CHARACTERIZATION OF GRANULES CONTAINING SOLID DISPERSIONS OF CURCUMIN/LACTOSE /GELUCIRE® 50/13 OBTAINED BY HOT MELT GRANULATION

TF03

Teixeira, C. C. (1), ccorreia@fcfrp.usp.br; Paiva Júnior,  E.   (1); Araújo, R.  R. (1); Freitas, L.  A. P. (1).

Faculdade de Ciências Farmacêuticas de Ribeirão PretoUniversidade de São PauloVia do Café s/n, Campus USP, Ribeirão Preto, SP, 14040-903, Brazil

Introduction. A large number of drugs present low solubility in water, thus their application in therapy is restricted due to low bioavailability. Hence, several researches have been developed aiming to overcome this problem.  Solid dispersions have shown to be an interesting method for enhancing the solubility of poorly soluble drugs. The greatest challenge in applying this approach is to select the polymeric system, which must present low melting point and high compatibility with the drug and which also allows the processing at low temperatures.  Polymeric excipients such as long chain PEG, PVP and Gelucire® have proved to be suitable in the production of these formulations.  The preparation of solid dispersions by hot melt coating technique is an alternative to improve the solubility of many drugs and yield solid dispersions with reproducible physico-chemical properties. Objective. The aim of this work was to evaluate the pharmacotechnical properties of granules composed of spray-dried lactose and ternary dispersions containing curcumin. Materials and Methods. The study followed a 2² full factorial design  in order to evaluate the influence of the ratio of Curcumin:Gelucire® 50/13  (mixture A), and the proportion of Lactose:mixture A on the characteristics of the dried powder, such as angle of repose, Hausner Factor, Carr Index, particle size distribution and granulation yield. Results and Discussion. Granules repose angles were always below 35º, indicating good flow. The compressibility parameters varied in an acceptable range, the Hausner Factor was below 1.25 and Carr Index was below 12%. The yield during the Fluidized Bed Hot Melt Granulation process varied from 57 to 65%. Particle size distributions were used to predict d50, which varied from 590 to 910 mm for the conditions studied. The results of the analysis of variance (ANOVA) showed that the drug/carrier and lactose content in the granules did not affect significantly their densities, flowabilities and compressibilities. This result is interesting since it indicates that curcumin/carrier content in granules can be increased without affecting their pharmacotechnical properties. Furthermore, all solid dispersions showed adequate flow and compressibility properties, which are important to predict the behavior of the granules during die filling and how well it will be compressed, and the formulation stability.