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Aceclofenac slow-release preparation providing an optimum pharmacological clinical effect when administered once a day

A technology of aceclofenac and controlled-release preparations, which is applied in the field of controlled-release oral preparations and controlled-release preparations, can solve the problems of difficult-to-adjust aceclofenac, and achieve the effects of reducing the frequency of administration, rapid analgesia and anti-inflammatory effects

Active Publication Date: 2015-04-01
KOREA UNITED PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] Although hydroxypropylmethylcellulose (HPMC) and carbomer (pH-dependent and pH-independent polymers, respectively) have been used to control the dissolution rate, HPMC and carbomer have the following disadvantages: only use Carbomer to control the dissolution of aceclofenac in alkaline solution and HPMC to maintain the matrix form of the tablet, it is difficult to precisely regulate the dissolution of aceclofenac in the stomach (which is an acidic condition)

Method used

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  • Aceclofenac slow-release preparation providing an optimum pharmacological clinical effect when administered once a day
  • Aceclofenac slow-release preparation providing an optimum pharmacological clinical effect when administered once a day
  • Aceclofenac slow-release preparation providing an optimum pharmacological clinical effect when administered once a day

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0071] To confirm the interaction and compatibility between aceclofenac and excipients, the following tests were performed:

[0072] After manually mixing 200 mg of aceclofenac with each excipient, an accelerated test was performed at room temperature for 1 hour, and the mixture was allowed to stand for 1 month in an atmosphere with a humidity of 75% for content testing and softening substance testing. The test results are shown in Table 1.

[0073] [Table 1]

[0074]

experiment example 2

[0076] The degree of solubilization of aceclofenac was measured by the following test method.

[0077] 20 mg of aceclofenac was dispersed in 40 ml of water and then dissolved by adding 10 mg of a solubilizing agent. The aceclofenac suspension was allowed to stand at room temperature for 24 hours and then filtered with a 0.45 μm membrane filter. Then, the filtrate was passed through HPLC to confirm the solubility and softening of aceclofenac. The results are shown in Table 2.

[0078] UV detector: Jasco UV-975

[0079] Wavelength: 282nm

[0080] Column: Haisil ODS 15cm*4.6mm

[0081] Mobile phase: -65%MeOH:35%0.02M Potassium dihydrogen phosphate

[0082] Flow rate: 1.0ml / min

[0083] Injection volume: 20μl

[0084] [Table 2]

[0085]

[0086] The results of adding aceclofenac to each excipient solution (mg / ml) (n=3, mean ± S.D.) for confirming the softening substance of aceclofenac are shown in Table 3.

[0087] [table 3]

[0088]

[0089] The % of related subst...

experiment example 3

[0091] Formation of the immediate-release layer portion was determined by measuring physical properties between aceclofenac and each excipient.

[0092] -testing method

[0093] A fluidity test, a hardness test, and a friability test were performed on a mixture prepared by mixing aceclofenac with each of the excipients and then mixed with a lubricant to select suitable excipients. The test results are shown in Table 4.

[0094] [Table 4]

[0095]

[0096]

[0097]

[0098]

[0099]

[0100]

[0101] According to the test results, in terms of physical properties, crospovidone and poloxamer are the most suitable disintegrants and solubilizers, respectively, and the ratio of these two components is most preferably 1.2:1 to 1.7:1. It can be noted that when these two ingredients are included beyond the above mentioned ratios, the formulation is not suitable in terms of dissolution rate.

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Abstract

Provided is a controlled-release preparation administered orally once a day that exhibits an optimum pharmacological clinical effect, prepared in the form of a bilayered tablet, a dual tablet, or a multilayered tablet including an immediate-release layer containing aceclofenac, a water-soluble additive, an insoluble additive, a solubilizer, a disintegrating agent and a filler, and a slow-release layer containing aceclofenac, a slow-release base, a disintegrating agent, a binder, a filler, a fluidizer, a solubilizer, and a lubricant.

Description

technical field [0001] The present invention relates to a sustained-release tablet for improved release of a desired drug, which exhibits improved solubilization and controlled release of insoluble components such as aceclofenac, diclofenac, or pharmaceutically acceptable salts thereof Almost linear release pattern and enhanced bioavailability due to improved dissolution rate, thus exhibiting the best pharmacological clinical effect when administered orally to patients. In particular, the present invention relates to a controlled-release oral preparation consisting of an immediate-release layer containing aceclofenac and a sustained-release layer that uniformly and meticulously controls drug release. [0002] The present invention improves the solubility of insoluble aceclofenac under acidic conditions (gastric juice) by adding a solubilizing agent, thus has rapid analgesic and anti-inflammatory effects, and uses polymers for controlled release to control the release of aceclo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/216A61K9/22A61K9/20A61K47/38A61P11/00
CPCA61K31/216A61K9/209A61P11/00
Inventor 李凡珍郑元台崔然雄南圭烈赵相珉张宰常崔珉智
Owner KOREA UNITED PHARMA
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