Umamahesh Balekari | Kakatiya University (original) (raw)

Papers by Umamahesh Balekari

International Journal of Pharmacy and Pharmaceutical Sciences, Nov 18, 2015

Objective: A simple, precise, and accurate stability indicating high-performance thin-layer chrom... more 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.

Biochemistry & pharmacology, Dec 4, 2013

Pharmacognosy Research, 2016

Aim: Abrus precatorius leaves methanolic extract (APME) was evaluated for in vivo antihyperglycem... more Aim: Abrus precatorius leaves methanolic extract (APME) was evaluated for in vivo antihyperglycemic activity and in vitro insulinotropic effect. Materials and Methods: In vivo antihyperglycemic and insulin secretagogue activities were assessed in streptozotocin-induced diabetic rats by oral administration of APME (200 mg/kg body weight [bw]) for 28 days. In vitro insulin secretion mechanisms were studied using mouse insulinoma beta cells (MIN6-β). In vivo body weight and blood glucose and in vivo and in vitro insulin levels were estimated. Results: In diabetic rats, APME treatment significantly restored body weight (26.39%), blood glucose (32.39%), and insulin levels (73.95%) in comparison to diabetic control rats. In MIN6-β cells, APME potentiated insulin secretion in a dependent manner of glucose (3-16.7 mM) and extract (5-500 μg/mL) concentration. Insulin secretagogue effect was demonstrated in the presence of 3-isobutyl-1-methyl xanthine, glibenclamide, elevated extracellular calcium, and K + depolarized media. Insulin release was reduced in the presence of nifedipine, ethylene glycol tetra acetic acid (calcium blocking agents), and diazoxide (potassium channel opener). Conclusion: The study suggests that APME antihyperglycemic activity might involve the insulin secretagogue effect by pancreatic beta cells physiological pathways via K +-ATP channel dependent and independently, along with an effect on Ca 2+ channels.

Barringtonia asiatica is used in folklore medicine in fomenting, sealing of secondary infection, ... more Barringtonia asiatica is used in folklore medicine in fomenting, sealing of secondary infection, healing of wounds and skin eruptions. There was no scientific evidence justifying the use of bark of Barringtonia asiatica , therefore the present study was aimed at evaluation of wound healing activity of the plant. In the present study the bark of Barringtonia asiatica were studied for wound healing activity by incorporating extract in simple ointment base B.P. in concentration of 2% (w/w) and 4% (w/w) .Wound healing activity was studied in three types of model in rats viz. excision, incision and burn wound model. The results were also comparable to those of a standard drug, nitrofurazone in terms of wound contracting ability, wound closure time, tensile strength. The statistical data indicated that the wound with ointment containing 4% w/w alcoholic extract exhibited significant (P < 0.001) wound contracting ability and period of epithelization. Significant tensile strength was obs...

Asian Journal of Pharmaceutical and Clinical Research, 2017

Objective: The objective of the present study was to prepare and evaluate a novel oral formulatio... more Objective: The objective of the present study was to prepare and evaluate a novel oral formulation of nanoparticles for the systemic delivery of low molecular weight heparin (LMWH). Methods: Nanoparticles were prepared by polyelectrolyte complexation (PEC) method using polymers sodium alginate and chitosan. Entrapment efficiency of LMWH in nanoparticles was found to be ̴88%. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X‑ray diffraction (XRD), Scanning electron microscopy (SEM) studies carried for nanoparticles. In vitro release studies were performed for the formulations. Ex vivo permeation studies were performed optimized formulation by using small intestine of rat and in vivo studies were conducted on rat model.Results: In vitro release studies demonstrated that the release of LMWH was negligible in the stomach and high in the small intestine. FTIR has indicated that there is no interaction between the ingredients in nanoparticle. DSC...

International Journal of Pharmaceutical Investigation, 2016

The objective of the present work was to prepare and evaluate a novel oral formulation for system... more The objective of the present work was to prepare and evaluate a novel oral formulation for systemic delivery of low molecular weight heparin (LMWH). The formulation consisted of Eudragit S 100-coated positively charged liposomes encapsulating LMWH and a penetration enhancer. Materials and Methods: Positively charged liposomes were first prepared by the thin film hydration method using lipid (soy phosphotidylcholine and cholesterol) and stearyl amine (SA) in the optimum ratio of 16:1, along with cetylpyridinium chloride (CPC) as a penetration enhancer. Prepared liposomes were coated with negatively charged Eudragit S 100 (0.3% w/v). The formulations were studied for various in vitro and in vivo properties. Differential scanning calorimetry (DSC), x-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) studies, and in vitro drug release were used for in vitro characterization of the formulations. Ex vivo permeation studies were performed by using distal small intestine of rat. Oral absorption studies were conducted with the rat model. Results: Coating of the liposomes was confirmed by SEM and particle size determination studies. In vitro release studies of coated liposomes have demonstrated that the release of LMWH was in the following order: Stomach < small intestine < distal small intestine < colon. Ex vivo permeation studies have shown a fivefold increase in permeation of LMWH with Eudragit S 100-coated liposomes compared to uncoated, uncharged liposomes. Oral absorption studies have showed that with Eudragit-coated liposomes, the oral bioavailability of LMWH was improved, compared to plain LMWH solution. This is revealed by a threefold increase in the area under the curve (AUC) of the plasma concentration time curve. Conclusion: A novel formulation for oral delivery of LMWH was thus successfully prepared and evaluated.

Ethiopian Pharmaceutical Journal, 2015

A rapid, simple, specific and precise high-performance thin-layer chromatography (HPTLC) method w... more A rapid, simple, specific and precise high-performance thin-layer chromatography (HPTLC) method was developed for the simultaneous estimation of sitagliptin (STG) and metformin (MET) content in a fixed dose pharmaceutical formulation and also in bulk drug. In the developed method, aluminium backed silica gel 60 F 254 HPTLC plates were employed as stationary phase with BuOH, CHCl 3 , MeOH, (CH 3 CH 2 ) 2 NH 2 and HCOOH in a ratio of 4:0.5:2.5:1.5:0.06 (v/v) as a mobile phase, and chromatograms were scanned densitometrically at 206 nm. For STG and MET, Rf values were found to be 0.76 and 0.27, respectively. The linearity curve for the drugs was obtained in the concentration range of 2 - 7 μg per band and 20 - 70 μg per band, respectively. Correlation coefficients for STG and MET were 0.999 and 0.997, respectively. The developed method was confirmed by validating it as per the ICH guidelines. The limits of detection (LOD) and limits of quantification (LOQ) for STG and MET were found to be 0.014 & 0.042, and 0.013 & 0.040 μg per band, respectively. The developed method was found to be precise, accurate (mean recovery was within the range of 98 - 102%), specific and robust. Therefore, the method can be used for the simultaneous quality control analysis of the STG and MET in bulk drugs and pharmaceutical formulations. Keywords: Simultaneous Estimation, Sitagliptin, Metformin, Fixed Dose Pharmaceutical Formulation, HPTLC

Pharmacology & Pharmacy, 2015

Since ancient times, traditional medicines have been in the usage for the treatment of Diabetes m... more Since ancient times, traditional medicines have been in the usage for the treatment of Diabetes mellitus. An edible fruit from traditional medicinal plant Capparis zeylanica (CZ) was studied for its anti diabetic, insulin secretagogue activities and mechanisms involved in it. In Streptozotocin induced diabetes rats, oral administration of Capparis zeylanica methanolic extract (CZME) (200 mg/kg body weight) for 28 days showed a significant reduction in blood glucose levels by 35.53% and enhanced circulating insulin levels by 81.82% than the diabetic control rats. The insulin secretagogue activity mechanisms of the extract were evaluated by using mouse insulinoma beta cell line (MIN6-β). The extract stimulated insulin release in dependent manner of glucose concentration (3-16.7 mM) and extract dose (5-500 μg/mL). The insulin releasing effect of the extract was significantly enhanced by 3-isobutyl-1-methyl xanthine, glibenclamide, elevated extracellular calcium and K + depolarized media. This insulin release was significantly reduced in calcium blocking conditions (by nifedipine and EGTA), in the presence of potassium channel opener (diazoxide). Hence, anti diabetic activity of CZME might be a result of its stimulatory effect on insulin release from pancreatic beta cells via K ATP channel dependent and independent ways. These results indicate that CZ fruits have the potential to use in diabetes therapy.

Hygeia:journal for drugs and medicines, 2014

A half yearly scientific, international, open access journal for drugs and medicines Research art... more A half yearly scientific, international, open access journal for drugs and medicines Research article section: Herbal drug analysis/toxicology D.O.

Journal of Pharmaceutical Sciences & Emerging Drugs, 2014

Insulinotropic Agents from Medicinal Plants Diabetes is a group of metabolic diseases characteriz... more Insulinotropic Agents from Medicinal Plants Diabetes is a group of metabolic diseases characterized by hyperglycemia resulting from lack of insulin secretion or insulin sensitivity or both. Enhancement of insulin levels and insulin sensitivity is the primary target in the treatment of diabetes. Current treatment options, such as dietary modifications, oral hypoglycemic drugs and insulin have limitations of their own. In view of this, several medicinal plants have been studied for anti-diabetic activity using various in vitro and in vivo methods. Therefore, researchers have been focusing research to find an effective and safe antihyperglycemic drug for clinical use from natural sources. The present review emphasizes on phytochemicals and medicinal plant extracts with insulinotropic activity to reduce hyperglycemia. This review also categorized phytochemicals and plant extracts based on their mode of action like insulin secretagogues, insulin mimetics and both.