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Extended-release levetiracetam and method of preparation

A technology of prolonged release and granules, which is applied in botany equipment and methods, pharmaceutical formulations, plant growth regulators, etc., and can solve the problem of increasing dosage form size

Inactive Publication Date: 2015-05-13
PHARMTAK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When a large number of excipients are used to control release, the dosage form size becomes large, causing problems for oral administration

Method used

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  • Extended-release levetiracetam and method of preparation
  • Extended-release levetiracetam and method of preparation
  • Extended-release levetiracetam and method of preparation

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0205] extended release composition

[0206] This example shows an example of an extended release composition that does not contain a hydrophilic polymer.

[0207] Table 1

[0208]

[0209] make up means enough

[0210] Levetiracetam was granulated with an aqueous ethylcellulose dispersion with or without other ingredients such as plasticizers and subsequently dried in a fluid bed apparatus to produce depot granules free of hydrophilic polymers. The ethylcellulose used was E-7 19040 (Colorcon) and diluted with water to a final solids content of about 10-15% w / w. The depot particles can be filled into capsules or sachets.

[0211] The depot granules are then blended with lactose and colloidal silicon dioxide and lubricated with magnesium stearate. The colloidal silicon dioxide can be blended before, after, or at the same time as the lactose. The final blend is then filled into capsules or sachets, or compressed into tablets. For example, the blend can be formulated...

Embodiment approach 2

[0213] Extended release composition with hydrophilic polymer

[0214] The following examples show embodiments of extended release compositions incorporating hydrophilic polymers in depot particles.

[0215] Table 2

[0216]

[0217] Depot particles were produced as in Example 1 except that the release rate modifier with or without plasticizer was added to the aqueous ethylcellulose dispersion. The release rate modifier can be a hydrophilic excipient, preferably a hydrophilic polymer, eg, hydroxypropylmethylcellulose. In this example, the release rate modifier is Methocel TM Hydrophilic polymer sold under the E5 Premium LV trademark.

[0218] An aqueous ethylcellulose dispersion with a release rate modifier was used to coat levetiracetam to produce depot particles as in Example 1. The depot particles can be filled into capsules or sachets.

[0219] The dry depot granules are blended with lactose and lubricated with magnesium stearate. The final blend is then filled i...

example 3

[0221] extragranular release rate modifier

[0222] This example shows an embodiment of an extended release composition incorporating a hydrophilic polymer in a depot granule and an extragranular release rate modifier.

[0223] table 3

[0224]

[0225] Depot particles were produced as in Example 2. The depot particles can be filled into capsules or sachets.

[0226] The depot granules are then blended with lactose and colloidal silicon dioxide and a release rate modifier, and then lubricated with magnesium stearate. The lactose, release rate modifier and colloidal silicon dioxide may be blended, individually or together, in any order, with the magnesium stearate added last. The release rate modifier blended with the depot particles is a hydrophilic polymer according to Methocel TM Hydroxypropyl methylcellulose sold under the trademark K100M Premium CR. The final blend is then filled into capsules or sachets, or compressed into tablets. For example, the blend can b...

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Abstract

Described herein is a pharmaceutical composition comprising levetiracetam as an active ingredient to provide prolonged release characteristic to allow once a day dosage regime. The innovative formulation comprises levetiracetam and a hydrophobic polymer with or without additional release rate modifier(s). The formulation may comprise other pharmaceutically acceptable excipients. This invention also describes the processes of preparing such dosage forms.

Description

[0001] Cross-References to Related Applications [0002] This application claims the benefit of US Provisional Application No. 61 / 680,789, filed August 8, 2012, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates to extended release dosage forms of levetiracetam, including pharmaceutical compositions, and methods for producing them. Background technique [0004] The chemical name of levetiracetam (one single enantiomer) is (-)-(S)-α-ethyl-2-oxo-1-pyrrolidineacetamide and its molecular formula is C 8 h 14 N 2 o 2 And its molecular weight is 170.21. Use levetiracetam as a primary antiepileptic drug (AED). It has the following structural formula: [0005] [0006] Levetiracetam is very soluble in water (104g / 100mL). It is challenging to develop a dosage form to control or delay the release of levetiracetam from the dosage form when placed in water or administered by oral route. [0007] US Patent No. 7,858...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/36A61K31/40
CPCA61K9/2054A61K9/2081A61K9/5047A61K31/4015A61K9/146
Inventor I-L·T·苏J-C·李
Owner PHARMTAK