Formulation and Evaluation of Fast Disintegrating Losartan Potassium Tablets by Formal Experimental Design

Abstract

In the treatment of hypertension fast onset of action is the major concern. The problem of slow onset of action of drugs can be overcome by development of appropriate dosage forms. Fast disintegrating tablets in mouth are best suited and have gained popularity in the oral antihypertensive drug therapy. These are advantageous over other conventional systems in terms of patient compliance, rapid onset of action, accurate dosing, good chemical stability, convenience of self-administration and compactness. Losartan potassium is widely used as an antihypertensive drug, which is a potent drug candidate for developing in to Fast Dissolving Tablets (FDT’s). It has low bioavailability due to first pass metabolism. Hence the main objective of the study was to formulate fast dissolving tablets of Losartan potassium to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablet of Losartan potassium were formulated by using microcrystalline cellulose with different concentration of super disintegrants like sodium starch glycolate and Isabgol Mucilage. All the batches were prepared by direct compression.
 API characterization studies were conducted to check the purity of API .The tablets were evaluated for Pre compression parameters and post compression parameters. Before the formulation of the tablets IR spectroscopic studies were also performed to check the compatibility with the excipients.
 A 23 full factorial design was applied to investigate the combine effect of 3 formulation variables. Here the concentration of Isabgol mucilage, concentration of Sodium Starch Glycolate and concentration of Microcrystalline Cellulose were taken as independent variable X1, X2 & X3 respectively and their effect of disintegration time is studied as dependent parameter. To represent the data Design Expert software is used.

Physicochemical characteristics of the pharmaceutically active ingredient in potassium losartan 50 mg tablets acquired by the Peruvian state and private sector Mayar Luis Ganoza-Yupanqui1,2,* ; José Carlo Uribe-Villarreal2 ; Luz Angélica

“…Los espectrogramas de ATR-FTIR del estándar secundario de losartán potásico (Figura 2) fueron comparados con el IFA contenido en las tabletas de losartán potásico 50 mg de 7 laboratorios farmacéuticos analizados: sector público (Figura 3), innovador (Figura 4), multifuente-1 (Figura 5), multifuente-2 (Figura 6), multifuente-3 (Figura 7), multifuente-4 (Figura 8) y multifuente-5 (Figura 9). El estándar secundario de losartán potásico presentó las señales características de cada grupo funcional (Tabla 1) que concuerda con lo reportado por Vidyadhara et al (2013), sin embargo las tabletas de LP 50 mg adquiridas por el estado peruano (sector público), presentaron una pequeña señal a 3524 cm -1 , que también se observó en el innovador a 3523 cm -1 , y más notorio en el muntifuente-3 (Figura 7), esta señal es característica de amina secundaria de derivados de tetrazol, imidazol o pirrol (Gómez et al, 2012), señal que no apareció en el estándar secundario por presentar un catión potasio en lugar del hidrógeno del enlace N-H. La combinación del IFA con diferentes tipos de excipientes genera espectrogramas variados para cada medicamento (Birajdar-Shivprasad et al, 2014;El-Deen et al, 2017;Phani et al, 2018). Figura 5.…”

Review article: sodium starch glycolate as a super disintegrant

“…However, the sorption limits of potato starch and the modified starches between 10%-70% RH are comparative. it creates the impression that the sorption limit between 10%-70% RH is not drastically influenced by the kind of cross-linking and sodium carboxymethylation (in sodium starch glycolates) and gelatinization (in pregelatinized starch) and that the superdisintegrant properties of the sodium starch glycolates are an outcome of some water-structure collaboration that is well beyond the accessible number of hydration sites [21][22][23][24].…”