RADS Journal of Pharmacy and Pharmaceutical Sciences

Virtual Screening, Molecular Docking Study, Characterization, And In-Vitro Antibacterial Evaluation of Piperazine Derivatives

2023-03-09T07:10:32+00:00

Background: Bacterial infections and the dilemma of increasing resistance against the available antibiotics demanded new medicines in this field without the wastage of time and material. Docking has been considered as an In-Silico technology that utilizes computer tools to find and screen most susceptible compounds (ligands) against the target proteins (enzymes) with less time and cost consumption.

Objective: This research plan presentsderivatization as a potential and viable answer to explicate the issues of bacterial resistance by applying In-Silicotools to find new analogues with antibacterial activity.

Methodology: First of all a library of piperazine containing compounds was virtually scrutinized against three antimicrobial enzymes Dihydropteroate synthetase, Isoleucyl transfer RNA synthetase, and DNA gyrasehaving PDB IDs 2VEG, 1JZQ, and 3TTZ, respectively using Molecular Operating Environment (MOE version 2015.01) software. Five compounds were selected from the docking study which were then further obtained and explored for their antibacterial potential by KirbyBauer method.

Results: It was observed that almost all the five compounds were effective in inhibiting the growth of tested bacterial strains. Compound C-1, C-3 and C-4 were proved to be the most active antibacterial agents who could be related to their docking score as well as to the binding of ligand at the binding pocket site.

Conclusion: The outcomes of the present study are encouraging enough to support the use of In-Silico tool and derivatization in the rapid discovery of antibacterial agents to overcome the problem of bacterial resistance.

Characterization of Modified Tiger Nut (Cyperus Esculentus) Starches: Functional and Physicotechnical Properties

2023-03-09T07:14:35+00:00

Background and Objective: Starches and their modified products have a wide range of applications in pharmaceutical manufacturing and food processing industries. The purpose of this study was to characterize native and modified tiger nut (Cyperus esculentus) starch.

Methodology: The native starch (NCS) was extracted and subjected to acidic (ACS), pre-gelatinization (PCS) and enzymatic (ECS) modifications. The native starch was evaluated for phytochemical and elemental composition and characterized with the modified starches in terms of their physicochemical (organoleptic, chemical test, solubility, pH, amylose-amylopectin ratio, gel formation, moisture content, loss on drying, swelling, hydration and moisture sorption capacities, paste clarity, browning, charring and gelatinization temperatures) and physicotechnical (powder bulk and flow parameters) properties. The thermal and particle characteristics of the starches were also evaluated using differential scanning calorimetry and scanning electron microscopy (SEM), respectively.

Results: The starch extraction yield was 15.60%. Phytochemical and elemental composition were similar to other studies. Modified starches exhibited significantly (p < 0.05) better flow, lower moisture content, increased swelling and hydration capacity and lower gelatinization, browning and charring temperatures. A significant increase in swelling and hydration capacities were observed for ACS and PCS while a significant reduction in water sorption capacity was noticed for ECS. SEM showed differences in particle morphology (sizes, shapes and distribution) between the native and modified starches.

Conclusion: Modification of C. esculentus native starch resulted in products with improved functional and physicotechnical properties in terms of swelling, hydration and water sorption capacities as well as in flowability.

Development and Validation of RP HPLC Method for Simultaneous Determination of Cefoperazone sodium and Sulbactam sodium in Dry Injection

2023-03-09T07:22:58+00:00

Background: Various analytical techniques are attempted for the qualitative and quantitative study of Cefoperazone sodium and Sulbactam sodium in different pharmaceutical dosage forms. These analytical techniques are not, easy, cost effective, eco-friendly and are so much laborious.

Objective: The main objectives of the study was to develop a simple, green, cost-effective, reproducible and precise isocratic RP-HPLC method for Cefoperazone Sodium and Sulbactam Sodium quantitative and qualitative studies in pure and dry injection powder form in compliance with ICH- Guidelines Q2 (R1).

Methodology: The chromatographic separation was carried out on a reversed phase C18 (250mm x 4.6 mm) 5 µm in an isocratic mode using tetrabutylammonium hydroxide solution and acetonitrile (8:3) as mobile phase adjusted pH 4.0 with dilute phosphoric acid and maintained flow rate 1.0 ml/minute at 220 nm. The retention time of Sulbactam sodium and Cefoparazone sodium was 7.4 min and 16.7 min respectively. All HPLC injection volume was 20µl in analysis.

Result: The chromatographic separation was carried out on a reversed phase C18 (250mm x 4.6 mm) 5 µm in an isocratic mode using tetrabutylammonium hydroxide solution and acetonitrile (8:3) as mobile phase adjusted pH 4.0 with dilute phosphoric acid and maintained flow rate 1.0 ml/minute the retention time of Sulbactam sodium and Cefoparazone sodium was 7.4 min and 16.7 min respectively. All HPLC injection volume was 20µl and the retention time for Cefoperazone sodium and Sulbactam sodium was noted about 7.4 min and 16.7 min respectively.

Conclusion: A simple, precise, accurate and cost effective method has been developed by using RP-HPLC. The available method is simple and reliable to determine the Cefoperazone sodium and Sulbactam sodium in different pharmaceutical formulations and in their pure forms.

Study Of Antibacterial and Physicochemical Properties of Local and International Brands of Moxifloxacin Used in Clinical Patient Care in Pakistan

2023-03-09T07:27:12+00:00

Objective: Moxifloxacin antibiotic belongs to fourth-generation fluoroquinolone class and used to treat various Gram-positive and Gram-negative bacterial. The present work designed to evaluate the pharmaceutical quality attributes and antibacterial activity of five different local and international brands of moxifloxacin 400mg tablets (B1-B5) available in Pakistan with different price ranges.

Methodology: Different physicochemical parameters including weight, thickness variation, disintegration time, chemical assay and in vitro dissolution evaluation were performed on above mentioned brands of moxifloxacin. Disk diffusion method (Bauer-Kirby susceptibility test) were also used to evaluate the in-vitro antibacterial activity of these brands on three standard bacterial culture of Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli by micro dilution minimum inhibitory concentration (MIC) assay technique and compared with their respective reference standard (A).

Results: All the brands was found to be similar according to compendial quality standards tested for physicochemical evaluation with more than 90% drug release in 0.1N HCl (pH 1.2). All brands exhibited good in vitro activity (zone of inhibition: 26 – 38 mm) against all the standard cultures in terms of clinical effectiveness despite of little variation in price.

Conclusion: It was concluded that a good pharmaceutical association was observed amongst all the local and international brands of moxifloaxcin and each product were also observed within a particular microbial limits exhibits satisfactory effectiveness required for the treatment of particular infectious disease conditions. This study also help medical practitioner to prescribe alternative antibiotic product to the patients in case of unavailability of the brand and for those who are unable to afford the costly treatment.

Prevalence of Oral Infections and Associated Demographic Factors Among Patients in Benin City Metropolis, Nigeria

2023-03-09T07:31:43+00:00

Introduction: In Nigeria, the incidence of orodental infections and demographics of affected patients are poorly documented. This study aims to evaluate the trends, demographics and comorbidities among patients with oral infections in two study centers in Benin City.

Materials and Methods: This study evaluated five hundred and ninety-eight patients from the outpatient departments in the Dental Clinics of the University of Benin Teaching Hospital and Central Hospital, Benin City, Nigeria. Patient data collected were age, gender, diagnoses, duration of symptoms, preferred chewing side, position of extracted tooth/teeth, and underlying reported health conditions.

Results: A total of 56.86% of our respondents were females. The highest occurrence of oral infections was within the age range of 21-30 years (27.26%). The most encountered diagnoses were periodontitis (55.85%) and caries (19.57%). Retained roots (3.34%) and fractures (6.52%) accounted for non-infectious diagnoses. Comorbid conditions in the population were peptic ulcer, hypertension and/or diabetes mellitus. Time frame for seeking medical care showed that 236 patients reported for care within one week. Other observed time frames were 1-4 weeks (208) and greater than four weeks (154).

Conclusion: Patients between 20-30 years in both sexes were more predisposed to oral diseases with acute apical periodontitis being the most prevalent, followed by dental caries. Peptic ulcer, hypertension and/or diabetes were the coexisting chronic conditions of the study participants.

Anti-Motility and Anti-Diarrheal Activities of Lippia Nodiflora and Withania Somnifera Against Castor Oil and Magnesium Sulphate-Induced Diarrhea in Mice

2023-03-09T07:41:44+00:00

Objective: The ongoing exploration is planned to narrate anti-motility and anti-diarrheal potential of L. nodiflora (LN.Cr) and W. somnifera (WS.Cr) hydro-alcoholic extract and their flavonoids and alkaloids rich fractions in case of castor oil and MgSO₄-mediated diarrhea in mice.

Methodology: Locally collected whole plant of Lippia nodiflora and roots of Withania somnifera were dried, pulverized and soaked into aqueous methanol to get hydro-alcoholic extracts. Alkaloids and flavonoids were separated from dried sample of each plant.

Result: L. nodiflora and W. somnifera showed significant inhibition (56.2 and 52%) of intestinal transport of charcoal like atropine (63%) and intestinal fluid accumulation (68 and 66%) in mice, respectively in dose-dependent manner with dosage range at 100-300 mg/kg. LN.Cr and WS.Cr showed dose-dependent safety in case of castor oil (67% and 63.3%) and magnesium sulphate-mediated diarrhea (69.2 % & 67%) at the highest tested dose of 300 and 200mg/kg, respectively in mice, like loperamide (73%). Isolated alkaloids and flavonoids also brought significant blockage of charcoal meal transit and safety against castor oil-mediated diarrhea.

Conclusion: This work suggested that L. nodiflora and W. somnifera extracts and their isolated alkaloids and flavonoids showed antidiarrheal activity by inhibiting intestinal motility, secretion of fluid and possibly inhibition of autacoids and prostaglandin. Antidiarrheal effects of flavonoids were more pronounced than alkaloids and crude extracts of both plants.

Social Support, Marital Satisfaction, Quality of Life and Locus of Control in Mothers with Chronically Ill and Healthy Children

2023-03-09T07:44:53+00:00

Objective: The present study aims compare social support, marital satisfaction, quality of life and locus of control between mothers of chronically ill and healthy children.

Material and methods: A causal comparative study was carried out on 200 mothers including 100 mothers of chronically ill children and 100 mothers of healthy children; aged between 19 to 55 years (MA=34.24; SD=6.41). The healthy group was blocked and matched on age and gender of the child. Participants were administered The Multidimensional Scale of Perceived Social Support, WHO Quality of Life-BREF, Marital Satisfaction Scale, Rotter’s Locus of Control Scale and Demographic Form, respectively. Results were evaluated using Independent Sample t test, Cohen’s d, and MANOVA. Results: Social support (t=-8.55, p<.05, d=1.21; CI, -21.92 to -13.7), marital satisfaction (t=-4.70, p<.05, d=0.35; CI, -17.43 to-7.12) and quality of life [Environmental F(1,198)= 45.88, p<.00; Physical F(1,198)= 36.44, p<.00; Psychological F(1,198)= 50.65, p<.00; Social F(1,198)= 53.18, p<.00] scores were significantly higher in mothers of healthy children in comparison to mothers of chronically ill children, whereas locus of control scores showed no difference.

Conclusion: The mothers of healthy children reported better social support, quality of life and marital satisfaction in comparison to mothers of chronically ill children. However, locus of control failed to support any statistically significant difference between the two groups.

Screening of Ethanolic Extract for Antioxidant and anti-bacterial Activities of Some Selected Plants from Cholistan Desert

2023-03-09T07:47:38+00:00

Objective: Increase in the drug resistance and development of new strains is a source of discomfort for researchers working in developing countries. For restoration of life and health, it is essential to develop new pharmaceutical products that could replace the resistant antibiotics. Traditional medicine from Cholistan desert plays a novel role in this concern. Plant remedies and their formulations have been used extensively for the treatment of various diseases. Tinospora cordifolia (T. cordifolia) and Moringa olifera (M. olifera) possess different pharmacological activities. The aim of this study is to estimate the antioxidant and antibacterial screening of ethanolic extract of T. cordifolia and M. olifera.

Method: Antioxidant activity was done by DPPH method and anti-bacterial activity was done by agar disk diffusion and well diffusion method. Ciprofloxacin was used as the standard drug.

Results: Antioxidant activity indicates the % inhibition of 79.43345±0.16 and 89.15352±0.9 of T. cordifolia and M. olifera which is comparable with standard (Ascorbic acid) shows percent inhibition 93.74±0.14. Antibacterial activity was done with four gram negative bacterial strains and result was comparable with standard drug. In disk diffusion method ethanolic extract of M. olifera showed maximum zone of inhibition 30mm against Micrococcus Luteus and E coli, and T. cordifoli, and 20mm against Micrococcus Luteus. While in Well diffusion method M. olifera showed maximum zone of inhibition (19mm) against Bordetella bronchiseptica and T. cordifolia 17mm against Micrococcus Luteus. However, the observed zone of inhibition is less than standard Ciprofloxacin zone of inhibition.

Conclusion: It is concluded from the fact that T. cordifolia and M. olifera possess anti-bacterial potential against particular microorganism.