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Sustained release tablet comprising pregabalin through two-phase release-controlling system

A technology of pregabalin and sustained-release tablets, which is applied in the directions of nervous system diseases, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc., to achieve the effects of enhancing flotation and swelling.

Active Publication Date: 2014-04-02
YUHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the dosage form is not gastroretentive, a problem arises in that it releases pregabalin not only in the upper small intestine (the main site of absorption of pregabalin), but also in other gastrointestinal sites such as the stomach and lower small intestine Pregabalin

Method used

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  • Sustained release tablet comprising pregabalin through two-phase release-controlling system
  • Sustained release tablet comprising pregabalin through two-phase release-controlling system
  • Sustained release tablet comprising pregabalin through two-phase release-controlling system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 34

[0035] Sustained-release tablets were prepared according to the ingredients and amounts shown in Tables 1 to 5. The amounts in Tables 1 to 5 represent the weight (mg) of each ingredient in each tablet. Pregabalin and hydroxypropyl methylcellulose (Metolose TM 90SH-100,000cps SR, Shinetsu) into a high-speed stirrer, and then a binder solution (prepared by dissolving hydroxypropyl cellulose (HPC JF) in a 50% ethanol solution) was added thereto. The mixture was granulated by spinning at 250 rpm for 3 minutes. The resulting granules are dried and then screened with a milling machine. The resulting granules are mixed with polyethylene oxide (Polyox301 and / or Polyox303), and supplementary flotation agents (crospovidone or sodium starch glycolate), diluents (hydroxypropylcellulose or microcrystalline cellulose) or lubricants (colloidal silicon dioxide) for 5 minutes. Magnesium stearate was blended with the mixture for an additional 3 minutes, followed by compression to obtain ext...

experiment example 1

[0049] Experimental Example 1: In Vitro Dissolution Test

[0050] The tablets prepared in Examples 1 to 34 were subjected to a dissolution test according to "Dissolution Test 2 (Paddle Method)" of the Korean Pharmacopoeia. 900ml of 0.06N HCl solution was used as the dissolution medium, and the dissolution test was performed at 37±0.5°C with a paddle rotation speed of 50rpm. Aliquots were removed from the dissolution medium at 0.5, 1, 2, 3, 4, 6, 8, 12, 16 and 24 minutes. Each sample was analyzed by HPLC (at 210 nm) to calculate the dissolution rate. The results are shown in Tables 6-10. As shown in Tables 6 to 10,

[0051] Tablets prepared according to the present invention exhibit an excellent sustained release dissolution profile.

[0052]

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[0055]

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[0058]

[0059]

[0060]

[0061]

[0062]

[0063]

experiment example 2

[0064] Experimental Example 2: Measurement of floating-initiation time and floating-maintenance time

[0065] The tablets prepared in the above examples were subjected to a dissolution test according to "Dissolution Test 2 (Paddle Method)" of the Korean Pharmacopoeia. 900ml of 0.06N HCl solution was used as the dissolution medium, and the dissolution test was performed at 37±0.5°C with a paddle rotation speed of 50rpm. The floating lag time was measured, followed by the maintenance of floating time, up to 24 hours. The results are shown in Tables 11 to 13. As shown in Tables 11 to 13, the tablets prepared according to the present invention started to float within 30 minutes; and each tablet maintained floating for at least 24 hours.

[0066]

[0067]

[0068]

[0069]

[0070]

[0071]

[0072] floating time

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Abstract

The invention provides a sustained release tablet having two-phase release-controlling system, which consists of a first release-controlling phase comprising pregabalin or its salt and hydroxypropyl methylcellulose; and a second release-controlling phase comprising polyethylene oxide as a swelling polymer, the first release-controlling phase being homogeneously dispersed in the second release-controlling phase.

Description

technical field [0001] The present invention relates to a sustained-release tablet with a two-phase controlled-release system, which consists of a first controlled-release phase comprising pregabalin or a salt thereof and hydroxypropylmethylcellulose, and polyethylene oxide as a swelling polymer. The composition of the second controlled-release phase, the first controlled-release phase is uniformly dispersed in the second controlled-release phase. Background technique [0002] Pregabalin, whose chemical name is (S)-(+)-3-aminomethyl-5-methylhexanoic acid, can bind to the α-2-δ subunit of the calcium channel and bind to the inner It is related to the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), which is involved in the regulation of brain nerve activity. Pregabalin helps treat epilepsy, neuropathic pain, and fibromyalgia, among others. Pregabalin is marketed in an immediate release (IR) dosage form, such as capsules with 75 mg, 150 mg or 300 mg contents, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/20A61K31/197A61K47/38
CPCA61K9/2059A61K31/197A61K9/2054A61K9/2095A61K9/0065A61K9/209A61K9/2027A61K9/2031A61P25/04A61P25/08A61P43/00
Inventor 禹政勳罗云婌郑杨洙玄昌根朴隆植
Owner YUHAN
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