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Pharmaceutical compositions comprising lobeglitazone for oral administration

A technology of lobeglitazone and composition, applied in the field of pharmaceutical compositions containing lobeglitazone, can solve the problems of reduced effect, limited utility, reduced proportion and the like

Active Publication Date: 2017-08-18
CHONG KUN DONG CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it does not make sense to increase the dissolution rate by using an excess of polymer or by using an excess of surfactant to prepare a solid dispersion to increase the dissolution rate, as its effect is significantly reduced due to the amount of dissolved poorly soluble drug compared to that of the surfactant. dose proportional reduction
[0014] In addition, it is possible to secure stability with a pH control agent by allowing a drug decomposed at a certain pH level to exist in a stable pH range where the drug cannot be decomposed, but its utility is very limited when considering various pH levels of the human body, and its application is mostly limited to liquid formulations

Method used

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  • Pharmaceutical compositions comprising lobeglitazone for oral administration
  • Pharmaceutical compositions comprising lobeglitazone for oral administration
  • Pharmaceutical compositions comprising lobeglitazone for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-4 and comparative example 1-4

[0057] Embodiment 1-4 and comparative example 1-4: the preparation of the tablet comprising lobeglitazone sulfate of the present invention

[0058] A pharmaceutical composition including lobeglitazone sulfate was prepared with the composition shown in Table 1 below.

[0059] 1) Active ingredient development

[0060] Lobeglitazone sulfate was triturated by using lactose hydrate (spray-dried) and mixed with croscarmellose sodium (Ac-di-sol, DMV-Fonterra Excipients GmBH, Germany).

[0061] 2) Preparation of binding solution

[0062]Blue No. 2 dye was added to purified water, and it was ground and stirred by a homogenizer (HG-150, Daihan Scientific). Povidone K-30 (Daebong LS, Korea) was added thereto, and the mixture was stirred and dissolved. Then, a binding solution was prepared by sieving through a 350-mesh sieve.

[0063] 3) Granule preparation

[0064] The mixture of 1) above and the binding solution of 2) above were put into a high-speed mixer (LFS-GS-2J, Fukae...

experiment example 1

[0071] Experimental Example 1: Measurement of Hardness and Friability of Prepared Tablets

[0072] The hardness, friability and angle of repose of the tablets obtained from Examples 1-4 and Comparative Examples 1-4 of the present invention were measured by the following methods, and the measurement results are shown in Table 2 below.

[0073] [measurement of hardness]

[0074] - Hardness tester: BH-225 (Pharmatest Apparatebau, GmbH, Germany)

[0075] -Measurement method: Calculate the average value of 10 cycle measurements

[0076] [Measurement of friability]

[0077] - Friability tester: SVM-102 (Pharmatest Apparatebau, GmbH, Germany)

[0078] - Measurement method: 20 tablets, friability is measured after 100 rotations

[0079] [Table 2]

[0080]

[0081] As shown in Table 2, when 10 wt% or more of the water-soluble cellulose derivative was included, the prepared tablet had high hardness and low friability. It was confirmed that Comparative Example 1 was insufficie...

experiment example 2

[0082] Experimental Example 2: Dissolution Test

[0083] The dissolution of the preparations obtained from Examples 1-4 and Comparative Examples 2-4 was tested according to the second method (paddle) of the dissolution test specified in the Korean Pharmacopoeia (10th edition) and analyzed by the following method. The results of the dissolution test are presented in Table 3 and figure 1 shown in .

[0084] [Method of Dissolution Test]

[0085] -Instrument: Hanson SR 8 (Hanson Research, U.S.A.)

[0086] -Dissolution medium: pH 1.2 medium 900mL

[0087] -Temperature of dissolution medium: 37±0.5°C

[0088] -Speed ​​speed: 50rpm

[0089] - Amount of sample: one piece per container

[0090] [Analysis method: Conditions of HPLC liquid chromatography]

[0091] - Detector: UV-Vis spectrometer (measured wavelength: 250nm)

[0092] - Column: X-Terra RP 18 (4.6 x 250mm, 5μm) or equivalent

[0093] -Mobile phase: 50mM ammonium nitrate (pH 5.0) buffer solution: acetonitrile=55:4...

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Abstract

The present invention relates to pharmaceutical compositions for oral administration comprising lobeglitazone. The pharmaceutical compositions of the present invention have excellent dissolution rate and express prompt pharmacological effects by comprising cellulose derivatives.

Description

[0001] 【Technical field】 [0002] The present invention relates to pharmaceutical compositions comprising lobeglitazone for oral administration having improved solubility and dissolution rate. [0003] 【Background technique】 [0004] Lobeglitazone is a drug in the glitazone series developed by Chong Kun Dang Pharmaceutical Corp., and it is the 20th new drug approved in Korea. Lobeglitazone is used as an orally administered antidiabetic agent and has an activity of improving insulin resistance. In particular, lobeglitazone is used as an agent for type 2 diabetes. In addition, lobeglitazone can be very useful for obese diabetic patients because lobeglitazone has no cardiovascular side effects that are found on existing drugs in the glitazone series, especially Rosiglitazone from GSK Controversy exists. [0005] As illustrated in Formula I below, lobeglitazone has a 2,4-thiazolidinedione moiety, and N-methylaminoethoxybenzyl acts as a linker to the 2,4-thiazolidinedione moiety ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/506A61K47/38A61P3/10A61P5/50
CPCA61K9/2018A61K9/2027A61K9/2054A61K31/506A61P5/50A61P3/10A61K9/0053A61K9/20A61K31/427A61K47/38
Inventor 郑大永申宅桓周珉载朴信政林宗来
Owner CHONG KUN DONG CORP
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