scholarly journals Chemical and Toxicological Analysis of Antiretroviral Drugs

2019 ◽  
Vol 8 (4) ◽  
pp. 53-60
Author(s):  
T. N. Komarov ◽  
M. V. Belova ◽  
D. D. Stolyarova ◽  
I. E. Shohin ◽  
D. S. Bogdanova ◽  
...  
Keyword(s):  
Side Effects ◽  
Sample Preparation ◽  
Highly Active Antiretroviral Therapy ◽  
High Performance ◽  
Biological Fluids ◽  
Screening Method ◽  
Acute Poisoning ◽  
Antiretroviral Drugs ◽  
Precipitation Method ◽  
Relevant Today

Introduction. Human Immunodeficiency Virus (HIV) is one of the main socially significant infection all over the world. HIV-positive patients take medical care, including antiretroviral drugs (ARVs) pharmacotherapy. Like all drugs, ARVs have lots of side effects that should be taken when prescribing drugs as part of highly active antiretroviral therapy. There are many cases when side effects of ARVs caused patients to enter the toxicology department. Therefore, the development of new methods for the analysis of ARV in biological fluids for the timely diagnosis of treatment of poisoning of this group of drugs is relevant today.Aim. The aim of this study is development of screening analysis of atazanavir, abacavir, nevirapine, ritonavir, lopinavir, zidovudine, darunavir and efavirenz in the urine to identify these drugs as possible toxicants for poisoning by high-performance liquid chromatography with tandem massselective detection (HPLC-MS/MS).Materials and methods. Identification of ARV was performed by HPLC-MS/MS. Methanol precipitation method was used as a sample preparation.Results and discussion. The optimal conditions for sample preparation, chromatographic separation, and mass-spectrometric detection were selected to determine the studied ARVs. This method was tested on urine samples from patients in the Department of Acute Poisoning and Somatopsychiatric Disorders (OOSPD) with acute ARV poisoning.Conclusion. This screening method for analyse atazanavir, abacavir, nevirapine, ritonavir, lopinavir, zidovudine, darunavir and efavirenz in human urine has been developed by HPLC-MS/MS. The developed method can be used to identify these drugs as possible toxicants in case of poisoning. The prospect for the development of the topic is the inclusion of new molecules in the method and quantitative determination of the studied ARVs. 

Measurement of Dextropropoxyphene and Nordextropropoxyphene in Biological Fluids

1984 ◽  
Vol 3 (1_suppl) ◽  
pp. 103s-114S ◽  
Author(s):  
R.J. Flanagan ◽  
J.D. Ramsey ◽  
I. Jane
Keyword(s):  
Liquid Chromatography ◽  
High Performance ◽  
Solid Phase ◽  
Biological Fluids ◽  
Plasma Concentrations ◽  
Acute Poisoning ◽  
Oral Dosage ◽  
Gas Liquid Chromatography ◽  
Sensitivity And Selectivity ◽  
Plasma Metabolite

1 Detection, identification and measurement of dextropropoxyphene and its principal plasma metabolite, nordextropropoxyphene, can be important in the diagnosis of acute poisoning. 2 A combination of thin-layer chromatography (TLC) and gas-liquid chromatography (GLC) of solvent or solid-phase extracts of urine or gastric contents usually serves to detect these and many other compounds, and an homogeneous enzyme immunoassay (EMIT-DAU) is also available for dextropropoxyphene. 3 Measurement of dextropropoxyphene by GLC is complicated by the instability of this compound under certain conditions. However, a relatively polar stationary phase such as Carbowax 20M together with nitrogen-selective detection can give adequate sensitivity and selectivity for the measurement of the plasma concentrations attained after overdosage. 4 High-performance liquid chromatography (HPLC) has not been widely applied in the assay of dextropropoxyphene and nordextropropoxyphene since these compounds have no pronounced ultraviolet absorption or fluorescence spectra. However, electrochemical oxidation detection can be used with a silica column/non-aqueous ionic eluent system. This gives good selectivity and sensitivity, and can facilitate the measurement of both compounds in plasma specimens after single oral dosage.

Ultrafiltration-Based Sample Preparation for Pharmaceutical Analysis

2020 ◽  
Vol 16 ◽  
Author(s):  
Mustafa Çelebier
Keyword(s):  
Sample Preparation ◽  
Pharmaceutical Analysis ◽  
High Performance ◽  
Solid Phase ◽  
Biological Fluids ◽  
Total Concentration ◽  
Free Concentration ◽  
Pharmaceutical Ingredients ◽  
Matrix Components ◽  
Preparation Techniques

Abstract: Pharmaceutical analysis plays an important role in all steps of drug development processes. Analysis of active pharmaceutical ingredients in biological samples needs sample preparation techniques to prevent the signal of the analyte from interferences coming from matrix components. Ultrafiltration is a well-known technique used in food and pharmaceutical industry. Commercial ultrafiltration devices have been frequently used on proteomics and metabolomics studies for sample preparation. In pharmaceutical analysis, these devices have been employed to analyze free concentration of drugs in biological fluids after filtration. However, they have been rarely used to determine the total concentration of targeted compounds when it is compared with some other common sample preparation techniques. Ultrafiltration-based sample preparation might be used to clean-up the sample easily from matrix components especially on bioanalysis performed with high performance liquid chromatography (HPLC). In case of using protein precipitation agents on filtration procedure, the quantitative recovery of this non-selective unique technique is competitive with solid phase extraction

Therapy for HIV

2011 ◽  
Vol 23 (1) ◽  
pp. 23-27 ◽  
Author(s):  
B.S. Peters ◽  
K. Conway
Keyword(s):  
Side Effects ◽  
Highly Active Antiretroviral Therapy ◽  
Antiretroviral Drugs ◽  
New Drugs ◽  
Future Research ◽  
Strict Adherence ◽  
Highly Active ◽  
The Cost ◽  
Hiv Lipodystrophy

Initial therapies for HIV infection comprised nucleoside analogues, but as single or dual agents, they failed to prevent disease progression. When a new class of drug was introduced, the protease inhibitors, an effective triple therapy became possible—namely, highly active antiretroviral therapy, or HAART. HAART reduced viral replication almost completely and enabled immune system recovery. The probability of classical infections and tumors attributed to HIV were dramatically reduced, and life expectancy correspondingly increased. The initial disadvantages of HAART included the need for strict adherence to prevent drug resistance, the cost that initially precluded their widespread use in the developing world, and the short- and long-term side effects. One of the most disabling long-term complications was HIV lipodystrophy, which in extreme cases lead to severe peripheral fat wasting and central fat gain. In recent years, many of these disadvantages have been addressed: Once-daily drug combinations improve adherence; global access to HAART has been markedly improved; and new drugs enable patients to avoid many of the initial side effects. Future research will determine at what CD4 count HAART should be initiated, and new approaches such as immunotherapeutic HIV vaccines are being tested with the aim to delay or obviate the need for antiretroviral drugs.

Development and Characterization Colchicine-Loaded PEGylated Gelatin Nanoparticles for Targeted Delivery to Tumor

2013 ◽  
Vol 6 (2) ◽  
pp. 2058-2063
Author(s):  
G D Chandrethiya ◽  
P K Shelat ◽  
M N Zaveri
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
High Performance ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Spherical Particles ◽  
Precipitation Method ◽  
Antitumoral Activity ◽  
Gelatin Nanoparticles

PEGylated gelatin nanoparticles loaded with colchicine were prepared by ethanol precipitation method. Poly-(ethylene glycol)-5000-monomethylether (MPEG 5000), a hydrophilic polymer, was used to pegylate gelatin.  Gluteraldehyde was used as cross-linking agent. To obtain a high quality product, major formulation parameters were optimized.  Spherical particles with mean particles of 193 nm were measured by a Malvern particle size analyzer. Entrapment efficiency was found to be 71.7 ± 1.4% and determined with reverse phase high performance liquid charomatography (RP-HPLC). The in vitro drug release study was performed by dialysis bag method for a period of 168 hours. Lyophilizaton study showed sucrose at lower concentrations proved the best cryoprotectant for this formulation.  Stability study revealed that lyophilized nanoparticles were equally effective (p < 0.05) after one year of storage at 2-8°C with ambient humidity. In vitro antitumoral activity was accessed using the MCF-7 cell line by MTT assay.  The IC50 value was found to be 0.034 μg/ml for the prepared formulation. The results indicate that PEGylated gelatin nanoparticles could be utilized as a potential drug delivery for targeted drug delivery of tumors.  

Reversed-Phase High Performance Liquid Chromatographic Analysis of Three First Line Anti-Tuberculosis Drugs

2019 ◽  
Vol 69 (12) ◽  
pp. 3590-3592
Author(s):  
Nela Bibire ◽  
Romeo Iulian Olariu ◽  
Luminita Agoroaei ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Fluids ◽  
Gradient Elution ◽  
High Performance Liquid Chromatographic ◽  
Reversed Phase ◽  
Assay Method ◽  
Active Pharmaceutical Ingredients ◽  
First Line ◽  
Pharmaceutical Ingredients ◽  
Liquid Chromatographic

Active pharmaceutical ingredients such as isoniazid, pyrazinamide and rifampicin are among the most important first-line anti-tuberculosis drugs. A simple, rapid and sensitive reversed phase-high performance liquid chromatographic assay method for the simultaneous determination of isoniazid, pyrazinamide and rifampicin has been developed. Separation of the interest compounds was achieved in a 10 min chromatographic run in gradient elution mode on a Zorbax SB-C18 stainless steel column (150 � 4 mm, 5 mm) using a guard column containing the same stationary phase. The gradient elution was carried out with a mobile phase of 10% CH3CN aqueous solution for channel A and 50% CH3CN in pH = 6.8 phosphate buffer (20 mM), to which 1.5 mL triethylamine were added for channel B. Quantification of the analyzed substances was carried out spectrophotometrically at 269 nm. Detection limits of 0.48 mg/L for isoniazid, 0.52 mg/L for pyrazinamide and 0.48 mg/L for rifampicin were established for the developed assay method. The present work showed that the proposed analysis method was advantageous for simple and rapid analysis of the active pharmaceutical ingredients in pharmaceuticals and biological fluids.

An Overview of Antiretroviral Agents for Treating HIV Infection in Paediatric Population

2020 ◽  
Vol 27 (5) ◽  
pp. 760-794 ◽  
Author(s):  
Rita Melo ◽  
Agostinho Lemos ◽  
António J. Preto ◽  
Beatriz Bueschbell ◽  
Pedro Matos-Filipe ◽  
...  
Keyword(s):  
Hiv Infection ◽  
Reverse Transcriptase ◽  
Targeted Delivery ◽  
Highly Active Antiretroviral Therapy ◽  
Antiretroviral Drugs ◽  
Viral Reservoir ◽  
Reverse Transcriptase Inhibitors ◽  
Replication Process ◽  
Antiretroviral Agents ◽  
Multiple Drugs

Paediatric Acquired ImmunoDeficiency Syndrome (AIDS) is a life-threatening and infectious disease in which the Human Immunodeficiency Virus (HIV) is mainly transmitted through Mother-To- Child Transmission (MTCT) during pregnancy, labour and delivery, or breastfeeding. This review provides an overview of the distinct therapeutic alternatives to abolish the systemic viral replication in paediatric HIV-1 infection. Numerous classes of antiretroviral agents have emerged as therapeutic tools for downregulation of different steps in the HIV replication process. These classes encompass Non- Nucleoside Analogue Reverse Transcriptase Inhibitors (NNRTIs), Nucleoside/Nucleotide Analogue Reverse Transcriptase Inhibitors (NRTIs/NtRTIs), INtegrase Inhibitors (INIs), Protease Inhibitors (PIs), and Entry Inhibitors (EIs). Co-administration of certain antiretroviral drugs with Pharmacokinetic Enhancers (PEs) may boost the effectiveness of the primary therapeutic agent. The combination of multiple antiretroviral drug regimens (Highly Active AntiRetroviral Therapy - HAART) is currently the standard therapeutic approach for HIV infection. So far, the use of HAART offers the best opportunity for prolonged and maximal viral suppression, and preservation of the immune system upon HIV infection. Still, the frequent administration of high doses of multiple drugs, their inefficient ability to reach the viral reservoirs in adequate doses, the development of drug resistance, and the lack of patient compliance compromise the complete HIV elimination. The development of nanotechnology-based drug delivery systems may enable targeted delivery of antiretroviral agents to inaccessible viral reservoir sites at therapeutic concentrations. In addition, the application of Computer-Aided Drug Design (CADD) approaches has provided valuable tools for the development of anti-HIV drug candidates with favourable pharmacodynamics and pharmacokinetic properties.

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