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1.
J Pharm Biomed Anal ; 39(3-4): 801-4, 2005 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-15950425

RESUMO

In the present study, simultaneous quantification of stavudine (SV), lamivudine (LV) and nevirapine (NV) in tablets by UV spectroscopy, reverse phase HPLC (RP-HPLC) and HPTLC methods were developed. In the UV multi-component spectral method, SV, LV and NV was quantified at 266, 271 and 315 nm, respectively. In the RP-HPLC method, the drugs were resolved using a mobile phase of 20 mM sodium phosphate buffer (containing 8 mM 1-octanesulphonicacid sodium salt):acetonitrile (4:1, v/v) with pH adjusted to 3.5 using phosphoric acid on a C18-ODS-Hypersil (5 microm, 250 mm x 4.6 mm) column in isocratic mode. The retention time of SV, LV and NV was 2.85, 4.33 and 8.39 min, respectively. In the HPTLC method, the chromatograms were developed using a mobile phase of chloroform:methanol (9:1, v/v) on precoated plate of silica gel 60 F254 and quantified by densitometric absorbance mode at 265 nm. The Rf of SV, LV and NV were 0.21-0.27, 0.62-0.72 and 0.82-0.93, respectively. Recovery values of 99.16-101.89%, percentage relative standard deviation of <0.7 and correlation coefficient (linear dynamic range) of 0.9843-0.9999 shows that the developed methods were accurate and precise. These methods can be employed for the routine analysis of tablets containing SV, LV and NV.


Assuntos
Fármacos Anti-HIV/análise , Cromatografia Líquida de Alta Pressão/métodos , Lamivudina/análise , Nevirapina/análise , Espectrofotometria Ultravioleta/métodos , Estavudina/análise , Acetonitrilas/química , Fármacos Anti-HIV/química , Cromatografia em Camada Fina , Densitometria , Concentração de Íons de Hidrogênio , Lamivudina/química , Nevirapina/química , Ácidos Fosfóricos/química , Inibidores da Transcriptase Reversa/análise , Inibidores da Transcriptase Reversa/química , Sódio/química , Estavudina/química , Ácidos Sulfônicos/química , Comprimidos , Fatores de Tempo , Raios Ultravioleta
2.
Biol Pharm Bull ; 26(2): 188-93, 2003 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-12576678

RESUMO

In the present study, a new series of 2,6-diaryl-3-methyl-4-piperidones was synthesized by Mannich reaction (condensation) of ethyl-methyl ketone, substituted aromatic aldehydes and ammonium acetate. Oximes and thiosemicarbazone derivatives of 2,6-diaryl-3-methyl-4-piperidones were synthesized by reaction with hydroxylamine hydrochloride and thiosemicarbazide respectively. The chemical structures were confirmed by means of IR, 1H-, 13C-NMR and mass spectral data. The compounds were screened for acute toxicity, analgesic, local anaesthetic and antifungal activity. 2-(4-Methylphenyl)-3-methyl-6-(4-chlorophenyl)-piperidin-4-one 2 exhibited the highest analgesic and local anaesthetic activity. The oximes and thiosemicarbazones were completely devoid of analgesic and local anaesthetic activity. 2-(4-Methylphenyl)-3-methyl-6-(4-hydroxyphenyl)-piperidin-4-oxime 21 and 2-(4-methoxyphenyl)-3-methyl-6-(4-chlorophenyl)-piperidin-4-oxime 17 exhibited potent antifungal activity against Aspergillus niger. Antifungal activity against Candida albicans was observed only with 2-(4-dimethylaminophenyl)-3-methyl-6-(4-chlorophenyl)-piperidin-4-oxime 20. 2,6-Diaryl-3-methyl-4-piperidones did not exhibit antifungal property.


Assuntos
Piperidonas/síntese química , Piperidonas/farmacologia , Analgésicos/síntese química , Analgésicos/farmacologia , Anestésicos Locais/síntese química , Anestésicos Locais/farmacologia , Animais , Antifúngicos/síntese química , Antifúngicos/farmacologia , Camundongos , Medição da Dor/efeitos dos fármacos , Medição da Dor/métodos , Ranidae
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