

[0072] Measured according to the prescription, the levetiracetam is pulverized through a 100-mesh sieve, and the povidone K30 is prepared into a 5% solution with purified water to be used as a binder. Add the blank ball core (diameter 350 micron-450 micron) in the sugar-coating machine (diameter 60 centimeters), adjust the rotating speed 20-25 rev / min, elevation angle 10-20 °, make the blank ball core be in motion, then put 5 100% povidone K30 aqueous solution binder is sprayed in through a spray gun (atomization pressure 0.02 MPa, atomization distance 10-20 cm), an...

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Abstract

The invention relates to a levetiracetam slow release pellet capsule preparation and a preparation method thereof. The levetiracetam slow release pellet capsule preparation comprises the following components in percentage by mass: 50-70 percent of levetiracetam, 15-30 percent of blank pellet, 5-10 percent of hydroxypropylmethyl cellulose or polyvidone, 7-15 percent of ethylcellulose or acrylic resin, 1-8 percent of talc powder and 0.5-2 percent of cataloid. The preparation method comprises the following steps: coating levetiracetam fine powder on the blank pellet by a binding agent to be madeinto a medicine-contained pellet; coating an isolating layer on the medicine-contained pellet; coating a slow release coating film on the medicine-contained pellet coated with the isolating layer to prepare a slow release pellet; and mixing the slow release pellet, the talc powder and the cataloid and filling the mixture into a capsule. The levetiracetam is made into the slow release capsule preparation by a pellet and slow release technology, and the slow release preparation can stabilize blood medicine concentration, reduce the generating frequency and degree of the side effect and fundamentally solve the problems of great influence on a tablet by gastric pyloric sphincter and big differences of gastric emptying individuals.

Description

technical field [0001] The invention relates to a levetiracetam sustained-release pellet capsule preparation and a preparation method thereof. Background technique [0002] Levetiracetam (Levetiracetam, LEV) is levoethylpiracetam in piracetam derivatives, and its chemical name is (S)-α-ethyl-2-oxo-1-pyrrolidine ethyl Amide, molecular formula: C 8 h 14 N 2 o 2 , molecular weight: 170.21. Good water solubility (104mg / ml). Levetiracetam is rapidly absorbed after oral administration, and its absolute bioavailability is close to 100%. The plasma concentration reaches the maximum after 0.6-1.3 hours of administration. The blood concentration has a linear relationship with the dosage. The plasma half-life of healthy adults is 7±1 hours. It is about 10-11 hours for the elderly, which is related to the decline of renal function. The main side effects of levetiracetam are drowsiness, fatigue, dizziness, difficulty with coordination, and behavioral disturbances. These side e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K31/40A61K47/38A61K47/32A61P25/08
Inventor 马克刘亚梅杨昕周学海杨艳红
Owner 天津药物研究院药业有限责任公司
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