Desenvolvimento e avaliação de pellets contendo extrato de Pothomorphe umbellata (pariparoba) via extrusão esferonização
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2011-08-31
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Universidade Federal de Goiás
Resumo
Pothomorphe umbellata (L.) Miq. Piperaceae is known in Brazil as "caapeba", "caapeba
North" or "Pariparoba" being widely used as an analgesic, anti-inflammatory and antispasmodic.
According to scientific studies, 4-nerolidylcatechol (4-CN) is the main secondary
metabolite of P. umbellata, has antioxidant activity greater than that of vitamin E. The
incorporation of the extracts of P. umbellata (L.) Miq. in solid dosage forms is an interesting
strategy to enable its use as an oral antioxidant and stabilizing its active labile 4-NC. Pellets
are oral dosage forms which have good flow properties due to their spherical shape, narrow
size distribution, in addition, the pellets allow to obtain uniform dispersion of doses of drug
and incorporation of large amounts of active substances incompatible in the same
pharmaceutical form. The objective of this study was to obtain an extract of P. umbellata,
develop and characterize a multi-particulate solid dosage form and evaluate the stability of
the developed formulations containing 4-NC. The roots of the plant material of P. umbellata
was subjected to analysis of content, residual moisture, determination of swelling index, total
ash content and granulometric determination. The identification of plant constituents of the
sample was made by thin layer chromatography (TLC). Obtaining the hydroalcoholic extract
was made by percolation. Quantitation of 4-NC was performed by High Performance Liquid
Chromatography (HPLC-UV-Vis). The analytical method was validated for the parameters
required in Resolution N°. 899, ANVISA. The determination of antioxidant activity of the
isolated 4-NC and the percolated was evaluated using UV-Vis spectrophotometer using a
technique that measures the activity of scavenging free radical 2,2-diphenyl-1-picril-hydrazyl
(DPPH •). The pellets were produced by extrusion technique / spheronisation using
granulation liquid consisting of the percolated, colloidal silicon dioxide and polysorbate 80.
The excipients were microcrystalline cellulose, lactose and hydroxypropyl methylcellulose
(HPMC). The drying of the pellets was done in an oven and fluidized bed coating. HPMC,
povidone and copolymer (polyvinyl alcohol polyethylene glycol graft copolymer) were tested
in the polymer coating. Accelerated photostability study was performed according to
standards described by the ICH International Conference on Harmonisation evaluating 4-NC
degradation in the extraction solution (percolated) and the solid dosage form (uncoated and
coated pellets). The pellets were characterized by size distribution, morphology and friability.
The external morphology of the pellets was evaluated through a stereomicroscope and the
thickness of the coating was observed by Scanning Electron Microscopy (SEM). The result
obtained for the moisture content was 6.33 ± 0.305% for total ash content: 8.25% ± 0.61 and
swelling index of 3.30 ± 0.87mL and an average particle size of the powder was 170.26μm.
The analytical method for 4-NC was linear in the range 10 to 200µg/mL. LQ and LD were
calculated 1.42 and 0.42 µg/mL. The accuracy showed less than 5.0% relative standard
deviation (RSD). The percolation process was efficient in the extraction of 4-NC. The
production of pellets from the extrusion technique/spheronisation was presenting a
satisfactory product was uniform with an average size of 1000 μm. In the study of antioxidant
activity, the effective concentration (EC50) value found for the isolated 4-NC and present in
the percolated was about two times more potent than vitamin E. In the study of photostability
of 4-NC present in the coated pellets, the copolymer coating was used in which offered more
protection to the active 4-NC against photodegradation. Given the impossibility of obtaining
solid dosage forms with pure active, the use of the extract containing the 4-NC is considered
more advantageous since the pharmaceutical technology can improve the stability of the
asset against degradation.
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ARAÚJO JÚNIOR, César Aparício de. Desenvolvimento e avaliação de pellets contendo extrato de Pothomorphe umbellata (pariparoba) via extrusão esferonização. 2011. 121 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2011.