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1.
Pakistan Journal of Pharmaceutical Sciences. 2012; 25 (2): 429-433
em Inglês | IMEMR | ID: emr-128901

RESUMO

The surface activity of some non-steroidal anti-inflammatory agents like ibuprofen was investigated extensively. This fact has attracted the researchers to extend this behavior to other agents like piroxicam. Piroxicam molecules are expected to orient at the interface of oil and aqueous phase. The aim of this study was, firstly, to assess the surface and interfacial tension behaviour of newly synthesised palm oil esters and various pH phosphate buffers. Furthermore, the surface and interfacial tension activity of piroxicam was studied. All the measurements of surface and interfacial tension were made using the tensiometer. The study revealed that piroxicam has no effect on surface tension values of all pH phosphate buffers and palm oil esters. Similarly, various concentrations of piroxicam did not affect the interfacial tensions between the oil phase and the buffer phases. Accordingly, the interfacial tension values of all mixtures of oil and phosphate buffers were considerably high which indicates the immiscibility. It could be concluded that piroxicam has no surface activity. Additionally, there is no surface pressure activity of piroxicam at the interface of palm oil esters and phosphate buffers in the presence of Tweens and Spans


Assuntos
Proteínas Modificadoras da Atividade de Receptores , Óleos de Plantas , Soluções Tampão , Ésteres , Fosfatos
2.
Khartoum Pharmacy Journal. 2005; 8 (1): 9-13
em Inglês | IMEMR | ID: emr-72972

RESUMO

cytochrome P450s [CYPs] are members associated heme protein and hepatic microsomal enzymes, which play important role in drugs metabolism and detoxification. Seven of the 57 known human isoforms of P450s responsible for metabolism of more than 90% of the currently used drugs, CYP1A2, CYP2C9, CYP2C18, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. Some. of them, CYP2D6, CYP2C9 and CYP2C19, have been shown to be polymorphic as a result of single nuclcotide polymorphisms [SNPs], gene deletions, and gene duplications. The effect of the polymorphisms ranges from a complete loss of functional protein to an increase in enzyme activity and can impact the drug development and clinical application. Most pharmaceutical companies have increasingly screened out compounds that are metabolized solely by polymorphic CYPs. Retrospective studies showed that one of the major causes of the new chemical entities [NCE] failure to reach the clinical stage was related to pharmacokinetic and toxicological issues. Therefore the industry has invested in the science and technology of absorption, distribution, metabolism, excretion and toxicity [ADMET] in order to reduce NCE attribution rates.. Drug metabolism is the most important determinant of the ADMET of most compounds and the role CYP450 is predominant. Overall, current trends in the industry have been fueled by increased managed healthcare, the desire to minimize the need for therapeutic drug monitoring and CYP genotyping in medical practice, and a very competitive marketplace


Assuntos
Sistema Enzimático do Citocromo P-450/genética , Sistema Enzimático do Citocromo P-450/farmacocinética , Sistema Enzimático do Citocromo P-450/metabolismo , Inativação Metabólica/métodos , Inativação Metabólica/genética , Avaliação de Medicamentos , Preparações Farmacêuticas/metabolismo
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