Open Access Original Research Article

Optimisation of Alfuzosin Hydrochloride Organogels for Transdermal Delivery

D. Prasanthi, Kuruva Jyothirmai, P. K. Lakshmi

Journal of Pharmaceutical Research International, Page 1-16
DOI: 10.9734/BJPR/2016/24433

Introduction: The purpose of present research was to prepare and optimise alfuzosin hydrochloride (AH) organogels for transdermal delivery using box-behnken design.

Methods: Organogels were prepared by fluid filled fiber mechanism. In box-behnken design, the effect of gelling agent, concentration of gelling agent, apolar solvent and permeation enhancer on flux and Q24 was studied. The prepared organogels were evaluated for physicochemical properties and in vitro diffusion studies, ex vivo permeation, skin irritation and stability studies.

Results: All the formulations have shown better physicochemical properties. Ex-vivo skin permeation studies reveals that, Tween80 based organogel formulated using 70% w/w of Tween80, IPM as apolar solvent and Tween20 as permeation enhancer has shown maximum drug release of 89.53% for 24 hrs with flux of 33.03±0.19 μg/cm2/hr and Q24 of 914.05±1.42 μg/cm2. Modified backward model was the best fit model in box-behnken design. Permeability coefficient, lag time and skin content were found to be 3.303±0.02 cm/hr, 0.45±0.30 hr and 240.66±9.89 μg/g respectively. The transdemal flux was enhanced by 8.34 times over pure drug solution. Skin irritation studies showed irritation potential of ‘0’, thus proving to be non-irritant. The formulations were stable at room temperature for 1 month.

Conclusion: Results suggested that Tween80 based organogels are better carriers for transdermal delivery of AH when compared with soyalecithin and Span80: Tween80 based organogels.

Open Access Original Research Article

Antimalarial Activity of Root Bark Extract and Fractions of Callichilia stenopetala Stapf (Apocynaceae) against Plasmodium berghei in Mice

C. I. Orabueze, S. A. Adesegun, H. A. B. Coker, S. O. Ogbonnia, D. Ota

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/22979

Introduction: Malaria is a life threatening disease caused by infection of red cells by Plasmodium parasites and is very prevalent due to emergence of resistance to the parasites. The plant Callichilia stenopetala Stapf (family Apocynaceae) is commonly used by traditional practitioners in South-East part of Nigeria as a remedy for the treatment of malaria, “re-current” fever and other ailments. The aim of this study was to investigate antimalarial activities and phytochemical constituents of this plant.

Methods: The methanol extract of root bark of Callichilia stenopetala was suspended in water and partitioned between hexane, chloroform and ethyl acetate successively to obtain various fractions. A four–day suppressive and curative techniques were used to determine parasite inhibition. Antiplasmodial effect of the crude extract and the fractions against early infection was evaluated in chloroquine sensitive Plasmodium berghei berghei NK-65 infected mice. The two most active chemosuppressive fractions (hexane and chloroform) were studied for their effect against established infection using curative test procedure. Phytochemical analysis of the extract was carried out using standard procedures and oral acute toxicity in mice was also evaluated. 

Results: The phytochemical analysis showed the presence of alkaloids, saponins, steroidal and phenolic compounds. Anthraquinones and cardiac glycosides were not detected. At a dose of 8000 mgkg-1, no mortalities or evidence of adverse effects was observed in acute toxicity test. The crude extract, the hexane fraction and the chloroform fraction demonstrated intrinsic chemosuppressive antimalarial properties that were dose-dependent. The tested fractions produced significant (p < 0.05), dose dependent activity against the parasite in the curative test compared with the standard drug chloroquine.

Conclusion: The results uphold the folkloric use of C. stenopetala root bark as antimalarial agent. The plant could be considered as a potential source of new antimalarial whose activity resides mainly in the hexane fraction.

Open Access Original Research Article

Amelioration Effect of Emblica officinalis Extract on Ovary in Endosulfan Induced Swiss Albino Mice

Preety Sinha, Arti Kumari

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/17669

Background: In the present time use of pesticides has become very common by the farmers for the better yield of crops. Endosulfan, a chlorinated cyclodiene insecticide, is widely and very liberally used in agricultural sector. But it has created deleterious effects on human health.  

Objective: In the present study amelioration effect of Emblica officinalis (E. officinalis) extract on ovary in Endosulfan induced Swiss albino mice was studied.

Materials and Methods: Three groups were formed, each with six mice. The control group of mice received distilled water as drinking water. The second group was exposed to Endosulfan @ 3 mg/kg body weight daily for 6 weeks by Gavage method. The third group was exposed to Endosulfan @ 3 mg/kg body weight daily for 6 weeks followed by 6 weeks exposed to E. officinalis (100 mg/kg body weight) extract. Animals were sacrificed after the schedule treatment.

Results and Discussion: Light microscopic observations showed various histopathological deformities in sections of treated ovary and improper development of follicle such as detached ova and degeneration of follicular cells due to Endosulfan exposure were also found. The present studies also indicate that alterations were found to be significantly ameliorated in E. officinalis extract treated group.

Conclusion: It may be concluded from this study that E. officinalis have a potent capacity to control Endosulfan induced toxicity.

Open Access Original Research Article

Effect of Vitellaria paradoxa Stem Bark Ingestion on Kidney Functions in Wistar Rats

A. S. Mainasara, T. Oduola, U. Musa, A. S. Mshelia, A. O. Muhammed, A. S. Ajayi

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/24996

Background: Vitellaria paradoxa is used in the treatment of different diseases in several parts of Nigeria without regard for its safety.

Aim: This study was aimed at investigating the effect of ingestion of Vitellaria paradoxa stem bark extract on the kidney functions in Wistar rats.

Place and Duration of the Study: The study was carried out in the Department of Chemical Pathology, Faculty of Medical Laboratory Sciences, Usmanu Danfodiyo University, Sokoto, Nigeria.

Methods: The oral acute toxicity (LD50) of the extract was determined in 30 Wistar rats divided into six of five per group. Group 1 was the control and received distilled water. Different doses of 5, 50, 300, 2000, and 5000 mg/kg were administered once to the study groups (2, 3, 4, 5 and 6) respectively. A sub-chronic toxicity study was carried out in 30 Wistar rats, divided into six of 5 rats per group. Group 1 served as control and was given distilled water and standard rat pellets. The remaining 5 groups were administered different doses of 50, 100, 200, 300 and 400 mg/kg of the extract respectively daily for 30 days. Urea (Ur), Creatinine (Cr), Sodium (Na+), Potassium (K+), Chloride (Cl), and Bicarbonate (HCO-3) were assayed using standard techniques. Body weights of the rats were taken twice weekly.

Results: No mortality or signs of toxicity were recorded in the rats after 24 hours and up to 14 days post-oral treatment, an indication that LD50 of the extract is greater than 5000 mg/kg. In sub-chronic toxicity study, the results did not show treatment-related abnormalities in all the parameters. There were no significant differences (p>0.05) in the values of the control and test groups with the exception of urea which was significantly lower (p<0.05) in groups 3(3.67±0.55), 4 (3.53±0.65), 5(2.90±0.80) and 6(5.0±0.69) than the control group (6.27±.31) but were within the reference range. Weekly body weights of the rats showed no significant differences (p>0.05) between the control and the test groups. Histology results revealed normocytic normochromic cells.

Conclusion: From our findings, ingestion of Vitellaria paradoxa stem bark extract produced no harmful effect on kidney function in Wistar rats.

Open Access Original Research Article

Phytochemical and Antibacterial Studies on Aqueous Ethanol Extract of Thesium viride (Santalaceae)

S. Shehu, M. S. Abubakar, G. Ibrahim, U. Iliyasu

Journal of Pharmaceutical Research International, Page 1-6
DOI: 10.9734/BJPR/2016/23046

Thesium viride Hill (Santalaceae) is a sub-shrub hemiparasite that grows up to 45 cm tall and widely distributed in Europe, Asia and Africa. It is used ethno medicinally in ulcer, jaundice and splenomegally. Phytochemical screening was carried out on the aqueous ethanol extract of the whole plant by using standard phytochemical methods. Antibacterial studies were also carried out on the aqueous ethanol extract by using diffusion method and broth dilution methods. The aqueous ethanol extract of the plant was found to contain alkaloids, flavonoids, anthraquinones, saponins and cardiac glycosides. The aqueous extract was found to be active against Staphylococcus aureus, Streptococcus faecalis, Escherichia coli, Helicobacter pylori and Shigella dysenteriae and had minimum inhibitory concentrations (MIC) of 10, 5, 5, 5, and 5 mg/ml and also minimum bactericidal concentration (MBC) of 20, 20, 20, 10, and 10 mg/ml respectively. The extract was also found to be inactive against Corynbacterium ulcerans and Salmonella typhii. Zones of inhibition produced by aqueous ethanol extract of plant were less than those produced by ciprofloxacin (5 μg/ml). The aqueous ethanol extract of the plant could serve as an antibacterial agent on the sensitive bacteria based on the study.

Open Access Original Research Article

An Observational Prospective Study on Prevalence and Monitoring of Adverse Drug Reactions in Tertiary Care Teaching Hospital

Sneha Gangisetty, Sowmya Nadendla, Prem kumar Goka, Zahedabano ., N. Lakshmi Prasanthi, Nallani Venkata Rama Rao, Rama Rao Nadendla

Journal of Pharmaceutical Research International, Page 1-9
DOI: 10.9734/BJPR/2016/24288

Objective: To study the prevalence of ADRs in the in-patient departments of General Medicine, Pediatrics, Dermatology at tertiary care hospital.

Materials and Methods: An Observational Prospective Study was designed from February to July 2015 in which Prevalence of ADR was calculated. A total of 107 ADR’s were observed from 1334 patients. ADR’s were evaluated for causality by WHO-UMC Scale, Naranjo’s scale, Severity by Hartwig & Siegel scale, Preventability by Schumock & Thornton and classification by Rawling & Thompson criteria.

Results: Prevalence of ADR’s was found to be 8.02% and male to female ratio was 0.81. ADR’s mostly occurred in the age group 31-40 (27.10%). Skin was found to be the most commonly affected organ system (24.29%) among which rashes and urticaria were the most common type of ADR’S reported, majority of the adverse drug reactions were due to Antimicrobials (22.42%). For Casuality of ADR’s according to Naranjo Scale 26.16% of adverse drug reactions were assessed to be probable, using WHO-UMC scale 33.64% were considered as probable. Similarly Severity assessment shows majority of the reactions as moderate (53.27%).

Conclusion: By early detection of adverse drug reactions, necessary action can be taken to prevent mortality & morbidity from such reactions.

Open Access Review Article

A Comprehensive Review on Bioequivalence Studies in Human Subjects

Muhammad Zaman, Sherjeel Adnan, Muhammad Farooq, Ali Aun, Muhammad Uzair Yousaf, Ayesha Naseer, Maryam Shareef

Journal of Pharmaceutical Research International, Page 1-8
DOI: 10.9734/BJPR/2016/23976

Aims: Purpose of the current review was to provide information about the bioequivalence and the bioequivalence study steps in human subjects to conduct bioequivalence studies easily as well as to increase the use of alternative generic products and to decrease the healthcare cost.

Methodology: For this review different research and review articles were studied. The steps of bioequivalence studies on human subjects were closely understood.

Bioequivalence gained increasing attention during the last 3 decades after it became clear that marketed products having the same amounts of the drug may exhibit marked differences in their therapeutic responses, which is making difficulties for physicians and pharmacists for choosing therapeutically equivalent drug for patient. Generally, these differences were caused mainly by impaired absorption. Now a considerable body of evidence has accumulated indicating that drug response is better correlated with the plasma concentration or with the amount of drug in the body than with the dose administered. Consequently, on the basis of simple pharmacokinetic concepts and parameters, bioavailability and bioequivalence studies have been established as acceptable surrogates for expensive, complicated and lengthy clinical trials and are used extensively worldwide to establish and ensure consistent quality and a reliable, therapeutically effective performance of marketed dosage forms.

Conclusion: This study provides the basic information and specifications which are required to fulfill while performing the bioequivalence studies.