Effect of lipid and cellulose based matrix former on the release of highly soluble drug from extruded/spheronized, sintered and compacted pellets.

BACKGROUND: The study was to develop an extended release (ER) encapsulated and compacted pellets of Atenolol using hydrophobic (wax based and polymeric based) and high viscosity grade hydrophilic matrix formers to control the release of this highly water soluble drug by extrusion/spheronization (ES). Atenolol is used for cardiovascular diseases and available as an immediate release (IR) tablet dosage form. The lipids, Carnauba wax (CW), Glyceryl monostearate (GMS) and cellulose based i.e. Hydroxypropyl methylcellulose (HPMC) and Ethyl cellulose (EC) were used in preparing Atenolol ER pellets. Thermal sintering and compaction techniques were also applied to control the burst release of Atenolol. METHOD: For this purpose, thirty-six trial formulations (F1-F36) were designed by Response Surface Methodology (RSM), using Design-Expert 10 software, keeping (HPMC K4M, K15 M & K100 M), (EC 7FP, 10FP & 100FP), waxes (GMS, & CW), their combinations, sintering temperature and duration, as input variables. Dissolution studies were performed in pH, 1.2, 4.5 and 6.8 dissolution media. Drug release kinetics using different models such as zero order, first order, Korsmeyer-Peppas, Hixon Crowell, Baker-Lonsdale and Higuchi kinetics were studied with the help of DDsolver, an excel based add-in program. RESULTS: The formulations F35 and F36 showed compliance with Korsmeyer-Peppas Super case II transport model (R2 = 0.975-0.971) in dissolution medium pH 4.5. No drug excipient interaction observed by FTIR. Stereomicroscopy showed that sintered combination pellets, (F35), were highly spherical (AR = 1.061, and sphericity = 0.943). The cross-sectional SEM magnification (at 7000X) of F34 and F35 showed dense cross-linking. The results revealed that the optimized formulations were F35 (sintered pellets) and F36 (compacted pellets) effectively controlling the drug release for 12 h. CONCLUSION: Extended-release encapsulated, and compacted pellets were successfully prepared after the combination of lipids CW (10%) and GMS (20%) with EC (10FP 20% & 100FP 20%). Sintering and compaction, in addition, stabilized the system and controlled the initial burst release of the drug. Extended release (ER) Atenolol is an effective alternative of IR tablets in controlling hypertension and treating other cardiovascular diseases.

Quality evaluation and in vitro interaction studies between levofloxacin 250mg and diclofenac sodium 50mg tablets.

Fluoroquinolones are broad-spectrum antibiotics, work against Gram-positive and Gram-negative bacteria and are a clinically proven option for many resistant infections. Among fluoroquinolones Levofloxacin works best against acute sinusitis, inflammation of the lower airways, acute exacerbation of chronic bronchitis, community acquired pneumonia, complicated urinary tract infection including Pyelonephritis, chronic bacterial prostatitis and skin and soft tissue infection. Levofloxacin is a frequently prescribed antibacterial agent with Diclofenac Sodium for pain management in infectious conditions. The objective of the present work is to evaluate the level of interaction between Levofloxacin and Diclofenac Sodium. In this work market available brands of both drugs were also evaluated for quality.The physiochemical parameters like weight variation, thickness variation, and mechanical strength were determined. Similarly the percentage drug release and content uniformity test were also analyzed; the tested quality attributes were found within the recommended pharmacopeia ranges except brand L(6) that had high drug content 124.629±3.614 while brand L(4) and L(5) were not found similar in pH 1.2. When subjected to model dependent analysis Levofloxacin showed compliance with (first order, Higuchi, Hixson Crowell and Weibull) at pH (1.2, 4.5 and 6.8). However Diclofenac Sodium showed adherence with (first order, Hixson Crowell and Weibull) at pH (1.2, 4.5 and 6.8) but following Higuchi at pH 1.2 and 4.5 only. The interaction studies were also performed spectrophotometrically and simultaneous equation was used to estimate the percentage availability of both the drugs at pH 4.5, 6.8, FaSSGF and FaSSIF. The studies showed that the percent availability of Levofloxacin was increased significantly in FaSSIF i.e. 129.173±0.323 at 45 minutes in the presence of Diclofenac Sodium.

Perspectives about Pandemic Influenza and Its Prophylactic Measures among Final Year Pharmacy Students in Karachi, Pakistan.

AIMS: In flu pandemics, pharmacy students' knowledge, attitudes, and practices are critical to save patients life. The objective of study was to determine the knowledge of and attitude toward the pandemic influenza among the pharmacy students of Karachi, Pakistan. SETTINGS AND DESIGNS: The cross-sectional study was conducted from September to December 2014 by adopting a prevalidated questionnaire distributed to senior pharmacy students (final year) in seven private and public sector universities of Karachi. MATERIALS AND METHODS: A total of 443 pharmacy students responded the survey. Data regarding sociodemographic characteristics of the students, perceptions, level of knowledge and attitudes toward influenza, and prophylactic measures were collected. STATISTICAL ANALYSIS: To compute the correlation between different variables, data were analyzed using Pearson's Chi-square statistic method. P < 0.05 was considered statistical significance for all analysis. RESULTS: Influenza was identified as a viral disease (n = 423; 95.48%) and 282 (71.2%) students correctly identified it as disease affecting humans and pigs. Textbooks reported as most common source of knowledge (n = 282; 64%). Most common symptoms identified were fever (81.94%), sore throat (64.1%), and nonproductive cough (43.34%). The most common preventive measures were covering nose and mouth (268; 60.5%) and wearing protective coverings (254; 57.3%). Only half of the students correctly reported about the route of administration (180; 40.6%) and strains in vaccine (186; 41.98%). The best time for administration of such vaccine was known by only 156 pharmacy students (35.34%). The majority of the students (82.6%) had no idea about the manifestation of influenza pandemic. Knowledge regarding influenza differed according to gender and institutions differing in their affiliation with tertiary care hospitals. CONCLUSION: It was observed that knowledge about disease progression, transmission, vaccination, and treatment in pharmacy students, especially those who are not getting clinical training in tertiary care hospitals was limited. There is an urgent need to develop awareness programs to increase knowledge of influenza among clinical pharmacists as they are more susceptible to infections and community as a whole.