Open Access Original Research Article

Influence of Some Starch Mucilages on Compression Behaviour and Quality Parameters of Paracetamol Tablets

Musiliu O. Adedokun, Oludele A. Itiola

Journal of Pharmaceutical Research International, Page 176-194
DOI: 10.9734/BJPR/2013/2120

Aims: To evaluate the effect of mucilages of natural and pregelatinized forms of trifoliate yams, rice and official corn starch binders on a paracetamol tablet formulation.
Methodology: Natural starches from two trifoliate yam varieties, and rice were isolated and pregelatinized. Both starch forms were then incorporated into a paracetamol tablet formulation as binders. The influence of the binders on compaction of granules and quality of tablets was assessed. Particle, bulk and tapped densities were measured for all the batches of the prepared paracetamol granules. The Heckel and Kawakita plots from which mean yield pressure, Py and another pressure term Pk, which indicates the pressure required to reduce the volume of the granule bed by 50%, were derived respectively. Both were employed to assess the compaction behaviour of the granules. Quality of the compressed tablets was studied using tensile strength, friability, disintegration time and dissolution properties as evaluation parameters.
Results: Pregelatinized starch mucilages generally show lower values of both Py and Pk than natural starch mucilages. Increased concentration of starch mucilage binder also yielded lower values of both Py and Pk. Tablets containing natural starches exhibited higher Tensile strength and lower friability than those formulated with pregelatinized starch binders. Generally, Disintegration time (Dt) and the time taken for 80 % paracetamol to be released (t80) were higher for formulations containing natural starch binders than those containing pregelatinized binders The drug dissolution rate constants k1 and k2, were higher for formulations containing pregelatinized binders.
Conclusion: The results obtained are suggestive of the fact that the use of mucilage of pregelatinized starch (rather than natural starch), as well as increase in concentration of the material, would yield formulations with faster onset of plastic deformation as well as higher total plastic deformation. The experimental starches compared well with the standard official corn starch and may thus be developed as substitutes in some tablet formulations.

Open Access Original Research Article

Anti-Bacterial Effect of Different Fractionations of Acetic Acid Leaf Extract of Parinari curatellifolia

Eze, Henry Tochukwu, Wurochekke, Abdullahi Usman

Journal of Pharmaceutical Research International, Page 195-201
DOI: 10.9734/BJPR/2013/1772

The research was aimed at determining the anti-bacterial effect of different fractions of acetic acid leaf extract of Parinari curatellifolia. The research was conducted in laboratory unit of peace specialist hospital, Yola, Nigeria between May and November, 2011. Different solvent extracts of the leaf were prepared using the soxhlet apparatus. Disc diffusion method was used to test for the anti-bacterial activities of the different solvent extracts. The Minimum Inhibitory Concentration (MIC) of the acetic acid extract which gave the highest zones of inhibition against the microbial isolates used revealed that the MIC for Streptococcus pyogenes and Pseudomonas sp is 5mg/ml while that for Klebsiella sp and Staphylococcus aureus is 50mg/ml The acetic acid extract was fractionated with different solvents using the column chromatography. Four fractions (TiA, TiB, TiC, and TiD) were obtained from the column. Fraction TiC gave the highest zone of inhibition ranging from 10.0±0.6 to 17.3±0.9 against the test organisms. This is significantly (P=0.5) different from the crude acetic acid extract with inhibition zones ranging from 20.0±0.6 to 28.3±0.3. Inhibition zones were measured using a metre rule. Fraction TiB did not have any anti-bacterial activity against all the test organisms. Fraction TiC gave three bands on thin layer chromatography with Rf values of 0.38, 0.36, and 0.23. The activities of the separated fractions were lower compared to the crude extract. This may be due to synergistic effect of various secondary metabolites present in the crude extract. Results were discussed in respect to the anti-bacterial effect of the different fractions.

Open Access Original Research Article

Determination of Antioxidant Activity and Phytoconstituent Screening of Euphorbia heterophylla Linn

Muhammad Athar Abbasi, Hina Saleem, Aziz-ur-Rehman ., Tauheeda Riaz, Muhammad Ajaib

Journal of Pharmaceutical Research International, Page 202-216
DOI: 10.9734/BJPR/2013/1925

Aim: To carry out qualitative determination of phytochemicals and evaluate antioxidant potential of Euphorbia heterophylla Linn.
Place and Duration of Study: Department of Chemistry, Government College University Lahore, Pakistan, between October, 2011 and February, 2012.
Material and Method: The methanolic extract of the plant was dissolved in distilled water and partitioned with n-hexane, chloroform, ethyl acetate and n-butanol sequentially. The antioxidant potential of all these fractions and remaining aqueous fraction was analyzed by these methods: 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging activity, total antioxidant activity, Ferric Reducing Antioxidant Power (FRAP) assay, Ferric Thiocyanate (FTC) assay while Folin-Ciocalteu colorimetric method was used to analyse total phenolic content. Phytochemical analysis were performed on the plant extracts to detect the presence of secondary metabolites.
Results: Phytochemical screening revealed phenolics and flavonoids in abundance in chloroform soluble fraction, ethyl acetate soluble fraction and n-butanol soluble fraction. Also the ethyl acetate soluble fraction, n-butanol soluble fraction and remaining aqueous fraction contained saponins and sugars. Terpenoids were detected in all other fractions except the aqueous fraction. Alkaloids were determined in ethyl acetate and n-butanol soluble fraction only while tannins and cardiac glycosides were present in n-butanol soluble fraction and ethyl acetate soluble fraction respectively. Antioxidant assays revealed that Ethyl acetate soluble fraction exhibited highest percent inhibition of DPPH radical i.e. 80.09±0.87% at a concentration of 120 μg/ml as compared to other fractions. IC50 value of ethyl acetate fraction was found to be 36.85±1.8 μg/ml relative to ascorbic acid having IC50 value 58.8±0.89 μg/ml. It also showed the highest value of total antioxidant activity i.e. 0.918±0.08 as well as highest FRAP value 200.05±0.4 TE μM/ml, highest amount of total phenolic compounds (190.1±1.21 GAE mg/g) and highest percentage of inhibition of lipid peroxidation (54.23±0.57%). Chloroform soluble fraction showed IC50 value of 149.84±1.02, total antioxidant activity 0.739±0.06; FRAP value115.15±0.2 μM/ml, total phenolic content 137.1±1.4 GAE mg/g and 41.31±0.53% percent inhibition of lipid peroxidation. n-Butanol soluble fraction showed IC50value of 117.67±0.7, total antioxidant activity 0.532±0.03, FRAP value127.5±0.9 μM/ml, total phenolic content 93.5±0.3 GAE mg/g and 32.15±0.9% percent inhibition of lipid peroxidation. n-Hexane soluble fraction showed IC50 value of 769.7±1.5, antioxidant activity 0.174±0.07, FRAP value 98.26±0.8 μM/ml, total phenolic content 19.5±1.23 GAE mg/g and 12.09±0.8% percent inhibition of lipid peroxidation. Aqueous fraction showed IC50 value of 669.3±1.04, antioxidant activity 0.152±0.041; FRAP value 68.7±0.3 μM/ml, total phenolic content 36.3±0.9 GAE mg/g and 25.01±0.96% percent inhibition of lipid peroxidation.
Conclusion: Ethyl acetate soluble fraction was found to be rich in natural antioxidants and a good source of phytochemicals.

Open Access Original Research Article

A Study of Some Effects of Aqueous Extract of Neem (Azadirachta Indica) Leaves on the Lead Acetate Induced Neurotoxicity in the Superficial Layers of Superior Colliculus of Adult Wistar Rats (Rattus norvegicus)

Fakunle Ponle Bamidele, Ajibade Adeshina John, Oyewo Emmanuel Bukoye, Adeyemi Oluwaseun Hannah

Journal of Pharmaceutical Research International, Page 217-231
DOI: 10.9734/BJPR/2013/2344

Aim: To investigate some neuroprotective effects of aqueous extract of Neem leaves against damaging actions of lead acetate induced neurotoxicity in the superficial layers of the superior colliculus of adult wistar rats.
Study Design: Histological and Biochemical study.
Place and Duration of study: Department of Anatomy, Faculty of Basic Medical Sciences, LAUTECH, Nigeria between January 2012 and August 2012.
Methodology: 40 adult wistar rats (average weight 200±16.2g) were randomly assigned into 4 groups (N=10) of Control C, Treatments T1, T2 and T3 and treated with distilled water, 1% lead acetate and 200mg/kg b.wt of aqueous extract of neem, 1% lead acetate, and 200 mg/kg b.wt of aqueous extract of neem respectively for14days.They were sacrificed by cervical dislocation and processed for routine histopathological studies, bioassay of some antioxidant parameters as well as lipid peroxidation.
Results: Statistically significant (P=0.05) body weight, wet brain weight as well as neuronal cell loss was recorded in T2 while T1 and T3 showed statistically insignificant weight loss compared to control. Oxidative stress enzymes Superoxide dismutase, Glutathione reductase and Glutathione peroxidase levels were significantly (P=0.05) reduced in T2 compared to the control but relatively increased in T1 and T3. T3 and T1 respectively recorded 65% and 55% increments above T2 in Glutathion levels while Lipid peroxidation level was drastically reduced in T3 and to some extent in T1 compared to increased level in T2. Group T2 showed sparsely distributed pyknotic pyramidal neurons with obliterated soma and few glial cells while T1 sections appeared less distorted. Neem offers some ameliorative protection to the pyramidal neuronal and glial cells of the superficial layers of the superior colliculus against lead compared to T2, however the control and T3 sections relatively appeared normal.
Conclusion: Neem offers ameliorative protection to the pyramidal neuronal and glial cells of the superficial layers of the superior colliculus against lead acetate induced neurotoxicity in wistar rats and also further affirms its antioxidative potential.

Open Access Original Research Article

Prasarani Sandhan, a Polyherbal Preparation, Shows Anti-nociceptive and Anti-inflammatory Activities

Mehdi Bin Samad, Ashraf-ul Kabir, Ninadh Malrina D’Costa, J. M. A. Hannan

Journal of Pharmaceutical Research International, Page 232-246
DOI: 10.9734/BJPR/2013/2310

Aims: Prasarani Sandhan (PRS) is an Ayurvedic formulation approved by the “National formulary of Ayurvedic Medicine 2011”, of Bangladesh. It is traditionally used in arthritic pain, lumbago and sciatia. Sparse scientific evidence is available to support the efficacy of this preparation. Hence, we planned to document scientific evidences of the pharmacological activity of this preparation.
Study Design: Our present study aims to elucidate the probable anti-nociceptive and anti-inflammatory mechanisms of PRS.
Place and Duration of the study: The experiments were performed at the pharmacology lab of North South University during the period of October 2010 to July 2011.
Methodology: Two thermal anti-nociceptive models were used, the hot-plate test and tail immersion test, to find out the possible role of the central nervous system in its action. Three in-vivo analgesic and anti-inflammatory models, carrageenan induced paw edema, acetic-acid writhing, and formalin induced paw lick tests, were carried out to test its potential anti-inflammatory and peripheral analgesic properties.
Result: The study of PRS (20mL/kg and 40mL/kg) showed no involvement of the CNS in anti-nociceptive activity of PRS. Carrageenan induced paw edema and acetic acid writhing tests both gave significant results (P=.05), indicating possible peripheral analgesic and anti-inflammatory action. Formalin induced paw-licking test (with and without naloxone co-administration), a differentiator of nurogenic pain (CNS modulated) and inflammatory pain (peripheral nociception), showed that PRS had significant effect in suppressing inflammatory pain (P=.05) but not neurogenic pain.
Conclusion: Compiling the results of the experiments, it can be reported that PRS has anti-inflammatory and peripheral analgesic action.

Open Access Original Research Article

Combined Oral Arginine and Monosodium Glutamate Exposure Induces Adverse Response on the Prostate Function and Testis Histology of Rats

Egbuonu A. C. Cemaluk, Ejikeme P. Madus, L. U. S. Ezeanyika, O. Obidoa

Journal of Pharmaceutical Research International, Page 247-258
DOI: 10.9734/BJPR/2013/2172

Aims: This study investigated the effect of exposure to arginine (ARG) and glutamate (GLU), or its variant, monosodium glutamate (MSG) on the prostate function and testis histology of rats.
Study Design: Exposure to either ARG, GLU, monosodium glutamate (MSG), ARG plus GLU or ARG plus MSG was per oral for 4 consecutive weeks. On the last day of the experiment, rats were food-deprived for 15 h before collecting their blood and testis samples.
Place and Duration of Study: Department of Biochemistry and Department of Veterinary Pathology, University of Nigeria Nsukka, Nigeria, between June 2005 and June 2006.
Methodology: Total and prostatic acid phosphatase activities in serum were determined by the method of Walter and Schutt. Testis sections were stained and mounted using haematoxylin and eosin (H&E), for histology.
Results: On comparison with control, the results showed that ARG, GLU, or arginine together with monosodium glutamate (ARG+MSG) induced a significant (p<0.05 and p<0.01) elevation whereas, ARG+GLU caused a reduction (p<0.05 and p<0.01), in serum total acid phosphatase (TAP) and prostatic acid phosphatase (PAP) activities. MSG-induced reduction in TAP activity (20.76 ± 0.18 I.U/L), however, was not statistically significant (p>0.05 and p>0.01). Histological examination of the testis sections revealed varying degree of degeneration characterized by necrosis in ARG+GLU and ARG+MSG groups relative to control and ARG, GLU or MSG groups.
Conclusion: Results may indicate variable treatment related adverse effect on the prostate function and the testis histology of the rats. The possible effect, however, appeared higher following concomitant exposure to ARG and MSG. Thus, caution should be exercised in the simultaneous ingestion of arginine and monosodium glutamate in animals. Further work however, is required to address some shortcomings (including small sample size) of this study to validate reliability.

Open Access Original Research Article

Stability Indicating Methods for Determination of Nalbuphine- Hydrochloride

M. M. Fouad, S. A. Abdel Razeq, Z. A. Elsayed, L. A. Hussin

Journal of Pharmaceutical Research International, Page 259-272
DOI: 10.9734/BJPR/2013/2443

Three simple, sensitive and reproducible spectrometric methods for the selective determination of nalbuphine–HCl in presence of its oxidative degradate were investigated. The first method depended on the quantitative densitometric evaluation of thin layer chromatograms of the drug at 284 nm using chloroform–methanol–acetic acid (7:3:0.05 v/v/v) as a mobile phase, in a concentration range of 10-30 µg/spot. The second one used the pH induced difference absorbance (∆A) between 0.1M NaOH and 0.1 M HCl drug solutions at 299 nm to determine 20-160 µg mL-1 of the drug. The third method was a bivariate calibration algorithm for the determination of nalbuphine–HCl over concentration range of 20-200 µg mL-1. The proposed methods selectively analysed the drug in presence of up to 80% of its oxidative degradate with mean recoveries of 100.63±1.03 for densitometric method and up to 90% with recoveries of 99.97±1.16 and 100.09±1.47% regarding the two other methods, respectively. The three proposed methods were successfully applied to analyse nalbuphine– HCl in its preparations, the results obtained were statistically analysed and found to be in accordance with those given by the compendial method.

Open Access Original Research Article

Ethanopharmacological and Phytochemical Aspects of Ocimum sanctum Linn- The Elixir of Life

Baby Joseph, Vrundha M. Nair

Journal of Pharmaceutical Research International, Page 273-292
DOI: 10.9734/BJPR/2013/2433

Ocimum sanctum Linn. (Tulsi), a sacred and traditional medicinal plant of India which belongs to the family Lamiaceae possesses innumerable health benefits and therefore regarded as the “Elixir of Life”. The entire plant body including its leaves, stem, root, inflorescence and seed are proved to be significant medicinal value and hence it is one among the inevitable plant used in the preparation of various ayurvedic pharmacological products. The plant is a rich source of various components including eugenol, Vicenin- 2, linoleic acid, oleic acid, rosmarinic acid, Ocimarin, isorientin, orientin, isovitexin, aesculectin, aesculin, chlorgrnic acid, galuteolin, circineol, gallic acid, Citronellal, Camphene, Sabinene, Dimethyl benzene, Myrecene, Ethyl benzene, Limocene, Vitamin C, Calcium, Phosphorous and many more. The plant truly deserves the title ‘Elixir of Life’ due to its Ethanopharmacological properties such as Anti- diabetic, Anti- cancerous, Analgesic, Anti- inflammatory, Radiopreotective, Hepatoprotective, Anti- microbial, Immunomodulatory effect, cardioprotective, Anti- coagulant, Anti- fertility, Anti- oxidant, Neuroprotective and the line-up found to be multitudinous. This review elucidates in- depth literature survey particularly focussing the phytochemical constituents of Tulsi as well as extrapolating its Ethanopharmacological property.

Open Access Review Article

Methodological Challenges in Observational Research: A Pharmacoepidemiological Perspective

Ayad K. Ali

Journal of Pharmaceutical Research International, Page 161-175
DOI: 10.9734/BJPR/2013/2838

Pharmacoepidemiology is the science of studying the effects of utilizing pharmaceutical and biological products in the population, and in most cases this science is conducted in observational epidemiological designs, including retrospective database analysis. Observational pharmacoepidemiology is associated with a myriad of methodological challenges that affect study conclusions and related causal inferences. However, if these challenges are addressed and effectively dealt with, observational studies can have important and impactful clinical, regulatory, and public health outcomes. This article examines common challenges in retrospective database analysis and serves as an introductory text to important methodological concepts in research involving medication use, including confounding by indication, time-dependent confounding, informative censoring, depletion of susceptibles, and immortal time bias.