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Use of (s) - esmolol for controlling venous irritation associated with the treatment of a cardiac disorder

一种刺激性、用途的技术，应用在心血管系统疾病、酯类有效成分、退热药等方向，能够解决降低应激患者心率等问题

Inactive Publication Date: 2013-10-09
BAXTER INT INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the higher infusion concentrations required to reduce heart rate in stressed patients cannot usually be used due to concerns that significant venous irritation may occur
As a result, effective esmolol HCl administration often takes longer than it would if administered at higher infusion concentrations

Method used

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  • Use of (s) - esmolol for controlling venous irritation associated with the treatment of a cardiac disorder
  • Use of (s) - esmolol for controlling venous irritation associated with the treatment of a cardiac disorder
  • Use of (s) - esmolol for controlling venous irritation associated with the treatment of a cardiac disorder

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] The rabbit ear vein irritation test was used to evaluate the relative potential of the following compositions to cause venous irritation in human patients: (i) containing 3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenyl The composition of the racemic mixture of methyl propionate hydrochloride ("racemate" in Table 1), and (ii) containing (S)-3-[4-(2-hydroxy-3-isopropyl) (R)-3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionate hydrochloride Composition of acid methyl ester hydrochloride ("S-isomer" in Table 1). The choice of rabbit as the test system is based on the established knowledge that it can be accepted for vascular stimulation research. Hessov and Bojen- , Europ J Intens Care Med, 2:97-101 (1976); Hessov et al., Intens Care Med, 5:79-81 (1979); Johnson et al., J Oral Maxil Surg, 47:819-822 (1989); Hoover Et al. Fundam Appl Toxicol, 14:589-597 (1990). The rabbit model may be more sensitive than humans, but nonetheless is still suitable for therapeutic conce...

Embodiment 2

[0105] The study described in Example 1 was extended to evaluate the relative potential of the following compositions to cause venous irritation in human patients: (i) containing 3-[4-(2-hydroxy-3-isopropylamino)propoxy] The composition of the racemic mixture of phenylpropionic acid methyl ester hydrochloride ("racemate" in Table 1), and (ii) containing 88mg / mL or 133mg / mL(S)-3-[4-( 2-hydroxy-3-isopropylamino)propoxy]phenylpropionic acid methyl ester hydrochloride and substantially free of (R)-3-[4-(2-hydroxy-3-isopropylamino) ) Composition of propoxy]phenylpropionic acid methyl ester hydrochloride ("S-isomer" in Table 1).

[0106] Sixteen 15-week-old female New Zealand white rabbits weighing in the range of 2–3 kg were tested. The rabbits are reported to be free of specific pathogens, as determined by serological, bacteriological and parasitological tests. Upon arrival, the animals were quarantined for 7 days. Only rabbits showing no signs of clinical disease were used in thi...

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Abstract

A pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3- isopropylamino) propoxy] phenylpropionate in a concentration between about 75 mM and about 150 mM, which is substantially free of the R-isomer or pharmaceutically acceptable salt thereof, is provided. A method of treating a cardiac disorder is also provided and includes administering to a subject in need thereof a therapeutically effective amount of a pharmaceutical composition comprising (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy] phenylpropionate hydrochloride, wherein the (S)-methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy] phenylpropionate hydrochloride is present at a concentration between about 75 mM and about 150 mM and wherein the pharmaceutical composition is substantially free of (R)-methyl-3-[4-(2-hydroxy-3-isopropylamino) propoxy] phenylpropionate or pharmaceutically acceptable salt thereof.

Description

[0001] Cross reference with related applications [0002] The benefits of U.S. Provisional Patent Application Serial No. 61 / 436,995 filed on January 27, 2011 under 35 U.S.C. §119(e) are hereby claimed, and the entire disclosure of the provisional application is hereby incorporated by reference. Technical field [0003] The present invention relates to a composition and method for treating heart disorders while minimizing venous stimulation, the method comprising administering a therapeutically effective amount of a pharmaceutical composition comprising the S-isomer of esmolol. Background technique [0004] Esmolol hydrochloride (3-[4-(2-hydroxy-3-isopropylamino)propoxy]phenylpropionic acid methyl ester hydrochloride) is S- and R-isomers 50:50 racemic mixture. Esmolol hydrochloride is a fast-acting beta-blocker used to treat heart diseases such as tachycardia and hypertension. Most currently available beta-blockers have a relatively long onset time. However, in clinical care situa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/24A61P9/06
CPCA61K31/24A61P9/00A61P9/04A61P9/06A61P9/12A61P29/00A61P43/00
Inventor 杰罗姆·H·盖斯杰夫·麦基巴莱特·拉比诺
Owner BAXTER INT INC
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