Characterization and quality evaluation of primaquine diphosphate raw materials

Este trabalho objetivou caracterizar e avaliar a qualidade de matérias-primas (MPs) de primaquina de diferentes fornecedores, designadas amostras A, B, C e D. Os resultados de características físicas, solubilidade, faixa de fusão, perda por dessecação e identificação mostraram estar de acordo com o preconizado pelas literaturas oficiais para todas as amostras. Os difratogramas apontaram que todas as MPs apresentaram características cristalinas semelhantes. Nas imagens obtidas por microscopia eletrônica de varredura a amostra D demonstrou um tamanho maior de partícula. A pureza do fármaco por titulação potenciométrica, variou de 98,8 a 101,1% para todas as amostras, estando de acordo com as especificações farmacopéicas e, por cromatografia líquida de alta eficiência, as amostras A e B demonstraram estar com a pureza inadequada (90,7 e 93,1% respectivamente), revelando a presença da impureza quinocida.This work aimed to the characterization and quality evaluation of primaquine diphosphate raw materials provenient from different suppliers, designated A, B, C and D. The results of physical characteristics, solubility, melting range, loss on drying and identification were in accordance with the recommended official literature for all samples. The diffractograms showed that all samples have similar crystal characteristics. In scanning electron microscopy images the sample D shows a larger particle size. The drug content available by potentiometric titration, ranged from 98.8 to 101.1%, in accordance with the pharmacopoeia specifications and the results obtained by high performance liquid chromatography indicated that the samples A and B have an inappropriate content (90.7 and 93.1%, respectively), revealing the quinocide impurity presence.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation study of quercetin-loaded lipid-based nanocarriers obtained by hot solvent diffusion method

Lipid-based nanocarriers were prepared by hot solvent diffusion technique. Tristearin (TS) and/or castor oil were employed as oily phase, and Lutrol F68® or Solutol HS15® and lecithin were employed as surfactant and cosurfactant, respectively. The influence of the formulation variables on surface charge and size of the nanocarriers and their ability to load and control the release of quercetin were investigated. Solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and microemulsions (ME) were obtained depending on the formulation composition. Querecetin (QU) entrapment efficacy was higher than 99 % for all formulations. However, drug content was greatly affected by the formulation composition. ME exhibited the highest capacity to load QU, reaching a concentration around 1,300 times higher than its aqueous solubility. QU release profiles exhibited biphasic kinetics for all formulations. However, the release rate of QU was affected by the properties of the nanocarrier.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development, evaluation and physical chemical characterization of acyclovir/chitosan microparticles produced by spray-drying technique

Micropartículas de aciclovir/quitosana de liberação prolongada foram desenvolvidas pela técnica de spray-drying, apresentando uma eficiência de encapsulação em torno de 90%. Os resultados obtidos por calorimetria exploratória diferencial (DSC), microscopia eletrônica de varredura (MEV) e difração de raios-X de pó (DRX) apontaram a formação de um sistema amorfo. Nas análises obtidas por termogravimetria (TG) foi observado que as micropartículas são termicamente estáveis até a temperatura de 242,4 °C. Os espectros na região do infravermelho (IV) indicaram que não ocorreram interações químicas, entre o fármaco e a quitosana. O revestimento do aciclovir com o biopolímero promoveu uma liberação do fármaco por um período de 2 horas, seguindo o modelo proposto por Higuchi. Dessa forma, conclui-se que o revestimento além de propiciar uma liberação prolongada do fármaco, contribuiu para aumentar a solubilidade do mesmo, uma vez que as micropartículas desenvolvidas apresentaram caráter amorfo.Delayed release acyclovir/chitosan microparticles were developed by spray drying technique with entrapment efficiency about 90%. The results obtained by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray powder diffraction (XRPD) had pointed that an amorphous system was formed. The analysis obtained by thermogravimetry (TG) indicated that the microparticles were thermal stable until temperature of 242,4 ºC. The Fourier transforms infrared (FT-IR) did not present any interactions between acyclovir and chitosan. The covering of drug with chitosan promoted a delayed release of acyclovir during 2 h, following the model considered for Higuchi. In this way, it was concluded that the covering promotes an acyclovir delayed release and improving the solubility of the drug, a time that the microparticles developed presented amorphous characteristics.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Development, evaluation and physical chemical characterization of acyclovir/chitosan microparticles produced by spray-drying technique

Micropartículas de aciclovir/quitosana de liberação prolongada foram desenvolvidas pela técnica de spray-drying, apresentando uma eficiência de encapsulação em torno de 90%. Os resultados obtidos por calorimetria exploratória diferencial (DSC), microscopia eletrônica de varredura (MEV) e difração de raios-X de pó (DRX) apontaram a formação de um sistema amorfo. Nas análises obtidas por termogravimetria (TG) foi observado que as micropartículas são termicamente estáveis até a temperatura de 242,4 °C. Os espectros na região do infravermelho (IV) indicaram que não ocorreram interações químicas, entre o fármaco e a quitosana. O revestimento do aciclovir com o biopolímero promoveu uma liberação do fármaco por um período de 2 horas, seguindo o modelo proposto por Higuchi. Dessa forma, conclui-se que o revestimento além de propiciar uma liberação prolongada do fármaco, contribuiu para aumentar a solubilidade do mesmo, uma vez que as micropartículas desenvolvidas apresentaram caráter amorfo.Delayed release acyclovir/chitosan microparticles were developed by spray drying technique with entrapment efficiency about 90%. The results obtained by differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray powder diffraction (XRPD) had pointed that an amorphous system was formed. The analysis obtained by thermogravimetry (TG) indicated that the microparticles were thermal stable until temperature of 242,4 ºC. The Fourier transforms infrared (FT-IR) did not present any interactions between acyclovir and chitosan. The covering of drug with chitosan promoted a delayed release of acyclovir during 2 h, following the model considered for Higuchi. In this way, it was concluded that the covering promotes an acyclovir delayed release and improving the solubility of the drug, a time that the microparticles developed presented amorphous characteristics.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Evaluation of physicochemical characteristics of suspensions containing hydrochlorothiazide developed for pediatric use

Hydrochlorothiazide (HCTZ) is a thiazide diuretic used in pediatric patients despite the lack of a liquid form commercially available. Pediatric suspensions containing 0.6% of CMC-Na (F1) or 0.6% of HPMC (F2) were developed and their physicochemical characteristics were analyzed. The in vivo activity of the F1 and F2 was carried out in rats. The formulation F1 showed zeta potential value of -22.6 mV ± 1.6, while for F2 the found value was -2.01 mV ± 2.3. The mean particle size found for F1 and F2 were 44.1 μm ± 2.3 and 16.3 μm ± 1.9, respectively. The F1 sediment was easily redispersed with soft agitation of 13.3 s. On the other hand, F2 with non-charged HPMC, was denser and more difficult to redisperse. Both formulations showed an increase in urinary volume and electrolytes excretion (Na+, K+, Cl-) in rats.Colegio de Farmacéuticos de la Provincia de Buenos Aire