Anil Bhandari

Synthesis and evaluation of some new benzothiazole derivatives as potential antimicrobial agents

As benzothiazole has proven to be good antimicrobial agent, a novel series of Schiff bases of benzothiazole derivatives were synthesized. Thus condensation of 5-[2-(1,3-benzothiazol-2-yl-amino) ethyl]-4-amino-3-mercapto-(4H)-1,2,4-triazole 5 with appropriate aromatic aldehydes afforded 5-[2-(1,3-benzothiazol-2-yl-amino)ethyl]-4-(arylideneamino)-3-mercapto-(4H)-1,2,4-triazoles 6a-g. Structures of the synthesized compounds were elucidated on the basis of elemental analyses and spectral data. All the synthesized compounds were screened for their antimicrobial activity.

Preparation, characterization and permeation studies of a nanovesicular system containing diclofenac for transdermal delivery.

Abstract Context: Transdermal formulations contain permeation enhancer which causes skin damage. Ceramide 2 is natural lipid found in stratum corneum (SC). Objective: Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, cholesteryl sulfate were formulated and analyzed for physical and biological properties. Diclofenac was used as a model drug. Materials and method: The vesicles were prepared using the film hydration method and characterized for physical parameters, in vitro drug release, accelerated stability studies and formulated into gel. Respective gels were compared with a commercial formulation (CEG) and plain carbopol gel (CG) containing drug for ex vivo, in vivo drug permeation and anti-inflammatory activity. Results: The vesicles were stable with optimum physical parameters. DCG-1 showed 92.89% in vitro drug release. Ceramide vesicles showed drug release between 18 and 25 μg/cm2 whereas CG and CEG released 0.33 and 1.35 μg/cm2 drug, respectively. DCG-1 and CEG showed corresponding Cmax at 6 and 4 h, respectively. DCG-1 showed six times AUC than CEG. DCG-1 inhibited edema by 86.37% by 4th hour of application. Discussion: The presence of ceramide 2 specifically promotes the drug permeation through SC and dermis and also contribute towards stability and non-irritancy. Conclusion: The composition of the nanovesicle played an important role in physical properties and drug permeation.

Pharmacist involvement in the patient care improves outcome in hypertension patients

Objective: The main objective of this study was to assess the effects of pharmaceutical care interventions in patients with essential hypertension in Lakshmi Pat Singhania Institute of Cardiology, Kanpur, India. Methods: The study was carried out from July 2010 to August 2011. Pharmaceutical care was provided for 54 patients (intervention group) which was comprised of the patient education, the prescription assistance and the life style modifications and motivation for health. Then the clinical outcome as well as health related quality of life (HRQOL) were compared with the control group (48 patients) in which the pharmaceutical care was not provided. Furthermore, the effect of pharmaceutical care intervention on HRQOL was assessed using Short Form-36 (SF-36), a general health related quality of life questionnaire used to evaluate the QOL of patients. Blood pressure (BP) measurements and QOL survey was performed at baseline and at the follow-up session. Findings: The difference between blood pressure readings from the baseline to the second follow-up was significant for systolic [(P = 0.0001), 12.24 mmHg] and diastolic BP [(P = 0.001), 5.17 mmHg] in the intervention group. The questionnaire used to evaluate the QOL of patients also showed improvement in the mean score for intervention group. Conclusion: Results from our study showed that applying pharmaceutical care to hypertensive patients can help in the control of these patients’ blood pressure, and consequently lower the risk that hypertension poses in cardiovascular disease. Successful implementation of pharmaceutical care has the potential to increase patients’ satisfaction with their pharmacists’ activities and may increase patients’ expectations that pharmacists will work on their behalf to assist them with their healthcare needs.

Polymers for colon targeted drug delivery

The colon targeted drug delivery has a number of important implications in the field of pharmacotherapy. Oral colon targeted drug delivery systems have recently gained importance for delivering a variety of therapeutic agents for both local and systemic administration. Targeting of drugs to the colon via oral administration protect the drug from degradation or release in the stomach and small intestine. It also ensures abrupt or controlled release of the drug in the proximal colon. Various drug delivery systems have been designed that deliver the drug quantitatively to the colon and then trigger the release of drug. This review will cover different types of polymers which can be used in formulation of colon targeted drug delivery systems.

Strychnos nux-vomica seeds: Pharmacognostical standardization, extraction, and antidiabetic activity.

Background: Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite. Objective: The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed. Materials and Methods: Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard. Results: Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected. Conclusion: S. nux-vomica extracts show antihyperglycemic activity in experimental animals.

A pharmacological evaluation of antidiarrhoeal activity of leaves extract of Murraya koenigii in experimentally induced diarrhoea in rats

Abstract Objective To evaluate anti-diarrhoeal activity of aqueous and alcoholic extract of the leaves of Murraya koenigii (M. koenigii)by using models of castor oil induced diarrhoea, charcoal meal test and PGE2 induced diarrhoea. Methods Alcoholic extract (400 mg/kg) and aqueous extract (200 mg/kg) of leaves of Murraya koenigii were used with loperamide as standard. Albino Wistar rats of both sexes weighing between 150–250 g were used for the anti-diarrhoeal activity. Results The result suggested that it could act centrally and inhibit the PGE2 to give anti-diarrhoeal effects. Result of charcoal meal test also suggested its anti-muscarnic activity. Conclusions These findings indicate that aqueous extract of the leaves of M. koenigii displays good anti-diarrhoeal activity, corroborating the folk use of M. koenigii preparations and contributing for its pharmacological validation.

SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF PYRIDAZINONE DERIVATIVES

Two series of pyridazinone derivatives (19-34) were synthesized and evaluated for antitubercular activities against Mycobacterium tuberculosis H 37 Rv strain. The results illustrated that among the synthesized compounds, compound 25, 5-(4-hydroxy-3-methoxybenzyl)-3-(4-chloro-phenyl)-1,6-dihydro-6-pyridazinone emerged as a lead compound with good antitubercular activity. Four more compounds, (21, 22, 29 & 33) were significant in their antitubercular action.

Correlation of haloperidol levels between saliva and plasma of acutely ill schizophrenic patients.

OBJECTIVE Clinical usefulness of monitoring haloperidol in salivary samples based on plasma:saliva correlation. DESIGN AND METHODS Plasma and saliva samples of schizophrenic patients [N=105] were analyzed by highly sensitive reverse phase liquid chromatographic method to measure haloperidol at 240 nm using UV-PDA detector. Mobile phase consist of acetonitrile and water [50:50], pH 2.5 (0.1% acetic acid and 0.05 M KHPO(4)) at flow rate 1.4 mL/min. Method was linear over 3-200 ng/mL. RESULTS Observed therapeutic range was 5-19 ng/mL [11.66±3.97] and 17-54 ng/mL [27.52±11.51] for plasma and saliva respectively. Mean S:P was found to be 2.36. CONCLUSION Current study showed significantly high correlation [r=0.93, p<0.0001] between haloperidol levels in saliva and plasma with linear relationship. It is therefore concluded that monitoring of salivary concentration can be a clinically beneficial substitute. Patients showing clinical improvement [N=90] were within salivary concentration range of 17-54 ng/mL, which can be an appropriate steady state monitoring range for haloperidol in saliva.

Antihyperglycemic and antihyperlipidemic effects of Salvadora persica in streptozotocin-induced diabetic rats.

Abstract Context: Many synthetic antidiabetic components show toxic and/or mutagenic effects. Hence, attention has been given to naturally occurring antidiabetic components. Identification of effective antidiabetic components from plants origin is an ideal strategy for new drug development. The fresh root, bark, and leaves of Salvadora persica L. (Salvadoraceae) have been used in folk medicine for the treatment of a wide range of medical problems such as cough, asthma, scurvy, piles, rheumatism, leprosy, and gonorrhea disorders. Objective: The S. persica root extract was investigated for the reduction of the risk of diabetes in diabetic rats. Material and methods: The hydro-alcoholic root extract, 200 and 400 mg/kg, was fed to streptozotocin-induced diabetic rats for 21 d. Blood serum glucose, lipid profile, body weight, and food intake were monitored at 0, 7, 14, and 21 d after induction of diabetes. Results: S. persica hydro-alcoholic root extract was not toxic at doses up to 1200 mg/kg. Significant reduction of blood glucose and lipid profile in diabetic rats treated with 400 mg/kg hydro-alcoholic root extract after 21 d versus diabetic control and glibenclamide-treated rats. The glibenclamide and root extract-treated group’s peak values of blood glucose significantly decreased from 281.50 to 106 mg/dL and 285.50 to 150.25 mg/dL, respectively. Hence, in this study, observations showed that root hydro-alcoholic reduced the blood glucose level in diabetic rats but values did not return to normal controls. Conclusion: The research suggests that the root extract was significantly effective when compared with control and standard in the treatment of hyperlipidemia and hyperglycemia in diabetic rats. Therefore, it may be beneficial to diabetic patients.

Pharmacognostic standardization with various plant parts of Desmostachya bipinnata

Abstract Context: Desmostachya bipinnata (L.) Stapf [Gramineae (Poaceae)] has been traditionally used to treat various disorders such as asthma, kidney stone, diarrhea, wound healing, etc. Objective: The present study involves pharmacognostic, botanical, and preliminary phytochemical examination of various plant parts and powders of D. bipinnata. Materials and methods: Leaves, stem, roots, underground and aerial part powders were microscopically examined. Pharmacognostic standardization parameters were determined as per the WHO guidelines. Parameters, including extractive value in different solvents, ash values, and loss on drying, were determined. Preliminary phytochemical studies, fluorescence analysis, and chromatographic profiling were performed for the correct identification of this crude drug and some of its phytoconstituents. Results: Microscopical studies showed various characteristic features including, collateral vascular bundle, bundle sheath cells, and bulliform cells in leaf, conjoint, collateral and closed vascular bundles, and sclerenchymatous sheath in stem; and silica bodies in root. Phytochemical screening and chromatographic profile of aerial plant parts revealed the presence of alkaloids, tannins, flavonoids, steroids, glycosides, and coumarins. Underground plants parts indicated the presence of glycosides, steroids, flavonoids, coumarins, and alkaloids. Discussion and conclusion: The results of the performed studies are helpful in correct identification, characterisation of D. bipinnata. Preliminary phytochemical studies and chromatographic profiling may be helpful in further isolation and purification of lead compounds from different extracts.