Characteristics, complexation and analytical methods of darunavir

What is it? Darunavir is a protease inhibitor used in the treatment of HIV infection. It is an important drug of therapy cocktail for patients infected with the virus. On the market there are darunavir ethanolate tablets of 75, 150, 300, 400, 600 and 800mg, because this is the most stable form. It is commercialized by Janssen-Cilag with the name PrezistaTM. Why we started? This drug has low water solubility and poor bioavailability, therefore requires administration in doses relatively high to the success of the therapeutic effect. The complexation of drugs by using cyclodextrin is welcome in this respect to improve the solubility and hence increase the dissolution rate of poorly soluble drugs. A monograph about this compound has not been described, thus it is an extremely important quality control of darunavir to demonstrate its effectiveness and safety. What we did? Some existing analytical techniques have been discussed in this manuscript, focusing on bioanalytical and pharmaceutical quality control applications. What we found? This review showed the published analytical methods reported for the determination of darunavir and discuss about its characteristics and complexation with cyclodextrin.

Validation of analytical methodology for quantification of cefazolin sodium by liquid chromatography

A reversed-phase high performance liquid chromatography method was validated for the determination of cefazolin sodium in lyophilized powder for solution for injection to be applied for quality control in pharmaceutical industry. The liquid chromatography method was conducted on a Zorbax Eclipse Plus C18 column (250 x 4.6 mm, 5 μm), maintained at room temperature. The mobile phase consisted of purified water: acetonitrile (60: 40 v/v), adjusted to pH 8 with triethylamine. The flow rate was of 0.5 mL min-1 and effluents were monitored at 270 nm. The retention time for cefazolin sodium was 3.6 min. The method proved to be linear (r2 =0.9999) over the concentration range of 30-80 µg mL-1. The selectivity of the method was proven through degradation studies. The method demonstrated satisfactory results for precision, accuracy, limits of detection and quantitation. The robustness of this method was evaluated using the Plackett–Burman fractional factorial experimental design with a matrix of 15 experiments and the statistical treatment proposed by Youden and Steiner. Finally, the proposed method could be also an advantageous option for the analysis of cefazolin sodium, contributing to improve the quality control and to assure the therapeutic efficacy

Development and validation of an economic, environmental friendly and stability-indicating analytical method for determination of ampicillin sodium for injection by RP-HPLC

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Development of an innovative, ecological and stability-indicating analytical method for semiquantitative analysis of ampicillin sodium for injection by thin layer chromatography (TLC)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

A critical review of analytical methods for determination of ertapenem sodium

Antimicrobials have unquestionable importance in the control of many diseases; however the constant concern with evolution of resistant microorganisms is increasing. The ertapenem sodium is a β-lactam antibiotic of the carbapenem class, which it has a broader activity spectrum than most other β-lactam antimicrobials, and is more resistant to the enzyme β-lactamase, which is the main mechanism of resistance of many bacteria. The progress of microbial resistance to existing antibiotics is alarming. Thus we need to preserve antimicrobials that still have activity against these pathogens. In this context, the quality control has a key role to ensure the correct dosage, by contributing preventively to minimize the development of resistant microorganisms. Study of the physicochemical characteristics of the drug and the quantification of the content of active substance are of fundamental importance for the pharmaceutical industry to ensure the quality of the product sold. This work presents a literature survey of existing methods for ertapenem sodium quantification which was performed. Ertapenem sodium can be analyzed by many types of assays; however the HPLC is the most used method. This review will examine the published analytical methods reported for determination of ertapenem sodium, in biological fluids and formulations.

Doxycycline hyclate: a review of properties, applications and analytical methods

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Analytical solution for transient one-dimensional couette flow considering constant and time-dependent pressure gradients

This paperaims to determine the velocity profile, in transient state, for a parallel incompressible flow known as Couette flow. The Navier-Stokes equations were applied upon this flow. Analytical solutions, based in Fourier series and integral transforms, were obtained for the one-dimensional transient Couette flow, taking into account constant and time-dependent pressure gradients acting on the fluid since the same instant when the plate starts it´s movement. Taking advantage of the orthogonality and superposition properties solutions were foundfor both considered cases. Considering a time-dependent pressure gradient, it was found a general solution for the Couette flow for a particular time function. It was found that the solution for a time-dependent pressure gradient includes the solutions for a zero pressure gradient and for a constant pressure gradient.

GIS-based analytical tools for transport planning: spatial regression models for transportation demand forecast

Considering the importance of spatial issues in transport planning, the main objective of this study was to analyze the results obtained from different approaches of spatial regression models. In the case of spatial autocorrelation, spatial dependence patterns should be incorporated in the models, since that dependence may affect the predictive power of these models. The results obtained with the spatial regression models were also compared with the results of a multiple linear regression model that is typically used in trips generation estimations. The findings support the hypothesis that the inclusion of spatial effects in regression models is important, since the best results were obtained with alternative models (spatial regression models or the ones with spatial variables included). This was observed in a case study carried out in the city of Porto Alegre, in the state of Rio Grande do Sul, Brazil, in the stages of specification and calibration of the models, with two distinct datasets.

Influences of the harvest season on analytical characteristics of syrah grapes and wines produced in the northeast region of Brazil

The present study evaluated the main physical and chemical characteristics of Syrah grapes, coming from the tropical region of São Francisco river valley, harvested at different times and their relationship with analytical characteristics of resulting wines. Grapes came from the first half of 2009 harvest, collected at Casa Nova - Bahia, a semi-arid and hot region, comprising an interval from 84 days after pruning (84 dap) to the beginning of grape over-ripening, 133 days after pruning (133 dap). Harvests at 84, 91, 98, 105, 112, 119, 126 and 133 dap, were analyzed for pH, soluble solids and acidity in grapes, which were then processed for wine production. Maximum sugar/acidity ratio (s/a = 56) were observed in grapes harvested between 126 and 133 dap, coincided with the highest concentration of anthocyanins (851 mg L-1 ) and total tannins (2.6 g L-1 ) in the resulting wines, indicating that grapes collected between 126 and 133 dap showed the best potential for winemaking in the tropical climate of São Francisco river valley. This result was confirmed by the analytical characterization of wines, that, between 126 and 133 dap, showed 12.8% alcohol, 31 g L-1 dry extract, 5.6 g L-1 ashes and a TPI of 58, using only one pumping per day, for 5 days maceration. Syrah grapes considered in the present work presented a good evolution of maturation, and grapes harvested between 126 and 133 days after pruning, showed the best oenological potential for the development of red wine. The use of pH and soluble solids appeared useful parameters in the estimation of maturation degree and quality potential of grapes for winemaking.