ABSTRACT
Objective: The objectives of this study were to identify stable anhydrous emulsions via pseudo ternary phase diagram, optimize artemether-loaded batches using factorial design and subsequently evaluate the antimalarial activity. Methodology: Using labrasol®, triacetin® and lauroglycol 90® as the surfactant, oil and co-surfactant respectively, pseudo ternary phase diagram was generated from the quantitative titration of water with the anhydrous emulsion. Stable combinations from the phase diagram were subjected to a 23 full factorial experimental design. The 22 softwaregenerated formulations were experimentally formulated and characterized for droplet size, polydispersity index, viscosity and thermodynamic stability. Droplet size was chosen and subsequently fitted into the Response column of the software, thus prompting the generation of graphs and Desirability table of 125 predicted formulations. Out of the 125 predictions, three with the least droplet sizes (less than 100 nm) were adjudged as optimized batches. Subsequently, they were formulated, converted to powder by adsorption on magnesium aluminum metasilicate and evaluated. Antimalarial effectiveness of the drug-loaded formulation was also investigated. Results: Triacetin® most significantly (P<0.05) contributed to droplet size variation. The droplet size of the experimental formulations approximated that of the statistical predictions. The anhydrous emulsions (AEs) were powderable and the granulations rated fair and passable according to Carr’s scale. Artemether-loaded anhydrous emulsion (AE) demonstrated highest antimalarial activity. Conclusion: We therefore conclude that optimization proved a useful tool for the identification of excipient proportions with optimal effects.
ABSTRACT
As traditional drug delivery poses many disadvantages such as difficulty in consumption, the granules were opted to replace t ablet dosage forms available in the market. A 23 full factorial design was employed for the formulation and characterization of the granule dosage form of oxcarbazepine. From regression equations we can assess the impact of each factor on the response further contour plots helped to pre-analyze the desired target factor values, in addition optimization process helped to analyze the values of dependent variables. Thus as of the results achieved a preferred response of flow property and drug release was obtained. In the current study, an attempt has been made to minimize possible number of experiments in the formulation of granule dosage forms. Polyvidone is a hydrophilic binder and primellose is a good disintegrate to obtain higher dissolution rate. A part, microwave assisted drying process plays a major role in achieving desired flow properties of granules.
ABSTRACT
As traditional drug delivery poses many disadvantages such as difficulty in consumption, the granules were opted to replace t ablet dosage forms available in the market. A 23 full factorial design was employed for the formulation and characterization of the granule dosage form of oxcarbazepine. From regression equations we can assess the impact of each factor on the response further contour plots helped to pre-analyze the desired target factor values, in addition optimization process helped to analyze the values of dependent variables. Thus as of the results achieved a preferred response of flow property and drug release was obtained. In the current study, an attempt has been made to minimize possible number of experiments in the formulation of granule dosage forms. Polyvidone is a hydrophilic binder and primellose is a good disintegrate to obtain higher dissolution rate. A part, microwave assisted drying process plays a major role in achieving desired flow properties of granules.
ABSTRACT
A novel "Powder Solution Technology" involves absorption and adsorption efficiency which makes use of liquid medications, drug suspensions admixed with suitable carriers, coating materials and formulated into free flowing, dry looking, non adherent and compressible powder forms. Based upon a new mathematical model expression, improved flow characteristics and hardness of the formulation has been achieved by changing the proportion of Avicel ® PH 200 and Aerosil ® PH 200 from 50:1 ratio to 5:1 and in which the drug is dispersed in an almost molecularly state. Due to their significantly improved wetting properties a greater drug surface area is exposed to the dissolution media, resulting in an increased dissolution rate and bio availability. By using the Liquisolid technique, sustained drug delivery systems were developed for the water soluble drugs in which hydrophobic non-volatile solvents are used as vehicles.
A nova "Tecnologia da Solução Sólida" envolve eficiência de absorção e de adsorção, faz uso de medicações líquidas, suspensões de fármacos e misturas com transportadores adequados, materiais de cobertura e é formulada em formas sólidas em fluxo livre, secas, não aderentes e compressíveis. Com base em novo modelo matemático, características aprimoradas de fluxo e dureza da formulação foram alcançadas modificando-se a proporção de Avicel ® PH 200 e Aerosil ® PH 200 de 50:1 para 5:1, na qual o fármaco é disperso quase que no estado molecular. Devido às propriedades de umidificação significativamente aprimoradas e à área do fármaco exposta ao meio de dissolução, que resulta na velocidade de dissolução, a biodisponibilidade foi aumentada. Utilizando a técnica Liquisólido, desenvolveram-se sistemas de liberação controlada de fármacos solúveis em água, nos quais solventes hidrofóbicos não voláteis foram usados como veículos.