화학공학소재연구정보센터
Powder Technology, Vol.301, 839-847, 2016
Dry powder formulation from fruits of Physalis peruviana L. standardized extract with hypoglycemic activity
The aims of this study were to develop a dry powder formulation from standardized extract of fruits of Physalis peruviana L., for oral administration, and to choose the best drying process for retaining the hypoglycemic activity, applying a factorial type experimental design. The development of a pharmaceutical formulation from an herbal extract has technological complications arising from inappropriate pharmaceutical characteristics related to its extract nature as a multicomponent system. P. peruviana extract showed the following technology difficulties: high hygroscopicity (which affects its flow, blend uniformity and stability), reduced flow properties (poor, non-uniform flow), high cohesivity, and low compressibility. To solve these problems, physical state changes of the extract (e.g. by absorption processes in a substrate) could contribute to improving its physical properties. The selection of excipients for use in the formulation was based on a compatibility study with binary solid mixtures (extract and each excipient) analyzed trough HPLC, and additionally, applying a factorial statistical experimental design to choose the best absorbent for the extract and the best drying method, evaluating like response variables: particle size, bulk and tap densities, angle of repose and hygroscopicity. Finally, a hypoglycemic assay was conducted in mice, using the best formulation. According to the compatibility study, the following excipients may be considered promising for use in a possible solid formulation from the ethanolic extract of fruits of P. peruviana: Disintegrants, absorbents and diluents: microcrystalline cellulose and corn starch; binder: polyvinylpyrrolidone. From the extract and the excipients selected as absorbents and binder (microcrystalline cellulose PH 101, 102, 200, corn starch and polyvinylpyrrolidone), different granules were produced, which were dried by two methods. The factorial experimental design showed that microcrystalline cellulose PH 102 and corn starch were the best absorbents, and that drying in a fluidized bed was the best method, offering advantages in terms of physicochemical properties such as particle size, density, voluminosity, flowability and hygroscopicity, compared to the initial extract and to the other formulations. The hypoglycemic assay showed that the activity of the extract remained after its transformation to a solid state. The results suggest that the dry powder formulation obtained from the ethanolic extract of fruits of P. peruviana may be of use as a future phytotherapeutic product, or a more stable intermediate herbal product than the extract, as an adjuvant in the treatment of diabetes. (C) 2016 Elsevier B.V. All rights reserved.