Asian Journal of Pharmaceutical Research

Abstract

The objective of this research was to formulate fast dissolving tablets of Doxazosin mesylate that disintegrate in the oral cavity upon contact with saliva and there by improve therapeutic efficacy. Doxazosin mesylate is used for the treatment of the signs and symptoms of benign Prostatic Hyperplasia. Fast dissolving tablets of Doxazosin mesylate were prepared by direct compression method using superdisintegrant addition method, by using sublimation method and effervescent method. Thirty two formulations were prepared and evaluated for hardness, thickness, friability, weight variation, drug content, in vitro disintegration time, in vitro dispersion time, wetting time, water absorption ratio and in vitro dissolution studies.

FTIR and DSC studies revealed that there was no chemical interaction between the drug and the excipients. Formulation S8 was found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. The formulation S8 containing camphor (8%) as subliming agent was found to be the optimized combinations. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for formulation S8 for 60 days. The results of stability studies indicated no significant changes with respect to physicochemical properties, in vitro disintegration time, wetting time and in vitro drug release.

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Abstract

Montelukast sodium is an anti-asthmatic, mainly prevents leukotriene mediated effect associated with asthma. Mouth dissolving tablets of montelukast sodium was prepared by direct compression method using superdisintegrants such as croscarmellose sodium, crospovidone and sodium starch glycolate.

Mouth dissolving tablets (MDTs) disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrants or maximizing pore structure in the formulation. The tablets were prepared using various diluents like MCC, Lactose and superdisintegrants namely Crosscarmellose sodium, Crosspovidone and Sodium starch glycollate in different concentrations. Pre-compression parameters such as angle of repose, bulk density, tapped density, compressibility index, Hausner's ratio were carried out to study the flow properties of powder to achieve uniformity of tablet weight and the values were within permissible limits.The prepared tablets were evaluated for hardness, thickness, weight variation, friability, % drug content, wetting time, water absorption ratio, in vitro disintegration time, in vitro dispersion time and in vitro drug release.The formulation M12 and L12 was found to be the best on the basis of wetting time, in vitro disintegration time and in vitro drug release. Stability studies were carried out at 25°C±2°C/60%±5% RH and 40°C±2°C/75%±5% RH for a period of 60 days for the selected formulations. The formulation M12 and L12 containing Crospovidone (8%) as superdisintegrant and microcrystalline cellulose and lactose as diluents was respectively found to be the optimized combination.

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Oral controlled drug delivery systems have received much attention of the researchers during the past two decades. The rationale for developing a controlled release formulation is to enhance its therapeutic benefits, reducing its side effects and improving the management of diseased condition.

Studies have been carried out for developing oral controlled release matrix tablet formulations of labetalol by using polymeric materials like polyox WSR 301, polyox WSR 303, polymethacrylates, ethyl cellulose, xanthan gum, guar gum, karaya gum and sodium alginate.

The prepared matrix tablets were evaluated for weight uniformity, hardness, friability and drug content. The matrix tablets were then evaluated for the influence of polymer concentration, polymer type and nature of diluents on the drug release from matrix by in vitro dissolution studies. FTIR Spectral studies shown that drug and excipients used were compatible with each other. Selected formulations of Labetalol were subjected to accelerated stability studies. The formulations were stored at 400C±2°C, 75±5%RH for 3 months. No significant changes were observed from the prepared tablets during the study period.

The results of present research work clearly indicated that the nature and level of poly (ethylene oxides) in the matrix tablets greatly influenced the drug release properties. Both the Polyox WSR 301 and Polyox WSR 303 were suitable for preparing the matrix tablets of labetalol. Among the two polymers used, high molecular weight polymer, POLYOX WSR 303 effectively extended the drug release for prolonged period of time than low molecular weight POLYOX WSR 301. Insoluble diluents like microcrystalline cellulose, dicalcium phosphate and slightly soluble diluent like starch 1500 can be used as release rate modifiers in the formulation of controlled release matrix tablets.

A combination of hydrophilic gums, hydrophobic eudragits and ethyl cellulose with high molecular weight poly (ethylene oxides) led to prolonged release of drug up to 22 hrs. Thus present research work fulfilled the objective of developing once a day formulations of Labetalol as matrix tablets employing poly (ethylene oxides).

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