Development studies of captopril certified reference material

Nogueira, Raquel Fernandes Pupo; Rego, Eliane Cristina Pires do; Sousa, Marcus V. B.; Wollinger, Wagner; Silva, Thaís Elias da; Moreira, Gabriela F.; Barin, Juliano Smanioto; Laporta, Lorenzo; Mesko, Márcia F.; Bittencourt, Celso Figueiredo; Rodrigues, Janaína Marques; Cunha, Valnei Smarçaro da

doi:10.1590/s1984-82502011000200015

Cited by 9 publications

(1 citation statement)

References 8 publications

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“…The thermal characteristic of pure captopril and F-optimized formula were shown in Figure 3. The differential scanning calorimetry thermogram of captopril indicates endothermic peak (T peak 103 to 107 °C) corresponding to its melting point, which is in agreement with values reported in the literature (Nogueira, Rego et al 2011). Moreover, this characteristic peak was retained in also the F-optimize formulation.…”

Section: Differential Scanning Calorimetrysupporting

confidence: 91%

Design and Optimization of Captopril Sublingual Tablets: Enhancement of Pharmacokinetic Parameters in Human

Kadry

Omar

Sherbiny

et al. 2016

Al-Azhar Journal of Pharmaceutical Sciences

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Oral mucous membrane of drug delivery is considered to be a promising alternative to the oral route. Sublingual route is a useful when rapid onset of action is desired than orally administered tablets. The objective of this study was to develop the sublingual tablet of captopril and improve its bioavailability. Captopril is the drug of choice in treatment of hypertension crisis or acute heart failure. Improvement of drug absorption and bioavailability was achieved by decreasing the pH of the mouth using citric acid. A 3 2 full factorial design was applied to optimize the formulations. Nine batches were prepared and evaluated to developing and optimizing sublingual tablets of water soluble drug (captopril). The optimization design was used to obtained the concentration of mixture superdisintegrants X 1 (crosscarmellose sodium, crosspovidone and sodium starch glycolate at 1:1:1 ratio) and using microcrystalline cellulose containing silicon dioxide (Prosolv-SMCC®) as a diluent (X 2 ). Disintegration time and t 90 values used as dependent variables for optimization to obtain the desirable optimized formula. According to the results, the selected variables have a strong influence on disintegration time and T 90 of captopril sublingual tablets. The lowest disintegration time (13.04 sec) and t 90 (2.78 min) were showed by sublingual formulations composed of 7.82 % of superdisintegrants combination (X 1 ) with 30.50 % of prosolv-SMCC (X 2 ). So, this formula was chosen as the optimized formula. The F-optimized formula was compared with the marketed tablet pharmaburst® formula. It is clear from the result that the F-optimize formula had a very significant lower disintegration time than Fpharmaburst (12.2 and 16.3 sec respectively), and t 90 (3.2 and 5.0 minute respectively). The pharmacokinetic parameter for the F-optimized showed a significant (P ≤ 0.05) increase in maximum plasma concentration from 180.0 to 286.5ng/mL, and a shortening of the time taken to reach maximum plasma concentration to 45 min in comparison with the marketed tablet. Finally, the F-optimize improved oral absorption of captopril sublingual and a subsequent acceleration of clinical effect, which is favored for hypertensive crises and cardiac disorders.

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Section: Differential Scanning Calorimetrysupporting

confidence: 91%

Design and Optimization of Captopril Sublingual Tablets: Enhancement of Pharmacokinetic Parameters in Human

Kadry

Omar

Sherbiny

et al. 2016

Al-Azhar Journal of Pharmaceutical Sciences

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Synthesis and characterization of octopamine sulfate, norfenefrine sulfate and etilefrine sulfate reference materials for doping control

Kalita,

Pawar,

Vernekar

et al. 2023

J of Chemical Tech & Biotech

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BACKGROUND: Doping is the use of prohibited substances by athletes to improve their performance. World Anti-Doping Agency (WADA)-accredited laboratories require various metabolite reference standards of the prohibited chemical substances or drugs for routine quality control. Therefore, it was proposed to develop efficient synthetic methodologies for highly pure reference materials of Phase II metabolites of octopamine, norfenefrine and etilefrine, which are prohibited in sports by WADA under the S6 stimulant category. The reference materials were characterized using various analytical techniques. New highperformance liquid chromatography with diode-array detection (HPLC-DAD) methods were developed for purity assessment.RESULTS: The synthesized Phase II metabolite reference standards, i.e. octopamine sulfate, norfenefrine sulfate and etilefrine sulfate, were confirmed by 1 H NMR, 13 C NMR, liquid chromatography-high-resolution mass spectrometry (LC-HRMS), attenuated total reflectance Fourier transform infrared and thermogravimetric analysis. In the LC-HRMS study, the mass error value of synthesized compounds was less than 10 ppm (error) which confirms the identity of the reference materials. New HPLC-DAD method were developed to ensure the purity of the reference materials. We used the HILIC column as metabolite reference standards are highly polar. The mobile phase was composed of water and acetonitrile in fixed composition. The HPLC-DAD purity of the developed reference materials was observed as 100%.CONCLUSION: We have developed reproducible synthetic routes for octopamine sulfate, norfenefrine sulfate and etilefrine sulfate, which are prohibited in sports by WADA. The synthesized metabolites were characterized using different advanced analytical techniques. These reference standards will be helpful to all WADA-accredited laboratories in routine anti-doping testing.

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Traceability of measurement results in chemistry: a case study of certification of three new pharmaceutical reference materials

et al. 2012

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Development studies of captopril certified reference material

Cited by 9 publications

References 8 publications

Design and Optimization of Captopril Sublingual Tablets: Enhancement of Pharmacokinetic Parameters in Human

Design and Optimization of Captopril Sublingual Tablets: Enhancement of Pharmacokinetic Parameters in Human

Synthesis and characterization of octopamine sulfate, norfenefrine sulfate and etilefrine sulfate reference materials for doping control

Traceability of measurement results in chemistry: a case study of certification of three new pharmaceutical reference materials

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