RESUMO
OBJECTIVE: To evaluate the antidiabetic effects of the aqueous extract of Elaeocarpus ganitrus (EAG) in experimental animals. MATERIALS AND METHODS: The hypoglycemic activity of the EGA was evaluated in normoglycemic rats by single dose at three graded dose levels, viz. 250, 500 and 1000 mg/kg of body weight. Antihyperglycemic activity of the extract was also evaluated at the same dose levels in streptozotocin (STZ) (60 mg/kg, i.p.)-induced diabetic rats during a 30-day treatment period. Metformin (500 mg/kg) was used as the reference drug. Fasting blood glucose and lipid parameters, viz. triglycerides, total cholesterol, high-density lipoprotein and low-density lipoprotein levels were measured. Acute oral toxicity of the EGA extract was carried out in Swiss albino mice. RESULTS: In normoglycemic rats, EGA showed a significant (P < 0.01) hypoglycemic effect at 2 h. In STZ-induced diabetic rats, the EGA treatment significantly (P < 0.05) decreased the blood glucose level in a dose-dependent manner during the 30 days of treatment period. EGA modulated lipid profile changes in STZ-diabetic rats in a dose-dependant manner. In the acute oral toxicity study, EGA showed no mortality till the 5 g/kg dose in mice. CONCLUSION: The present investigation shows that EAG seeds has potential antidiabetic effects.
RESUMO
The purpose of this research was to prepare a floating drug delivery system of diltiazem hydrochloride (DTZ). Floating matrix tablets of DTZ were developed to prolong gastric residence time and increase its bioavailability. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by direct compression technique, using polymers such as hydroxypropylmethylcellulose (HPMC, Methocel K100M CR), Compritol 888 ATO, alone or in combination and other standard excipients. Sodium bicarbonate was incorporated as a gas-generating agent. The effects of sodium bicarbonate and succinic acid on drug release profile and floating properties were investigated. A 3(2) factorial design was applied to systematically optimize the drug release profile. The amounts of Methocel K100M CR (X1) and Compritol 888 ATO (X2) were selected as independent variables. The time required for 50% (t50) and 85% (t85) drug dissolution were selected as dependent variables. The results of factorial design indicated that a high level of both Methocel K100M CR (X1) and Compritol 888 ATO (X2) favors the preparation of floating controlled release of DTZ tablets. Comparable release profiles between the commercial product and the designed system were obtained. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which had a higher value of correlation coefficient (r). While tablet hardness had little or no effect on the release kinetics and was found to be a determining factor with regards to the buoyancy of the tablets.
