Desenvolvimento de cÃpsula gelatinosa mole de Ã-Lapachona para terapias antineoplÃsticas em humanos

AUTOR(ES)
DATA DE PUBLICAÇÃO

2004

RESUMO

The β-Lapachone (C15H14O3, MM 242,3), designated chemically as (3,4-dihydro-2,2- dimethyl-2H-naphtol[1,2-b]pyran-5,6-dione), is an o-naphtoquinone isolated from the lapacho tree (Tabebuia avellandae), of the family Bignonaceae. Recent researches have been demonstrating its excellent antineoplasic potential, acting against several types of human cancer by a peculiar apoptosis mechanism, especially the ones of very slow cellular cycle, as the case of some prostate lineages resistant to the conventional treatments. The development of a new pharmaceutical form leading to improved drug bioavailability, intending the accomplishment of clinical rehearsals in humans and proving the effectiveness of the β-Lapachone in antineoplasic therapies are subjects of great interest for the clinical oncology. This study proposed the development of β-Lapachone soft gelatin capsules, following the procedures and norms preconized by the Good Manufacturing Practices and Control, starting from a qualitative and quantitative planning of the excipients, regarding its incorporation in quimiotherapic treatment protocols. The initial stage consisted into the physicochemical characterization and pharmacotecnics of the active, proving the importance of obtaining a raw material with high degree of purity, without the presence of its isomer α-Lapachone. In this work a HPLC analytical methodology was developed and validated (column C18, mobile phase acetonitrile:acetic acid 0,25% (1:1), flow 2mL/min, detector λ 254nm), following the parameters described at the Resolution number 899 from ANVISA, which allows quantifying the raw material and the finished product, besides impurities and degradation products. Stability studies of the active demonstrated that the β-Lapachone suffers physical degradation in the presence of fluorescent light. Batch in semi-industrial scale are being accomplished for the optimization of the developed soft capsule formulation and stability of the product taking in account different involucres. After that, the transposition to the industrial scale will be performed

ASSUNTO(S)

β -lapachona -lapachone stability purificaÃÃo validaÃÃo por clae cÃpsula gelatinosa mole β purification validation for hplc soft gelatin capsules caracterizaÃÃo characterization estabilidade farmacia

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