Open Access Original Research Article

Formulation Development and Application of Natural Clay as Binder in Metronidazole Tablets

M. A. Momoh, E. C. Ibezim, S. A. Chime, M. O. Adedokun, I. V. Onysih, A. L. E. Uzondu, B. B. Kabeletoge, M. K. Maduka

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/7243

Aims: The aim of the work is to study the binder properties of native clay in metronidazole tablets.

Study Design: Extraction of clay, formulation of tablets and in vitro evaluation of the formulations.

Place and Duration of Study: Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka 410001, Nigeria. The study was carried out from August 2011 to September 2012.

Methodology: Granules were prepared by wet granulation using 7.5, 10 and 12.5% w/w clay and gelatin as binders respectively. The pre-compression test was performed on the granules including the flow rate and the loose densities. The tablets were analysed by determining the weight, disintegration time, friability, hardness and drug content. In vitro drug release was also studied in 0.1 N HCl.

Results: Results show that drug content ranged from 195.3 ± 0.07 to 208.2 ± 0.03 mg in all the formulations and show that metronidazole was not degraded by the clay. Tablets hardness range of 2.38 ± 0.55 to 5.99 ± 0.10 kgf for tablets formulated with 12.5 and 10% w/w of clay, while tablets formulated with gelatin had hardness of 5.99 ± 0.10 and 5.69 ± 0.99 kgf. Tablets containing 7.5, 10 and 12.5.5% w/w of clay exhibited disintegration time of 1.4, 3.6 and 24 min while. About 80.3, 58.2 and 36.8% of metronidazole were released from C1, C2 and C3 tablets formulated with 7.5, 10 and 12.5% of clay as binder respectively at 5 min, while 42.1 and 10.1% were released from tablets formulated with 7.5 and 10% w/w of gelatin as binder. Tablets formulated with clay had higher release of drug than those formulated with gelatin (p < 0.05).

Conclusion: Therefore, clay could be used as binder in formulating metronidazole tablets.

Open Access Original Research Article

Ameliorative Effect of Nigella sativa Oil against Paracetamol Induced Hepatic and Renal Damages in Rats

Mohammed Nazer Hasan, Rahat Ali Khan, Mohammed Nasiruddin, Aijaz Ahmed Khan

Journal of Pharmaceutical Research International, Page 1-10
DOI: 10.9734/BJPR/2016/27597

mol (750 mg/kg) only and Group III to IV were test groups treated with Paracetamol (750 mg/kg) and Nigella sativa oil (1 & 2 ml/kg respectively) for 7 days. On 8th day all rats were sacrificed and blood were collected for liver and renal function tests and tissue samples for histo-pathological examination.

Results: Paracetamol caused marked hepatic and renal damages which were prevented by Nigella sativa oil in dose dependent manner.

Conclusion: Nigella sativa oil showed significant hepato- and reno-protection against Paracetamol induced damages.

Open Access Original Research Article

HPTLC Fingerprinting of Phenolic Acids and Assessment of Antioxidant Potential of Pouzolzia bennettiana Wight a Medicinal Plant from Nilgiri Hills

P. N. Preethi, G. Jeya Jothi, Aiyalu Rajasekaran, Ramasamy Arivukkarasu

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28661

Aim: To screen the secondary metabolites, evaluate the antioxidant potential and identify phenolic acids of methanolic extract of leaf and stem of Pouzolzia bennettiana Wight.

Study Design: The study aimed to determine the antioxidant potential using various assays and to identify the secondary metabolites using HPTLC fingerprinting.

Place and Duration of Study: KMCH college of Pharmacy, between April 2015 and December 2015.

Methodology: The methanolic leaf and stem extract of Pouzolzia bennettiana Wight was screened for its phytochemical components, quantitative analysis of phenols and flavonoids, antioxidant activity by DPPH, ABTS, FRAP and TAC assay. Few phenolic acids responsible for antioxidant activity was identified by HPTLC fingerprinting.

Results: The important secondary metabolites such as flavonoids, tannins, terpenoids, saponins and sterols were identified in the methanolic leaf and stem extract along with primary metabolites such as carbohydrates and proteins. The total phenol and flavonoid content of leaf extract was found to be 34.65 µg and 33.36 µg/100 µg of extract respectively whereas stem extract possessed 31.74 µg and 12.58 µg/100 µg of extract respectively. The antioxidant potential of the methanol extract of leaf and stem was evaluated and the leaf extract showed significant activities in all antioxidant assays compared to the reference antioxidant whereas the stem possessed less antioxidant activity. The HPTLC fingerprinting of leaf extract revealed the presence of the following phenolic acids orcinol, ferulic acid, benzoic acid and resorcinol. The stem extract identified phloroglucinol, ferulic acid and resorcinol.

Conclusion: These results suggest that Pouzolzia bennettiana Wight may act as a potential natural antioxidant offering effective protection from free radicals. The antioxidant effect may be due to the presence of phenolic acids. The phenolic acids identified possess various other applications along with antioxidant activity.

Open Access Original Research Article

A Lectin with Larvicidal Potential from the Fresh Leaves of Agelanthus brunneus (Engl.) Van Tiegh Loranthaceae

Imoh I. Johnny, Adenike Kuku, Oludele O. Odekanyin, Simeon K. Adesina

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28577

Aims: This study reports the physicochemical properties and larvicidal activities of a lectin isolated from the leaves of Agelanthus brunneus (Engl.) Van Tiegh with a view to exploring its potential application and usage.

Methods: The fresh leaves were homogenized with PBS and partial purification of the lectin was carried out by gel filtration on Sephadex G-75; physicochemical and biological properties of the purified lectin were also determined.

Results: The results revealed that lectin from A. brunneus leaves agglutinated non-specifically the red blood cells of the human ABO system as well as the rabbit erythrocytes and the haemagglutinating activity was inhibited by lactose. The lectin was stable over a broad temperature range (up to 70°C) and maximum activity was observed in the 3 - 7 pH range. EDTA had no inhibitory effect on its haemagglutinating activity. Lectin activity was found to be maximal when photosynthesis was at its peak. The lectin was found to be toxic on Culex quinquefasciatus (Say) with LC50 of 0.24 mg/ml.

Conclusion: The findings of the present study clearly revealed that the lactose-specific lectin from A. brunneus was an effective larvicidal agent against C. quinquefasciatus mosquito larvae and could be developed as biological control agent.

Open Access Original Research Article

Development of a Monolithic HPLC-ECD Method for the Determination of Ropinirole HCl in Mouse Sera and Dosage Forms

Mohamed Hefnawy, Abdulrhman Al-Majed, Mostafa Mohammed, Sabry Attia, Mohamed Rizk, Rasha Th. El-Eryan

Journal of Pharmaceutical Research International, Page 1-11
DOI: 10.9734/BJPR/2016/28757

Aim: A highly selective, sensitive, and rapid to establish an innovative way to determine Ropinirole HCl in mouse sera and pharmaceutical formulations.

Study Design: High-performance liquid chromatography (HPLC) method with electrochemical detector (ECD) was developed.

Place and Duration of Study: College of Pharmacy, King Saud University, between May 2015 and December 2015.

Methodology: The chromatographic separation was achieved on a reversed phase RP-18e Chromolith Performance column (100 mm × 4.6 mm) with a mobile phase of methanol: 50 mM sodium dihydrogen phosphate (pH 4.5) (10:90, v/v) pumped at a flow rate of 2.0 mLmin-1. Paracetamol was used as an internal standard (IS). Ropinirole HCl and the IS were extracted from mouse sera by using the deproteinisation procedure, followed by injection of an aliquot of the supernatant into the chromatographic system. The separation of the studied drugs was achieved within 3 min.

Results: The proposed HPLC-ECD method was validated for its selectivity, linearity, accuracy, precision, robustness and stability. The calibration curves in serum showed excellent linearity (r = 0.9980) over concentrations ranging from 10 to 2400 ng mL−1 for ROP with limit of detection (LOD) equal to 2.5 ng mL−1 which is lower than those obtained with a UV-VIS detector.

Conclusion: The method was successfully utilised for Ropinirole HCl quantification in mouse sera samples and good recoveries were obtained without interference from endogenous uric acid and dopamine. Moreover, the assay was successfully applied in a pharmacokinetic study. In addition, the proposed HPLC-ECD method was applied in the determination of ROP content in tablet dosage forms, with good recoveries were obtained without interference from their excipients; Na+, K+, Ca2+, Mg2+, lactate, sucrose, lactose and starch.

Open Access Original Research Article

Adsorption Kinetics and Equilibrium of Ciprofloxacin from Aqueous Solutions Using Corylus avellana (Hazelnut) Activated Carbon

Davoud Balarak, Ferdos Kord Mostafapour, Hossein Azarpira

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/29357

The adsorption of Ciprofloxacin (CIP) from aqueous solutions by hazelnut shell activated carbon (HSAC) was studied in a batch adsorption system. Factors influencing CIP adsorption such as contact time (10-180 min), initial CIP concentration (25–200 mg/L), pH (3–11), adsorbent dosage (0.3–3.0 g/L) and temperature (293–323 K) were investigated. The adsorption process was relatively fast and equilibrium was established about 60 min. Maximum adsorption of CIP occurred at around pH 6. A comparison of the kinetic models on the overall adsorption rate showed that the adsorption system was best described by the pseudo second-order kinetics. The adsorption equilibrium data fitted best with the Langmuir isotherm and the monolayer adsorption capacity of CIP was determined as 61.25, 67.39, 73.64 mg/g at 273, 298 and 323 K, respectively. Thermodynamic parameters were calculated for the CIP–HSAC system and the positive value of ΔH0 (3.064 kJ/mol) and negative values of ΔG0 showed that the adsorption was endothermic, spontaneous and physical in nature.

Open Access Original Research Article

Simultaneous Spectrophotometric Determination of Paracetamol and Dantrolene Sodium by Chemometric Methods

Mohammed Salem Rizk, Maha Sultan, Ibrahim Hassan Habib, Dalia Mohamed, Rehab Moussa Tony

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/29078

Aim: Simultaneous determination of Paracetamol (PAR) and Dantrolene Sodium (DAN) in pharmaceutical formulations was carried spectrophotometrically.

Study Design: Two different chemometric techniques namely Partial Least-Squares (PLS) and Classical Least Squares (CLS). In both techniques, a full factorial experimental design was done using three levels and both components in mixtures.

Methodology: This design was used to prepare the concentration data matrix in solvent composed of 2.5 mM NaOH solution. The wavelength range of 220 – 500 nm was chosen with the intervals of Δλ= 1 nm, through which the corresponding absorbance data matrix was measured. Both of the absorbance and concentration data matrices were used to obtain regression. The regression was used for the prediction of the unknown concentrations of PAR and DAN in their mixture. Neither chemical separation steps nor prior graphical treatment of the overlapped spectra was required for this procedure.

Results: The linearity of calibration curve was fulfilled over concentrations of 1-20 and 1.5 – 15 μg/mL for PAR and DAN, respectively.

Conclusion: Validation was done for multivariate methods using both authentic mixtures and pharmaceutical preparations. Assessment of accuracy and precision was done for each method and results were compared.