Modification of the Microtox® Basic Solid Phase Test: A new application for the ecotoxicological studies on poorly soluble antihypertensive drugs

Turek, Marika; Różycka‐Sokołowska, Ewa; Owsianik, Krzysztof; Marciniak, Bernard; Bałczewski, Piotr

doi:10.1016/j.jhazmat.2020.122839

Cited by 6 publications

(13 citation statements)

References 73 publications

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“…The investigated molar ratio of VAL and NIC fully corresponded to the recommended daily dosages of VAL, and taking into account the immunomodulatory properties of NIC and its preventive role in the treatment of lung tissue damage, it was suggested that this type of co-amorphous formulation could be used in supporting treatment of COVID-19. 186 An important achievement is the development of a coamorphous formulation of VAL with SACB 183 �this combination has so far been commercially offered in the form of a co-crystal. Liu et al obtained co-amorphous VAL/SACB (molar ratio 1:1), which were additionally cospray dried with lactose monohydrate and microcrystalline cellulose.…”

Section: Valsartan (Val)mentioning

confidence: 99%

“…The equilibrium solubility of the obtained co-amorphous products was even 24 times higher than that of VAL itself. The investigated molar ratio of VAL and NIC fully corresponded to the recommended daily dosages of VAL, and taking into account the immunomodulatory properties of NIC and its preventive role in the treatment of lung tissue damage, it was suggested that this type of co-amorphous formulation could be used in supporting treatment of COVID-19 …”

Section: Arb’s Co-amorphous Solidsmentioning

confidence: 99%

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New Perspectives for Antihypertensive Sartans as Components of Co-crystals and Co-amorphous Solids with Improved Properties and Multipurpose Activity

Turek,

Różycka-Sokołowska,

Owsianik

et al. 2023

Mol. Pharmaceutics

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Section: Valsartan (Val)mentioning

confidence: 99%

Section: Arb’s Co-amorphous Solidsmentioning

confidence: 99%

New Perspectives for Antihypertensive Sartans as Components of Co-crystals and Co-amorphous Solids with Improved Properties and Multipurpose Activity

Turek,

Różycka-Sokołowska,

Owsianik

et al. 2023

Mol. Pharmaceutics

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“…However, studies carried out in the city of Guarujá, São Paulo, Brazil, detected a signi cant amounts of losartan (3.6 ng/L -548.0 ng/L) showing that the compound may present moderate to severe risks for algae, crustaceans and sh (Roveri et al, 2020a). Losartan effects were evaluated through inhibition tests with aquatic plants (Lemna minor) (Godoy et al, 2015) and bacteria (Aliivibrio scheri) (Turek et al, 2020), but no signi cant toxic effects were observed. Losartan is present in urine in signi cant concentrations, around 35% (Guateque-Londoño et al, 2020), not being completely removed in WWTPs (Gurke et al, 2015).…”

Section: Ecological Risk Assessmentmentioning

confidence: 99%

First report on the occurrence of pharmaceuticals and cocaine in the coastal waters of Santa Catarina, Brazil, and its related ecological risk assessment

Pisetta

Roveri

Guimarães

et al. 2022

Environ Sci Pollut Res

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The worldwide occurrence of pharmaceuticals and personal care products (PPCPs) in aquatic ecosystems is reason for concern, since these emerging micro pollutants, includes a large and diverse group of organic compounds, with continuous input, high environmental persistence and potential threat to biota and human health. The aim of this study was to evaluate, for the rst time, the occurrence of twenty-seven PPCPs of various therapeutic classes (including cocaine and its primary metabolite, benzoylecgonine), in the coastal waters of Santa Catarina, southern Brazil. Water samples were taken in November 2020, during the low tide periods, at eight sampling points located along the coast of Santa Catarina, covering its entire geographical extension. Sampling was carried out in triplicate and at different depths of the water column. Nine compounds were detected through liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS): caffeine (12.58-119.80 ng/L), diclofenac (1.398-7.920 ng/L), losartan (0.432-3.200 ng/L), cocaine (0.0248-0.1686 ng/L) and benzoylecgonine (0.0146-1.094 ng/L) were quanti ed in 100% of the samples; carbamazepine (0.0242-0.2720 ng/L) was quanti ed in 75% of the samples; acetaminophen (0.212-10.040 ng/L) was quanti ed in 60% of the samples; and both atenolol (1.13-2.50 ng/L) and orphenadrine (0.073-0.0886 ng/L) were quanti ed in 25% of the samples. The other PPCPs were below the limit of detection (LOD). The highest occurrence of these compounds was detected in the northern and central coastal region of Santa Catarina, namely in Penha and Palhoça cities. The sources of these compounds may be associated with areas with high population density, awaited by tourism, with consequent production of sanitary sewage and solid waste. The ecological risk assessment of these substances in the aquatic ecosystems showed that 67% and 77% of the compounds respectively presented no ecological risk, acute and chronic, but 44% presented low to moderate risks for acute and chronic effects in the three trophic levels evaluated. The occurrence of these chemical compounds can imply deleterious effects on the environmental health of Santa Catarina coastal zone, and therefore deserve more acute and directed attention.

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“…Therefore, in our previous work, we paid attention to the occurrence of API–API, API–excipient, and excipient–excipient antagonistic/synergistic interactions based on the example of poorly soluble antihypertensive angiotensin II receptor blockers (ARBs) [ 10 ]. The study of these interactions was possible thanks to the developed modification of the standard Microtox ® Basic Solid Phase Test protocol, which allowed us to reliably assess the ecotoxicity of poorly soluble APIs in tests of both individual compounds and mixtures.…”

Section: Introductionmentioning

confidence: 99%

Can Pharmaceutical Excipients Threaten the Aquatic Environment? A Risk Assessment Based on the Microtox® Biotest

Turek,

Różycka-Sokołowska,

Koprowski

et al. 2023

Molecules

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The ecotoxicological impact of pharmaceuticals has received considerable attention, primarily focusing on active pharmaceutical ingredients (APIs) while largely neglecting the potential hazards posed by pharmaceutical excipients. Therefore, we analyzed the ecotoxicity of 16 commonly used pharmaceutical excipients, as well as 26 API–excipient and excipient–excipient mixtures utilizing the Microtox® test. In this way, we assessed the potential risks that pharmaceutical excipients, generally considered safe, might pose to the aquatic environment. We investigated both their individual ecotoxicity and their interactions with tablet ingredients using concentration addition (CA) and independent action (IA) models to shed light on the often-overlooked ecotoxicological consequences of these substances. The CA model gave a more accurate prediction of toxicity and should be recommended for modeling the toxicity of combinations of drugs with different effects. A challenge when studying the ecotoxicological impact of some pharmaceutical excipients is their poor water solubility, which hinders the use of standard aquatic ecotoxicity testing techniques. Therefore, we used a modification of the Microtox® Basic Solid Phase protocol developed for poorly soluble substances. The results obtained suggest the high toxicity of some excipients, i.e., SLS and meglumine, and confirm the occurrence of interactions between APIs and excipients. Through this research, we hope to foster a better understanding of the ecological impact of pharmaceutical excipients, prompting the development of risk assessment strategies within the pharmaceutical industry.

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Modification of the Microtox® Basic Solid Phase Test: A new application for the ecotoxicological studies on poorly soluble antihypertensive drugs

Cited by 6 publications

References 73 publications

New Perspectives for Antihypertensive Sartans as Components of Co-crystals and Co-amorphous Solids with Improved Properties and Multipurpose Activity

New Perspectives for Antihypertensive Sartans as Components of Co-crystals and Co-amorphous Solids with Improved Properties and Multipurpose Activity

First report on the occurrence of pharmaceuticals and cocaine in the coastal waters of Santa Catarina, Brazil, and its related ecological risk assessment

Can Pharmaceutical Excipients Threaten the Aquatic Environment? A Risk Assessment Based on the Microtox® Biotest

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