Open Access Original Research Article

Formulation and Evaluation of Optimized Clotrimazole Emulgel Formulations

Ghada E. Yassin

Journal of Pharmaceutical Research International, Page 1014-1030
DOI: 10.9734/BJPR/2014/8495

Aims: The aim of the present study was to develop an emulgel formulation of Clotrimazole using carbopol 934 or hydroxyl propyl methyl cellulose 2910 as a gelling agent. The influence of the type of gelling agent and the concentration of both the oil phase and the emulsifying agent on the release of the drug and its microbial activity were investigated using 23 factorial designs. In addition, rheological properties were also evaluated.
Methodology: Within the major group of semisolid preparations, emulgel has emerged as a promising drug delivery system for the delivery of hydrophobic drugs. Different emulgel formulations were optimized using a 23 factorial design considering three independent factors at two levels; gelling agent (carbopol 934 and hydroxyl propyl methyl cellulose, liquid paraffin (2.5% and 5%) and emulsifying agent (1.5 and 2.5%). The amount of drug released (Y1) and the antifungalactivity (Y2) were chosen as two dependent responses. The prepared emulgel were also evaluated for their physical properties, pH, drug content and rheological properties.
Results: The prepared emulgel exhibited higher release when compared with canest in cream as a market product. Rheological study revealed that the emulgel exhibited a thixotropic behavior. Candida albicans was used as a model fungus to evaluate the antifungal activity of the prepared formulations achieved using canestin cream as a control. Stability studies revealed no significant differences before and after storage for the selected formula.
Conclusion: It was suggested that Clotrimazole emulgel formulation (F6) prepared using HPMC 2910 as gelling agent, emulsifying agent in its high level and liquid paraffin in its low level was the formula of choice since it showed the highest drug release and the highest antifungal activity.

Open Access Original Research Article

In vivo Antioxidant Activity and Anti Hyperglycemic Relevant Enzyme Inhibition Properties of Petroleum Ether Extract of Traditionaly Processed Ocimum canum Leaves

Alok Kumar Dash, Jhansee Mishra, Deepak Kumar Dash

Journal of Pharmaceutical Research International, Page 1031-1040
DOI: 10.9734/BJPR/2014/8782

Objective: To investigate the antihyperglycemic and antioxidant properties of the petroleum ether extract of Ocimum canum leaves in streptozotocin-induced diabetic rats.
Place and Duration of Study: Pinacle Biomedical Research institute (PBRI), Bhopal april 2013-december 2013.
Methods: Hyperglycemia was induced in rats by streptozotocin (STZ, 45 mg/kg body weight). Three days after STZ induction, diabetic rats received Ocimum extract 100 mg/kg and 200 mg/kg body weight daily for 28days. Glibenclamide (600 µgm/kg) served as reference. Blood glucose levels were measured on every 7th day during 28 days. Serum biochemical parameters such as low density lipoprotein (LDL), very low density lipoprotein (VLDL), high density lipoprotein (HDL), atherogenic index and the activities of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and alkaline phosphatase (ALP) were estimated. Antioxidant enzymes like (catalase (CAT), superoxide dismutase (SOD), reduced glutathione (GSH), serum thiobarbituric (TBAR) were measured in the diabetic rats. Therefore, Ocimum canum demonstrated remarkable antidiabetic activity in STZ induced diabetic rats. The potential antidiabetic action is possible due to its modulation of endogenous antioxidant status.
Results: Administration of the extracts for 28 days caused a significant (P <0.01) reduction in blood glucose levels in diabetic rats. The extracts also improved other altered biochemical parameters associated with diabetes. Furthermore, the extracts have favorable effects on the histopathological changes of the pancreas, in STZ induced diabetic rats. The extracts also showed significant (P <0.05) antioxidant activity.
Conclusions: Ocimum canum possesses antihyperglycemic and antioxidant properties as well as improves lipid profile.

Open Access Original Research Article

Hepatotoxicity of Ethanol Extract of Adenium obesum Stem Bark in Wistar Rats

Samson Eneojo Abalaka, Muhammad Yakasai Fatihu, Najume Doguwar Giginya Ibrahim, Suleiman Folorunsho Ambali

Journal of Pharmaceutical Research International, Page 1041-1052
DOI: 10.9734/BJPR/2014/7667

Aims: Adenium obesum is a known medicinal plant thereby creating the need for the evaluation of its toxicity and histopathological effects on the liver of female Wistar rats orally administered ethanol extract of the plant’s stem bark.
Place and Duration of Study: Department of Veterinary Pathology, Ahmadu Bello University, Zaria, Nigeria, between January 2011 and January 2012.
Methodology: Ethanol extraction of A. obesum stem bark was performed prior to screening it for its phytochemical constituents. Female rats per group were orally administered by gavage pre-defined doses (300mgkg-1, 2000mgkg-1 and 5000 mgkg-1) of the extract separatively in a stepwise procedure and observed for signs of toxicity. Control rats were administered distilled water placebo.
Results: The extract contained some alkaloids, saponins, tannins, flavonoids, glycosides, steroids and triterpens with no anthraquinones. Exposed rats did not show signs of toxicity and neither was there any mortality. Changes in aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase activities were non-significant (p>0.05). Congestion and fatty degenerative changes were seen in the liver of the exposed rats, which were not significantly (p>0.05) different in exposed rats compared to the control.
Conclusion: Adenium obesum did not cause major hepatic damage in the exposed rats and therefore, it is a safe oral medicinal plant within the extract dose and exposure period used in the study.

Open Access Original Research Article

Effect of Low Radiation Dose on Cisplatin Induced Hepato- Testicular Damage in Male Rats

H. A. Fahmy, O. A. Gharib

Journal of Pharmaceutical Research International, Page 1053-1066
DOI: 10.9734/BJPR/2014/8980

Aim: The aim of this study was to evaluate the synergistic effect of low radiation dose with the chemotherapeutic drug in order to find possible way to lessen the harmful effects during chemo-radiotherapy.
Study Design: Randomized controlled experiment.
Place and Duration of Study: Experimental Animal Unit, Drug Radiation Research Department, National Center for Radiation Research and Technology, Cairo Egypt.
Methodology: Estimation of antioxidant activity of low radiation dose on oxidative stress induced by cisplatin administration at a dose of 10 mg/kg b. wt. in male albino rat.
Results: Results of experiment revealed that cisplatin administration caused a significant increase in serum alanine transaminase (GPT) activity (38.58±2.060) and FSH level (8.162±1.424) accompanied with a decrease in serum albumin (3.492±0.253), and Butyry Cholein Esterase (BChE) (65.35 12.61). In Liver and testis, GSH content (68.00±2.391& 24.93±4.778) as well as cytochromes P450 levels (0.3875±0.0727 & 0.2167±0.0459) showed a significant decrease as compared to the normal control level respectively. In addition the level of Fe, Cu and Zn showed no significant changes in liver and appeared to be significantly decrease as in case of corresponding trace elements in testis organs. On the other hand, exposing to low dose of radiation (0.5 Gy) post-cisplatin treatment effectively prevented these alterations and maintained the antioxidant status.
Conclusion: Data from present results revealed that low radiation dose have the existence as an antioxidant and antitumor agents which may be useful to use as a synergistic agents with the chemotherapeutic drug.

Open Access Original Research Article

Ameliorative Effects of Alcohol on Human Diabetic Volunteers – A Prospective Study

B. Venkata Raman, A. Naga Vamsi Krishna, V. Chandra Prakash, M. Pardha Saradhi, L. A. Samuel, G. Uma Ramani, N. Ch. Varadacharyulu

Journal of Pharmaceutical Research International, Page 1067-1078
DOI: 10.9734/BJPR/2014/4857

Aims: The purpose of this study is to assess and confirm the ameliorative effects of alcohol consumption on biochemical indices of blood i.e., blood glucose, HbA1c, NO2, NO3, lipid profiles, hs-CRP (high sensitive C–Reactive protein) and membrane lipid peroxidation of diabetics.
Study Design: Pre-clinical and Biochemical experimental study.
Place and Duration of Study: Department of Biochemistry, Acharya Nagarjuna University and Dept. of Biotechnology, K L University, Guntur, A.P and Dept. of Biochemistry, Katuri Medical College, Katuri Nagar, Guntur, A.P and Dept. of Biochemistry, Sri Krishna Devaraya University, Anantapur, A.P and Dept. of Basic Sciences, Madanapalle Institute of Technology and Science (MITS), Post Box No: 14, Angallu (V), Madanapalle, A. P., India, during 2008– 2013.
Methodology: The study is conducted on 4 groups (n= 1200) of people of different ages ranging from 35 to 50 years at community health centers in Prakasam, Warangal, Srikakulam districts of Andhra Pradesh, India. The first group consists of type-II diabetic patients who have been consuming alcohol (arithmetic mean ranging from 14.16 to 31.61ml/day) moderately for the past 3 to 10 years. The second group consists of non-diabetic, moderately alcohol consuming healthy individuals. The third group consists of patients who are type-II diabetics (who do not drink) taking medical treatment for minimum period of 1 year. The fourth group consists of non-drinking, non-diabetic healthy individuals. Relationships of alcohol intake with lipid profile, hs-CRP and HBA1c are compared among the three groups.
Results: In lipid profile analysis of moderately drinking diabetic group, the HDL levels are found to be higher while the remaining factors such as total cholesterol, LDL, VLDL (P<0.05), triglycerides (P<0.01) and membrane lipid peroxidation are significantly lower. Fasting serum glucose levels are lowered, while serum nitrites and nitrates are found to be significantly higher. These differences are not found in abstainers group and Diabetic group who do not drink.
Conclusion: Moderate consumption of alcohol in diabetic individuals is found to have an inverse association with the risky factors like LDL cholesterol, Triglycerides, etc. that are the etiological factors for some of the sequelae of diabetes mellitus i.e., coronary heart diseases, Retinopathy, etc. and has a direct association with the positive factors such as HDL and nitric oxide production. Experimental results are very significant and indicate that moderate consumption of alcohol has ameliorative effects on diabetics.

Open Access Original Research Article

Effect of Aqueous Extract of Guava (Psidium guajava) Leaf on Blood Glucose and Liver Enzymes in Alloxan Induced Diabetic Rats

Chioma Christiana Ogueri, Ify Elekwa, Victor Chibueze Ude, Amadike Eziuche Ugbogu

Journal of Pharmaceutical Research International, Page 1079-1087
DOI: 10.9734/BJPR/2014/7244

Aim: The aim of this study is to determine the effect of aqueous extract of Psidium guajava leaf on blood glucose level and liver enzymes of alloxan –induced diabetic rat.
Study Design: The animals were grouped into six of 6 rats each. Groups A, B, C and E were induced diabetes by intraperitoneal injection of alloxan monohydrate with a dose of 100mg/kg body weight. The extract was administered through gastric tube per kilogram body weight as follows: group A 200mg/kg, group B 150mg/kg, group C100mg/kg, group D none (normal control), group E none (untreated diabetic control) and group F150mg/kg (extract control).
Methodology: Blood samples were collected by cardiac puncture after fasting overnight and standard methods were used for the extraction of spices, determination of fasting blood glucose and liver enzymes.
Place and Duration of Study: The study was carried out at Abia State University Uturu-Nigeria and the entire experiments lasted between December 2011 and July 2012.
Result: The results showed a significant (P<0.05) decrease in the blood glucose level compared to untreated diabetic control. There was no significant (P<0.05) difference observed in alkaline phosphatase (ALP) and aspartate aminotransferase (AST) activity compared to all the controls (normal, untreated and extract control) while alanine aminotransferase (ALT) activity decreased significantly (P<0.05) compared to untreated diabetic control.
Conclusion: Therefore, this result revealed that aqueous extract of Psidium guajava leaf possess anti-hyperglycemic properties with no side effect on selected liver enzymes compared to normal control and since the leaf did not show interference with functional integrity of the liver tissues it has a better potential for treatment of diabetes.

Open Access Original Research Article

A Comparative Analysis of Electronic Prescribing Near Misses in King Saud Medical City, Riyadh, Saudi Arabia

Dalal S. Al-Dossari, Ibrahim A. Al-Zaagi, Siham D. Al-Saud, Abdullah M. Al-Bedah, Naseem A. Qureshi

Journal of Pharmaceutical Research International, Page 1088-1104
DOI: 10.9734/BJPR/2014/8607

Background: A “near miss” or close call is a medication error that happened but did not result in injury or damage to the patient. These medication errors (MEs) are captured and corrected before affecting the patient either fortuitously or purposefully by designed system controls imbedded in electronic health record (EHR) as well as electronic prescribing systems (EPS).
Objective: This study analyzed the reported electronic prescribing near misses (NMs) in King Saud Medical City (KSMC) in Riyadh city.
Methods: The ME report forms were consecutively collected over a period of one year, from 1 January to 31 December, 2012. These forms were evaluated for data abstraction and a comparative analysis of NMs/NM report forms of first 6-month (n=1025, timeline 1) versus second 6-month (n=2398, timeline 2) was carried out. No systematic intervention prior to timeline 2 was used in this study.
Results: The total number of MEs/NMs report forms was 3423 and total number of reported NMs was 7415, as each form could contain more than one NM. Drug prescription items, medication dispensing stages, NM makers and identifiers, underlying causes, sites of errors, prescribed drugs and suggested actions to avoid NM errors all differed significantly between the two timelines, which could be attributed to natural, real world practices in KSMC.
Conclusion: This prospective study found significant differences in factors related to NMs between two six month periods in a single year. Reasons for these differences between two timeframes remain poorly understood. NMs comparative studies using systematic interventions are warranted in the Kingdom of Saudi Arabia.

Open Access Original Research Article

Fresh and Decayed Stem Juice of Musa acuminata x balbisiana (Musa paradisiaca) Reduce the Force and Rate of Contractility of an Isolated Perfused Rabbit Heart

Oliver Nalumansi, Godfrey S. Bbosa, Aloysius Lubega, Bernadina Onegi

Journal of Pharmaceutical Research International, Page 1105-1115
DOI: 10.9734/BJPR/2014/6529

Background: Decaying stem juice of Musa acuminata × balbisiana is commonly used by local communities and traditional herbalist in Central Uganda in the management of cardiovascular conditions like hypertension.
Aims: The study investigated the ionotropic and chronotropic effect of fresh and decaying stem juice of Musa acuminata × balbisiana on the isolated perfused rabbit heart.
Materials and Methods: Methods.
Study Design: An experimental study.
Place and Duration of Study: Study was done at the Dept of Pharmacology & Therapeutics Pharmacology Lab between December 2012 to March 2013.
Experimental Procedure: An experimental study determined the effects of fresh and decayed stem juices of Musa acuminate X balbisiana on the rate and force of contraction of an isolated rabbit heart using Langendorff’s heart perfusion experiment and methods. The heart rate (beats/minute) was determined. The force of contraction of the heart was determined by measuring the height of each peak on the kymogram.
Results: The force and rate of contractility of an isolated perfused rabbit decreased with increasing doses of the stem juice from 0.156 mg/mL to 100mg/mL for both the fresh and decayed stem juice of M. acuminata. The decrease could be associated with the high [K+] ions that decrease the membrane potential or cause hyperpolarization the myocardial cell membranes leading to reduced force and rate of heart contractility. The effect of the fresh stem juice was short lived and at very high concentrations, it caused a cardiac arrest while the effect of the decayed stem juice was prolonged.
Conclusion: Fresh and decayed stem juice of Musa acuminata × balbisiana have compounds that cause a negative ionotropic and chronotropic effect on an isolated perfused rabbit heart.

Open Access Original Research Article

Renoprotective Effect of Sitagliptin ( Dipeptidyl Peptidase- 4 Inhibitor) aganist Cisplatin Induced Nephrotoxicity in Mice

Amany shalaby, Hala Abdel Malek

Journal of Pharmaceutical Research International, Page 1116-1129
DOI: 10.9734/BJPR/2014/9297

Back Ground and Objectives: Despite the therapeutic benefits of cisplatin (CDDP), its use clinically is often limited due to dose-related nephrotoxicity. On the meanwhile, DPP 4 inhibitors could attenuate kidney injury, so in the present work, it was aimed to investigate the effect of one of DPP 4 inhibitors (sitagliptin) on cisplatin induced nephrotoxicity in mice.
Materials and Methods: 48 male balb-c mice were equally divided into 4 groups, control, sitagliptin group, cisplatin group and cisplatin plus sitagliptin group. The mice were sacrificed at 72h after cisplatin injection. Blood urea nitrogen (BUN) & serum creatinine, renal tissue of antioxidant enzymes, lipid peroxidation, TNF-alpha (TNF-α) were measured as well as histopathological scoring of renal injury.
Results: The results demonstrated that sitagliptin significantly ameliorated the nephrotoxic effect of cisplatin with increased activity of antioxidant enzymes, improved kidney function, renal histopathological scoring and decreased tissue level of TNF-α.

Conclusions: It can be concluded that sitagliptin may play a protective effect against cisplatin induced acute nephrotoxicity via antioxidant and anti-inflammatory pathway.

Open Access Original Research Article

Optimization of the Cultural Parameters for Improved Production of Antimicrobial Metabolites by Streptomyces gulbargensis DAS 131

Usha Kiranmayi Mangamuri, Muvva Vijayalakshmi, Sudhakar Poda, Dayanand Agasar

Journal of Pharmaceutical Research International, Page 1130-1145
DOI: 10.9734/BJPR/2014/7085

Aims: To investigate the influence of appropriate culture medium by optimizing the cultural conditions affecting the growth and bioactive metabolite production by Streptomyces gulbargensis DAS 131 under submerged culture conditions in order to reduce the cost of fermentation process to improve the formation of antimicrobial compounds.
Place and Duration of Study: Department of Botany and Microbiology, January 2012 to May 2012.
Methodology: The impact of environmental parameters such as incubation period, pH, temperature and salt concentration and effect of various nutrients such as carbon and nitrogen sources and minerals on the antimicrobial metabolite production by Streptomyces gulbargensis DAS 131 was evaluated by employing agar well diffusion assay. Growth was measured in the form of dry mycelial weight.
Results: The optimum pH and temperature for bioactive metabolite production were 7 and 35°C respectively. Highest antimicrobial metabolite production was found when the strain was inoculated into the medium amended with glucose at the concentration of 2%, soya peptone at the rate of 1% and NaCl at the concentration of 5% and incubated for six days under shaking conditions. The metabolites showed good antimicrobial activity against Gram positive and Gram negative bacteria, as well as unicellular and multicellular fungi.
Conclusion: S. gulbargensis DAS 131 isolated from the semi-arid soils of Gulbarga, Northern Karnataka province, India exhibited broad spectrum antimicrobial activity. It was found that the antimicrobial metabolite production by the strain was positively influenced by carbohydrates, nitrogen sources and minerals.