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Pharmaceutical composition comprising nebivolol with improved dissolution rate

A composition and drug technology, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of drug efficacy reduction, drug oral absorption effect and bioavailability reduction, etc., to reduce preparation costs , maintain pharmacological effect, constant pharmacological effect

Active Publication Date: 2018-08-28
ELYSON PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral absorption and bioavailability of the drug may be reduced when administered in a formulation that reduces the rate of dissolution of the drug, which can lead to reduced efficacy of the drug in the body

Method used

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  • Pharmaceutical composition comprising nebivolol with improved dissolution rate
  • Pharmaceutical composition comprising nebivolol with improved dissolution rate
  • Pharmaceutical composition comprising nebivolol with improved dissolution rate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0053] According to the composition shown in Table 1, Nebivolol hydrochloride was mixed with additives, and purified water with Tween-80 dissolved in it was added. The mixture is used to prepare granules according to the wet granulation method. Subsequently, magnesium oxide, magnesium carbonate or magnesium aluminum silicate and other additives as an alkalizing agent are post-mixed with the particles, and colloidal silica and magnesium stearate as lubricants are added thereto. The resultant was compressed into tablets (239.2 mg / tablet) using a tablet press (STP Machinery Co., Ltd., ZP198 Model) with a circular punch with a diameter of 8.6 mm.

[0054] Table 1 below shows the component content of each tablet.

[0055] [Table 1]

[0056]

Embodiment 4 and 5

[0058] According to the composition shown in Table 2, nebivolol hydrochloride was mixed with additives, and purified water was added thereto. The mixture is used to prepare granules according to the wet granulation method. Subsequently, magnesium oxide, magnesium carbonate, or magnesium aluminum silicate as an alkalizing agent and the remaining additives are post-mixed with the particles, and colloidal silica and magnesium stearate as lubricants are added thereto. The resultant was compressed into tablets (350.0 mg / tablet) using a tablet press (STPMachinery Co., Ltd., ZP198 Model) with a circular punch with a diameter of 10.0 mm.

Embodiment 6 and 7

[0060] According to the ingredients shown in Table 2, Nebivolol hydrochloride was mixed with additives, and a mixture of purified water and ethanol in which BHA and Tween-80 were dissolved was added. The mixture is used to prepare granules according to the wet granulation method. Subsequently, the rosuvastatin calcium, the magnesium aluminum silicate as the alkalizing agent and the remaining additives are post-mixed with the particles, and the colloidal silicon dioxide and magnesium stearate as the lubricant are added thereto. Using a tablet press (STPMachinery Co., Ltd., ZP198 Model) with a circular punch with a diameter of 10.0 mm or 7.5 mm, the resultant was compressed into tablets (350.0 mg / tablet: Example 6; 147.0 mg / tablet: implementation Example 7).

[0061] Film-coated tablets were prepared by spraying Opadry 03B28796 (Colorcon, Inc.) dissolved in 80% ethanol water to the tablets obtained above.

[0062] Table 2 below shows the component content of each tablet.

[0063] [T...

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Abstract

The present invention relates to a pharmaceutical composition comprising nebivolol with an improved dissolution rate and a preparation method thereof. The pharmaceutical composition, containing nebivolol or a pharmaceutically acceptable salt thereof, an alkalizing agent, and a pharmaceutically acceptable additive, for prevention or treatment of cardiovascular diseases, does not cause a decrease inthe dissolution rate of nebivolol and can significantly improve the dissolution rate, not only at low pH, such as pH 1.2, but also at a relatively high pH of 5 to 7, so that an improved therapeutic effect can be expected. In addition, the pharmaceutical composition can reduce the preparation cost since the micronization of nebivolol or the addition of a wetting agent is not required, and can minimize the occurrence of a deviation of bioavailability due to pre- or post-meal intake since there is little deviation of the dissolution rate due to the pH change, thereby maintaining a constant pharmaceutical action, and thus, the pharmaceutical composition is very useful in the preparation of a composite preparation containing a nebivolol preparation, or another active ingredient, such as rosuvastatin calcium.

Description

Technical field [0001] The invention relates to a pharmaceutical composition capable of improving the dissolution rate of nebivolol and a preparation method thereof. More specifically, the present invention relates to a pharmaceutical composition having an improved dissolution rate, which comprises nebivolol or a pharmaceutically acceptable salt thereof as an active ingredient, an alkalizing agent and a pharmaceutically acceptable additive. Background technique [0002] Beta-blockers are used to treat hypertension, angina pectoris, myocardial infarction, cardiac abnormalities, migraine or essential tremor. [0003] Nebivolol is a β-receptor blocker, which is a derivative of 2,2'-iminobisethanol shown in the following chemical structure 1, and has a centrosymmetric structure with four chiral centers. [0004] [Chemical Structure 1] [0005] [0006] Nebivolol is a mixture of D- and L-type enantiomers. It is a β-receptor blocker, highly selective for β1-adrenergic receptors, and has th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/02A61K31/352A61K31/505
CPCA61K47/02A61K31/352A61K31/505A61P9/00
Inventor 董乙瑗许泓九金海阳申惠卿朴孝珍朴相根
Owner ELYSON PHARM CO LTD
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