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Pharmaceutical combination preparation comprising ezetimibe and losartan

A technology of ezetimibe and losartan, applied in the field of drug combination preparations, can solve the problems of reduced productivity and low particle fluidity, and achieve the effect of ensuring biological equivalence

Active Publication Date: 2021-12-03
HANMI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the flowability of the granules is low, there is a problem of reduced productivity during the manufacture of tablets and capsules

Method used

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  • Pharmaceutical combination preparation comprising ezetimibe and losartan
  • Pharmaceutical combination preparation comprising ezetimibe and losartan
  • Pharmaceutical combination preparation comprising ezetimibe and losartan

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Preparation of a bilayer tablet comprising ezetimibe and losartan

[0060] Coated bilayer tablets containing ezetimibe and losartan as active ingredients were prepared according to the composition shown in Table 1 below.

[0061] Specifically, ezetimibe was placed in a fluidized bed granulator together with lactose hydrate, microcrystalline cellulose, croscarmellose sodium and sodium lauryl sulfate and mixed for 3 minutes. To this was added a binder solution in which povidone was dissolved in water and the delivery pump was set to 2 rpm and combined for about 50 minutes of granulation. The resulting product was dried in a fluidized bed dryer at 45° C. and then sieved through a 0.6 mm mesh size to yield ezetimibe granules. At this time, the content of particles with a diameter greater than 250 μm in the ezetimibe particles was 5% by weight.

[0062] Losartan potassium was placed in a mixer with lactose hydrate, microcrystalline cellulose and crospovidone and...

Embodiment 2

[0065] Example 2: Preparation of a bilayer tablet comprising ezetimibe and losartan

[0066] A coated bilayer tablet containing ezetimibe and losartan as active ingredients was prepared in the same manner as in Example 1 according to the composition shown in Table 1 below.

Embodiment 3

[0067] Example 3: Preparation of capsules containing microtablets comprising ezetimibe and losartan

[0068] Capsules containing coated microtablets each containing ezetimibe and losartan as active ingredients were prepared according to the composition shown in Table 1 below.

[0069] Specifically, ezetimibe granules and losartan granules were prepared in the same manner as in Example 1. Microtablets containing losartan (303 mg / 30T) and microtablets containing ezetimibe (157 mg / 10T) (which are 2 mm in diameter and have a hardness of about 1.5 kp ). Microtablets containing losartan and microtablets containing ezetimibe were coated separately using a fluidized bed coater according to the coating formulation shown in Table 1, and filled to size 0 In hard capsules.

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Abstract

The present invention relates to a pharmaceutical combination preparation comprising ezetimibe and losartan. When the pharmaceutical combination preparation is dissolved in a solution of pH 4.0 to 5.0, the amount of losartan dissolved within 10 minutes is 5,700 (mu)g or less, and the amount of ezetimibe dissolved within 10 minutes is 270 (mu)g or more. Dissolution in the solution of pH 4.0 to 5.0 is carried out under conditions of a temperature of 37 DEG C and a paddle speed of 50 rpm in 500 mL of an acetic acid buffer, according to the United States Pharmacopeia, for a pharmaceutical combination preparation comprising 20 mg of ezetimibe and 183 mg of losartan.

Description

technical field [0001] The present invention relates to a pharmaceutical combination preparation comprising ezetimibe and losartan. More specifically, the present invention relates to pharmaceutical combination formulations comprising ezetimibe and losartan, wherein the dissolution rate between each drug is minimally affected. [0002] This application claims the benefit of priority based on Korean Patent Application No. 10-2019-0045295 filed on April 18, 2019, the entire contents of which are incorporated herein by reference. Background technique [0003] Losartan (losartan) is 2-butyl-4-chloro-1-[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl] - the common name for 1H-imidazole-5-methanol, and disclosed in U.S. Patent Nos. 5,608,075, 5,138,069, 5,153,197, etc., and in particular, losartan calcium is currently sold under the trade name commercially available. Losartan is used to treat hypertension and heart failure by blocking the binding of angiotensin II, a vasocons...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K9/20A61K47/12A61K47/20A61K31/397A61K31/4178A61K31/4422A61K31/505
CPCA61K31/4178A61K31/4422A61K31/505A61K31/397A61K9/2086A61K9/2866A61K9/2853A61K9/4808A61K9/2077A61K2300/00A61K9/209A61K9/2013A61K47/12A61K47/20
Inventor 曹赫俊金民旭林昊泽金用镒
Owner HANMI PHARMA
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