DEVELOPMENT AND STANDARDIZATION OF Rapanea ferruginea MEZ. (MIRSINACEAE) DRY EXTRACT OBTAINED FROM SPRAY DRYING AND EVALUATION IN VIVO OF ITS ANTINOCICEPTIVE ACTIVITY / DESENVOLVIMENTO E PADRONIZAÇÃO DE EXTRATO SECO DE Rapanea ferruginea MEZ. (MIRSINACEAE) OBTIDO POR SPRAY DRYING E AVALIAÇÃO IN VIVO DA ATIVIDADE ANTINOCICEPTIVA

Thaisa Baccarin

Rapanea ferruginea is a pantropical species that grows in various parts of Brazil. It is popularly known in Brazil as canela-azeitona or capororoca. Studies carried out in past by the NIQFAR research group have shown that this plant presents biological effects, including antiinflamatory, hypoglicemic and analgesic effects. This work seeks to develop and standardize a dry extract from husks of R. ferruginea, and to evaluate its antinociceptive activity in vivo. The extraction process was dynamic maceration, varying the alcoholic degree of the extractor liquid, extraction time, and particle size of the plant drug. For the quantification of mirsinoic acid B (MAB) in the extracts, an HPLC method was developed and validated. The extractive solutions were characterized by pH, dry residue, TLC and HPLC profile and MAB concentration. The drying process was optimized by spray-drying. Sample variables (concentration of solids and excipients) (samples 1-9) and process variables (sample flow and enter temperature) (samples 10-18) were selected. The dry extracts were characterized by humidity, hygroscopicity, morphological and flow properties, TLC and HPLC profile and AMB quantification. Biological validation of the technological development process was performed by the in vivo formalin test. The analytical method developed proved to be linear at a MAB range of concentration of 5-100 μg/mL, and showed accuracy of 101%, precision and robustness for MAB quantification. In the optimization of the extraction process, it was found that an alcoholic degree of 90 GL and extraction time of two hours, without particle separation, represents the best technological conditions for AMB extraction. Aerosil was selected as the excipient for obtaining the dried extracts. All the batches of samples presented poor particle flow. The MAB concentration in samples 1-9 was higher in the extracts with lower concentration of solids, while in samples 10-18, the MAB concentration was not significantly affected by the process variables. The samples with lower Aerosil concentration presented higher hygroscopicity. The particle size of samples 1-9 was between 19 and 34 μm, this increase being observed in the extracts with higher concentrations of solids. All the dried extracts 8 and concentrated extracts tested in the formalin test showed a better response in inflammatory pain, and there was no relation with MAB concentration. This study enabled the best conditions to be determined for obtaining standardized, biomonitored dry extract of R. ferruginea contributing to the development of a new phytotherapic drug.

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