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Pharmaceutical composition of pranlukast solid-dispersion with improved initial dissolution rate and the method of preparing the same

A technology of solid dispersion and composition, applied in the directions of drug combination, active ingredients of heterocyclic compounds, allergic diseases, etc., can solve the problems of sticking to gelatin, high drug elimination rate, and achieve the effect of Cmax improvement

Active Publication Date: 2008-10-08
SK CHEM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the present invention described above may have serious problems in that it may take a relatively long period of time to reach an effective concentration, and the maximum plasma concentration may be low because the elimination rate of the drug is higher than the absorption rate
Furthermore, the above-mentioned problem of water-soluble polymers sticking to gelatin cannot be solved even by using an excessive amount of disintegrant, which poses serious problems in the commercialization of such solid dispersions

Method used

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  • Pharmaceutical composition of pranlukast solid-dispersion with improved initial dissolution rate and the method of preparing the same
  • Pharmaceutical composition of pranlukast solid-dispersion with improved initial dissolution rate and the method of preparing the same
  • Pharmaceutical composition of pranlukast solid-dispersion with improved initial dissolution rate and the method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0028] Embodiment 1-3: Prepare the pharmaceutical composition of pranlukast solid dispersion by using anticoagulant

[0029] A solid dispersion of prankast was prepared by thermally melting solid prankast with crospovidone, which is a water-soluble polymer, and the solid dispersion of prankast thus prepared was verified by using XRD (X-ray Diffraction) The body is amorphous.

[0030] 6 g of the solid dispersion of pranlukast specified in Table 1 and 0.06 g of anticoagulant were mixed in a double-jacketed beaker at 60° C. for 30 minutes to prepare granules. The granules were cooled at room temperature and sieved through a 20-mesh sieve, thereby obtaining a granule pharmaceutical composition of pranlukast solid dispersion.

[0031] The pharmaceutical composition of pranlukast solid dispersion is thoroughly mixed with a lubricant and filled into capsules by using a manual capsule filling machine.

[0032] Table 1

[0033]

Embodiment 4-15

[0042] Embodiment 4-15: By using different amounts of anticoagulants to prepare the pharmaceutical composition of pranlukast solid dispersion

[0043] By mixing 1 g of the same pranlukast solid dispersion as in Examples 1-3 with an anticoagulant at 60° C. in the proportions specified in Table 3, followed by the same procedure as described in Examples 1-3 To prepare the granular pharmaceutical composition of pranlukast solid dispersion.

[0044] table 3

[0045]

experiment example 1

[0046] Experimental example 1: Measuring the dissolution rate over time

[0047] The commodity Onon in embodiment 1-15 and comparative example 1-4 and comparative example 5 Capsules prepared in Capsules were subjected to a dissolution test at a temperature of 37.5° C. in a dissolution medium of pH 6.8 with stirring at a speed of 50 rpm for 60 minutes. The time-dependent solubility was analyzed using HPLC, and the dissolution rate was calculated using Mathematical Formula 1 below, as provided in Table 4.

[0048] Mathematical formula 1

[0049]

[0050] Wherein C represents the weight (mg) of pranlukast in each capsule.

[0051] Table 4

[0052]

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Abstract

The present invention relates to a pharmaceutical composition of pranlukast solid-dispersion with an improved initial dissolution rate and the preparation method thereof. More particularly, it relates to a pharmaceutical composition of pranlukast solid-dispersion prepared by mixing pranlukast solid-dispersion and anticoagulation agent with a certain range of HLB at a elevated temperature, which can be further granulated and capsulated, thus enabling to improve initial dissolution rate of pranlukast by solving the serious problem of pranlukast solid-dispersion to stick to capsule walls and, to improve bioavailability because it shows superior Cmax and AUC based on the same administration dose, as comared to the commercial pharmaceutical composition of pranlukast formulated by conventional method, along with the preparation method thereof.

Description

technical field [0001] The present invention relates to a pharmaceutical composition of pranlukast solid dispersion with improved initial dissolution rate and a process for its preparation. More specifically, the present invention relates to the pharmaceutical composition and the preparation method thereof of the pranlukast solid dispersion prepared by mixing the prankast solid dispersion and the anticoagulant with a certain range of HLB at elevated temperature, which can be further This pharmaceutical composition is granulated and encapsulated, thereby being able to improve the initial dissolution rate of prankast by solving the serious problem that the solid dispersion of prankast sticks to the capsule wall, and to improve the bioavailability, because based on At the same administered dose, it exhibited better Cmax and AUC than commercial pranlukast pharmaceutical compositions formulated by conventional methods. [0002] Pranlukast, namely 4-oxo-8-[4-(4-phenylbutoxy)benzoyl...

Claims

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Application Information

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IPC IPC(8): A61K9/14
CPCA61K31/41A61K9/1641A61K9/2031A61P11/06A61P27/16A61P37/08A61P43/00A61K9/14A61K9/50
Inventor 吴畯教吴龙镐申昊喆严基安闵东铣金雄植郑知善
Owner SK CHEM CO LTD
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