Volume 3, Issue 1, January – March 2011[/su_heading][/su_spoiler][/su_panel]
1. Dermatopharmacokinetic Approach to Evaluate and Compare the Pharmacokinetic Profile of Marketed Preparations of Diclofenac Sodium
Mayee R V, Rawat S S
In this single-dose-one arm, open label three way parallel design, pharmacokinetic study of three marketed formulations of Diclofenac Sodium using 12 healthy Indian male subjects the pharmacokinetic parameters of three marketed Diclofenac Sodium topical formulations were compared . Marketed Diclofenac Sodium topical formulations (A, B & C) were applied on the pre-marked forearms of the subjects as per the dosing schedule. Treatment sample C was used as a reference sample. Subjects received treatment A, treatment B & treatment C on both the arms simultaneously, following open label three way parallel design. Skin Stratum Corneum samples were collected in sterile glass test tubes during the study period. The samples were collected pre-dose and at 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, & 6.0 hours post-dose application. The Stratum Corneum samples were analysed for Diclofenac Sodium concentrations only. Pharmacokinetic parameters of Diclofenac sodium were calculated as Cmax, tmax, AUC (0-t) and AUC (0-∞) Diclofenac Sodium was estimated in Stratum Corneum using a validated Spectroscopic method. If the point estimate of the geometric mean ratio and the confidence intervals for the entire log transformed pharmacokinetic parameters [Cmax, AUC (0-t) and AUC (0-∞)] were entirely included in the range of 80-125%, then the treatments were claimed to be bio-equivalent. A total of 12 subjects were enrolled in this study. The bioequivalence values of the test drug A were Cmax of 23.767±2.398 μg/mL, tmax of 1.75 ±0.261 h, AUC0-t of 100.507± 10.455 h. μg/mL, AUC0-∞ of 178.286± 22.859 h. μg/mL; of the test drug B Cmax of 31.1± 2.742 μg/mL, tmax of 1.75 ±0.261 h, AUC0-t of 103.555± 10.072 h. μg/mL, AUC0-∞ of 166.971± 47.627 h. μg/mL; and of test drug C Cmax of 24.084± 2.216 μg/mL, tmax of 1.75 ±0.261 h, AUC0-t of 100.586±11.15 h. μg/mL, AUC0-∞ of 179.887± 21.553 h. μg/mL.
2. Effect of Sinapic acid on Antiperoxidative and Antioxidant Potential in Normal and Streptozotocin-induced Diabetes in Wistar Rats
Ganesan Kanchana, Wilson Jerine Shyni, Palanisamy Malini, Murugan Rajadurai
The present study was aimed to investigate the effect of Sinapic acid on antioxidant potential in normal and Streptozotocininduced diabetic rats. Diabetes was induced in female wistar rats by a single intraperitoneal administration of Streptozotocin (45 mg/ kg BW). Rats were divided into six groups: normal (untreated), normal + Sinapic acid (15mg/kg), normal + Sinapic acid (30 mg/kg), diabetic control, diabetic + Sinapic acid (15mg/kg) and diabetic + Sinapic acid (30 mg/kg). Diabetic rats exhibited elevated levels of lipid peroxidation markers such as thiobarbituric acid reactive substances and hydroperoxides in plasma and tissues and decreased levels of antioxidants superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPX), reduced glutathione (GSH), ceruloplasmin, vitamin C and vitamin E in serum and tissues. Oral administration of Sinapic acid for a period of 35 days significantly decreased lipid peroxidation markers and increased the antioxidants suggesting the antioxidant potential of Sinapic acid in diabetic rats.
3. Evaluation of Lantana camara Linn. (Verbenaceae) for Antiurolithiatic and Antioxidant Activities in Rats
Mayee R., Thosar A.
The roots of Lantana camara Linn. are recommended for kidney stone disorders in the Indian traditional system of medicine. Ethanolic extract of Lantana camara Linn. leaves were evaluated for antiurolithiatic activity against 0.75% v/v ethylene glycol and 2% w/v ammonium chloride induced calcium oxalate urolithiasis and for antioxidant activity against hyperoxaluria induced oxidative stress in male albino rats. Ethylene glycol and ammonium chloride administration increased the deposition of calcium and oxalate in the kidneys; also increased urinary excretion of calcium oxalate and creatinine in the preventive and curative control rats. In these groups, increased levels of malondialdehyde, depleted levels of antioxidant enzymes, reduced glutathione and catalase were observed. On treatment with the extract, a significant reduction in the deposition of calcium, oxalate and also urinary excretion of calcium, oxalate and creatinine was observed, indicating its antiurolithiatic effect. The extract administration also decreased the extent of lipid peroxidation and hence enhanced the levels of antioxidant enzymes in the kidneys of urolithic rats, reflecting its antioxidant efficacy against hyperoxaluria induced renal oxidative stress. Results of the present study support the traditional claim of Lantana camara Linn. leaves in treating renal calculi.
4. Comparison between Marketed Formulations of Diclofenac Gel, Emugel and Spray for the Evaluation of Effect of Pressure and Temperature on Their Bioavailability
Mayee R, Rawat S, Atre K, Mane P
This study involves research to assess the pharmacokinetics of Diclofenac Sodium Marketed formulations as well as the effect of pressure and temperature on its bioavailability by Dermatopharmacokinetic method. This drug is used for the treatment of local pain. This was a single-dose-three arm, open label pharmacokinetic study of marketed formulations of Diclofenac Sodium using 12 healthy Indian male subjects. A marketed Diclofenac Sodium topical formulation was applied on the pre-marked forearms of the subjects as per the dosing schedule. Gel and Emugel formulation was applied on one forearm whereas the spray was applied on the other arm. Subjects received treatment on both arms in normal conditions of temperature and pressure & same treatment with the application of sufficient pressure in the second period & heat in the third period of the study. The study was conducted following open label three way parallel design. A washout period of two days was kept between the three periods of the study. Skin Stratum corneum samples were collected in sterile glass test tubes during each period. The samples were collected pre-dose and at 0.5, 1.0, 1.5, 2.0, 3.0, 4.0, & 6.0 hours post-dose application. The Stratum corneum samples were analysed for Diclofenac Sodium concentrations only. Pharmacokinetic parameters of Diclofenac sodium were calculated as Cmax, tmax, AUC (0-t) and AUC (0-∞) Diclofenac Sodium was estimated in Stratum corneum using a validated Spectroscopic method. A total of 12 subjects were enrolled in this study. The bioequivalence values of the test drug are mentioned in the Tables 1-4 and the graphical representation is shown in the Fig. 1-16. This study demonstrated that the bioavailability of the topical formulations increased with the help of pressure and temperature in case of the Gel and Emugel formulations whereas there was negligible effect of temperature and pressure on the Spray formulation of Diclofenac.