Enhancement of dissolution rate of racecadotril by liquisolid compact technology

Abstract The current investigation was used to improve the rate of dissolution of an anti-diarrheal drug i.e., racecadotril (RT) at low pH conditions (i.e., in the stomach) by reducing the water secretion and electrolyte in to the intestine by liquisolid tablets. Different formulations (liquisolid) were prepared using Avicel PH 102 as a carrier. Aerosil 200 as a coating material and sodium starch glycolate used as a disintegrant. Polyethylene glycol 200 was used as a non-volatile vehicle to dissolve the drug. FTIR, DSC, XRD and dissolution studies were conducted to characterise liquisolid tablets. Characterisation studies indicated that no interactions between carrier and drug. Solid state characterization had shown a reduction in crystallinity that further supports increment in solubility and dissolution. The optimised formulation showed a significant increase in dissolution i.e., 99.54±0.62% in 30 min compared to directly compressible tablets (38.47±0.26%). The % dissolution efficiency of racecadotril liquisolid tablets 76.86% compared to marketed tablet (27.56%) and conventional direct compression tablet (17.11%). Significant reduction in mean dissolution time of racecadotril from liquisolid tablets (6.84 min) compared to direct compression tablet (44.57 min), indicating faster release of drug and faster onset of action. Formulation of liquisolid tablets could enhance solubility, dissolution and bioavailability of racecadotril

Revalidation of key role of water absorption in disintegration process of Chinese materia medica dispersible tablets: Exemplifying by Jianghuang Qingzhi Dispersible Tablets / 中草药

Objective: The purpose of this paper is to verify the key role of water absorption in the process of disintegration of Chinese materia medica (CMM) dispersible tablets, so as to provide the solution idea for slow disintegration of CMM dispersible tablets. Methods: In this paper, the influence of water absorption of raw materials and auxiliary materials on disintegration process was verified using oily Jianghuang Qingzhi Tablets (JQT) as research object. The water absorption and disintegrating process of different drugs, JQT with different materials, and modified dispersible tablet were determined. Results: The water absorption of JQT was lower than that of lactose tablets, and the disintegrating process was slower. The water absorption of different materials prescription of JQT was: CMS-Na-PVPP (1∶1) > PVPP > CMS-Na, and disintegrating process is the same as the former order. The water absorption of JQT after modification enhanced, and disintegration time was significantly shortened. It indicated that the water absorption of raw materials and excipients was stronger, the disintegration was faster. Conclusion: The study proves that water absorption is a key role in the disintegration of CMM dispersible tablets. And co-grinding of silica powder and raw materials is important technology to solve the problem of slow disintegration of CMM dispersible tablets.

Influência da temperatura de secagem e da concentração de Aerosil®200 nas características dos extratos secos por aspersão da Schinus terebinthifolius Raddi (Anacardiaceae) / Influence of the drying temperature and the Aerosil®200 concentration on the characteristics of Spray-dried extracts from Schinus terebinthifolius Raddi (Anarcadiaceae)

A Schinus terebinthifolius Raddi é muito usada na medicina popular e atualmente como fitomedicamento pelas propriedades antimicrobiana, cicatrizante e antiinflamatória. O objetivo deste trabalho foi avaliar a influência da temperatura de entrada e a concentração de Aerosil®200 nas características de extratos secos por aspersão da Schinus terebinthifolius Raddi. Os extratos preparados com etanol 70 °GL foram secos em Mini-spray dryer, Buchi B191, com adição do adjuvante tecnológico numa proporção de 20:80; 25:75 e 30:70 (p/p) Aerosil®200: resíduo seco, variando a temperatura de entrada de 120 °C a 160 °C. A umidade residual, o rendimento final do produto e o aumento da massa frente à umidade relativa controlada de 90 por cento foram usados como critério de avaliação. A análise de superfície de resposta revelou que à medida que a temperatura e a concentração de Aerosil aumentam, diminui a umidade residual dos extratos, bem como sua higroscopicidade. As melhores condições de secagem foram a temperatura de entrada de 140 °C e 30 por cento do adjuvante, resultando em rendimento acima de 80 por cento.

Schinus terebinthifolius Raddi has been used in the Brazilian folk medicine since a long time and now as phytopharmaceutical because of its antimicrobial, cicatrizant and anti-inflammatory properties. The aim of this work was to evaluate the influence of the inlet temperature and the Aerosil concentration on the characteristics of the spray-dried extracts from Schinus terebinthifolius Raddi by spray-drying method. The extracts were prepared from a 70 °GL ethanolic extract with a Buchi B 191 Mini-spray dryer with technological adjuvant into a ratio of 20:80; 25:75 and 30:70 (w/w) Aerosil®200: dried residue, in the inlet temperature range from 120 °C to 160 °C. The residual humidity, final yield and the moisture uptake profile at 90 percent Relative Humidity (RH) were used as evaluation criteria. The response surface analysis showed that increasing the temperature and the Aerosil®200 concentration, lead to lower residual humidity and moisture uptakes. The best drying parameters were the inlet temperature of 140 °C and 30 percent of Aerosil®200 concentration, resulting in yields over 80 percent.