Abstract:
:Docetaxel (DTX) is an anti-cancer compound derived from 10-deacetyl baccatin III which is indicated for treatment of breast, lung, prostate, gastro-esophageal, and head and neck cancers. Epimerization of DTX at the C-7 hydroxyl position has intrigued chemists and has been implicated in loss of potency, as well as in the development of resistance in tumour cells. For localized controlled delivery of this agent, silicone films were prepared from a commercially available silicone kit. High levels of epimeric degradants were unexpectedly found in the in vitro release media. Herein, we discuss this anomalous DTX degradation to epimeric impurities, and discuss the possible reasons for degradation. Systematic stability studies were performed on the release media and the silicone kit components. It was found that release media and tin-based catalyst present in the silicone kit could be responsible for the epimeric conversion. This unusual case of chemical incompatibility can affect product performance and can even lead to development of resistance in tumour cells towards DTX.
journal_name
Drug Test Analjournal_title
Drug testing and analysisauthors
Mohsin S,Arellano IH,Choudhury NR,Garg Sdoi
10.1002/dta.1617subject
Has Abstractpub_date
2014-10-01 00:00:00pages
1076-84issue
10eissn
1942-7603issn
1942-7611journal_volume
6pub_type
杂志文章abstract::Inhibition of acetylcholinesterase (AChE) is the main mechanism of action of organophosphorus compounds (OP), and AChE reactivators (oximes) are at present the only causal therapeutic approach. Being the key target of OP toxicity, AChE may serve as a valuable tool for diagnosis of OP exposure as well as for the invest...
journal_title:Drug testing and analysis
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abstract::Increasing numbers of new psychoactive substances (NPS) among them fentanyl derivatives has been reported by the European monitoring centre for drugs and drug addiction (EMCDDA). Butyrfentanyl is a new fentanyl derivative whose potency ratio was found to be seven compared to morphine and 0.13 compared to fentanyl. Sev...
journal_title:Drug testing and analysis
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abstract::Formestane (4-hydroxy-androstenedione) is an aromatase inhibitor prohibited in sports and included, since 2004, in the list of prohibited substances updated yearly by the World Anti-Doping Agency (WADA). Since the endogenous production of formestane has been described, it is mandatory for the anti-doping laboratories ...
journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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abstract::Hemp nuts are mature cannabis seeds obtained after shelling and that are commonly used in traditional Chinese medicine for treating functional constipation. In this work, we screened hemp nut products, classified them, and verified the legality of consuming them. A total of 18 products were purchased from Taiwan, Chin...
journal_title:Drug testing and analysis
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abstract::Indole-, indazole-, or azaindole-based synthetic cannabinoids (SCs), bearing a cumyl substituent are a widespread, recreationally used subgroup of new psychoactive substances (NPS). The latest cumyl-derivative, CUMYL-PEGACLONE, emerged in December 2016 on the German drug market. The substance features a novel γ-carbol...
journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 杂志文章
doi:10.1002/dta.409
更新日期:2012-07-01 00:00:00
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 杂志文章
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更新日期:2018-02-18 00:00:00
abstract::'All scientific work is incomplete-whether it be observational or experimental. All scientific work is liable to be upset or modified by advancing knowledge. That does not confer upon us a freedom to ignore the knowledge we already have, or to postpone the action that it appears to demand at a given time.' ...
journal_title:Drug testing and analysis
pub_type: 杂志文章
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journal_title:Drug testing and analysis
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abstract::Drug and alcohol abuse is a concern for many European companies, especially those having safety-critical jobs. It is not uncommon for European companies to establish a drug policy with little or no provision for drug testing. The European Union (EU) has launched a number of initiatives in its fight against drugs. Ther...
journal_title:Drug testing and analysis
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更新日期:2010-08-01 00:00:00
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 杂志文章
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abstract::Sulfate metabolites have been described as long-term metabolites for some anabolic androgenic steroids (AAS). 4-chlorometandienone (4Cl-MTD) is one of the most frequently detected AAS in sports drug testing and it is commonly detected by monitoring metabolites excreted free or conjugated with glucuronic acid. Sulfatio...
journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 杂志文章
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journal_title:Drug testing and analysis
pub_type: 杂志文章
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更新日期:2015-08-01 00:00:00
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 杂志文章
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journal_title:Drug testing and analysis
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journal_title:Drug testing and analysis
pub_type: 信件
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