Open Access Original Research Article

Ethanol Extracts of Terminalia ivorensis (Chev A.) Stem Bark Attenuates the Positive, Negative and Cognitive Symptoms of Psychosis in Experimental Animal Models

Benneth Ben-Azu, Adegbuyi Oladele Aderibigbe, Olusegun Adebayo Adeoluwa, Ezekiel Oluwagbenga Iwalewa

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/28629

Aims: This study was undertaken to evaluate the antipsychotic property of the ethanol extract of T. ivorensis (EETI) stem bark in mice

Study Design: The study used experimental animal models predictive of human psychosis in mice

Place and Duration of Study: Neuropharmacology Laboratory, Department of Pharmacology and Therapeutics, Faculty of Basic Medical Sciences, University of Ibadan, Oyo State, Nigeria, between June 2013 and July 2014.

Methodology: Antipsychotic activity of EETI [125-1000 mg/kg, per os (p.o.)] was assessed based on the inhibition of stereotyped behavior induced by apomorphine (1 mg/kg, i.p.) or ketamine (10 mg/kg, i.p.) and ketamine-induced hyperactivity for positive symptoms in mice. Ketamine-enhanced immobility in forced swim test (FST) and reversal treatment of ketamine-induced cognitive dysfunction for negative and cognitive symptoms in mice respectively, and drug-induced ptosis and catalepsy in mice were also employed to further evaluate the antipsychotic property of EETI.

Results: EETI (125-1000 mg/kg, p.o.) significantly (p<0.05) inhibited apomorphine or ketamine-induced stereotypy, and ketamine-induced hyperactivity. Moreover, EETI significantly (p<0.05) attenuated the enhanced immobility and ameliorated the cognitive dysfunction by ketamine (30 and 20 mg/kg, i.p.), respectively in mice. EETI also dose dependently depleted the monoamine as indexed by the ptosis paradigm, however did not demonstrate cataleptic behavior as indexed on the catalepsy scale which suggest lack of expyramidal symptoms.

Conclusion: This study provides valuable evidence which suggests that T. ivorensis contain biologically active constituents that possess antipsychotic activity. Thus, justifying its ethnomedicinal claims in the management of psychotic disorders.

Open Access Original Research Article

Screening Potential Inhibitors of 11β-hydroxysteroid Dehydrogenase Type 1 for Antidiabetic Drug Development from TCM (Traditional Chinese Medicine) Compound Library

Minh-Quang Bui, Dac-Thanh Van, Ly Le

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2016/27829

Aims: 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) is an enzyme being responsible for converting cortisone to cortisol which promotes gluconeogenesis in the liver and oppose the action of insulin by directly inhibiting β-cell insulin secretion in the pancreas and peripheral glucose uptake in the muscle. The present study was carried out to screen the potential inhibitors of 11βHSD1 for antidiabetic drug development.

Study Design: From Traditional Chinese Medicine (TCM) compounds, there are 30 chosen compounds can be made the antidiabetic drugs by Autodock Vina and MD simulations method.

Place and Duration of Study: Institute for Computational Science and Technology.

Methodology: Screening the compounds from Traditional Chinese Medicine compounds then docking to the refined protein and calculate the predicted Ki.

Results: 30 chosen compounds and their structures can be used as the antidiabetic drug.

Conclusion: The result promises the new antidiabetic drug with low cost, and safer.

Open Access Original Research Article

Immunization Services: Involvement of Community Pharmacies in Lagos State, Nigeria

Fowowe Oluwadamilola, Aina Bolajoko

Journal of Pharmaceutical Research International, Page 1-12
DOI: 10.9734/BJPR/2016/27442

Aims: The aim of this study was to evaluate the current practice of Community Pharmacies in immunization services, and evaluate the level of willingness of Community Pharmacists to participate in immunization services.

Study Design: A cross sectional study design.

Place and Duration of Study: The study was carried out in the metropolitan area of Lagos State, Nigeria, with sixteen (16) local government areas (LGAs) between October 2015 and January 2016

Methodology:

Sampling methods: Systematic sampling method was used. Sample size was calculated to be 203, at 95% confidence level, 5% margin of error and 50% fraction of responses.

Study instrument: Data was collected using a validated self-administered questionnaires which consisted of two sections;   Section A: Demographic Characteristics of respondents.

Section B: Knowledge, attitude and current participation level, willingness and preparedness of Community Pharmacists.

Data analysis: Data obtained were analyzed using Statistical Package for the Social Sciences Version 21. Descriptive analysis and frequency tables were generated for analysis.

Results: The study revealed that Community Pharmacies in Lagos state are to various extents largely involved in immunization services and generally well equipped with most of the required infrastructure to stock vaccines, with a high percentage found to stock and sell vaccines (84.2%).

Also, while the study revealed that only 43.4% could interpret vaccine vial monitors and most (73.6%) knew what vaccine vial monitors were, 96.2% were willing to undergo training to administer vaccines.

Conclusion: Findings of this study show that Community Pharmacies in Lagos state are to various extents already involved in the provision of immunization services, and enrolling Community Pharmacists in the immunization administration is the next big step in improving immunization coverage and vaccine uptake in Nigeria.

Open Access Original Research Article

New Validated Fluorescence Quenching Based Procedure for the Determination of Cilostazol and Clopidogrel in Bulk, Tablets and Biological Fluids, With Application of Stern-volmer Equation

F. Ibrahim, M. Sharaf El-Din, Heba Abd El-Aziz

Journal of Pharmaceutical Research International, Page 1-15
DOI: 10.9734/BJPR/2016/28329

Aims: A very Sensitive, simple and selective Spectrofluorimetric method for the determination of Cilostazol or Clopidogrel through their reaction with fluorescein dye is developed. Determination was performed on raw material, tablet dosage form and extended for determination of cilostazol in spiked human plasma.

Study Design: Quenching reaction between fluorescein dye and tertiary amine containing drugs.

Place and Duration of the Study: This experiment was applied on analytical chemistry lab in faculty of pharmacy, analytical chemistry department, during the period (from 5 April to 10 May, 2016).

Methodology: The formed ion-pair complex between the reagent and each drug results in decrease in the fluorescence intensity of the reagent, this decrease (fluorescence quenching ΔF) is directly proportional to concentration of both drugs at the range of (0.001-0.08 μg ml-1) and (0.01-0.50 μg ml-1) for cilostazol (CIL) and Clopidogrel (CLP), respectively. For cilostazol (limit of detection) LOD is (0.0003μg mL-1) and (limit of quantitation) LOQ is (0.0008 μg ml-1). For clopidogrel LOD is (0.0025 μg ml-1) and LOQ is (0.0076 μg ml-1). The affecting factors on fluorescence intensity of the product are carefully investigated and optimized.  Using the optimized experimental conditions, the proposed quenching method is validated according to International Conference of Harmonization guidelines. The proposed method is perfectly applied to the analysis of commercial tablets containing each drug separately.

Results: Statistical comparisons of the results with those of the reference methods illustrate good agreement and confirm that there was no significant difference in the accuracy and precision between the proposed and reference one for both drugs, respectively. The proposed method is extended for the in vitro determination of CIL in spiked human plasma as preliminary investigation; the mean recovery (n=5) was 99.80.

Conclusion: Owing to the simplicity, quickness and cheapness of the present study, it can be applied for the routine quality control of the studied drug in its dosage forms.

Open Access Original Research Article

Effect of Ciklavit® - a Nigerian Poly-herbal Formulation on the Dissolution Profile of Proguanil Tablets: Potential for Herb-drug Interaction

Moshood O. Akinleye, Ogochukwu U. Amaeze, Omotoke T. Opeodu, Omotunde O. Okubanjo

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/28298

Aim: Herb-drug interaction is a growing concern due to the increasing consumption of herbal medicines among populations globally. Assessment of potential interaction of herbs with concomitantly administered drugs is thus very necessary to ensure patient safety. The aim of this study was to determine the effect of Ciklavit® on the in vitro release profile of proguanil tablets as indicator of potential in vivo herb-drug interaction.

Methodology: Physicochemical characteristics of proguanil tablets namely hardness, friability, weight uniformity, disintegration and chemical assay were evaluated as described in official compendia. In vitrodissolution of proguanil tablets was studied alone and with Ciklavit® in three different dissolution media with pH 1.2, 4.5 and 6.8 respectively using USP dissolution apparatus II at 75 rpm. Analysis of proguanil was done using High Performance Liquid Chromatography coupled with a UV detector. Dissolution data was analyzed and percentage proguanil released in all dissolution media determined; dissolution profiles were compared using a model dependent approach – dissolution efficiency.

Results: Ciklavit® caused 51.6, 61.0 and 57.1% inhibition of proguanil release in vitro at gastro-enteric simulated pH 1.2, 4.5 and 6.8 respectively; this inhibition was statistically significant (P < .001). Release profiles for proguanil alone and proguanil with Ciklavit® showed difference in dissolution efficiency of 56.2%, 64.8% and 59.2% at pH 1.2, 4.5 and 6.8 respectively.

Conclusion: Ciklavit® significantly decreased the dissolution of proguanil tablets at all simulated gastro-enteric pH studied. Further studies are needed to assess herb-drug interaction in vivo.

Open Access Original Research Article

Preparation of Poly(3-hydroxybutyrate) Micro- and Nanoparticles as Hydrophobic Drugs Carrier Using Self-emulsifying Nanoemulsion Method

Rafael A. Bini, Daniel A. Moraes, Laudemir C. Varanda

Journal of Pharmaceutical Research International, Page 1-14
DOI: 10.9734/BJPR/2016/28070

Aims: To correlate the different sizes and morphologies of polymeric particles prepared through the oil-in-water micro- and nanoemulsions.

Study Design: Poly(3-hydroxybutyrate) (PHB) micro- and nanoparticles were prepared using oil-in-water micro- and nanoemulsions based on the sodium dodecyl sulfate (SD) micellar system.

Place and Duration of Study: Chemistry Institute of São Carlos at University of São Paulo, São Carlos, São Paulo, Brazil, between September 2012 and June of 2014.

Methodology: The microemulsion domains of the sodium dodecyl sulfate (SD) micellar system were obtained by the pseudo-ternary phase diagram. The self-emulsifying nanoemulsions were formed by low-energy method by addition of NaCl to SD micellar system. Poly(3-hydroxybutyrate) particles were prepared using the in micro- and nanoemulsion domains determined. The encapsulation of Ibuprofen (IBU) was performed only via nanoemulsion method. The average size and size distribution of both the micellar systems and the polymeric particles were determined by dynamic light scattering (DLS, Zetasizer Nano-ZS, Malvern). The samples also were analyzed using the by Fourier transformed infrared spectroscopy (FTIR Prestige-21), PerkinElmer's LAMBDA 35 UV/Vis Spectrophotometer (Perkin Elmer) and by scanning electron microscopy (Zeiss LEO 440).

Results: Polymeric particles with different sizes and morphologies were prepared through the oil-in-water micro- and nanoemulsions. However, DLS measurements indicated that the precipitation of PHB did not occur inside micelles, but by an interfacial precipitation process. Despite, varying the oil content in microemulsion system, polymeric microparticles were obtained, while nanoparticles with size distribution around with 250-710 nm were prepared in nanoemulsion domain. The nanoemulsion method was used for encapsulating ibuprofen. Results indicated a non-Fickian release profile with biphasic pattern, with release around with 91.4% at 48 h.

Conclusion: The nanoemulsion method presented more suitable than microemulsion for preparing polymeric nanoparticles, as well to encapsulate lipophilic drugs, demonstrating versatility for future applications in biomedical area as versatile carrier.

Open Access Original Research Article

Effect of Drugs Used in the Treatment of Diabetes & Hypertension in Urea & the Creatinine Level in Streptozotocin Induced Diabetes in Rats

Khidir A. M. Hassan

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/25434

Co-morbidity of diabetes and hypertension have severe effects on kidney function, these  effects are due to the elevated pressure in the kidney due to hypertension and the oxidative stress caused by hyper glycemic. Uncontrolled hyperglycemia and hypertension lead to the growth of micro and macro vascular complications. Patients suffering from these diseases usually are treated with calcium channel blocking agents, aspirin and metformin. A combination of medications may have beneficial or adverse effects on the patients. The objective of this study is to see the effect of this combination on kidney function by measuring the serum levels of urea and creatinine in diabetic rats.

Blood samples were studied before treatment and after 10 days and analyzed for urea and creatinine. ANOVA test was done to compare the urea and creatinine levels in rats with STZ induced hyperglycemia after 10 days treatment. In case of urea and creatinine, there was a significant difference (p < 0.000) between the group treated with metformin alone and the control group, (Metformin + Nifedipine) group, and (Metformin + Aspirin) group. Again, there was no significant difference (P > 0.197) in creatinine level between the groups treated with (metformin + aspirin), (metformin + Nifedipine). These results conclude that using metformin when there is kidney dysfunction may aggravate the situation while the combination of metformin with aspirin and or with nifedipine as in case of diabetes associated with hypertension may be beneficial in attenuating the complications of diabetes and hypertension on the kidney, a further study may be needed to confirm this finding.