JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

7-12

Authors: Hanan Fatima Ahmed, Sabiha Naseem, Habeeb Unnisa, Asfia Amreen, Javed Akhtar Ansari, Rafia Sultana

Drug utilization evaluation of hepatoprotective drugs is important in view of the spectrum of effect and associated risks with their therapy. The study was designed to evaluate the effects and adverse effects of hepatoprotective agents. A prospective, observational study was carried out for a period of 6 months at Osmania General Hospital (a tertiary care hospital). 120 patients were evaluated receiving corticosteroids, pentoxifylline, ursodeoxycholic acid for observing a trend in hepatic parameters and its outcomes. Ursodeoxycholic acid (81.66%) was the most commonly prescribed drug in almost all cases of alcoholic liver diseases followed by pentoxifylline (10%) in hepatorenal syndrome and then prednisolone (8.33%) in fatty liver. 67 cases were reported to have the significant drop in liver transaminases and bilirubin levels. Ursodeoxycholic acid resulted in a drop of 25% serum bilirubin and 35% drop in serum ALT (alanine transaminase) and 33% drop in serum AST (aspartate transaminase) in patients in a time gap of 1 week. Among 120 cases 94 were males (78.05%) and 26 females (21.04%) and maximum patients with alcoholic liver disease belonged to age group of 30-40 years (27.6%). Ursodeoxycholic acid (300 mg once daily) is used as an off-label drug for all types of alcoholic liver disease and also for viral hepatitis. Though Ursodeoxycholic acid showed a significant drop in liver transaminases and serum bilirubin levels in cirrhotic patients a better alternative lie in liver transplantation as long as they remain abstinent from alcohol.

17-22

Authors: Dereje Debebe, Tesfaye Gabriel, Yonas Brhane, Abraham Temesgen, Muluken Nigatu, Tesfa Marew

The aim of present work was to undertake comparative in vitro quality evaluation of six marketed clotrimazole cream formulations in Ethiopia with respect to physico-chemical properties like viscosity, spreadability, extrudability, pH and drug content. In vitro clotrimazole release from cream formulations was also studied using synthetic cellulose acetate membrane at 37 ºC in a solvent containing methanol and PBS 7.4 in the ratio of 75:25 as receiver medium. The cumulative amounts of the drug released over 12 h (µg mm-2) were analyzed. All clotrimazole cream formulations showed good and smooth homogeneous appearance with white color. The pH of clotrimazole cream formulations ranged from 4-7, which is a physiologically acceptable pH range and in principle devoid of any skin irritation. Clotrimazole content ranged from 90-110%, ensuring the uniformity of the drug content in all formulations. The increase in diameter of clotrimazole cream formulations following the spreadability test was found to range from 4-6 cm. Cream formulation D (Clotri-Denk) exhibited highest viscosity values than other formulations, whereas formulation E (Chinese Clotrimazole BP) showed lowest viscosity value. Cream formulation F (Mycoril) showed better extrudability and spreadability as compared to other formulations. Drug release from all formulations was slow in the first 6 hrs. After the 6th hr, steady drug release continued for formulation D and E. Fast drug release was observed in formulations A (Candid) and B (Candigen), whereas for the formulations C (Canesten), D and E, steady drug release pattern was observed after the 6th hr. It can be concluded that all clotrimazole cream formulations fulfilled the quality criteria of in-house and pharmacopeias specifications.

29-32

Authors: Himanshu Gurjar, Himanshu Pandey, Amita Verma, Raghuveer Irchhaiya, Prem Prakash Singh

Bauhinia variegata commonly known as kachnar tree and is cultivated throughout India. literature survey revealed that the leaf of Bauhinia variegata is traditionally used as an astringent in diabetes. flowers are laxative.the present study was undertaken to evaluate the antidiabetic activity of ethanol extract of leaf of Bauhinia variegata extract was evaluated using albino wister rat i.e.alloxan induced diabetes in albino wister rat by glucometer method, with 50 mg/kg,100 mg/kg and 200 mg/kg and higher doses showed significant value represent at table no and figure 1,2,3,4 respectively with different successive extract and show the significant p value.

48-56

Authors: C Pradeep Kumar Reddy, C Gopinath

Objective: The objective of the study was to evaluate and optimize compression process variables of Esomeprazole (Multiunit particulate system) MUPS tablet. Materials and methods: A three-factor, two-level, full factorial design was used to investigate the influence process variables Viz. Main compression force, Pre-compression force and Turret speed. Responses studied were Weight variation, Hardness, Thickness, Friability, Content uniformity, Drug release in 0.1N HCl at 120min and drug release in pH 6.5 simulated intestinal fluid at 15 min. Results and discussion: Main compression force and the Pre-compression force had a significant influence on hardness, thickness, drug release in 0.1N HCl at 120min and drug release in pH 6.5 SIF at 15min. Higher compression force leads to breakage of pellets during compression which showed impact drug release at acid stage. Turret speed had significant impact on final weight variation and content uniformity. The optimized process parameters Main compression force: 11.33 kP, Pre-compression force: 2.72 Kp and Turret speed: 23.56 rpm showed desired physical characteristics and drug release in 0.1N HCl which will result in lesser degradation of API at acid stage. Conclusion: It is concluded that Compression process variables in preparation of Esomeprazole MUPS were successfully evaluated using Design of Experiment approach.

64-69

Authors: Manish Kumar Gupta, Surendra Kumar Swarnkar

Microspheres are solid, spherical particles of protein or polymer-based matrix which comprised of a fairly homogeneous mixture of polymer and active agents.It undergoes considerable presystemic metabolism (45-55%) which results in reduced bioavailability. Diltiazem hydrochloride was scanned in the Methanol, acid buffer, pH 1.2and phosphate buffer, pH 7.2. 10 mg of drug was dissolved in methanol in 100 ml in volumetric flask, and volume was made to 100 ml with same solvent. This stock solution was further diluted to get concentration of 10mcg/ml. This solution was scanned in UV-spectrophotometer and characteristic peak was observed at 239 nm for methanol,237 nm for acid buffer, pH 1.2 and phosphate buffer, pH 7.2. Standard curve of Diltiazem hydrochloride was plotted in Methanol, acid buffer (pH 1.2) and phosphate buffer (pH 7.2). The critical values for regression coefficient in each plot was less than 0.001 (i.e., P < 0.001). That indicates that there was high linear correlation between concentrations of drug with absorbance.

74-80

Authors: Alemseged Beyene Berha, Nathan Seyoum

Background: Irrational use of antibiotics is a worldwide problem that contributes to dramatically increasing resistance and causes significant mortality, morbidity, and increased health care costs. In order to ensure the quality of health and medical care for patients and the community as a whole the proper use of medicines is an important element. Evaluation of drug use patterns with the WHO core drug use indicators is showing progressively more essential to promote rational drug use in developing countries. The main aim of this study was to assess the drug prescription pattern using WHO prescribing indicators at the Medical Outpatient Pharmacy in Tikur Ambessa Specialized Hospital (TASH). Methods: A retrospective cross-sectional survey was designed to the claim data .A sample of 2000 prescriptions was selected using systematic random sampling to determine the prescribing pattern from a total of 6,462 prescriptions written by medical interns, residents and senior physicians for a one -year period from February 2015 to January 2016. The raw data was cleaned, entered and analyzed using SPSS version 21.0 of the computer software. The results were summarized using texts and tables. Results: The average number of drugs per encounter was 2.84 +1.58 in the range of 1 to 9. The total number of the drugs which were prescribed by generic name was 97.9%. Of these, the total number of prescribed drugs which were included in the Ethiopian National Essential Medicine List was 99.3%. The present study highlighted the under use of antibiotics which accounts 6.6% (378), with majority being Crystalline Penicillin 27.1 % (94), followed by Amoxicillin 17.8%(62) and Ciprofloxacin 14.1% (49). A total of 8.4% (480) drugs were prescribed as injections. Conclusion: On the basis of the finding of this study, the drug prescription pattern did not meet the WHO core drug use indicators criteria. It seems that there is a need for improvement of the prescribing patterns in the hospitals. Therefore, the federal ministry of health and drug regulatory body's commitment will be required to bring about changes in drug use policies, organize health systems and legislative structures as required in order to foster rational drug use in the country.

86-91

Authors: Dipak D Gadade, Sanjay S Pekamwar, Mahendra D Shirsat

In the current study, we attempted to improve the physicochemical properties of antiviral drug efavirenz through the cocrystal synthesis. The neat grinding performed to study the effect of coformer-fumaric acid (FA) on solubility and dissolution of efavirenz, which can serve as the green cocrystal synthesis approach. The prepared cocrystals were characterized for characteristics like powder flow properties, aqueous saturation solubility, in vitro powder dissolution study. The synthesized cocrystals were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction. The formation of a cocrystal of efavirenz and caffeine was confirmed by the characterization techniques which suggests the interactions between efavirenz and coformer-fumaric acid leads to cocrystal formation. The powder flow properties, solubility, and dissolution profile of efavirenz are significantly improved by its cocrystallization.

98-102

Authors: Bhuwanendra Singh, Rajendra Awasthi, Arshad Ahmad, Asif Saifi

Traditional medicinal system relies on the knowledge and clinical expertization of physicians to regulate the indigenous medicinal system for the sake of well being to humans. Considering the bioavailability issues of phytoconstituents, in this review, we have focused on the various aspects of phytosomes in drug delivery. Phytosome technology is used to enhance the absorption of poorly absorbed lipid soluble active constituents from the herb extracts. So, the article covers a brief introduction of phytosomes, their method of development along with its formulation and evaluation parameters such FTIR, NMR etc. Different types of dosages forms are described in the review, merits and demerits are also discussed along with diagrammatic representation of phytosome development technique. So, the article is the direction for future research to increase the absorption of phytoconstituents.

108-113

Authors: Lanan Wassy Soromou, Morlaye Kindia Sylla, Mohamed Keyra, Youssouf Sidime

Lipopolysaccharide (LPS) is a main causative agent of septic shock. In this study we investigated the possible effects of Rutin (RT) against LPS-induced endotoxemia model in vivo to determine whether RT could rescue mice from ensuing death after their exposure to LPS. To further understand the role of RT, the responses of cytokines were also assessed in serum isolated from blood collected at 0, 1.5, 3, 6, and 12h after LPS administration of the mice. In the study, RT showed suppressive effects on TNF-α, IL-6, and IL-1β production by LPS- challenged mice. Furthermore, RT protected mice by improving host survival against LPS challenge. The present findings reinforce the potential of RT, a natural compound as drug candidate for prevention of sepsis progression.