Iranian Journal of Pharmaceutical Sciences

The formulation of hydrophobic drugs for oral drug delivery is challenging due to poor solubility, poor dissolution and poor wetting of these drugs. Consequently, the aim of this study was to improve the dissolution of a model poorly water soluble drug, ibuprofen. Microparticles containing ibuprofen were produced by spray drying and spray chilling technology in the absence/presence of a hydrophilic
surfactant. Poloxamer 127, tri-block copolymer, was chosen as the hydrophilic surfactant to improve drug particle wettability and hence the dissolution rate. The prepared formulations were evaluated for in vitro dissolution and intrinsic solubility. In addition, the produced drug particles were characterised by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier transform
infrared spectroscopy (FT-IR). SEM revealed changes in the surface morphology of processed ibuprofen, suggesting the effective formation of the drug particles. DSC data showed shifting of the melting peak of the drug towards lower melting temperature in the prepared particles, indicating the possibility of drug /polymer interaction. The results of the dissolution studies of spray dried ibuprofen and spray dried ibuprofen/Poloxamer 127 particles significantly (p<0.05) increased the percentage of drug release compared to the control (ibuprofen raw material). For spray chilling, the prepared particles did not improve the dissolution of the drug. The dissolution was even less than that of the control. DSC and FT-IR results demonstrated that spray drying reduced drug crystallinity, but for spray chilled particles there was evidence of polymorphic changes in the drug with and without the surfactant. Consequently, it is believed that spray drying of ibuprofen is a useful tool to improve wettability, solubility and hence the dissolution behavior of poorly water soluble drugs, in contrast to spray chilling technique.

We are presenting a case illustrating atrial fibrillation (AF) following the use of methylprednisolone in a patient with pelvic and femur fracture. A48- year- old man with no significant past medical history, was admitted to the emergency department after injury in a car accident. He suffered a multiple bone fracture with chief complaints of pain and shortness of breath. He was transferred to the ICU. To prevent
fat embolism syndrome, he was treated with methylprednisolone 500 mg every 6 h. About 4 h after the second dose, his normal sinus rhythm changed to a sinus tachycardia and then to AF. The methylprednisolone therapy was discontinued. After about 8 h of methylprednisolone discontinuation, the patient's normal sinus rhythm returned. Corticosteroids have been utilized for prevention and treatment of fat embolism syndrome, although there is uncertainty about their effectiveness. Cardiac dysrhythmias have been reported following the use of methylprednisolone. One possible mechanism of methylprednisolone induced AF is the direct effect on cell membrane, resulting in potassium efflux, which in turn, may initiate cardiac dysrhythmias. Previous methylprednisolone-associated AF case reports suggest a higher chance of AF occurrence with higher dose of methylprednisolone. Corticosteroids should be used with caution, especially when high doses are indicated and in patients with high risk for arrhythmias.

Osteoporosis is a disease of high prevalence with increased bone loss. It has potential public health threat and that the health authorities had taken several measures for its control. In recent years, considerable attention has been given to physiopathology of osteoporosis. Oxidative stress has been proved to be involved in bone resorption. Oxidative stress occurs when balance between oxidants and biochemical antioxidants is disrupted because of excess reactive oxygen species. Thus, we measured catalase activity, as one of the marker of stress oxidative, in 138 women. Participants were selected by inclusion and exclusion criteria from those who were referred to Jamie Clinic in Tehran for BMD evaluation. Catalase antioxidant activity was 262.01±44.70 k/gHb in the group of subjects with osteoporosis in comparison with the group of healthy subjects, 273.77±46.92 k/gHb. The results show that catalase activity in patients with bone deficiency was less than in the control group, though it was not significant. This difference was more between control and patients group with more acute disease (T score -1.7) than patients group with milder disease (T score<-1).The results show that it may be useful to monitor osteoporosis in the more expanded sample size to obtain more definition results.

Diabetes mellitus is associated with disturbances of learning and memory and cognitive functioning. Aegle marmelos Corr. from Rutaceae family, is widely used in Iranian folk medicine for the treatment of diabetes mellitus. It decreases blood glucose level by improving glucose tolerance and also has lipid-lowering and antioxidant properties. Considering the beneficial antidiabetic potential of A. marmelos, this study was conducted to evaluate the effect of chronic oral administration of A. marmelos as cognitive enhancer, on learning and spatial memory in diabetic rats using Morris water maze test. Male Wistar rats were randomly divided into normal-control, diabetic-control, and A. marmelos-treated diabetic groups (100, 250 and 500 mg/kg, p.o., 4 weeks). Diabetes was induced by a single dose i.p. injection of streptozotocin (45 mg/kg). In each group of animals, spatial learning and memory parameters were analyzed. A. marmelos showed dose dependent improvement in spatial learning and memory parameters. Swimming time (Escape Latency) in normal-control and A. marmelos-treated diabetic animals rats was significantly lower than diabetic-control, while swimming speed was significantly higher. The study demonstrated that A. marmelos has a significant protective effect against diabetes-induced spatial learning and memory deficits. This effect can be attributed to hypoglycemic, hypolipidemic and antioxidant activity of A. marmelos.

In this study, we examined the antioxidant activities of methanolic extract of three endemic species of Salvia from Iran (S. lachnocalyx, S. reuterana and S. sahendica) employing various established in vitro systems including ferric reducing antioxidant power, Trolox equivalent antioxidant capacity assay and scavenging of 1,1-diphenyl-2-picrylhydrazyl radical. The results revealed that S. reuterana extract possess the highest antioxidant activity, total phenolic and flavonoid contents among these three species. Regarding the link between glycation and oxidation, we proposed that the S. reuterana extract might possess significant in vitro antiglycation activities as well. The S. reuterana extract also showed strong inhibitory effects on the production of Amadori products and advanced glycation end products from bovine serum albumin in the presence of fructose in term of protein carbonyl formation and thiol oxidation. The structural changes of bovine serum albumin (BSA) with fructose, in the presence of S. reuterana extract were evaluated by circular dichroism and fluorescence techniques. Regarding enhancing the helicity of the protein and preventing helix decrement in the secondary structure of BSA in the presence of fructose, it can be concluded that S. reuterana extract and its constituents may act as an anti-glycation agent for bovine serum albumin.

A series of angiotensin II (A II) receptor antagonist of some substituted 5-(biphenyl-4-ylmethyl) pyrazole were subjected to QSAR analysis using Hansch and Fujita-Ban model, by using combination of  thermodynamic, electronic, spatial descriptor and presence or absence of substituent respectively. Several QSAR model were obtained using stepwise regression analysis. Two models from both the method were selected on the basis of the statistical value that shows good significance with AII antagonistic activity. The best QSAR models further validated by leave one out cross validation method. The studies have help to ascertain the role of different substituent in explaining the observed antagonistic activity of this analogue. From Fujita-Ban model, it is predicted that butane and propane at position 1, COOH at
position 4 are essential for activity. Group like CH2CF3 at position 1 and COOH in place of tetrazole at R3 position contribute negative to the biological activity. In Hansch model it is predicted that molar refractivity at the 1 and 3 position shows positive contribution to the biological activity. Field effect at position 4 also shows positives contribution to the biological activity. Hydrogen donar at position R3 and field effect at position 1 contributes negatively to the biological activity.

The essential oil obtained by hydrodistillation of the aerial parts of Rosa damascenaMill. (Rosaceae) was analyzed by gas chromatography/mass spectrometry (GC/MS). The yield of the oil was 0.16% (v/w). Among 25 components, eight components, representing 99.98% of the oil, were characterized. Nonadecane (39.73%), heneicosane (32.38%), docosane (7.34%), citronellol (6.14%) and 9-nonadecene (5.69%), were found to be major constituents.

The volatile constituents of aerial parts of Euphorbia aellenii Rech.f. and E.microsciadea Boiss. were analyzed by gas chromatography (GC) and GC-mass spectrometry (MS) methods. The main volatile constituents of E. aellenii were phytol isomer (47.3%), camphene (31.9%) and caryophyllene oxide (20.6%), while the major volatile components of E. microsciadea were trans-anethole (74.5%), limonene (7.7%), hexadecanoic acid (6.8%), fenchone (6.0%) and phytol isomer (4.9%).