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Stabilized pharmaceutical composition

A composition and stable technology, applied in the directions of drug combinations, antipyretics, pharmaceutical formulations, etc., can solve problems such as stabilization or reduction that have not yet been discussed

Inactive Publication Date: 2013-01-09
EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAG (EGIS PHARMA PLC)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compositions of gabapentin based on the use of three groups of excipients are disclosed, but it has not been discussed which specific groups of excipients lead to stabilization or reduction of conversion of gabapentin to the corresponding lactam impurity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 / A

[0034] Comparative evaluation of the stability of pregabalin using different excipients

[0035] A preformulation study was performed to evaluate the effect of different physical blends of excipients on the stability of pregabalin. The percentage lactam content in the preformulation mixture was determined by HPLC.

[0036]

[0037]

[0038] The above table shows that the degradation of the active pregabalin to the lactam form over time can be prevented by the use of isomalt. It is evident from the above data that, compared with the commercially available formulation In comparison, lactam formation was considerably lower in the preformulation mixture of pregabalin and isomalt.

[0039] Example 1 / B

[0040] Comparative evaluation of the stability of pregabalin using non-reducing sugars

[0041] A preformulation study was performed to evaluate the effect of different physically mixed non-reducing sugars on the stability of pregabalin.

[0042] ...

Embodiment 2

[0045] Pregabalin capsule formulation with 25% drug content (1473-050-25)

[0046] Element

mg / capsule

Pregabalin

25

Isomalt

35

Partially Pregelatinized Starch, USP

35

Talc powder, USP

5

total

100

[0047] Pregabalin and all non-talc excipients were sieved and blended. To this blend was added sieved talc and blended further. This drug-excipient blend was filled into capsules using a manual capsule filling machine.

[0048] In Vitro Dissolution Studies

[0049] Use USP II type instrument in 900ml 0.1N HCl with 50rpm to the pregabalin capsule of present embodiment and commercially available Capsules were subjected to in vitro dissolution studies. The comparative dissolution characteristics are made into the following table:

[0050]

[0051] determination

[0052] The pregabalin capsule of the present embodiment is measured and compared with commercially available Preparation compari...

Embodiment 3

[0059] Pregabalin capsule formulation with 25% drug content (1573-093-25)

[0060] Element

mg / capsule

Pregabalin

25

Isomalt

51

Cornstarch, USP

5

Talc powder, USP

19

total

100

[0061] In Vitro Dissolution Studies

[0062] Use USP II type instrument in 900ml 10.1N HCl with 50rpm to the pregabalin capsule of present embodiment and commercially available Capsules were subjected to in vitro dissolution studies. The comparative dissolution characteristics are made into the following table:

[0063]

[0064] determination

[0065] The pregabalin capsule of the present embodiment is measured and compared with commercially available Preparation comparison, the results are as follows:

[0066] preparation

initially

1M 40℃ / 75%RH

LYRICA 25mg

102.9

99.2

Pregabalin capsule of the present invention

102.6

103.7

[0067] Stability study...

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PUM

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Abstract

The invention relates to stabilized pharmaceutical composition comprising pregabalin and a disaccharide or higher polyol as stabilizer and optionally a conventional pharmaceutically acceptable carrier. The stabilized pharmaceutical composition according to the invention is useful in the treatment of a number of diseases such as epilepsy, Alzheimer's disease or Parkinson's disease.

Description

field of invention [0001] The present invention relates to stable pharmaceutical compositions of gamma-aminobutyric acid ("GABA") analogs and methods for their preparation. In particular, the present invention relates to stable pharmaceutical compositions comprising GABA analogues and disaccharides or higher polyols as stabilizers. Background technique [0002] Gamma-aminobutyric acid ("GABA") is the major inhibitory neurotransmitter in the mammalian central nervous system. GABA binds to specific transmembrane receptors (Cl - -Channel-coupled GABA A Receptor and G-protein-coupled GABA B receptors) modulate neuronal excitability, leading to stabilization or hyperpolarization of the resting membrane potential. Attenuating GABAergic neurotransmission is implicated in the pathophysiology of several central nervous system disorders in humans, namely anxiety, seizures, dyskinesias, panic, depression, alcoholism, pain and manic behavior, whereby a large number has been synthesi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/195
CPCA61K9/4858A61K9/1623A61K31/195A61K31/197A61P1/00A61P13/00A61P13/12A61P25/00A61P25/08A61P25/16A61P25/18A61P25/20A61P25/22A61P25/24A61P25/28A61P29/00
Inventor K·S·亚达夫A·P·苏拉娜S·A·库卡尼R·R·普拉萨德
Owner EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAG (EGIS PHARMA PLC)
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