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 first -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.
Duloxetine hydrochloride is a selective serotonin and nor adrenaline reuptake inhibitor. 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 hepatic first-pass metabolism and susceptible to undergo degradation in acidic environment of stomach, which results in the poor bioavailability. The objective of the present study was to develop and evaluate the mucoadhesive buccal tablets (transmucosal delivery) of duloxetine hydrochloride with a goal of to increase the bioavailability and improve the patient compliance. Mucoadhesive buccal tablets were prepared by a wet granulation technique using mucoadhesive polymers like HPMC K4M, Carbopol 934P and PEO WSR 303. The tablets were evaluated for weight variation, thickness, hardness, friability, surface pH, swelling index, drug content uniformity, in vitro drug release, in vitro bioadhesion and ex vivo permeation studies. The physicochemical properties of all the formulations were shown to be within the limits. The optimized buccal tablets AA1, AB3 and AC1 showed prolonged drug release for a period of 6 h with the Higuchi model release profile. Further, ex vivo permeation studies for optimized tablets were conducted and shown enhanced drug permeation. Therefore, these results demonstrated that the optimized buccal formulation of duloxetine hydrochloride enhances the oral bioavailability by delivered through the buccal route.
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.
Objective: Kidney diseases are a major problem of worldwide proportions, and renal damage is very common since kidney has the capacity to excrete toxic substances. This study aimed to evaluate the protective effect of the ethanolic extract of Allium cepa Linn. (EEAC) plant leaves against gentamicininduced nephrotoxicity in rats.Methods: Nephroprotective activity was estimated by inducing gentamicin (100 mg/kg) to all the groups of animals; acute kidney dysfunction is an evidenced 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 dose of 200 and 400 mg/kg and also shown significant improvement by protecting the kidney from the oxidative stress. It is also identified that treatment with 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 group against the toxic control group animals in parameters including serum creatinine, total protein, kidney weights, and body weights. The histopathological studies were also evinced the protective effect of EEAC.
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