Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia)
Introduction. Allaforte® (JSC "Pharmcenter VILAR", Russia) is an antiarrhythmic long-acting drug. The dosage form of the drug Allaforte® provides a decrease in the frequency of taking the drug and also reduces the risk of side effects. It is relevant when taking antiarrhythmic drugs of the...
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LLC Center of Pharmaceutical Analytics (LLC «CPHA»)
2022-02-01
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| Series: | Разработка и регистрация лекарственных средств |
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| Online Access: | https://www.pharmjournal.ru/jour/article/view/1172 |
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| author | O. A. Archakova N. S. Bagaeva T. N. Komarov A. V. Rogov D. S. Shchelgacheva A. V. Suvorova P. K. Karnakova P. A. Karpova I. E. Shohin |
| author_facet | O. A. Archakova N. S. Bagaeva T. N. Komarov A. V. Rogov D. S. Shchelgacheva A. V. Suvorova P. K. Karnakova P. A. Karpova I. E. Shohin |
| author_sort | O. A. Archakova |
| collection | DOAJ |
| description | Introduction. Allaforte® (JSC "Pharmcenter VILAR", Russia) is an antiarrhythmic long-acting drug. The dosage form of the drug Allaforte® provides a decrease in the frequency of taking the drug and also reduces the risk of side effects. It is relevant when taking antiarrhythmic drugs of the IC class. However, the pharmacokinetics of this drug has not been studied on humans. Therefore, it is important to fully study the pharmacokinetics to ensure the maximum efficacy and safety of arrhythmia therapy.Aim. The aim is pharmacokinetics study of long-acting antiarrhythmic drug Allaforte® (JSC "Pharmcenter VILAR", Russia), 25 mg.Materials and methods. Concentration of lappaconitine and its active metabolite N-desacetyllappaconitine in human plasma determinates by high performance liquid chromatography with tandem mass-spectrometry. Pharmacokinetic parameters calculated by R Project 3.5.1 software (package «bear», version 2.8.3-2), originally created by Hsin-ya Lee and Yung-jin Lee, Taiwan.Results and discussion. Pharmacokinetic parameters of lappaconitine and N-desacetyllappaconitine were calculated. Averaged pharmacokinetic profiles (in linear and semi-log scale) of lappaconitine and N-desacetyllappaconitine after single administration under fasting were built. The means of the maximum concentrations (Cmax) determined in the blood plasma of volunteers after single administration Allaforte® are 5.09 ± 4.07 ng/ml for lappaconitine and 11.66 ± 6.21 ng/ml for N-deacetyllappaconitine (Mean ± SD). The peak time of the maximum concentrations (Tmax) is 4.43 ± 3.54 hours for lappaconitine and 4.04 ± 2.18 hours for N-deacetyllappaconitine. The means of the areas under the curve plasma concentration – time from 0 to 48 hours (AUC0-t) and under the curve plasma concentration–time from zero to infinity (AUC0-∞) of Allaforte® is 42.96 ± 34.48 ng ∙ h/ml and 71.24 ± 43.20 ng ∙ h/ml for lappaconitine; 167.42 ± 114.41 ng ∙ h/ml and 189.42 ± 115.20 ng ∙ h/ml for N-deacetyllappaconitine. Allaforte® was eliminated from blood plasma with means of terminal half-life (T1/2) 8.45 ± 5.10 hours for lappaconitine and 9.04 ± 2.57 hours for N-deacetyllappaconitine.Conclusion. Pharmacokinetics study of long-acting antiarrhythmic drug Allaforte® (JSC "Pharmcenter VILAR", Russia) after single administration was researched. Results of the study allows to conduct an effective therapy of arrhythmia by study drug and minimize side effects. |
| format | Article |
| id | doaj-art-23890b51eb3b49c4a095325e6cdb8f9f |
| institution | Matheson Library |
| issn | 2305-2066 2658-5049 |
| language | Russian |
| publishDate | 2022-02-01 |
| publisher | LLC Center of Pharmaceutical Analytics (LLC «CPHA») |
| record_format | Article |
| series | Разработка и регистрация лекарственных средств |
| spelling | doaj-art-23890b51eb3b49c4a095325e6cdb8f9f2025-08-03T19:23:57ZrusLLC Center of Pharmaceutical Analytics (LLC «CPHA»)Разработка и регистрация лекарственных средств2305-20662658-50492022-02-0111114014710.33380/2305-2066-2022-11-1-140-147946Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia)O. A. Archakova0N. S. Bagaeva1T. N. Komarov2A. V. Rogov3D. S. Shchelgacheva4A. V. Suvorova5P. K. Karnakova6P. A. Karpova7I. E. Shohin8LLC "CPHA"LLC "CPHA"LLC "CPHA"; National Research Nuclear University MEPhI (Moscow Engineering Physics Institute)JSC "Pharmcenter VILAR"LLC "CPHA"LLC "CPHA"LLC "CPHA"; I. M. Sechenov First MSMU of the Ministry of Health of the Russian Federation (Sechenov University)LLC "CPHA"; I. M. Sechenov First MSMU of the Ministry of Health of the Russian Federation (Sechenov University)LLC "CPHA"; National Research Nuclear University MEPhI (Moscow Engineering Physics Institute)Introduction. Allaforte® (JSC "Pharmcenter VILAR", Russia) is an antiarrhythmic long-acting drug. The dosage form of the drug Allaforte® provides a decrease in the frequency of taking the drug and also reduces the risk of side effects. It is relevant when taking antiarrhythmic drugs of the IC class. However, the pharmacokinetics of this drug has not been studied on humans. Therefore, it is important to fully study the pharmacokinetics to ensure the maximum efficacy and safety of arrhythmia therapy.Aim. The aim is pharmacokinetics study of long-acting antiarrhythmic drug Allaforte® (JSC "Pharmcenter VILAR", Russia), 25 mg.Materials and methods. Concentration of lappaconitine and its active metabolite N-desacetyllappaconitine in human plasma determinates by high performance liquid chromatography with tandem mass-spectrometry. Pharmacokinetic parameters calculated by R Project 3.5.1 software (package «bear», version 2.8.3-2), originally created by Hsin-ya Lee and Yung-jin Lee, Taiwan.Results and discussion. Pharmacokinetic parameters of lappaconitine and N-desacetyllappaconitine were calculated. Averaged pharmacokinetic profiles (in linear and semi-log scale) of lappaconitine and N-desacetyllappaconitine after single administration under fasting were built. The means of the maximum concentrations (Cmax) determined in the blood plasma of volunteers after single administration Allaforte® are 5.09 ± 4.07 ng/ml for lappaconitine and 11.66 ± 6.21 ng/ml for N-deacetyllappaconitine (Mean ± SD). The peak time of the maximum concentrations (Tmax) is 4.43 ± 3.54 hours for lappaconitine and 4.04 ± 2.18 hours for N-deacetyllappaconitine. The means of the areas under the curve plasma concentration – time from 0 to 48 hours (AUC0-t) and under the curve plasma concentration–time from zero to infinity (AUC0-∞) of Allaforte® is 42.96 ± 34.48 ng ∙ h/ml and 71.24 ± 43.20 ng ∙ h/ml for lappaconitine; 167.42 ± 114.41 ng ∙ h/ml and 189.42 ± 115.20 ng ∙ h/ml for N-deacetyllappaconitine. Allaforte® was eliminated from blood plasma with means of terminal half-life (T1/2) 8.45 ± 5.10 hours for lappaconitine and 9.04 ± 2.57 hours for N-deacetyllappaconitine.Conclusion. Pharmacokinetics study of long-acting antiarrhythmic drug Allaforte® (JSC "Pharmcenter VILAR", Russia) after single administration was researched. Results of the study allows to conduct an effective therapy of arrhythmia by study drug and minimize side effects.https://www.pharmjournal.ru/jour/article/view/1172lappaconitinen-desacetyllappaconitineallaforte®plasmapharmacokineticsarrhythmya |
| spellingShingle | O. A. Archakova N. S. Bagaeva T. N. Komarov A. V. Rogov D. S. Shchelgacheva A. V. Suvorova P. K. Karnakova P. A. Karpova I. E. Shohin Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) Разработка и регистрация лекарственных средств lappaconitine n-desacetyllappaconitine allaforte® plasma pharmacokinetics arrhythmya |
| title | Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) |
| title_full | Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) |
| title_fullStr | Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) |
| title_full_unstemmed | Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) |
| title_short | Pharmacokinetics Study of the Long-acting Antiarrhythmic Drug of Lappaconitine Hydrobromide (Allaforte®, JSC "Pharmcenter VILAR", Russia) |
| title_sort | pharmacokinetics study of the long acting antiarrhythmic drug of lappaconitine hydrobromide allaforte r jsc pharmcenter vilar russia |
| topic | lappaconitine n-desacetyllappaconitine allaforte® plasma pharmacokinetics arrhythmya |
| url | https://www.pharmjournal.ru/jour/article/view/1172 |
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