In the early stage of drug development the solubility of drug candidate is the most crucial physicochemical parameter to be defined for the selection of lead compound. Conventional shake flask method of solubility determination has now been replaced with more precise measurements like ultraviolet absorption, nephelometry, nuclear magnetic resonance and potentiometry. The development of a simple, rapid, sensitive and precise spectrophotometric method for the routine quantitative determination of samples will definitely reduce unnecessary tedious sample preparations and the cost of materials and labour. This article accounts for the measurement of solubility limit of few selected drugs by spectrophotometry using dilution technique. This has been done to optimize the method for rapid and convenient determination of drug solubility limit. Concentration of saturated solution of drug was determined from the absorbance versus concentration plots of various diluted solutions of drug as per Beer-Lambert law and was reported as drug solubility limit.

• MeSH
• indikátorové diluční techniky MeSH
• kofein analýza   chemie   MeSH
• oximy analýza   chemie   MeSH
• rozpouštědla MeSH
• rozpustnost * MeSH
• spektrofotometrie ultrafialová * MeSH
• takrin analýza   chemie   MeSH
• Publikační typ
• práce podpořená grantem MeSH

Two drugs were tested using electrochemical biosensor with immobilized acetylcholinesterase (AChE). The first was commercialized drug tacrine (known also as Cognex) used for treatment of cognitive manifestation of Alzheimer\'s disease (AD). The second one was its 7-methoxy derivate (7-MEOTA) that has not been marketed. We determined the IC50 (6.67+/-0.92)x10-7 M for tacrine and (1.66+/-1.43)x10-9 M for 7-MEOTA. In this in vitro study, 7-MEOTA acts as stronger inhibitor of AChE and in this way could be more favorable for treatment of cognitive manifestation of AD. Our study shows that biosensor technology could be used as a quick and cheap tool for testing of promising AChE inhibitors (AD drug candidates).

• MeSH
• acetylcholinesterasa chemie   MeSH
• algoritmy MeSH
• Alzheimerova nemoc farmakoterapie   MeSH
• biosenzitivní techniky MeSH
• cholinesterasové inhibitory analýza   MeSH
• elektrochemie MeSH
• enzymy imobilizované chemie   MeSH
• kinetika MeSH
• lidé MeSH
• nootropní látky analýza   MeSH
• takrin analogy a deriváty   analýza   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• práce podpořená grantem MeSH
• srovnávací studie MeSH