A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis

Rhodomyrtone has indisputable and undeniable potential as a new antibiotic for antibiotic-resistant Gram-positive bacteria. Therefore, the main objective of this study was to determine the pharmacokinetics profiles of orally administered rhodomyrtone in rats. A reverse-phase HPLC-UV method was devel...

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Main Authors: Tan Suwandecha, Boon-Ek Yingyongnarongkul, Kanokkan Towtawin, Supayang Piyawan Voravuthikunchai, Somchai Sriwiriyajan
Format: Article
Language:English
Published: MDPI AG 2024-02-01
Series:Antibiotics
Subjects:
Online Access:https://www.mdpi.com/2079-6382/13/2/156
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author Tan Suwandecha
Boon-Ek Yingyongnarongkul
Kanokkan Towtawin
Supayang Piyawan Voravuthikunchai
Somchai Sriwiriyajan
author_facet Tan Suwandecha
Boon-Ek Yingyongnarongkul
Kanokkan Towtawin
Supayang Piyawan Voravuthikunchai
Somchai Sriwiriyajan
author_sort Tan Suwandecha
collection DOAJ
description Rhodomyrtone has indisputable and undeniable potential as a new antibiotic for antibiotic-resistant Gram-positive bacteria. Therefore, the main objective of this study was to determine the pharmacokinetics profiles of orally administered rhodomyrtone in rats. A reverse-phase HPLC-UV method was developed, optimized and validated for the analysis of rhodomyrtone concentrations in rat plasma. The retention time of papaverine and rhodomyrtone was 3.928 and 5.937 min, with no interference with the excipients used. The lower limit of quantification (LLOQ) of rhodomyrtone in the plasma sample was 0.04 μg/mL, the accuracy of rhodomyrtone at the LLOQ level ranged from 93.64 to 106.36%, precision was 6.59%, 80–120% for accuracy and <20% CV for precision. The calibration curve was linear at concentrations ranging from 0.04 to 128 µg/mL with a correlation coefficient (r) value of equal to or greater than 0.999. Sprague Dawley rats received a single dose of rhodomyrtone at 50 and 100 mg/kg. Blood samples were collected from tail veins. The peak plasma concentration was observed at 2 h, and the area under the curve of rhodomyrtone at 50 mg/kg and 100 mg/kg was 3.41 ± 1.04 and 7.82 ± 1.53 μg·h/mL, respectively. The results demonstrated linear pharmacokinetics characteristics at the studied dosage range. The plasma concentration of rhodomyrtone was above the minimal inhibition concentrations of several common pathogenic bacteria of medical importance. The proposed HPLC-UV method is fast, cost-effective, reliable and reproducible, and it is proposed for the routine analysis of rhodomyrtone.
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spelling doaj.art-377f66bffe804c96972e05dd271ce40c2024-02-23T15:05:06ZengMDPI AGAntibiotics2079-63822024-02-0113215610.3390/antibiotics13020156A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma AnalysisTan Suwandecha0Boon-Ek Yingyongnarongkul1Kanokkan Towtawin2Supayang Piyawan Voravuthikunchai3Somchai Sriwiriyajan4School of Pharmacy and Drug and Cosmetic Excellence Center, Walailak University, Thaiburi, Thasala District, Nakhon Si Thammarat 80160, ThailandDepartment of Chemistry and Center of Excellence for Innovation in Chemistry (PERCH-CIC), Faculty of Science, Ramkhamhaeng University, Bangkok 10240, ThailandDivision of Health and Applied Science, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, ThailandCenter of Antimicrobial Biomaterial Innovation-Southeast Asia and Natural Product Research Center of Excellence, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, ThailandDivision of Health and Applied Science, Faculty of Science, Prince of Songkla University, Hat Yai, Songkhla 90110, ThailandRhodomyrtone has indisputable and undeniable potential as a new antibiotic for antibiotic-resistant Gram-positive bacteria. Therefore, the main objective of this study was to determine the pharmacokinetics profiles of orally administered rhodomyrtone in rats. A reverse-phase HPLC-UV method was developed, optimized and validated for the analysis of rhodomyrtone concentrations in rat plasma. The retention time of papaverine and rhodomyrtone was 3.928 and 5.937 min, with no interference with the excipients used. The lower limit of quantification (LLOQ) of rhodomyrtone in the plasma sample was 0.04 μg/mL, the accuracy of rhodomyrtone at the LLOQ level ranged from 93.64 to 106.36%, precision was 6.59%, 80–120% for accuracy and <20% CV for precision. The calibration curve was linear at concentrations ranging from 0.04 to 128 µg/mL with a correlation coefficient (r) value of equal to or greater than 0.999. Sprague Dawley rats received a single dose of rhodomyrtone at 50 and 100 mg/kg. Blood samples were collected from tail veins. The peak plasma concentration was observed at 2 h, and the area under the curve of rhodomyrtone at 50 mg/kg and 100 mg/kg was 3.41 ± 1.04 and 7.82 ± 1.53 μg·h/mL, respectively. The results demonstrated linear pharmacokinetics characteristics at the studied dosage range. The plasma concentration of rhodomyrtone was above the minimal inhibition concentrations of several common pathogenic bacteria of medical importance. The proposed HPLC-UV method is fast, cost-effective, reliable and reproducible, and it is proposed for the routine analysis of rhodomyrtone.https://www.mdpi.com/2079-6382/13/2/156rhodomyrtoneantibioticspharmacokineticsHPLCmethod validation
spellingShingle Tan Suwandecha
Boon-Ek Yingyongnarongkul
Kanokkan Towtawin
Supayang Piyawan Voravuthikunchai
Somchai Sriwiriyajan
A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
Antibiotics
rhodomyrtone
antibiotics
pharmacokinetics
HPLC
method validation
title A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
title_full A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
title_fullStr A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
title_full_unstemmed A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
title_short A Novel Antibiotic, Rhodomyrtone: Pharmacokinetic Studies in a Murine Model and Optimization and Validation of High-Performance Liquid Chromatographic Method for Plasma Analysis
title_sort novel antibiotic rhodomyrtone pharmacokinetic studies in a murine model and optimization and validation of high performance liquid chromatographic method for plasma analysis
topic rhodomyrtone
antibiotics
pharmacokinetics
HPLC
method validation
url https://www.mdpi.com/2079-6382/13/2/156
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