Pharmaceutical Sciences
Volume:21 Issue: 3, Nov 2015

Professor Mohammad Barzegar-Jalali was born on June 1945 in Ardabil, Iran. He received his Pharm.D from Tehran University of Medical Sciences (Tehran, Iran) in 1969 and PhD in pharmaceutics (1975 to 1979) from De Montfort University (Leicester, UK) with a dissertation entitled "studies on the bioavailability of drugs from peroral aqeous suspensions". He has worked as a full academic member at Faculty of Pharmacy, Tabriz University of Medical Sciences (TUOMS, Tabriz, Iran) from 1971, teaching physical pharmacy, pharmacokinetic, pharmacodynamic and biopharmacy to graduate and postgraduate students and has published more than 150 research and review articles in international peer-reviewed journals. Professor Barzegar-Jalali awarded two gold medals from the Iranian Razi Research Festival in 1996 and 2002 for his academic achievements. In 2015, he was appointed as the first distinguished professor of TUOMS and was selected as 1% of top scientist worldwide based on the Essential Science Indicators (ESI) ranking. His research field includes in the following issues: (a) formulation technologies for enhancing the solubility and dissolution of drugs and drug candidates including the use of nanotechnology and solid dispersions 1-5 (b) modeling of physicochemical and pharmacokinetic properties i.e. solubility prediction of drugs in solvent mixtures 6,7, correlation between physicochemical properties and anesthetic potencies 8 in-vitro-in vivo correlation (IVIVC) of drug nanosystems parameters for prediction purposes 9, modeling of drug release kinetic from nanoparticles 10, (c) pharmacokinetic studies such as determination of drug bioavailability 11,12. This special edition of Pharmaceutical Sciences (PS) is published in honor of Professor Mohammad Barzegar-Jalali for his lifelong efforts toward pharmacy training and research. This issue includes original scientific papers in his research filed. Our best wishes and congratulation for his well deserved awards and scientific efforts.

It is reported that the change in the number of water molecules in the crystalline mineral salts which is used as pharmaceutical ingredients, can cause variations in their physicochemical and pharmaceutical properties. The number of water molecules of these pharmaceutical ingredients is subordinate to Relative Humidity (RH) and temperature of the maintenance environments of the medicines. The aim of the present study was to investigate variation in water content of pharmaceutical solids including ferrous sulfate, barium sulfate and magnesium chloride in different percentage of RH and temperature. For this purpose, the pharmaceutical solids (both inside and outside the packaging) were subjected to various relative humidity at constant temperature for a given period of time, then change in their water content was determined with Thermo Gravimetry Analysis (TGA). To create a variety environments with different RH in constant temperature, the saturated salt solutions were put in a desiccator and the RH above mixtures of solids was determined with a Hygroscope at 25°C. According to the results obtained from TGA, the water content of pharmaceutical solids studied in this research (ferrous sulfate, barium sulfate and magnesium chloride) changed in different RH and temperatures. It is necessary to determine water uptake of Active Pharmaceutical Ingredients (APIs) and excipients in each stage of pharmaceutical development process. Furthermore, these results could be used to select an appropriate packaging to avoid adverse effects caused by water absorption by pharmaceutical solids. In cases where this is not possible, the allowable range of relative humidity for each pharmaceutical solid should be noted on its package.

The aim of this study was to prepare and characterize cefixime nanosuspensions in order to enhance the dissolution rate and solubility of this drug. Nanosuspensions were prepared using sonoprecipitation method and the effects of surfactant type, surfactant and solid content, sonication power input and interval of acid addition on the yield and particle size of nanosuspensions were investigated. Particle size and yield of the optimal nanosuspension formulation were 266±10 nm and 35±2%, respectively. Scanning electron microscopy (SEM) results showed a nearly spherical morphology for cefixime nanoparticles. Thermal analysis indicated that there was a partial crystalline structure in the nanoparticles and in vitro dissolution rate of the drug was significantly increased by the reduction in particles size. Sonoprecipitation was shown to be a successful method to produce cefixime nanosuspensions and the optimum conditions of the process were introduced.

Plant-derived materials are increasingly gaining attention as dietary supplements and due to their role in medicinal application. Rutin, a phenolic antioxidant, is a member of bioflavonoids which has been demonstrated to scavenge superoxide radicals and is believed to be a vital nourishing supplement due to its ability to strengthen and modulation of the permeability of the blood vessels walls. However, Rutin shows poor absorption when administered orally and its bioavailability is an important restrictive factor. The present study was aimed to prepare and characterize a stable Rutin-loaded nanophytosomal formulation to improve its antioxidant property and bioavailability. Rutin-loaded nanophytosomes were prepared by phosphatidylcholine (PC) and cholesterol by thin layer hydration method. The physicochemical properties of prepared nanophytosomes were evaluated using particle size analyses, Furrier transformation infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Stability of the prepared nanophytosomes was also investigated during three weeks of storage period. Results showed that formulation with the Rutin: PC molar ratio of 1:2 possess lowest particle size and the incorporation of cholesterol improved the physical stability of nanophytosome for over three weeks. FTIR and DSC analysis showed the formation of Rutin-phospholipid complex during the formulation development process. Results of the present study showed that nanophytosome can be introduced as a useful carrier for fortifying herbal medicinal compounds for application the formulation of various food and pharmaceutical products.

Poor aqueous solubility of drugs is still a challenging aspect in drug discovery and development. Solubilization techniques such as cosolvency and complexation are used to solubilize poorly soluble drugs. A number of mathematical models presented for predicting the solubility of drugs in water+cosolvent mixtures and the Jouyban-Acree model promises more accuracy when compared with other algorithms. Solubility of sodium phenytoin in binary mixtures of propylene glycol + water in the presence of beta-cyclodextrin (b-CD) along with the solubility of sodium phenytoin in this solvent mixture in the absence of b-CD using saturating shake flask method were studied. The generated solubility data was fitted to the Jouyban-Acree model and the solubility profile of drug in the presence of b-CD was compared with solubility data in the absence of b-CD. The solubility was increased by addition of propylene glycol and was decreased by addition of beta-cyclodextrin. The measured solubility data were used to evaluate the correlation ability of the Jouyban-Acree model employing the solubility data in monosolvent. These findings are supported by acceptable mean relative deviations values obtained when comparing the estimated and experimental solubilities. The addition of b-CD was decreased the solubilization power of propylene glycol.

Imatinib mesylat as an oral anticancer agent need a controlled released formulation to get steady and stable plasma concentration. The aim of the present study was to develop controlled release matrix tablet formulations of Imatinib using hydroxy propyl methyl Cellulose as a hydrophilic release retardant polymer and to study the effects of different formulation features like polymer viscosity grade, ratio of the polymer, compression force, and release medium on the in vitro release properties. The in vitro release studies were performed using US Pharmacopoeia type I apparatus. The release kinetics was analyzed by Korsmeyer–Peppas model and were also analyzed using statistical method and f2 metric values. The release profiles look like Higuchi’s square root kinetics model irrespective of the viscosity grade and polymer proportion. The results showed that the release rate of the drug is greatly affected by the drug/polymer ratio and viscosity grade. Also, the effect of release medium and compression force was showed to be significant on the release profiles. The release mechanism was found to be anomalous non-Fickian diffusion in all formulations. The formulations were found to be reproducible and stable. Controlled release formulations were developed with different release rates and profiles so that these formulations could be evaluated for more in vivo studies.

A quick and thoughtful liquid chromatography–tandem mass spectrometry (LC-MS) method has been established and authorized for the estimation of amlodipine and atorvastatin in human plasma. LC-MS with electrospray ionization (ESI) interface in positive ion mode was functioned under the multiple-reaction monitoring (MRM) mode was used for detection of analytes. Ethyl acetate was secondhand for extraction of analytes from plasma by simple liquid–liquid extraction technique. The re-formed samples with a C18 column by pumping acetonitrile-ammonium acetate buffer (10 mM, pH = 3.0), 70:30 (v/v) at a flow rate of 0.15 mL/min were chromatographed. The standard curves were established to be linear in the range of 0.2–20 ng/mL for atorvastatin and 0.1–10 ng/mL for amlodipine with mean correlation coefficient of ≥0.999 for each analyte. The lower limit of quantification for amlodipine and atorvastatin were demonstrated to be 0.1 ng/ml and 0.2 ng/ml respectively. The mean (SD) Cmax and Tmax values of amlodipine later supervision of the test and reference were: 6.58 (0.22) versus 6.64 (0.37) ng/mL, 6.12(0.86) versus 6.13 (0.73) hours respectively. The mean (SD) Cmax and Tmax values of atorvastatin later government of the test and reference, were 61.66 (3.05) versus 62.16 (0.76) ng/mL, 4.21(0.86) versus 4.22 (0.73) hours respectively. The results proposed the test formulation of amlodipine and atorvastatin is bioequivalence with reference formulation and the established evaluate method was successfully realistic to a pharmacokinetic and bioavailability trainings in 20 human male volunteers following oral administration of amlodipine and atorvastatin.