DEVELOPMENT AND VALIDATION OF STABILITY INDICATING HPTLC METHOD FOR SIMULTANEOUS DETERMINATION OF LINAGLIPTIN AND METFORMIN

Objective: A simple, precise, and accurate stability indicating high-performance thin-layer chromatography (HPTLC) method was developed and validated for simultaneous estimation of linagliptin and metformin active pharmaceutical ingredients and fixed dose combination.Methods: Linagliptin and metformin densitograms were developed on silica gel 60 F254 HPTLC plates with acetone: methanol: chloroform: formic acid (3:1:5:1v/v) as the mobile phase. Densitometric quantification was performed at 230 nm.Results: For linagliptin and metformin RF values were found as 0.72 and 0.19, respectively. The method was validated for precision, accuracy, specificity, and robustness. The linearity curves were obtained in the concentration range of 100–600 ng per spot by area with correlation coefficients of 0.999 and 0.99 for linagliptin and metformin, respectively. Limit of detection was found to be 5.19 and 8.72 ng per spot for linagliptin and metformin, respectively; lowest possible quantity to be quantified by the proposed method was found to be 15.74 and 26.44 ng per spot for linagliptin and metformin, respectively. From stability studies, the noninterference of the linagliptin and metformin degradants with drugs demonstrated the suitability of the developed method.Conclusion: The developed method was validated and found to be selective, specific and suitable for application in pharmaceutical analysis of these drugs in bulk and fixed dose combination.Â

Therapeutic Monitoring of Antiretroviral Drugs in Immunologically Stable HIV Patients on ART Treatment

In HIV, highly active anti-retroviral therapy helps patients to regain the immune CD4+ cell count. Among all antiretroviral therapy (ART) regimens tenofovir based regimen (TLE; Tenofovir (TDF) + Lamivudine (3TC) + Efavirenz (EFV)) has become the most preferred first line regimen. Present study aimed to identify the therapeutic levels of drugs in tenofovir based regimen in immunologically stable HIV patients. A total of 35 dried blood samples were obtained from HIV patients on TLE treatment visiting ART centre, Mahatma Gandhi Memorial (MGM) Hospital, Warangal, Telangana, during September 2017 to March 2018. Patients with good adherence, without history of smoking & alcoholism and with CD4+ cell count > 350 cells/mm3 were included. Estimation of drugs was done using pre validated liquid chromatographic method. In total of 35 patients, females were accounted for 62.86%. Patients of this study showed high percentage of illiterates (48.57%) and daily labors (34.29%). As EFV is a narrow therapeutic index drug it showed significant difference in its plasma therapeutic levels (0.005**) whereas TDF & 3TC were not. Total of 8.57% and 91.43% patients were showed EFV plasma levels below and above therapeutic levels respectively. Though the study patients observed with good immunological status, high percentage of patients identified with toxic levels of EFV concentrations. But none of the patients showed any symptoms of toxicity, they are at risk to develop clinical toxicity in future. Present study results suggesting dose adjustments and monitoring of drug levels in these patients to avoid early treatment failures and toxicity. Keywords: HIV, CD4+ cell count, Tenofovir regimen, Therapeutic level, Monitoring

Biological activities of plant extracts from Ficus elastica and Selaginella vogelli: an antimalarial, antitrypanosomal and cytotoxity evaluation

The cytotoxic, antiplasmodial, and antitrypanosomal activities of two medicinal plants traditionally used in Cameroon were evaluated. Wood of Ficus elastica Roxb. ex Hornem. aerial roots (Moraceae) and Selaginella vogelii Spring (Selaginellaceae) leaves were collected from two different sites in Cameroon. In vitro cell-growth inhibition activities were assessed on methanol extract of plant materials against Plasmodium falciparum strain 3D7 and Trypanosoma brucei brucei, as well as against HeLa human cervical carcinoma cells. Criteria for activity were an IC50 value 10 μg/mL. The extract of S. vogelii did not significantly reduce the viability of P. falciparum at a concentration of 25 μg/mL but dramatically affected the trypanosome growth with an IC50 of 2.4 μg/mL. In contrast, at the same concentration, the extract of F. elastica exhibited plasmodiacidal activity (IC50 value of 9.5 μg/mL) and trypanocidal (IC50 value of 0.9 μg/mL) activity. Both extracts presented low cytotoxic effects on HeLa cancer cell line. These results indicate that the selected medicinal plants could be further investigated for identifying compounds that may be responsible for the observed activities and that may represent new leads in parasitical drug discovery

Insulinotropic Activity of Methanolic Extract of Mesua ferrea Linn.

Mesua ferrea flowers have been used in the Indian traditional medicine for treating various diseases. In present study, the Mesua ferrea flowers methanolic extract (MFME, 200 mg/kg bw) was studied for anti diabetic activity and underlying mechanisms for its activity. In Streptozotocin induced diabetes rats model, MFME treatment enhanced plasma insulin levels by 69.53% (

Andrographolide Pretreatment Enhances the Bioavailability and Hypoglycemic Action of Glimepiride and Metformin

Herbal antidiabetic preparations are often used as an add-on therapy in diabetes. Hence, in the present investigation the effect of andrographolide (AD) on the pharmacokinetics and pharmacodynamics of glimepiride and metformin in normal as well as in STZ - induced diabetic rats was studied. In normal and diabetic rats the combination of glimepiride and metformin with AD increased significantly (p < 0.01) all the pharmacokinetic parameters, such as Cmax, AUC0 to n, AUCtotal, t½, MRT and decreased the clearance, Vd markedly as compared with the control group. In pharmacodynamic studies, the combination of glimepiride and metformin with AD provided significant protection against the diabetes induced alterations in the biochemical parameters. In addition, the combination of glimepiride and metformin with AD also improved the total antioxidant status and decreased lipid peroxide levels significantly in diabetic rats compared with AD, glimepiride and metformin alone treated groups. The results revealed that combination of glimepiride and metformin with AD led to the enhancement of the bioavailability of glimepiride and metformin by inhibiting the CYP450 enzymes. In conclusion, add-on preparations containing AD may increase the bioavailability of glimepiride and metformin, which suggested that AD might be beneficial as an adjuvant to glimepiride and metformin in a proper dose, in diabetic patients and hence the doses should be monitored