Iranian Journal of Pharmaceutical Sciences

The objective of present research was to design, evaluate and compare drug release from two different dosage forms in pulsatile drug delivery system (DDS) for Metoprolol tartarate (MT) as tablet and capsule. Pulsatile systems are gaining a lot of interest as they deliver the drug at the right site of action at the right time and inthe right amount, thus providing spatial and temporal delivery and in creasingpatient compliance. These systems are designed according to the circadian rhythm of the body. The principle rationale for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not desired. The release of the drug as a pulse after a lag time has to be designed in such a way that a complete and rapid drug release follows the lag time. Conclusively, the current study attained the successful comparison of drug release from two different pulsatile drug delivery systems.

Food packaging extensively uses plastic films and containers of petroleum-based polymers for their excellent functional properties and competitive price.Plastic packaging has become a central focus of waste reduction efforts, particularly in aesthetic terms of damage to flora and fauna. Presently, consumers require greater quality and longer shelf lives for their foodstuffs, while they demand a reduction in the quantity of packaging materials used. In the present study, poly-ethylenglycol (PEG), glycerol, and olive oil were incorporated into whey protein concentrate (WPC) through emulsification to produce films. Whey protein films were prepared by dispersing 10% whey protein concentrate in tap water and plasticized with different levels of glycerol, PEG or olive oil. The emulsion films were evaluated for mechanical properties, water vapor permeability (WVP) and opacity.Increasing the levels of glycerol or PEG in the films resulted in a decrease in modulus and tensile strength. Increasing glycerol content of the films at oil/protein ratios of 0.2 and 0.4 led to slight increases in elongation. Increasing the oil/proteinratio further resulted in a decrease in elongation for all films. No significant difference in WVPand opacity was observed between films made from mixtures of various proportions of whey protein concentrate-glycerol with increasing PEG (addition) at all levels of the plasticizer. These results suggest that a whey proteinbased edible films is a viable alternative packaging process for food and improvement of shelf life.

Urine specimens collected from in-patients and out-patients in Urmia Imam Hospital, northwest Iran, were cultured on blood agar and Eosin Methylene Blue agar. Isolated bacteria were identified according to standard microbiological tests and then subjected to sensitivity testing according to routine method of disk agar diffusion technique. Out of 8044 and 10425 urine specimens, 8.7% and 11.9% were identified as having urinary tract infection (UTI) in 2002 and 2006, respectively. The most prevalent bacteria belonged to enterobacteriaceae family and in the case of total susceptibility the upmost resistance was recorded against trimethoprim-sulfamethox-azole (62%) and gentamicin (50%) in 2002, and increased to 69% and 57% in 2006,respectively. The least resistance recorded was to ceftizoxim as 15.6% and 16.8 %in 2002 and 2006, respectively. Antibiotics susceptibility of in-patients wassignificantly lower than that of out-patients and this was more obvious for cephalosporins. Our findings show a remarkably high prevalence of resistance to the majority of commonly used antibiotics in UTIs, with a decreasing trend in their activities which probably is due to the high rate of antibiotics use in Iran as the first reason. Results of the present study underline the need for sensitivity tests prior to antibiotic therapy in UTI, which could help and guide in proper choosing of antibiotics and effective treatment and, therefore, prevention of antibiotic resistance.

Overdose of acetaminophen causes severe hepatic necrosis in humans and experimental animals. Studies on its hepatotoxicity remain a very active area since some of current data are still uncertain. In this study, freshly isolated rat hepatocytes were used to determine the effects of garlic extract and its component, allicin on the acetaminophen-induced cell cytotoxicity and to compare with the effect of N-acetyl cysteine as a standard treatment. Garlic extract was prepared via a standardmethod and its allicin and allyl mercaptan contents were determined using analytical and preparative high performance liquid chromatography (HPLC). Rat hepatocytes were isolated using collagenase perfusion and mitochondrial membrane potential and cell cytotoxicity were determined using Rhodamine 123 fluorescence and trypan blue exclusion, respectively. Inclusion of garlic extract and/or N-acetyl cysteine resulted in a reduction in the loss of mitochondrial membrane potential as well as cell death which occurred after acetaminophen addition and therefore,illustrated considerable hepatoprotective effects without significant differences between two treatments. In contrast, pure allicin was not effective significantly. The hepatoprotective effects of garlic extract may be due to the compounds other than allicin such as allyl mercaptan, as allicin has been shown to transform to allyl mercaptan as a major metabolite.

The methanolic extract of whole plants of Solanum nigrumL. was investigated for anti-inflammatory activity on the experimental animal models. The methanolic extract at a concentration of 100 mg.kg-1and 200 mg.kg-1, p.o.showed the significant dose dependent anti-inflammatory activity in carrageenin and egg white induced hind paw oedema in rats. Anti-inflammatory activity of the tested extract was comparable with that of the standard drug indomethacin (10 mg.kg-1) and cyproheptadine (8mg.kg-1). The results lend support to the traditional use of Solanum nigrumin the treatment of inflammatory diseases

Fenugreek (Trigonella foeum-graecumL.) has been used in Iranian traditional medicine for treatment of different kinds of inflammation disorders. In the present study, anti- inflammatory activity of the methanolic extract of the plant (at doses of 100, 200 and 400 mg/kg) were studied using carrageenan-induced edema method and compared with the effects of dexamethasone and ibuprofen. Various concentrations of the plant extract (2-5%) were also prepared as a cream and their anti-inflammatory effects were evaluated and compared with 1% hydrocortisone ointment as the reference drug. The results showed that the inhibition of edema by the plant extract at doses of 100 and 200 mg/kg were significantly different from the control group. This activity of the plant at doses of 100 and 200 was not significantly different from those of ibuprofen and dexamethasone. Among the prepared formulations of the plant, 3 and 5% creams of the fenugreek showed themost inhibition of edema which were not significant from hydrocortisone ointment.The results of the present study, therefore, support the traditional uses of this plant for inflammations. However, more research is needed for its use in clinical studies.

Flavonoids could serve as potent inhibitors of xanthine oxidase (XO). In the present study, the effects of Ruta graveolensL. extract and its major isolated flavonoids,quercetin and rutin, on guinea pig liver XO have been investigated. The inhibitory effects of R. graveolens, quercetin and its glycoside form, rutin, were assayed spectrophotometrically. R. graveolensextract showed moderate inhibition on XO activity. Interestingly, bovine milk and guinea pig liver XO were inhibited significantly at different ranges by either the extract or its flavonoids, whereas allopurinol acted with almost the same potency on both enzymes. Rutin inhibited the enzymes in a competitive manner, while quercetin was found to be a competitive and mixed inhibitor of guinea pig liver and bovine milk XO, respectively. In conclusion, R.graveolensextract can act as a good inhibitor of XO. Interestingly, it was shown that the inhibitory effects of flavonoids on XO could be species dependent.

An accurate and sensitive reversed-phase high-performance liquid chromatograph-ic method for determination of sertraline in human serum is described using 4-chloro-7-nitrobenzofurazan as pre-column derivatization agent. The drug and aninternal standard (azithrimycin) were extracted from serum using a mixture ofdiethyl ether-chloroform and subjected to the pre-column derivatization with thereagent. Analysis of the resulted derivatives was performed on a Lichrosorb CN(250×4.0 mm) column using a mobile phase composed of methanol and sodium phosphate buffer (0.05 M; pH 3.7) containing 2 ml/lit triethylamine (63:37 v/v).Detector response was monitored at excitation and emission wavelengths of 470 and537 nm, respectively. The calibration curve was linear over the concentration range of 2 to 640 ng/ml. The lower limits of detection and quantification were 0.5 and 2ng/ml, respectively. The validation of the analysis was carried out in terms of specificity, sensitivity, linearity, precision, accuracy and stability. The validated method was shown to be accurate, with intra-day and inter-day accuracy from 0.3 to 4.2%and precise, with intra-day and inter-day precision from 2.4 to 15.5%. The drug is detected at concentrations as low as 2 ng/ml in a 0.5 ml serum sample and the described method can be easily applied in human single-dose pharmacokinetic studies of sertraline.