The objective of the study was to formulate and evaluate gastro retentive floating drug delivery tablets of Losartan potassium. It is an orally active non-peptide angiotensin -II receptor antagonist, used in the treatment of hypertension due to mainly blockade of AT1 receptors. The main reason for low therapeutic effectiveness of Losartan potassium is its narrow therapeutic index, poor bioavailability (25-35%), and short biological half life (1.5-2h). Conventional tablets should be administered 3-4 times to maintain plasma drug concentration. So, to increase therapeutic efficacy, reduce frequency of administration sustained release floating matrix tablets of Losartan potassium were prepared. Present study demonstrates the formulation of sustained release floating matrix tablets of Losartan potassium with various grades of hydroxyl propyl methylcellulose to restrict the drug release preferably in upper part of intestine and to improve its bioavailability and to provide constant drug plasma levels thereby improving the patient compliance. Losartan potassium showed maximum absorbance at 256 nm so absorbance was measured at the same wavelength and found to obey Beer lamberts law in the concentration range of 10-40 mcg/ml. In the pre formulation study of IR spectra of pure drug with the different polymers showed no interaction, Differential scanning calorimetry experiments were carried out to find out the presence of any interaction among drug and the excipients. Pure drug and individual polymers were subjected to the study and no interactions were observed .12 formulation of sustained release of Losartan potassium were prepared and they were examined for physical properties and appearance like hardness, thickness, weight variation, thickness, hardness, friability uniformity of drug content floating lag time floating duration time and in-vitro drug release studies . I n the study all the powder blends showed good flow ability angle of repose below 25.98±0.07°-31.724±0.15°, compressibility index was found in the range of 12.5±0.16-16.92±1.9 g/cm 3 Weight variation 297.2±1.19-301.52±2.73mg, hardness 5.9±0.2-7±0.2kg/cm 2, thickness 4.506±0.04-4.86±0.03, friability 0.91-0.41, floating time <12hrs in vitro release for all formulations were found to be 61.18 -99.02.
Nebivolol Hydrochloride is selective Beta blocker having a unique character which distinguishes it from other beta blockers. It increases the release of nitric oxide which causes vasodilation which in turn improves the arterial compliance and decreases the peripheral vascular resistance. The objective of present investigation is to design, evaluate the physical parameters and to carry out the permeation studies of Nebivolol Hydrochloride antihypertensive Transdermal patch by employing suitable polymers such as Eudragit RL100, and Eudragit RS100. The drug and polymer compatibility study has been studied by FTIR and DSC studies. The prepared Nebivolol transdermal patches were subjected various evaluation parameters like weight variation, drug content, moisture content, moisture uptake, thickness uniformity, invitro diffusion study, after performing all evaluation tests, it is confirmed that formulation F2 is the optimized formulation and it shows better invitro diffusion compared to other formulations. Key words: Nebivolol Hydrochloride; TDDS; Eudragit RS100; Eudragit RL 100; Zero order model; Higuchi model; Korsmeyer’s model
Aceclofenac complex is prepared by kneading method of inclusion complexation. The aim of present work is to improve the solubility and dissolution properties of a poorly water soluble drug aceclofenac, by inclusion complexation technique. Two components namely β cyclodextrin and span 60 were used in this study, β CD is used as complexing agent and span 60 as surfactant which helps in increasing solubility and dissolution. The prepared Aceclofenac complex is evaluated in terms of compatibility, solubility, dissolution behavior with the help of FTIR, DSC, In vitro dissolution studies. The complexation parameter of β CD had an impact on the solubility of drug. The solubility of complexes was progressively improved when compared to pure Aceclofenac drug in water. The prepared Aceclofenac complexes were subjected to dissolution study. At the end of 60 min of dissolution study 22.32±0.42 of pure drug was dissolved. The prepared complexes showed 85.35±0.71 at 60 min. The percent of drug dissolved increased for the complexes prepared with high concentration of β CD. The study showed that complexing property of β CD and surfactant action of span 60 has its influence on both solubility and dissolution of the prepared inclusion complexes. MDT and % DE was evaluated for the all the prepared complexes. Aceclofenac complexes prepared with high concentration of β CD showed lower MDT and higher % DE compared to pure Aceclofenac. The pure and complexed Aceclofenac were characterized by DSC studies. DSC studies showed that there was no appreciable change in the melting endotherm of prepared complexes compared to that of pure drug. The drug release from the above follows Korsemeyer-Peppas model and release mechanism was Non- Fickinian. Keywords: Aceclofenac, inclusion complex, kneading method, complexing agent, solubility, dissolution.
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