A sensitive and efficient LC-MS/MS method for the bioanalysis of fosinopril diacid from human plasma and its application for a bioequivalence study in humans.

Fosinopril diacid is an angiotensin converting enzyme inhibitor with efficient antihypertensive action. It is an active metabolic product formed in the body from hydrolysis of its prodrug Fosinopril. A sensitive, rapid method with high recovery for Fosinopril diacid from human plasma was developed. Solid-phase extraction technique employing Waters Oasis SPE cartridges gave clean samples with very high recovery of 97%. The analyte along with its internal standard (Benazepril hydrochloride) were chromatographed on an XTerra RP8 column (4.6 × 50 mm, 5 µm) using methanol-ammonium acetate buffer (10 mm; 90:10, v/v) as the mobile phase. A triple quadrupole mass spectrometer equipped with electrospray ionization source operated in the negative ion mode was used for detection. Multiple reaction monitoring scan mode was used for monitoring the transitions from m/z 434.00 → 237.15 for Fosinopril diacid and m/z 423.10 → 174.00 for Benazepril hydrochloride. Beer-Lambert's law was obeyed in the range of 0.50-1,500.00 ng/ml (r = 0.9993). The stability of the drugs in human plasma and in stock solution was proved by performing stability tests as per US Food and Drug Administration guidelines. The method was successfully applied for a bioequivalence study of Fosinopril diacid in 36 healthy, adult, male volunteers under fasting conditions.

A Sensitive HPTLC Method for the Estimation of Glibenclamide, Rosiglitazone Maleate and Metformin Hydrochloride from a Multicomponent Dosage Form.

A sensitive, rapid and cost-effective method based on HPTLC with UV detection was developed for the quantitation of Glibenclamide (GLIBEN), Rosiglitazone maleate (ROSI) and Metformin hydrochloride (MET) from a combined dosage form. Pre-coated RP-18 F254s aluminum sheets were used as the stationary phase. Methanol-tetrahydrofuran-water-glacial acetic acid (16: 3.6: 4: 0.4, v/v) used as the mobile phase, along with chamber saturation of 10 min offered an optimum migration (Rf = 0.54, 0.62 and 0.80 for GLIBEN, ROSI and MET, respectively). TLC Scanner 3 was used for densitometric evaluation of the chromatograms. DigiStore 2 Documentation System with winCATS software version 1.4.10 was used for the quantitation and photodocumentation. The LOD for GLIBEN, ROSI and MET was found to be 80 ng, 80 ng and 48 ng, respectively. Moreover, the LOQ was 200 ng, 200 ng and 120 ng for GLIBEN, ROSI and MET, respectively. The method was linear for GLIBEN (r = 0.9991), ROSI (r = 0.9993) and MET (r = 0.9988) within the tested range (200-1000, 200-1000 and 120-600 ng/band, respectively). The method was found to be precise and accurate for all the three drugs. The method was applied for the analysis of Triglucored tablets, and it proved to be a reliable quality control tool for the routine analysis of GLIBEN, ROSI and MET in a combined dosage form.

Synthesis, characterization and evaluation of the suppression of insulin resistance in Type-II diabetes mellitus animals by treatment with metal complex.

The present study is characterized toward thespesone isolation from Thespesia populnea (Malvaceae). Subsequently it was modified and characterized to study its effect on diabetes related symptoms. The complex is administered to diabetes induced mice with the doses of 5, 10 and 20 mg/kg, p.o. and the effect of complex on the level of body weight, lipid profile and blood glucose was studied after 22 days. The results have indicated that diabetic mice show a significant (p < 0.01) decrease in the level of serum triglyceride, plasma glucose and increase in body weight. Hence the present investigation reveals that newly synthesized complex is useful in the management of Type-II diabetes mellitus because of its ability to reduce insulin resistance.

The isolation, Characterization and Preclinical Studies of Metal Complex of Thespesia populnea for the Potential Peroxisome Proliferator-activated Receptors-γ Agonist Activity.

BACKGROUND: Diabetes mellitus is an international public health problem since ancient days. The condition is predominantly more severe in developing countries like India where, life is more sedentary due to the even changing lifestyles in this fast-paced global scenario. Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes mellitus in India for years. The aim of this work is to explore the anti-diabetic activity of the isolated compound. MATERIALS AND METHODS: The sesquiterpene isolated from hexane fraction of bark of T. populnea modified synthetically then identified by using analytical techniques such as electron paramagnetic resonance spectra for confirmation and the anti-diabetic activity was evaluated by anti-hyperglycemic, hypoglycemic potential. RESULT: In the present work, we have studied the anti-hyperglycemic and hypoglycemic activity of the vanadium complex in glucose loaded and normal animals were shown significantly decreased in plasma blood glucose level. The results derived from preclinical studies confirm the potential of new sesquiterpene. CONCLUSION: The findings could provide evidence regarding the anti-diabetic potential of T. populnea by lowering blood glucose level. SUMMARY: Thespesia populnea is widely used in the ayurvedic system of medicine for treatment of diabetes in India. Present study aimed to explore the anti diabetic potential of isolated compound. Isolation of sesquiterpene from hexane fraction of bark of Thespesia populnea and modified synthetically then authenticated by using analytical techniques such as electron paramagnetic resonance spectra for confirmation. The modified complex was further assessed for its anti diabetic property in glucose loaded rats. Vanadium complex demonstrated significant reduction in plasma blood glucose level in glucose loaded animals. The results derived from preclinical studies confirm the potential of new sesquiterpene. The present findings conclude that anti diabetic potential of Thespesia populnea could be due to lowering blood glucose level by acting on PPAR-γ receptor.