Pharmaceutical composition containing pregabalin with improved stability and method for preparing same

A composition and stability technology, which is applied in drug delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as unstable structural characteristics, inability to ensure stability, and stability problems, so as to improve compliance , Improve dosage convenience and ensure stability

Inactive Publication Date: 2016-11-23
YUNGJIN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the inventors observed that the direct addition of excipients to pregabalin in the prior art resulted in a significant increase in the related compound
In other words, the use of excipients such as swelling agents or release-controlling agents creates stability issues when stability cannot be ensured due to the unstable structural features of pregabalin

Method used

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  • Pharmaceutical composition containing pregabalin with improved stability and method for preparing same
  • Pharmaceutical composition containing pregabalin with improved stability and method for preparing same
  • Pharmaceutical composition containing pregabalin with improved stability and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0023] The present inventors repeated and verified various prior art related to sustained release formulations of pregabalin. As a result, they found that because of the poor compatibility between pregabalin and various excipients, adding various excipients directly reduced the stability and increased the generation of related compounds. Therefore, ensuring that the main ingredient pregabalin The stability of Bahrain is the prerequisite for providing sustained-release preparations of pregabalin. When the stability of pregabalin is ensured to enhance its compatibility with excipients, a once-a-day formulation that remains in the upper part of the gastrointestinal tract for a longer period of time can finally be obtained, thereby completing the present invention.

[0024] The sustained-release pharmaceutical composition according to the present invention is formulated by forming a coating unit on the outer surface of a drug unit containing an active ingredient, and then mixing t...

preparation example 1-1

[0063] Preparation Example 1-1: Preparation of active ingredient-containing coating unit (1)

[0064] To prepare coated units containing the active ingredient (pregabalin), first 56 mg of mannitol and 24 mg of Kollicoat IR were completely dissolved in water to prepare a coating. The coating agent powder was used to coat 300 mg of pregabalin to prepare a pregabalin-coated unit with strong stability. In this regard, powder coating of pregabalin was performed using a fluidized bed coater (GlattGPCG2Labsystem, Germany) and operated under the following conditions: input air temperature 65 °C, product bed The temperature was 30 °C, the feed rate was 1.34 mL / min, the nozzle pressure was 1.5 bar and the nozzle diameter was 0.8 mm. In Table 1 the operating conditions of the fluidized bed coater are given.

[0065] [Table 1]

[0066]

[0067] The fluidized bed conditions in Table 1 are descriptions of the detailed conditions and preparation methods of the present invention, and ...

preparation example 1-2

[0068] Preparation Example 1-2: Preparation of Active Ingredient-Containing Coating Unit (2)

[0069] [Table 2]

[0070] raw material

[0071] Under the conditions of table 1, make 300g pregabalin fluidized in the fluidized bed coater, spray coating agent then; is 14.7wt%) and 24g of Kollicoat IR were completely dissolved in 1,176g of purified water to prepare a coating agent. This prepares a coated unit containing the main ingredient. Table 2 gives the ingredients used in their amounts and in wt% in the coated units thus formed.

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Abstract

The present invention relates to a sustained release composition containing pregabalin or a pharmaceutically acceptable salt thereof using a gastroretentive drug delivery system (GRDDS), an oral sustained release formulation containing the composition, and a method for preparing the same. The sustained release composition and the formulation containing the same, according to the present invention, provide a gastroretentive drug delivery system in which a coating portion including sugars or derivatives thereof and a plasticizer is introduced on an external surface of pregabalin having a less stable structure to ensure stability and improve compatibility with an excipient, simultaneously, and the release rate is effectively controlled to increase dosing convenience, leading to increase the compliance of a subject to be administered, and thus the present invention can exhibit improved treatment or prevention effects on various mental disorders, such as neuropathic pain, epilepsy, and fibromyalgia, which could not be previously easily accomplished due to the characteristics of pregabalin.

Description

technical field [0001] The disclosure relates to a pharmaceutical composition, a preparation method of the pharmaceutical composition, and an oral sustained-release preparation using the composition; wherein the pharmaceutical composition includes pregabalin and a pharmaceutically acceptable salt thereof, and has a stable Stability, using a gastric retention drug delivery system. Background technique [0002] Pregabalin, (S)-3-(aminomethyl)-5-methylhexanoic acid (IUPAC name; (3S-3-(aminomethyl)-5-methylhexanoic acid), refers to a compound known to have the molecular formula C 8 h 17 NO 2 And the compound with a molecular weight of 159.23 and its derivatives have a chemical structure similar to that of gamma-aminobutyric acid (GABA), but do not bind to GABA receptors. Pregabalin selectively binds to the alpha-2-delta subunit of presynaptic calcium channels in the central nervous system to reduce calcium influx at nerve terminals. The resulting decrease in calcium influx ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/10A61K47/38A61K9/22
CPCA61K47/10A61K47/36A61K47/38A61K31/197A61K9/2826A61K47/02A61K47/30
Inventor 安哉龙柳志石申大熙柳柄焕
Owner YUNGJIN PHARM CO LTD
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