Stability-indicating thin-layer chromatographic method for determination of darunavir in complex darunavir–β-cyclodextrin in the presence of its degradation products

Kogawa, Ana Carolina; Mendonça, Jacqueline Nakau; Lopes, Norberto Peporine; Salgado, Hérida Regina Nunes

doi:10.1039/c4ay00248b

Cited by 9 publications

(3 citation statements)

References 6 publications

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“…Method by Thin Layer Chromatography (TLC) and High-Performance Liquid Chromatography (HPLC) were developed for the identification and quantification of darunavir in the darunavir: β-cyclodextrin complex [20,21]. These methods were also able to identify degradation products of the complex, being considered methods indicative of stability.…”

Section: Methodsmentioning

confidence: 99%

Drug Optimization: Fighting Research to Achieve the Greatest Use of Darunavir

Kogawa¹,

Salgado²

2016

SM Anal Bioanal Technique

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Acquired Immunodeficiency Syndrome (AIDS) is the final stage of the disease caused by Human Immunodeficiency Virus (HIV). It attacks the defense cells of the body, leaving the body vulnerable to all kinds of diseases [1-3].Currently, treatment of HIV infection relies on the called Highly Active Antiretroviral Therapy (HAART) which proposes the combination of several drugs in a daily regimen [1,[4][5][6][7][8][9]. Therapeutic agents are divided according to their mechanism of action. Darunavir belongs to protease inhibitors such as atazanavir, fosamprenavir, indinavir, lopinavir/ritonavir, ritonavir, saquinavir, tipranavir [1,[10][11][12][13][14][15]. Darunavir: β-CyclodextrinDarunavir, an antiretroviral drug, has low solubility in water and requires administration in high doses [16,17]. So, it was complexed with β-cyclodextrin [18]. The complex has been studied and compared to free darunavir. CharacterizationDarunavir: β-cyclodextrin complex, by spectrophotometry in the infrared region, shows bands present in the free darunavir and other characteristic bands from complexation [19].The thermal studies, by thermogravimetry and differential scanning calorimetry with heat flux showed that the darunavir: β-cyclodextrin complex has a higher thermal stability than the free drug and also has characteristic behavior [19].The darunavir: β-cyclodextrin complex, by X-ray diffraction, shows crystalline form [19].These techniques can identify darunavir: β-cyclodextrin complex safely and effectively. SolubilityThe solubility of the darunavir: β-cyclodextrin complex was studied and the results were impressive and significant for science and for public health. The darunavir: β-cyclodextrin complex presented solubility 28 times higher than free darunavir in acetate buffer 0.05 M at pH 4.5, 23 times in water purified and 22 times in phosphate buffer 0.2 M at pH 6.8 [16].This study allows the use of smaller doses of the drug and therefore adverse effects are less frequent. This advantage for patients with AIDS is a great advance, since they are bodies debilitated by the virus and administer many medications daily. Analytical methodsMethod by Thin Layer Chromatography (TLC) and High-Performance Liquid Chromatography (HPLC) were developed for the identification and quantification of darunavir in the darunavir: β-cyclodextrin complex [20,21]. These methods were also able to identify degradation products of the complex, being considered methods indicative of stability.

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Section: Methodsmentioning

confidence: 99%

Drug Optimization: Fighting Research to Achieve the Greatest Use of Darunavir

Kogawa¹,

Salgado²

2016

SM Anal Bioanal Technique

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“…A simple HPLC method has been developed for the determination of 4-amino-N-(2-methyl propyl)benzene sulphonamide impurity from bulk darunavir [23], another selective RP-HPLC method was developed for the separation and quantification of darunavir from its process related substances [24]. A simple, selective and inexpensive stability-indicating thinlayer chromatographic (TLC) method was developed for the determination of darunavir in presence of darunavir-β-cyclodextrin complex and its degradation products [25]. Unfortunately, high detection levels and low separation efficiency are the disadvantages of reported HPLC methods.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of a selective, sensitive and stability indicating UPLC–MS/MS method for rapid, simultaneous determination of six process related impurities in darunavir drug substance

Reddy

Yusop

Aris

et al. 2016

Journal of Pharmaceutical and Biomedical Analysis

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“…The official specification for the doxycycline hyclate present in dosage form is from 95.0% to 105.0% [6]. However, HPLC demands expensive equipment and columns, organic solvents in the preparation of solutions and/or mobile phases and the analysis time is longer than the carried out on Infrared spectroscopy or Ultraviolet spectrophotometric or Thin layer chromatography [13], which generates a greater time spent by analysts in performing the test and the lower logistics of equipment usage [1].…”

Section: Introductionmentioning

confidence: 99%

Quantification of Doxycycline in Raw Material by an Eco-Friendly Method of Infrared Spectroscopy

Kogawa¹,

Mello²

2015

Pharm Anal Acta

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Doxycycline is a broad spectrum antibiotic used in the treatment of infectious diseases in humans and animals. It is distributed free of charge, by medical prescription, in Brazil through the public health system. Thus, since a considerable number of people have access to this drug, it is of great interest to control its quality. The purpose of the research was the development and validation of an eco-friendly method by Fourier-Transform Infrared (FT-IR) transmission spectroscopy for the determination of doxycycline in raw material. The raw material quality directly determines the quality of the drug. Through this analysis the method was completely validated according to the International Conference on Harmonization guidelines, showing accuracy, precision, selectivity, robustness and linearity. It was linear over the concentration range of 0.5-2.5 mg with correlation coefficient 0.9991 and limits of detection and quantification of 0.125 and 0.378 mg, respectively. Fourier-Transform Infrared (FT-IR) transmission spectroscopy method is considered environmentally friendly because it uses only the potassium bromide as reagent, which is cheap and safe for the operator, does not expose the operator to toxic solvents or harmful reagents, and optimizes equipment for being a rapid analysis. The validated method is useful to the routine quality control of doxycycline.

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Stability-indicating thin-layer chromatographic method for determination of darunavir in complex darunavir–β-cyclodextrin in the presence of its degradation products

Abstract: A method was developed to identify degradation products of the complex darunavir–β-cyclodextrin.

Cited by 9 publications

References 6 publications

Drug Optimization: Fighting Research to Achieve the Greatest Use of Darunavir

Drug Optimization: Fighting Research to Achieve the Greatest Use of Darunavir

Development and validation of a selective, sensitive and stability indicating UPLC–MS/MS method for rapid, simultaneous determination of six process related impurities in darunavir drug substance

Quantification of Doxycycline in Raw Material by an Eco-Friendly Method of Infrared Spectroscopy

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