Sustained-release preparations containing topiramate and the producing method thereof

A technology for topiramate and preparations, which is applied in the field of sustained-release preparations, can solve the problems of difficulty in swallowing preparations, poor sustained-release properties of pellets, and increase the total weight of preparations, and achieves the effects of improved drug wettability, stable release, and reduced dosage

Inactive Publication Date: 2007-06-27
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The problem encountered with these methods is that two or more coating steps and particle mixing steps are required to achieve subsequent drug release and content control, and if the formulation requires a higher drug content, the total volume of the particles will be smaller. Large, less sustained-release properties compared to compressed tablets due to the increased drug release area of ​​the pellets
Although increasing the solubility of the drug is beneficial to the control of drug release, in order to produce a considerable delayed-release effect, a large amount of sustained-release matrix material needs to be used, which unfavorably increases the total weight of the preparation
In particular, in the case of drugs such as topiramate with a daily maintenance dose of more than 200 mg, dosing is less frequent due to increased solubility, but the weight administered is higher, thereby increasing the weight of the drug formulation and making the formulation difficult to swallow

Method used

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  • Sustained-release preparations containing topiramate and the producing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 3

[0047] Embodiments 1 to 3: Preparation of matrix tablets containing topiramate

[0048]Glyceryl behenate was mixed with topiramate under heating to 70° C. until glyceryl behenate melted or softened. The mixture was cooled to room temperature to form a solid mass. The solid agglomerates were then crushed and passed through a 20 mesh screen. The sieved granules were mixed with the additives shown in Table 1, and the various mixtures were subjected to wet granulation (secondary granulation). The obtained granules were dried, and then magnesium stearate was added thereto. The mixture is compressed into corresponding tablets. The matrix tablet contained various components as shown in Table 1.

experiment example 1

[0058] Experimental Example 1: Surface Adhesion Test

[0059] A solid dispersion was prepared from the tablets prepared in Example 1 and Comparative Example 2 according to the same procedure, using the same amount of solid dispersant. Since the solid dispersion prepared from the tablet of Example 1 can block the surface adhesion of the primary granules through secondary granulation, no adhesion to the surface of the tablet punch or tablet die was observed during tablet compression. On the other hand, in the granules prepared in Comparative Example 2, despite the addition of a lubricant, serious surface blocking occurred, so the production of tablets could not be performed.

experiment example 2

[0060] Experimental Example 2: Dissolution Test

[0061] The release characteristics of the matrix tablets prepared in Examples 1-3 and Comparative Example 3 and the release characteristics of the preparation in Comparative Example 1 were observed using a USP dissolution tester. Under the conditions of pH 6.8, phosphate buffer, paddle method, 50rpm / 900ml, the percentage of drug dissolution from the tablet over time was measured. The results are shown in Table 2.

[0062] Table 2: Dissolution percentage (%) at different times

[0063]

time (hour)

Example 1

Example 2

Example 3

Comparative example 3

time

(min)

Comparative example 1

0

0.0

0.0

0.0

0.0

0.0

0.0

1

7.6

11.6

6.7

38.47

5

20.3

2

12.2

16.2

12.3

54.57

10

85.3

4

18.9

...

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PUM

PropertyMeasurementUnit
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Abstract

Disclosed herein are a sustained-release topiramate preparation and a method for producing the topiramate preparation. The sustained-release topiramate preparation is produced using double granules obtained by granulating topiramate or a pharmaceutically acceptable salt thereof using a solid dispersant by a solid dispersion method (first granulation), and further by granulating the granules using a release sustaining material by dry or wet granulation (second granulation).

Description

technical field [0001] The present invention relates to sustained-release preparations comprising topiramate and methods of preparing the preparations. Background technique [0002] Topiramate is a relatively water-soluble anticonvulsant drug with a solubility of only 9.8 mg / mL. Since commercially available formulations of topiramate disintegrate rapidly after oral administration, patients did not experience severe side effects in drug dissolution and absorption. However, the drug in the topiramate formulation is rapidly absorbed and the blood level is increased, resulting in the occurrence of adverse side effects, and inconvenience to the patient due to the twice-daily oral administration. In view of these shortcomings, it is necessary to provide a sustained-release preparation of topiramate. [0003] Immediate-release preparations acquire their pharmacological activity immediately after administration, while sustained-release preparations acquire their pharmacological ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/22
CPCA61K9/2077A61K9/2027A61P25/08A61K9/16A61K9/20A61K31/357
Inventor 朴晋佑申永姬申光炫金正铸
Owner AMOREPACIFIC CORP
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