FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISINTEGRATING TABLETS OF CINITAPRIDE HYDROGEN TARTARATE BY USING DIRECT COMPRESSION TECHNIQUE

Objective: In the present study, efforts were taken to develop fast disintegrating tablets of Cinitapride hydrogen tartrate, is a gastro-prokinetic agent and antiulcer agent with an objective to achieve rapid disintegration, and further improving the bioavailability of the drug. Also, to resolve the swallowing problems (Dysphasia) in pediatric, geriatric patients by rapid disintegration in saliva and improve the patient compliance.Methods: Fast disintegrating tablets were prepared by direct compression method using superdisintegrants like crospovidone (CP), croscarmellose sodium (CCS), sodium starch glycolate (SSG) and combination of super-disintegrants in different concentrations. The prepared formulations were evaluated for the pre-compression parameters like bulk density, tapped density, Carr's compressibility, Hausner's ratio and angle of repose. The prepared batches of fast disintegrating tablets of Cinitapride hydrogen tartarate were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time, water absorption ratio, and in vitro dissolution profile.Results: Bulk density and tapped density were found in the range of 0.412–0.432 g/cc and 0.507–0.528 g/cc respectively. In all formulations, tablet weight and thickness were within mean±9.5% and mean±5% respectively. Wetting time values lie between 19.76 to 39.53 sec. Water absorption ratio ranged from 57.30 to 78.82 %. The in vitro disintegration time for all the 12 formulations varied from 17.43 to 38.61 seconds. Formulation F8 which contained crosspovidone have recorded drug release 96.94±0.47% at the end of 30 min.Conclusion: The formulation containing crospovidone (F8) showed better performance in terms of disintegration time and drug release when compared to other formulations

NOVEL SUBCUTANEOUS SUSTAINED RELEASE NANOPARTICLES ENCAPSULATING LOW MOLECULAR WEIGHT HEPARIN (LMWH): PREPARATION, CHARACTERIZATION AND EVALUATION

Objective: The objective of the current research work was to prepare and evaluate novel subcutaneous sustained release polymeric nanoparticles for low molecular weight heparin (LMWH).Methods: In this study, we prepared subcutaneously administered polymeric nanoparticles encapsulating LMWH using different grades of polycaprolactons (PCL) (14k, 45k, 80k) and 0.1% Polyvinyl alcohol (PVA) solution as surfactant by employing water–in-oil in-water (w/o/w) emulsion and evaporation method. The formulated nanoparticles were evaluated for size, shape, zeta potential, in vitro drug release, and in vivo biological activity (anti factor Xa activity) using standard kit, antithrombotic activity in thrombosis induced rat model. Drug and polymer interactions in the nanoparticles were evaluated using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD).Results: Scanning electron microscopic (SEM) studies on the nanoparticles confirmed the formation of spherical particles with smooth surface. The size of the formed nanoparticles were about 415-495 nm. The % entrapment of nanoparticles was found to be between 69-81%. Nanoparticles showed slow and sustained pattern of release for about 59-65 % in 48 h. Optimized nanoparticles exhibited excellent improvement in pharmacokinetic parameters and showed good antithrombotic activity, Activated partial thromboplastin time (aPTT) activity when compared to free drug. FTIR studies indicated that there was no loss in chemical integrity of the drug upon fabrication into nanoparticles. XRD results demonstrated that the drug changed its physical form in the formulation.Conclusion: The results of this study revealed that subcutaneous nanoparticles were excellent candidates for sustained drug delivery of LMWH to avoid repeated subcutaneous administration.Keywords: Low molecular weight heparin, Subcutaneous, Stability, Polycaprolactone, Venous thrombosis, Activated partial thromboplastin timeÂ

DESIGN, DEVELOPMENT AND IN VITRO EVALUATION OF COMBINED FLOATING-BIOADHESIVE DRUG DELIVERY SYSTEMS OF ATENOLOL

Objective: A combination of the Floating-Bioadhesive system will overcome the drawbacks of floating & bioadhesive systems if used alone and will have a significant effect on improving the therapeutic effect of the drug involved. The present study involves the formulation and in vitro evaluation of atenolol floating-Bioadhesive tablet for prolonged residence in the stomach for the treatment of hypertension.Methods: The tablets were prepared by direct compression method using directly compressible polymers such as, Hydroxy Propyl Methyl Cellulose (HPMC) K15M, Guar gum, Carbopol, and sodium alginate. The tablets were evaluated for buoyancy test, mucoadhesion force, swelling study, drug content, ex-vivo mucoadhesion strength and in-vitro release profile. Sodium bicarbonate was used for producing the effervescent base for the buoyancy of tablets.Results: Formulation F9 contains polymer sodium alginate which has shown highest percentage cumulative drug release up to 99.12%. No significant change was observed in physical appearance, drug content, float ability or in vitro dissolution pattern after storage at 45 °C/75% RH for three months.Conclusion: In this present research work it was concluded that the cumulative drug release increased when the viscosity and concentration of the polymer was increased. The swelling properties were increased with increasing polymer concentration and contributed to the drug release from the tablet matrix.Â

EVALUATION FOR NEPHROPROTECTIVE ACTIVITY OF ETHANOLIC EXTRACT OF ALLIUM CEPA LINN. IN GENTAMICIN-INDUCED NEPHROTOXICITY IN RATS

ABSTRACTObjective: Kidney diseases are a major problem of worldwide proportions, and renal damage is very common since kidney has the capacity to excretetoxic substances. This study aimed to evaluate the protective effect of the ethanolic extract of Allium cepa Linn. (EEAC) plant leaves against gentamicininducednephrotoxicity in rats.Methods: Nephroprotective activity was estimated by inducing gentamicin (100 mg/kg) to all the groups of animals; acute kidney dysfunction is anevidenced by significant elevation of serum creatinine, total protein and decreased body weight with multiple histological damages.Results: Treatment with the A. cepa Linn. has shown significant (p<0.01 and p<0.001) dose-dependent improvement in the body weight at the doseof 200 and 400 mg/kg and also shown significant improvement by protecting the kidney from the oxidative stress. It is also identified that treatmentwith A. cepa significantly lowered the level of serum creatinine, total protein when compared with the toxic group.Conclusion: Nephroprotective activity of EEAC treatment was found compared with the standard group (Vitamin E – 250 mg/kg) and control groupagainst the toxic control group animals in parameters including serum creatinine, total protein, kidney weights, and body weights. The histopathologicalstudies were also evinced the protective effect of EEAC.Keywords: Nephroprotective activity, Gentamicin, Nephrotoxicity, Allium cepa Linn

Evaluation of anti ulcer activity of ethanolic root extract of Beta vulgaris in rats

Background: Beta vulgaris (chenopodiacea) is a plant reported for its variety of ethnic medicinal uses. Hence we have planned to screen anti ulcer activity of root of the plant with the alcoholic extract. Root powders successively extracted with alcohol and were subjected for phytochemical screening to identify different phytoconstituents.Methods: Anti ulcer activity was evaluated in various animal models like pylorus ligation and ethanol induced ulcer models in rats.Results: Preliminary phytochemical screening revealed the presence of alkaloids, flavonoids, carbohydrates, saponins, polyphenols. No mortality was observed with root extract up to maximum dose level of 4g/kg. Further alcoholic extract of 200 and 400mg/ kg / p.o significantly (p˂0.01) reduced the ulcer score, ulcer number, ulcer index, free acidity and total acidity in pylorus ligation and ethanol induced ulcer models in rats.Conclusions: The present study revealed that the root extract of Beta vulgaris has antiulcer activity

SYNTHESIS OF PRODRUGS OF MEFENAMIC ACID AND THEIR IN VIVO EVALUATION

Objective: The purpose of the study was to synthesize prodrugs of mefenamic acid, to be used as Anti inflammatory drug with fewer adverse effects. Methods: The drug was covalently bonded to PEG 1500 (polyethylene glycol) and PEG 6000 as such and with a linker glycine. The prodrugs were characterized by FT-I.R and N.M.R. For the drug release studies, all the prodrugs were subjected to pH 1.2 and pH 7.2. For the anti inflammatory activity, Carrageenan induced rat paw edema method was followed and for Ulcer protecting activity, Pylorus ligation method was used, the prodrugs were administered to male Sprague-Dawley rats. Results: The results suggested that the prodrugs of mefenamic acid, the drug release was higher at pH 7.2 than at pH 1.2. The result obtained for anti inflammatory activity was comparable to the standard drug of mefenamic acid. For ulcers, the prodrugs were found to possess Ulcer curing property higher than the standard drug. Conclusion: The prodrugs thus synthesized possess anti inflammatory activity as well as good ulcer protecting activity, can be used instead of standard drug

DESIGN AND IN VITRO CHARACTERIZATION OF MUCOADHESIVE BUCCAL PATCHES OF DULOXETINE HYDROCHLORIDE

Objective: Buccal mucosa is a potential site for the delivery of drugs to the systemic circulation, a drug administered through the buccal mucosa enters directly to the systemic circulation, thereby which bypass the drug from the ï¬rst-pass hepatic metabolism and adverse gastrointestinal effect. Duloxetine hydrochloride (DLX HCL) is a selective serotonin and noradrenaline reuptake inhibitor (SSNRI). It is used in the treatment of depression, diabetic peripheral neuropathic pain and in moderate to severe stress urinary incontinence in women.However, it undergoes extensive first-pass metabolism, and it is susceptible to undergo degradation in the acidic environment of the stomach, which results in the poor bioavailability. The objective of the present investigation is to design and evaluate the mucoadhesive buccal patches of DLX HCL with a goal of to increase the bioavailability and improve the patient compliance.Methods: Mucoadhesive buccal patches were prepared by solvent casting technique using mucoadhesive polymers. The patches were evaluated for weight variation, thickness, surface pH, folding endurance, moisture absorption, drug content uniformity, in vitro drug release, mechanical properties and ex vivo permeation studies.Results: The results of the optimised buccal patch F4 indicate that the mucoadhesive buccal patches of duloxetine hydrochloride may be a good choice for improving the bioavailability by bypassing the extensive first pass metabolism and acid degradation in the stomach.Conclusion: Duloxetine hydrochloride can be delivered through the buccal route of drug administration through the buccal patches