Determination of twelve antiretroviral agents in human plasma sample using reversed-phase high-performance liquid chromatography

Aymard, Guy; Legrand, Mayeule; Trichereau, N; Diquet, Bertrand

doi:10.1016/s0378-4347(00)00225-5

Cited by 184 publications

(113 citation statements)

References 47 publications

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“…Lamivudine (3TC), stavudine (d4T) and zidovudine (AZT) are some examples of nucleoside reverse transcriptase inhibitors for HIV (Human Immunodeficiency Virus) treatment (Aymard et al, 2000;Balint, 2001;Checa et al, 2005). Solubility data related to these antiretroviral drugs are scarce in the literature.…”

Section: Introductionmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

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Solubility and dissolution rate of drugs are of major importance in pre-formulation studies of pharmaceutical dosage forms. The solubility improvement allows the drugs to be potential biowaiver candidates and may be a good way to develop more dose-efficient formulations. Solubility behaviour of lamivudine, stavudine and zidovudine in individual solvents (under pH range of 1.2 to 7.5) was studied by equilibrium solubility and intrinsic dissolution methods. In solubility study by equilibrium method (shake-flask technique), known amounts of drug were added in each media until to reach saturation and the mixture was subjected to agitation of 150 rpm for 72 hours at 37 °C. In intrinsic dissolution test, known amount of each drug was compressed in the matrix of Wood's apparatus and subjected to dissolution in each media with agitation of 50 rpm at 37 °C. In solubility by equilibrium method, lamivudine and zidovudine can be considered as highly soluble drugs. Although stavudine present high solubility in pH 4.5, 6.8, 7.5 and water, the solubility determination in pH 1.2 was not possible due stability problems. Regarding to intrinsic dissolution, lamivudine and stavudine present high speed of dissolution. Considering a boundary value presented by Yu and colleagues (2004), all drugs studied present high solubility characteristics in intrinsic dissolution method. Based on the obtained results, intrinsic dissolution seems to be superior for solubility studies as an alternative method for biopharmaceutical classification purposes.Uniterms: Drugs/solubility. Drugs/dissolution rate. Intrinsic dissolution/method/biopharmaceutical classification. Biopharmaceutical Classification System.A solubilidade e a taxa de dissolução de fármacos são de grande importância em estudos de pré-formulação de formas farmacêuticas. A melhora na solubilidade permite que os fármacos sejam candidatos potenciais à bioisenção, podendo ser uma boa maneira para desenvolver formulações dose-eficientes. O comportamento de solubilidade da lamivudina, estavudina e zidovudina em solventes individuais (sob faixa de pH 1,2 a 7,5) foi estudado pelos métodos de solubilidade em equilíbrio e dissolução intrínseca. No estudo de solubilidade pelo método do equilíbrio (método de agitação de frascos), conhecidas quantidades do fármaco foram adicionadas em cada meio até atingirem a saturação e a mistura foi submetida à agitação de 150 rpm por 72 horas a 37 °C. No ensaio de dissolução intrínseca, conhecida quantidade de cada fármaco foi comprimida na matriz do aparato de Wood e submetida à dissolução em cada meio com agitação de 50 rpm a 37 °C. No método de solubilidade em equilíbrio, a lamivudina e a zidovudina podem ser consideradas como fármacos altamente solúveis. Embora a estavudina apresente alta solubilidade nos meios pH 4,5, 6,8, 7,5 e água, a determinação da solubilidade em pH 1,2 não foi possível devido a problemas de estabilidade. Com relação à dissolução intrínseca, a lamivudina e a estavudina apresentaram alta velocidade de dissolução. Considerando o valor ...

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Section: Introductionmentioning

confidence: 99%

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Dezani

Pereira

Caffaro

et al. 2013

Braz. J. Pharm. Sci.

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“…While indinavir does not affect early stages of the HIV replication cycle, it does interfere with the production of infectious HIV, limiting further infectious spread of the virus. In vitro studies indicate that the antiretroviral effects of HIV protease inhibitors and some NRTIs or Nonnucleoside reverse transcriptase inhibitors (NNRTIs) may be additive or synergistic (Burger et al, 1997;Aymard et al, 2000;Yamada et al, 2001;Justesen et al, 2003;Hurwitz, Schinazi, 2002;Chi et al, 2002;Rentsch, 2003). It is rapidly absorbed in the fasted state, with peak plasma concentration of 0.8 ± 0.3 hours (Lin, 1997;Yeh et al, 1999;Raffani, Haas, 2003).…”

Section: Introductionmentioning

confidence: 99%

Determination of indinavir in human plasma and its use in pharmacokinetic study

Gonçalves¹,

Pires²,

Bedor³

et al. 2007

Rev. Bras. Cienc. Farm.

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“…4,6,13,23 In 2006 Ramachandran et al 17 describes a bioanalytical method by HPLC with UV detection and application in 3 volunteers with 10 collected blood samples in different times after the administration of Efavirenz and did not show application of high-throughput samples.…”

Section: Discussionmentioning

confidence: 99%

“…This is because of its long half-life, which means effective concentrations are maintained for long periods. 3 Several methods are described in literature for the quantification of efavirenz in biological fluids by high performance liquid chromatography with ultraviolet detection (HPLC-UV), [4][5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22] HPLC with fluorescence detector, 23 liquid chromatography with mass spectrometry detection (LC-MS), 24 liquid chromatography with mass spectrometry in tandem detection(LC-MS/MS) [25][26][27][28][29] and matrix assisted laser desorption/ionization with time-of-flight in tandem detection (MALDI-TOF/ TOF). 30 When sample throughput is an important issue, such as in pharmacokinetic applications, the development of rugged methods with short analysis times becomes an important consideration.…”

Section: Introductionmentioning

confidence: 99%

A sensitive and robust lc-ms/ms method with monolithic column and electrospray ionization for the quantitation of efavirenz in human plasma: application to a bioequivalence study

Bedor¹,

Filho²,

Ramos³

et al. 2011

Quím. Nova

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Recebido em 12/7/10; aceito em 17/12/10; publicado na web em 25/3/11An LC-MS/MS method has been developed for the determination of efavirenz (EFZ) in human plasma using hydrochlorothiazide as internal standard (I.S.). An ESI negative mode with multiple reaction-monitoring was used monitoring the transitions m/z 313.88→69.24 (EFZ) and 296.02→204.76 (I.S.). Samples were extracted using liquid-liquid extraction. The total run time was 2.0 min. The separation was achieved with HPLC-RP using a monolithic column. The assay was linear in the concentration range of 100 -5000 ng mL -1 . The mean recovery was 83%. Intra-and inter-day precision were < 9.5% and < 8.9%, respectively and accuracy was in the range ± 8.33%. The method was successfully applied to a bioequivalence study.

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Determination of twelve antiretroviral agents in human plasma sample using reversed-phase high-performance liquid chromatography

Cited by 184 publications

References 47 publications

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Equilibrium solubility versus intrinsic dissolution: characterization of lamivudine, stavudine and zidovudine for BCS classification

Determination of indinavir in human plasma and its use in pharmacokinetic study

A sensitive and robust lc-ms/ms method with monolithic column and electrospray ionization for the quantitation of efavirenz in human plasma: application to a bioequivalence study

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