SUPRAMOLECULAR COMPLEX OF LAPPACONITINE HYDROBROMIDE AND THE MONOAMMONIUM SALT OF GLYCYRRHIZIC ACID: SYNTHESIS, PHYSICOCHEMICAL CHARACTERISTICS, AND ANTIARRHYTHMIC ACTIVITY

被引:2
|
作者
Ziyavitdinov, Zh F. [1 ]
Ishimov, U. Zh [1 ]
Berdiev, N. Sh [1 ]
Zhumaev, I. Z. [2 ]
Oshchepkova, Yu, I [1 ]
Usmanov, P. B. [2 ]
Salikhov, Sh, I [1 ]
机构
[1] Acad Sci Uzbek, AA Sadykov Inst Bioorgan Chem, 83 Mirzo Ulugbeka St, Tashkent 100125, Uzbekistan
[2] Natl Univ Uzbekistan, Inst Biophys & Biochem, 174 Talabalar St, Tashkent 100125, Uzbekistan
关键词
cardiovascular diseases; antiarrhythmic drugs; Allapinin (R); lappaconitine hydrobromide;
D O I
10.1007/s11094-022-02618-x
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The aim of the work was to create new dosage forms of lappaconitine hydrobromide characterized by a modified mechanism and nature of drug release and to study their specific activity on in vitro arrhythmia models in the papillary muscle of rat heart in comparison to the currently used drug Allapinin (R) (lappaconitine hydrobromide). Complexes of lappaconitine hydrobromide with the monoanunonium salt of glycyrrhizic acid (MASGA) in molar ratios of 1/2 and 1/4 were synthesized. The physicochemical characteristics of the obtained complexes were determined. Their biological activity was studied in comparison to Allapinin (R) with aconitine-induced arrhythmia in rats. The contractile activity of the papillary muscle disturbed by aconitine was restored by the 1/4 complex compound of lappaconitine hydrobromide with MASGA within 8 min after its introduction into the medium while a similar effect of the 1/2 complex and Allapinin (R) was observed after 10 and 15 min, respectively. Moreover, the restored contractile activity of the papillary muscle in the presence of the 1/4 complex was retained longer (130 min) as compared to Allapinin (R) (90 min). The obtained complex could be used to create a prolonged-action antiarrhythmic drug with improved properties.
引用
收藏
页码:167 / 173
页数:7
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