Impact of different organic acids on solubility enhancement of cefpodxime proxetil immediate release tablet and its stability studies

Cefpodoxime proxetil is a third generation cephalosporin antibiotic demonstrates pH dependent solubility and is highly soluble only in acidic pH. The purpose of this investigation was to design and develop immediate release tablets of cefpodoxime proxetil by direct compression method and determine the effect of different solid buffers [organic acids] such as fumaric acid [formulations F1-F4], maleic acid [formulations M1-M4] and citric acid [formulations C1- C4] by using cefpodoxime and acid in the ratios of 4:1, 2:1, 1:1 and 1:2 to achieve pH-independent release of the drug. Physical parameters and assay were found to be within the acceptable range as prescribed in USP 36 / NF 31. In vitro dissolution studies of each formulation were performed in distilled water, USP dissolution medium, HCl buffer solution of pH 1.2, phosphate buffer solutions of pH 4.5 and 6.8 to observe the drug release. The formulations F3, F4, M4 were selected for film coating on the basis of better drug release profile, to protect the drug from chemical degradation through hydrolysis. Film coated formulation F3, F4 and M4 showed a remarkable in vitro release of the drug [72.88+/-0.43 to 92.67+/-0.71%] within 30min of observation in all dissolution media and further evaluated by model independent and model dependent approaches. The drug release was found to be best fit to Weibull model as highest r[2] [adjusted] [0.924- 0.998] and lowest AIC [18.416-54.710] values were obtained in all dissolution media. R Gui[registered sign] applied for stability studies of F3 and F4 formulations, showing shelf lives of 28 and 27months at ambient and 33 months at accelerated temperatures. Formulation F4 was chosen as best formulation on the basis of physical properties, highest dissolution rate and stability studies

Formulation and Dissolution enhancement of Meloxicam tablets using Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and Povidone in combination

Meloxicam is a poor water soluble drug mostly prescribed in various rheumatic diseases. The present research study was design to formulate and increase the solubility of meloxicam in the tablet dosage form. A 32 full factorial design was employed to optimize meloxicam formulations. Polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer [PVCL-PVA-PEG graft copolymer] and Povidone were taken as independent variables while cumulative drug release at 90 minutes was selected as dependent variable. All trial formulations complied with official standards. Multiple regression by Microsoft Excel on cumulative drug release of the selected formulations [F1, F2, F6- F9] showed the positive effect of PVCL-PVA-PEG graft copolymer [[alpha] = 0.05] and a negative effect of Povidone [[alpha] = 0.05]. Formulation six [F6] [PVCL-PVA-PEG graft copolymer 3 mg and Povidone 22.5 mg / tablet] was considered as the optimal formulation based on its cumulative drug release. Dissolution kinetics by model dependent analysis predicted Weibull [R[2]=0.99] as the best fit model in describing meloxicam dissolution kinetics. The role of PVCL-PVA-PEG graft copolymer should be explored with other solubilizers in future studies

Perception and attitude of pharmacy students towards learning tools

Use of technology in education has increased worldwide. Teaching methodologies are shifting from traditional classroom lectures to e-learning and computer-based learning. Pakistani students are also now fathoming necessity of acquiring tools for strengthening their knowledge and skills. The objective of present study was to analyze the shifting trends [perception and attitudes] of Pakistani Pharmacy students towards learning tools. A survey based study conducted on 296 students from various years of Pharmacy, studying in a state owned university, Karachi, Pakistan. This study was initially piloted and Cronbach's-alpha was computed for evaluation of internal consistency of questionnaire [for perception; 0.660, for attitude; 0.777 respectively]. Data was computed by SPSS, version 16 [Crosstab] and Chisquare [P=0.05]. Most of the students strongly agreed [53%; [CHI][2]=495;P<0.05] that introducing technology will improve learning; books are reliable reading source [53%; [CHI][2]=437.23;P<0.05] or book-reading is essential [50%; [CHI][2]=360.36;P<0.05] while others disagreed that they only study from class lectures [31%; [CHI][2]=17.22;P<0.05]; not take classes [41%; [CHI][2]=48.21;P<0.05]; have used software [44%; [CHI][2]=46.54; P<0.05]. Majority of the students agreed on incorporating technology to improve learning. Other factors such as unavailability and expenditure of books influenced their ability to learn. This study might assist policy makers in developing policies that could improve learning

Antihyperglycemic and hypolipidemic effects of Hibiscus schizopetalus [Mast] Hook in alloxan-induced diabetic rats

The antihyperglycemic and hypolipidemic activities of Hibiscus schizopetalus [Mast] Hook [Malvaceae] flower and leaves extracts were investigated in alloxan-induced diabetic rats. The hypoglycemic activity of both the extracts [100mg/kg, body weight] was tested in fasting normal rat, glucose loaded rats. Observation on body weight was also recorded. The extracts showed a significant [P<0.001] reduction in blood glucose level in normal fasting rats. In glucose tolerance test, significant [P<0.01] decreased observed in all glucose loaded animals. While in alloxan induced diabetic rats, the percent blood glucose reduction was 59.94% and 45.14% in extracts treated groups. The results obtained were compared with the reference standard drug Tolbutamide [100mg/kg, body weight]. The diabetic rats showed sign of decreased in their body weight during the treatment period. Cholesterol and triglycerides levels were significantly decreased [P<0.001] by HFE. The results obtained demonstrated the potential hypoglycemic activity of methanolic extracts of H. schizopetalus. There is need of bioassay-directed assay of the active principles responsible for the anti-diabetic activity. The methanolic extracts showed the presence of carbohydrates, alkaloids, steroids, terpenes, saponins and glycosides.

Formulation development and evaluation of diltiazem HCl sustained release matrix tablets using HPMC K4M and K100M

The aim of this study was to develop a sustained release hydrophilic matrix tablet of Diltiazem HCl and evaluates the effect of formulation variables [e.g. lubricant, binder, polymer content and viscosity grades of HPMC] on drug release. Twelve different formulations [F1-F12] were prepared by direct compression. The results of the physical parameters and assay were found to be within the acceptable range. Rate of drug release was found to be slow as the fraction of the polymer was increased from 20-50%. The drug release rate from tablets containing K4M was effectively controlled by increasing the talc concentration, whereas the burst effect was reduced by increasing binder content. The drug release was higher with K4M as compare to K100M. Model-dependent and independent methods were used for data analysis and the best results were observed for K4M in Higuchi [R[2]=0.9903-0.9962] and K100M in Baker and Lonsdale [R[2]=0.9779-0.9941]. The release mechanism of all formulations was non-Fickian. F7 [50% K4M, 2% talc, 10% Avicel PH101] and F11 [40% K100M] were very close to targeted release profile. F12 [50% K100M] exhibited highest degree of swelling and lowest erosion. The f[1] and f[2] test were performed taking F11 as a reference formulation

Studies on antibacterial activity of some traditional medicinal plants used in folk medicine

Ethanolic extracts of eight medicinal plants commonly used in folk medicine were tested for their antibacterial activity against four Gram positive strains [Bacillus subtilis, Staphylococcus aureus, Staphylococcus epidermidis and, Streptococcus pneumoniae] and six Gram negative strains [Escherichia coli, Proteus vulgaris, Proteus mirabilis. Salmonella typhi para A, Salmonella typhi para B and Shigella dysenteriae] that were obtained from different pathological laboratories located in Karachi, Pakistan. Disc diffusion method was used to analyze antibacterial activity. Out of eight, five medicinal plants showed antibacterial activity against two or more than two microbial species. The most effective antimicrobial plant found to be Punica granatum followed by Curcuma zedoaria Rosc, Grewia asiatica L and Carissa carandas L, Curcuma caesia Roxb respectively. From these results, it is evident that medicinal plants could be used as a potential source of new antibacterial agents

Antimicrobial activity of erythromycin and clarithromycin against clinical isolates of Escherichia coli, Staphylococcus aureus, klebsiella and proteus by disc diffusion method

Fifty clinical isolates comprising of Escherichia coli, Staphylococcus aureus, Klebsiella and Proteus were collected from different local pathological laboratories and their resistant pattern against two well known macrolides; erythromycin and clarithromycin were studied using disc diffusion method. Klebsiella [41.67% against erythromycin and 58.34% against clarithromycin] and Proteus [66.67% against erythromycin and clarithromycin] species were found to be more resistant against the studied macrolides as compared to the rest of organisms. In case of Staphylococcus aureus and Escherichia.coli, resistant found were 27.78% and 23.54% against erythromycin and 22.23% and 35.30% against clarithromycin respectively. It is concluded from these figures that microbial resistance against these macrolides are increasing in our population which is alarming and therefore it is recommended to physicians to prescribe these antibiotics unless no other substitute is available in clinical practices

Formulation of aspirin tablets using fewer excipients by direct compression

The objective of the present study was to formulate aspirin tablets by direct compression method using fewer excipients and to compare this formulation with the other brands. Design formulation besides aspirin contained excipients that comprises of lactose, corn starch and aerosol. The blend was compressed on a single punch machine, tablets were subjected to various tests [uniformity of weights, diameter and thickness, hardness, disintegration, dissolution and assay of the drug] and the results were compared with some of the available brands. The studied formulation showed close resemblance with the available marketed brands and were also in compliance with the official specifications. Using the present approach, further studies should be designed using other actives and excipients to get a cost effective product

Studies of food drug interactions

Medicines can treat and alleviate many diseases provided that they must be taken properly to ensure that they are safe and useful. One issue related with the medicines is that whether to take on empty stomach or with food. The present work gives information regarding food-drug interactions that were studied by collecting seventy five prescriptions from various hospitals. In most of the collected prescriptions, food-drug interactions were detected using the literature available. It was also found that only few studies have been carried out so far on the effect of food on drug disposition in the Asian population. Thus more studies on food-drug interactions particularly in the local population is recommended in order to determine the effect of food and food components on drug disposition and to the kinetics of the drugs which has not yet well highlighted in this part of the world

Swine flu: are we the next victims?

Current pandemic influenza due to A [S-OIV A] [H1N1] virus is becoming more threatening day by day throughout the world. It is the time to provide relevant information to the masses regarding this destructing threat to the health of public. The objective of the present paper is to update the current status of swine flu and to provide information to general public, clinicians and other health professionals about H1N1

Bioequivalence studies of two brands of meloxicam tablets in healthy Pakistani volunteers

The pharmacokinetic parameters of two oral formulations of meloxicam tablets were compared in a randomized, single oral dose; two treatments cross over design in 12 healthy male volunteers belonging to Pakistan under fasting conditions. After an overnight fast, the volunteers received 30 mg meloxicam and the blood samples were collected up to 96 hours and drug concentrations were determined by a validated HPLC method. Various pharmacokinetic parameters were determined from the plasma concentration-time curves of both formulations. The 90% confidence intervals obtained by analysis of variance were 87-94% for Cmax and 88-97% for AUC0-t, that fell well within the acceptance range of 80-125%. Also, no significant difference [beta = 0.05, Wilcoxon Signed rank test] were detected between Tmax of both formulations. The two formulations were well tolerated and no adverse effect was reported during the study

Studies on the quantification and comparison of dissolution profiles of two brands of meloxicam tablets

A simple model independent approach using a similarity factor [f2] and a difference factor [f1] to compare dissolution profiles as proposed by Moore and Flanner was used to evaluate the in vitro equivalence of two brands of meloxicam tablets. Our results showed that the two meloxicam formulations are not equivalent in vitro. Thus it is recommended that the same formulations should be evaluated to in vivo studies in order to find whether a co-relation exists between in vitro dissolution and in vivo bioavailability

Screening of antibacterial activity of different brands of co-trimoxazole paediatric suspension available in the local market

Sulfonamides are the drug of choice for number of infections like pneumonia, toxoplasmosis, nocardiosis, urinary tract infections. Sulfonamides are most commonly used in combinations such as [Trimethoprim-Sulfamethoxazole] [TMP+SMZ] or co-trimoxazole. Sixty five isolates belonging to five different species, E. coli [22], S. aureus [18], Klebsiella [05], Pseudomonas [16] and Proteus [04] were used for screening antibacterial activity against different brands [A-G] of Co-trimoxazole by disc diffusion method. Brand G exhibited highest activity against E. coli with mean zone of inhibition 41mm +/-2.3 standard deviation. The antibacterial activity against other species S. aureus, Klebsiella and Pseudomonas were found as: [mean +/- standard deviation] observed as 39.73 mm +/- 10.59 mm +/- 38 mm +/- 2 and 24.93 mm +/- 5.32. However all isolates of Proteus were found resistant against different brands of co-trimoxazole

Intra-uterine fetal echo cardiography in high-risk pregnancies

The purpose of this study was to evaluate the accuracy of prenatal fetal echocardiography in detecting congenital heart defects pregnant women at high and low risk for structural cardiac anomalies. A prospective outcome of two cohorts study was performed, 50 pregnant women with non complicated [low risk] and 100 high risk pregnant patients underwent routine four chamber and left ventricular outflow tract evaluation whereas high risk, patients had detailed fetal echocardiographic examination. Accuracy of the ultrasonographic diagnosis was evaluated from neonatal discharge data. The study detects one fetus, had small sized apical muscular ventricular septal defect [VSD]. Fetuses of high risk group have smaller and diastolic, end systolic left ventricular cavity dimensions, interventricular septal thickness, left ventricular wall thickness, aortic root diameter and left atrial diameter than the matched control. It can be concluded that high risk cause studied showed changes in fetal heart chamber dimensions but not to the extent of known congenital fetal cardiac malformation