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Pharmaceutical composition comprising nebivolol with improved dissolution rate

A composition and drug technology, applied in the directions of medical preparations containing active ingredients, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of reduced drug efficacy, drug oral absorption effect and bioavailability, and reduce the preparation cost. , maintain the pharmacological effect, improve the effect of dissolution rate

Active Publication Date: 2021-07-30
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 dissolved with Tween-80 was added thereto. This mixture is used to prepare granules according to the wet granulation method. Subsequently, magnesium oxide, magnesium carbonate or magnesium aluminum silicate and the remaining additives are post-blended with the granules as alkalizing agents, and colloidal silicon dioxide and magnesium stearate are added as lubricants. The resultant was compressed into tablets (239.2 mg / tablet) using a tablet press machine (STP Machinery Co., Ltd., ZP198 Model) with a circular punch having a diameter of 8.6 mm.

[0054] Table 1 below shows the content of components per 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. This mixture is used to prepare granules according to the wet granulation method. Subsequently, magnesium oxide, magnesium carbonate or magnesium aluminum silicate and the remaining additives are post-blended with the granules as alkalizing agents, and colloidal silicon dioxide and magnesium stearate are added as lubricants. The resultant was compressed into tablets (350.0 mg / tablet) using a tablet press machine (STP Machinery Co., Ltd., ZP198 Model) with round punches having a diameter of 10.0 mm.

Embodiment 6 and 7

[0060] According to the composition 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 thereto. This mixture is used to prepare granules according to the wet granulation method. Subsequently, rosuvastatin calcium, magnesium aluminum silicate as an alkalizing agent and the remaining additives were post-blended with the granules, and colloidal silicon dioxide and magnesium stearate as lubricants were added thereto. 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 from the above obtained tablets by spraying Opadry 03B28796 (Colorcon, Inc.) dissolved in 80% ethanol water.

[0062] Table 2 below shows the content of components per tablet.

[0063] [Table 2]

[0064]

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Abstract

The invention relates to a pharmaceutical composition with improved nebivolol dissolution rate and a preparation method thereof. The pharmaceutical composition is used for preventing or treating cardiovascular diseases, and comprises nebivolol or a pharmaceutically acceptable salt thereof, an alkalinizing agent and a pharmaceutically acceptable additive, and the pharmaceutical composition does not reduce nebivolol However, the dissolution rate can be significantly improved not only at a low pH such as pH 1.2, but also at a relatively high pH of pH 5-7, so an improved therapeutic effect can be expected. In addition, since the pharmaceutical composition does not require micronized nebivolol and does not need to add a wetting agent, the pharmaceutical composition can reduce the preparation cost, and the dissolution rate deviation is small under the condition of pH change, and can make the biological The deviation of availability is minimized, thereby maintaining a constant pharmacological effect, and thus the pharmaceutical composition is very useful when preparing compound preparations containing nebivolol or other active ingredients such as rosuvastatin calcium.

Description

technical field [0001] The invention relates to a pharmaceutical composition with improved nebivolol dissolution rate and a preparation method thereof. More specifically, the present invention relates to a pharmaceutical composition having an improved dissolution rate, comprising 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 high blood pressure, angina pectoris, myocardial infarction, heart abnormalities, migraines, or essential tremor, among others. [0003] Nebivolol is a β-receptor blocker, which is a derivative of 2,2'-iminobisethanol shown in the following chemical structure formula 1, and has a centrosymmetric structure with four chiral centers. [0004] [Chemical Structural Formula 1] [0005] [0006] Nebivolol is a mixture of D- and L-enantiomers, it is a β-receptor blocker, highly selective for β1-adre...

Claims

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Application Information

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Patent Type & Authority Patents(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