K.S. Srilatha

ABSTRACTTreatment of hypertension with conventional dosage forms is not effective as the drugs do not reach the site of action in appropriate concentration and it is also requiring dosing. Thus, an effective and safe therapy of hypertension disorder using specific drug delivery system is a challenging task to the pharmaceutical technologists. Most commonly used method of modulating the drug release is to include it in a matrix system, because of their flexibility, hydrophilic polymer matrix system is widely used in oral controlled drug delivery to obtain a desirable drug release profile, cost effectiveness and broad regulatory acceptance. In present study we have prepared matrix tablet formulations using Prazosin as model drug and Ethyl Cellulose, Two grades of Hydroxy propyl methyl cellulose- HPMC-K4M &HPMC-K100M as polymers in different ratios. The developed matrix tablets were evaluated for different physical chemical evaluations like drug content, hardness, friability, swelling index etc. All the formulations had shown the results within prescribed limits. The In vitro drug release study indicates that formulation F7 containing EC, HPMC K100M in 1:2 ratio shown good release pattern for 14 hours compare to other formulations. The short-term stability study proven no change in the formulation upon ageing and it indicates good stability. Keywords: Prazosin, Matrix tablets, Ethyl Cellulose and HPMC-K4M & K100M.

ABSTRACTEtodolac is used for the management of rheumatoid osteoarthritis. The site of absorption of Etodolac is in the whole GI tract and has a long half-life of 7± 4 hrs. The aim of the study was to develop colon targeted compression coated tablets of Etodolac using HPMC as swellable, time-controlled polymer, Eudragit S 100 as a coating polymer guar gum and chitosan as carriers in the treatment of Osteoarthritis. All the formulations (F1 to F5) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Etodolac released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F3 released 95.24% of Etodolac. The results of the study showed that formulation F3 is most likely to provide targeting of Etodolac for local action in the colon owing to its minimal release of the drug in the first 5 h. The most satisfactory formulation was stable during stability studies conducted for 60 days as per ICH guidelines. It showed no significant changes in the physicochemical parameters, in vitro release pattern. The studies confirmed that, the designed formulation could be used potentially for colon delivery by controlling drug release in stomach and the small intestine.Keywords: Etodolac, rheumatoid osteoarthritis, HPMC and colon targeted.    

ABSTRACTThe 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°

ABSTRACTThis short communication reports the pharmacokinetic differences of the glucuronide-conjugated metabolites of magnoflorine and jatrorrhizine between Chinese and African male volunteers. From an earlier report, glucuronidation was determined to be one of the main metabolic pathways and these two compounds were reported to differ significantly between the two races. Pharmacokinetic parameters of half-life,t1/2, time to reach maximum concentration, Tmax, maximum plasma concentration, Cmax, volume of distribution, Vd, area under the concentration-time curve, AUC and clearance, CL were considered. Statistically significant differences were observed in almost all the parameters studied in terms of their glucuronide-conjugated metabolites. The findings indicate the differences in hepatic metabolism of these two compounds between the two races. Keywords: conjugate, glucuronide, metabolite, pharmacokinetics, races.