A Comparative Study of Different Proportions of Superdisintegrants: Formulation and Evaluation of Orally Disintegrating Tablets of Salbutamol Sulphate.

OBJECTIVES: Superdisintegrants play important role in disintegration of orally disintegrating tablets (ODTs). Action of three different superdisintegrants, viz. croscarmellose sodium, sodium starch glycolate and Indion 414, were studied individually or in their binary combinations for their fast disintegrant action in ODTs of salbutamol sulphate prepared by direct compression. MATERIALS AND METHODS: ODTs were prepared in three different superdisintegrant combinations A, B and C. In each combination, five formulations were prepared with superdisintegrants in ratios 10:90, 25:75, 50:50, 75:25, and 90:10. Three ODT formulations were prepared with single superdisintegrant and two ODT batches were prepared from marketed ODT excipient blends, viz. Prosolv-ODT and F-Melt. Prepared ODT formulations were evaluated and compared for weight variation, hardness, friability, wetting time, disintegration and drug release. RESULTS: All ODTs disintegrated quickly in 32 s or less. ODT formulation F3, containing croscarmellose sodium and sodium starch glycolate, disintegrated very quickly in 19.28±3.11 s. Results of F3 were compared with the batches (F19 and F20) containing marketed coprocessed excipients and found in good agreement for various evaluation parameters. Formulation F20 was hygroscopic, while F3 did not suffer this disadvantage. CONCLUSION: Thus, we may conclude that superdisintegrants in combinations may offer additive and/or synergistic disintegration possible due to their different mechanism.

Formulation Design and Optimization of Orodispersible Tablets of Quetiapine Fumarate by Sublimation Method.

The objective of present study was to formulate directly compressible orodispersible tablets of quetiapine fumarate by sublimation method with a view to enhance patient compliance. A full 3(2) factorial design was used to investigate the effect of two variables viz., concentration of Indion 414 and camphor. Indion 414 (3-5 % w/w) was used as superdisintegrant and camphor (5-15 % w/w) as subliming agent. The tablets were evaluated for thickness, weight variation, hardness, friability, content uniformity, wetting time, porosity, in vitro disintegration time and in vitro drug release. The formulation containing 5% w/w of Indion 414 and 5% w/w camphor was emerged as promising based on evaluation parameters. The disintegration time for optimized formulation was 18.66 s. The tablet surface was evaluated for presence of pores by scanning electron microscopy before and after sublimation. Differential scanning colorimetric study did not indicate any drug excipient incompatibility, either during mixing or after compression. The effect of independent variables on disintegration time, % drug release and friability is presented graphically by surface response plots. Short-term stability studies on the optimized formulation indicated no significant changes in drug content and in vitro disintegration time. The directly compressible orodispersible tablets of quetiapine fumarate with lower friability, greater drug release and shorter disintegration times were obtained using Indion 414 and camphor at optimum concentrations.

Taste Masked Orodispersible Formulation of Fexofenadine Hydrochloride Using Ion Exchange Resins.

The objective of this research work was to mask the intense bitter taste of fexofenadine hydrochloride using weak cation exchange resins and to formulate orodispersible tablet of taste masked drug-resin complex. Five resins indion 204, indion 234, indion 414, kyron T-114 and kyron T-314 were used. Depending on maximum drug loading capacity of resins indion 234 and kyron T-314 were finalized for further study. Drug-resin complex was optimized by considering parameters such as drug to resin ratio, soaking time of resins, stirring time, temperature and pH on maximum drug loading. The drug-resin complex was characterized by Fourier transform infrared spectroscopy. The drug-resin complex was also subjected to various evaluation studies such as taste mask evaluation by panel method, drug content and in vitro drug release at salivary and gastric pH. The orodispersible tablets of taste masked drug-resin complex for indion 234 and kyron T-314 were prepared by direct compression method. Formulated orodispersible tablets were subjected to various evaluation parameters such as diameter and thickness measurement, hardness test, weight variation test, in vitro United States Pharmacopoeia disintegration test, wetting time, test for content uniformity, assay, friability test and in vitro dissolution studies. The results indicate that orodispersible tablets of fexofenadine hydrochloride containing indion 234 and kyron T-314 are palatable and provide quick disintegration and fast drug release without addition of superdisintegrants.

Ion-exchange resin complexation: Masking the bitter taste of cefuroxime axetil / Complejación de la resina de intercambio de iones: enmascaramiento del sabor amargo de cefuroxime acetil

OBJECTIVE: the purpose of this research was to formulate taste masked complexes of cefuroxime axetil and to evaluate them for taste, drug loading and characterized by FTIR, XRD. Tablets were formulated of selected batches and evaluated for drug release and physical parameters. METHODS: complexation technique is used to prepare complexes of drug where ion exchange resins such as Indion® 214, Indion® 234 and Indion® 414 were used with a drug-resin ratio of 1:0.5, 1:1, 1:2. The drug resinates were characterized by Infrared Spectroscopy, DSC and X-Ray Diffraction pattern and evaluated for drug loading and taste. Direct compression method was used to formulate tablets. In vitro dissolution was carried out using USP II apparatus. RESULT: potential taste masking increased with increasing concentration of resin. Indion® 214 resin showed better taste masking effect as compared to Indion® 234 and Indion® 414. Percent of drug loading was maximum at drug : resin ratio of 1:1, after that it decreased. Prolonged (upto 5 h) and slow drug release was observed with resin 214 at higher concentration. CONCLUSIONS: out of three resins chosen, Indion® 214 at higher concentration exhibit excellent taste masking as well as sustained drug release action.

OBJETIVO: el objetivo de esta investigación fue formular los complejos con sabor amargo de cefuroxime acetil y evaluarlos por sabor, carga medicamentosa y caracterización por FTIR, XRD. Las tabletas fueron formuladas a partir de lotes seleccionados y evaluados en busca de la liberación medicamentosa y parámetros físicos. MÉTODOS: la técnica de complejación se utilizó para preparar complejos farmacológicos donde las resinas de intercambio iónico como Indion® 214, Indion® 234 y el Indion® 414 se emplearon a una proporción resina-medicamento de 1:0.5, 1:1, 1:2. Los resinados medicamentosos fueron caracterizados mediante espectroscopia infrarroja, DSC y el patrón de difracción-rayos-X, y evaluados para determinar la carga medicamentosa y el sabor. El método de compresión directa fue empleado para formular las tabletas. Se efectuó una disolución in vitro utilizando el equipo USP II. RESULTADOS: el posible enmascaramiento del sabor aumentó con la creciente concentración de resina. La resina Indion® 214 mostró el mejor enmascaramiento del gusto amargo en comparación con Indion® 234 e Indion® 414. El porcentaje de carga medicamentosa fue máximo en el fármaco: proporción de la resina 1:1, después disminuyó. Se observó una liberación medicamentosa prolongada (hasta 5 h) y lenta con la resina 214 a una mayor concentración. CONCLUSIONES: de las 3 resinas escogidas, Indion®214 a una mayor concentración muestra un excelente enmascaramiento del sabor así como una mantenida acción liberadora del fármaco.