Preparation of pellets containing Pothomorphe umbellata extracts by extrusion-spheronization: improvement of 4-nerolidylcatechol photostability
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Data
2013-02
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Resumo
Pothomorphe umbellata (L.) Miq., Piperaceae, has been extensively used
in Brazilian folk medicine and it is well known for its strong antioxidant properties.
However, its main active constituent, 4-nerolydilcatechol (4-NC), is sensitive to
ultraviolet and visible light, which can limit the use of intermediate and final herbal
preparations of this species. In the present work, coated multiparticulate solid dosage
forms of P. umbellata were obtained with the purpose of increasing the stability
of 4-NC. P. umbellata extract was used as a wetting liquid for the preparation of
pellets by extrusion-spheronization. Pellets were coated in a fluidized bed by three
different polymers (hydroxypropylmethylcellulose (HPMC), polyvynilpirrolidone
K-30 (PVP-K30), and polyvinyl alcohol-polyethylene glycol graft-copolymer (PVA-
PEG)). 4-NC photostability was evaluated by an accelerated photostability protocol.
Pellets showed a narrow size distribution and low friability. 4-NC photodegradation
followed a second order degradation kinetics with similar k values for the percolate,
uncoated pellets and HPMC coated pellets. Photoprotection was higher in pellets
coated with PVP-K30 and PVA-PEG. PVA-PEG coated pellets with 6 and 9% weight
gain resulted in a final concentration of 4-NC approximately cinco times higher than
uncoated pellets or liquid extracts, suggesting the potential of this formulation as a
multiparticulate solid dosage form for P. umbellata extracts.
Descrição
Palavras-chave
Extrusion-spheronization, Film coating, Herbal extracts, Multiparticulate solid dosage forms, Nerolidylcatechol, Photostability
Citação
Araújo-Júnior, César Aparício de et al. Preparation of pellets containing Photomorphe umbellata extracts by extrusion-spheronization: improvement of 4-nerolidylcathecol photostability. Revista Brasileira de Farmacognosia, Curtiba, v. 23, n. 1, p. 169-174, Jan./Feb. 2013.