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   2013| July-December  | Volume 2 | Issue 2  
    Online since January 9, 2018

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Design, formulation and physicochemical evaluation of acetaminophen effervescent tablets
Abolfazl Aslani, Parisa Eatesam
July-December 2013, 2(2):140-149
The main objective of this study was to design, formulate and evaluate the physicochemical properties of 500 mg acetaminophen effervescent tablets, in order to accelerate its analgesic and antipyretic effects in patients with pill swallowing problems. Formulations with 500 mg of acetaminophen were prepared with effervescent bases including tartaric acid, citric acid, sodium bicarbonate, and PEG6000. Flowability of powders and granules was determined by measurement of bulk and tapped density, compressibility index and Hausner's ratio. Three methods were applied to prepare tablets: direct compression, wet granulation and fusion. The effervescence time, hardness, pH, thickness, CO2 content, water content, weight variation, and content uniformity of the prepared tablets were investigated. In order to overcome the bitter taste of acetaminophen, different sweeteners and fruity essences such as orange, lemon, and cherry flavors were applied. Panel taste was performed using 20 volunteers. The physicochemical characteristics of three different methods of preparing tablets were pretty similar. Wet granulated formulations had higher hardness and better flowability while direct compressed tablets had stable effervescence time and better solubility. According to the panel taste, orange flavor was more acceptable. Wet granulated tablets which were prepared using alcohol and PVP had higher hardness and variable effervescence time in comparison to direct compressed tablets. Flowability of wet granulated formulations was better than the one with direct compressed formulations.
[ABSTRACT]   Full text not available  [PDF]
  2,497 379 -
Gastro retentive drug delivery systems: A review
Khosro Adibkia, Saeed Ghanbarzadeh, Ghobad Mohammadi, Rahimeh Bairami Atashgah, Araz Sabzevari
July-December 2013, 2(2):190-204
Gastric emptying is a complex and extremely variable process. This causes the unpredictability of the bioavailability of drug delivery systems. Gastro retentive drug delivery systems (GRDDS)s have received significant attention in the past decades primarily due to the fact that they can overcome the limitation of conventional oral controlled release drug delivery systems related to fast gastric emptying time. An optimum GRDDS can be defined as a system which remains in the stomach for a sufficient time interval and releases active ingredients in a controlled manner. This, significantly extends the duration of drug release, prolongs dosing interval and increases bioavailability of drugs and therefore improves compliance of the patients and effectiveness of pharmacotherapy. This article gives an overview of the main concepts used to design pharmaceutical dosage forms with prolonged gastric residence times as well as the parameters-affecting gastric emptying, advantages, shortcomings, formulation considerations and, factors that affect gastro retentive systems. The main emphasis is on the entire classification and different types of GRDDSs. Finally evaluation methods of these systems have been summarized.
[ABSTRACT]   Full text not available  [PDF]
  1,831 215 -
Essential oil composition of Ferula Assa-Foetida L. fruits from Western Iran
Gholamreza Bahrami, Reza Soltani, Seyed-Ebrahim Sajjadi, Mohammad-Reza Kanani, Reza Naderi, Nastaran Ghiasvand, Yalda Shokoohinia
July-December 2013, 2(2):90-97
Chemical composition of the essential oil of the fruit of Ferula assa-foetida L. obtained by steam distillation solvent extraction methodhas been studied by GC/MS for the first time. Fifty-four components, comprising 96.9% of the total oil, were identified.epi-α-Cadinol (23.15 %), germacrene B (10.98 %), α-gurjunene (6.18 %), (Z)-1-propenyl sec-butyl disulfide (5.89 %), 5-epi-7-epi-α-eudesmol (4.89 %), δ-cadinene (4.78 %), γ-cadinene (3.36 %) and germacrene D (3.09 %) were found to be the major constituents of the oil. The oil of the fruit of F. assa-foetida consisted of ten monoterpene hydrocarbons (6.14%), twenty-six sesquiterpene hydrocarbons (43.48%), nine oxygenated sesquiterpenes (37.77%), one oxygenated hydrocarbon (0.35%), and nine volatile sulfides (11.18%).
[ABSTRACT]   Full text not available  [PDF]
  1,736 201 -
The antiproliferative effects of petroleum ether extract of Artemisia Aucheri on human cancerous cell lines
Mahmoud Ghazi-Khansari, Mahdi Mojarrab, Farahnaz Ahmadi, Leila Hosseinzadeh
July-December 2013, 2(2):150-155
Different species of Artemisia (Asteraceae) have shown to exhibit antitumor activity. The aim of this study was to identify the anti-proliferative effect of Artemisia aucheri Boiss (A.aucheri) from Iran on cultured human cancer cells. Aerial parts of A. aucheri Boiss. were collected from Chahar Bagh region , Golestan province, Iran. The dried powdered aerial parts of A.aucheri were extracted with petroleum ether (40-60), dichloromethane, ethyl acetate, ethanol and ethanol-water (1:1 v/v), respectively. For biological investigation different concentrations of extracts were added to cultured cells and incubated for 24 h. MTT assay was employed to assess the cell viability. In addition, morphological changes of cells were assayed using phase contrast inverted microscope. Different extracts exert various growth inhibitory effects. In case of SKNMC, MCF-7 and A2780 cell lines, petroleum ether extract (IC50 values: 21.0, 26.0 and 28.0 μg/ml, respectively) showed the highest growth inhibitory effects. Dichloromethane extract showed IC50 values: 27.0, 35.0 and 55.0 μg/ml, respectively. This study showed the anti-proliferative effects of A.aucheri petroleum ether extract on malignant cell lines. Thus, the aforementioned may be considered as a promising chemotherapeutic agent in cancer treatment.
[ABSTRACT]   Full text not available  [PDF]
  1,645 157 -
Kinetic of mushroom tyrosinase inhibition by benzaldehyde derivatives
Shabnam Maghsoudi, Hadi Adibi, Marzieh Hamzeh, Mohammad Reza Ashrafi-Kooshk, Mostafa Rezaei-Tavirani, Reza Khodarahmi
July-December 2013, 2(2):156-164
Polyphenol oxidase (PPO), known as tyrosinase (EC, is a multifunctional copper-containing oxidase which catalyzes the rate-limiting step in the formation of melanin from tyrosine. This enzyme is responsible not only for enzymatic browning in plants but also for melanogenesis in mammals. Thus, tyrosinase inhibitors have a huge impact on industry and the economy. In the current study, at first the enzyme was purified and then we evaluated inhibitory potency of three benzaldehyde derivatives: 2,4-dihydroxybenzaldehyde, 3,4-dihydroxybenzaldehyde and 4-dimethylaminobenzaldehyde on diphenolase activity of the purified mushroom tyrosinase, compared to kojic acid. Despite their close structural similarity, 2,4-dihydroxybenzaldehyde was found as a potent and competitive inhibitor while a weak uncompetitive inhibition was observed for 4-dimethylaminobenzaldehyde. Further complementary studies on these types of inhibitors, as potential drug candidates for treating abnormal melanin pigmentation, are needed.
[ABSTRACT]   Full text not available  [PDF]
  1,620 178 -
Synthesis and cytotoxic evaluation of 6-amino-4-aryl-3-methyl-2,4-dihydropyrano[2,3-C]pyrazole-carbonitrile derivatives using borax with potential anticancer effects
Hadi Adibi, Leila Hosseinzadeh, Sepideh Farhadi, Farahnaz Ahmadi
July-December 2013, 2(2):116-124
A green and efficient one-pot, four-component synthesis of 6-amino-4-aryl-3-methyl-2,4-dihydropyrano[2,3-c]pyrazole-carbonitrile derivatives catalyzed by borax in water has been examined and described. This method has several advantages such as environmental friendliness, shorter reaction time, excellent yields, and simple workup procedure. The in vitro cytotoxic activity of the synthesized compounds was investigated against cancer cell lines (SW48, A549, KB, HepG2) in comparison with doxorubicin, a well-known anticancer drug, using MTT colorimetric assay. The synthesized compounds showed good and reasonable cytotoxicity compared with doxorubicin in some studied cell lines. The compounds 5b, 5c, 5g in KB cell line (IC50 = 8±2.217 μM, 7±2.77 μM, 7.5±1.49 μM respectively), 5f in A549 cell line (IC50 = 31.5±2.02 μM), 5g in HepG2 cell line (IC50 = 22.5±3.09 μM), 5e, and 5i in SW48 cell line (IC50 = 23±0.772 μM, 23±4.97 μM respectively) showed the best results in close to the control drug (IC50 = 6.8±0.78 μM, 6.3±0.65 μM, 5.4±0.5 μM, 4.3±0.12 μM in A549, HepG2, KB, and SW48 cell lines respectively).
[ABSTRACT]   Full text not available  [PDF]
  1,587 160 -
Design of intelligent polymer of gelatin- poly N-isopropyla-crylamide under gamma radiation for cellular applications
Saeed Heidari-Keshel, Bita Soleimani, Maryam Ebrahimi, Asghar Ashrafi Hafez, Razieh Fallahakbarpour, Mohammad Khaledian, Fatemeh Yousefi, Maryam Rostampour Kakroudi, Forough Fathi Arateh
July-December 2013, 2(2):171-178
Thermo-sensitive polymers were prepared by graft copolymerization of gelatin with N-Isopropylacrylamide via gamma radiation. Characterization of polymers such as DSC analysis, swelling in different ratios and cell assays were investigated. DSC and solubility analysis showed gelatin and N-Isopropylacrylamide monomers were grafted via gamma radiation successfully. Results show swelling of samples increased as gelatin increased. Swelling ratio and curves results administrated hyd-ro-philicity / hydrophobicity of hydrogel that this property is due to presence of N-Isopropylacrylamide in different temperatures. The polymer was tested for harvesting epithelial cells after carrying out cell culture at 37 °C and incubating the confluent cells at 10°C for spontaneous detachment of cell sheet from polymer surface without enzyme treatment. These unique properties of the hydrogel would make it a promising support for drug delivery systems and tissue regeneration.
[ABSTRACT]   Full text not available  [PDF]
  1,593 148 -
Reversed phase high performance liquid chromatographic method for determination of quetiapine fumarate in pharmaceutical formulation and in spiked human urine
Kanakapura B Vinay, Hosakere D Revanasiddappa, Nagaraju Rajendraprasad, Pavagada J Ramesh, Kanakapura Basavaiah
July-December 2013, 2(2):131-139
A precise and feasible reversed-phase high-performance liquid chromatographic method for the determination of an antipsychotic drug quetiapine fumarate (QTF) in pharmaceuticals and spiked human urine sample has been developed and validated. The analysis was carried out using a ODS (250 mm × 4.6 mm i.d., 5 μm particle size) chromatopack column. Mobile phase containing a mixture of acetonitrile and 0.1% phosphate buffer (pH 3.1) (40:60) was pumped at a flow rate of 1 mL/min with UV detection at 240 nm at ambient column temperature (25°C). The method showed good linearity in the range of 0.09 – 18 μg/mL QTF with limits of detection (LOD) and quantification (LOQ) values of 0.03 and 0.09 μg/mL, respectively. The suggested method was successfully applied for the analysis of QTF in bulk drug, tablets and human urine with average recoveries of 100.06, 100.26 and 98.83%, respectively. The intra- and inter-day RSD values were less than 5%. The method is accurate, precise, sensitive and selective for routine analysis in quality control laboratories.
[ABSTRACT]   Full text not available  [PDF]
  1,572 165 -
Cytotoxic effects of the essential oil from Achillea wilhelmsii C. Koch
Toraj Ahmadi-Jouibari, Mohammad Reza Nikbakht, Kamran Mansouri, Mohammad Bagher Majnooni
July-December 2013, 2(2):98-102
The cytotoxicity activity of the essential oils from the leaves of Achillea wilhelmsii C. Koch were studied on six tumor cell lines and a normal cell line with Lactate dehydrogenases (LDH) and trypan blue methods. The composition of the essential oil was also analyzed by Gas Chromatography–Mass spectrophotometery (GC-MS). The LDH test showed that the oil had marked cytotoxicity activity against all cancer cell lines. K562 (Human chronic myelogenous leukemia) and PC3 (Human prostate adenocarcinoma), were the most sensitive to the essential oil with IC50 value (the concentration of the essential oil causing 50% inhibition) of 12.62±1.3μg/ml and 15.88±2.4μg/ml, respectively. The least cytotoxic activity was exhibited on HUVEC (Human umbilical vein endothelial cell) and Hela (Human cervix carcinoma) cell lines with IC50 values of 19.85±3.2 and 46.34±2.7, respectively. Trypan blue assay approved these results. In conclusion, cytotoxic activities of the oil may be described by the presence of monoterpene derivatives. the results of this study suggest that the essential oil of A. wilhelmsii has a potential source for cancer therapy. As a significant result, HUVEC (as normal cells) exhibited the least sensitivity to cytotoxic effects of the oil, confirming its high selectivity and specialty against cancer cell lines.
[ABSTRACT]   Full text not available  [PDF]
  1,562 160 -
Simultaneous spectrophotometric determination of amlodipine and metoprolol by principal component regression multivariate calibration and comparison with HPLC
Mohsen Shahlaei, Farshid Hassanzadeh, Jaber Emami, Ehsan Sohrabi, Lotfollah Saghaie
July-December 2013, 2(2):179-189
Multi-drug therapy in high blood pressure is appreciated to achieve a normal blood pressure. A simple spectrophotometric method based on principal component analysis has been proposed for simultaneous determination of amlodipine (Amd) and metoprolol (Met) in pharmaceutical preparations. Calibration matrix contains 3.402 μgml-1 to 170.130 μg ml-1 amlodipine and 13.7 μg ml-1 to 68.5 μgml-1 metoprolol. The proposed method was validated by using a set of synthetic sample mixtures and subsequently applied to simultaneous determination of amlodipine and metoprolol in different pharmaceutical preparations.
[ABSTRACT]   Full text not available  [PDF]
  1,546 176 -
The study of essential oil of Hymenocrater longiflorus Benth growing in Paveh
Soheila Shahriari, Masume Khanahmadi, Reza Tahvilian
July-December 2013, 2(2):111-115
The genus Hymenocrater, belong to the Lamiaceae family, consist of 21 species throughout the world. In Iran, about 9 species are present, of which some are endemic. Plants belonging to these genuses are pharmacologically active and have been used in folk medicine all around the world. The aim of the present study was to detect the essential oils composition of Hymenocrater longiflorus Benth. collected from Paveh, Kermanshah province. Plant sample was dried in shade condition and the essential oil of the plant obtained by hydrodistillation by Clevenger type apparatus was analyzed by GC/MS. Yield of essential oil was (1.5 % v/w). The major components of the oil of H. longiflorus Benth were Hedycaryol (22.2), α- Cadinol (20.43), β-Bourbonene (5.76%), α-Terpineol (4.95%), Eudesmol <7-Epi-> (4.84%), β-Bourbonene (4.69%), Caryophylene oxide (4.32%) and Geijerene (4.08%), Caryophelen (2.99), Sabinene (2.6%), 1,8-Cineole (2.58%), δ-Amorphene (2.58%), δ-Caddinene (2.24%) and α-Pinene (2.07%) were the main compounds with the greatest content.
[ABSTRACT]   Full text not available  [PDF]
  1,532 164 -
Retinoic acid-oligomeric chitosan micelles as novel gene delivery carrier; in Vitro transfection study
Ali Fattahi, Mohammad-Ali Golozar, Jaleh Varshosaz
July-December 2013, 2(2):125-130
Amphiphilic cationic micelles have recently attracted much attention as non-viral vector. In the current study the retinoic acid-g-chitosan (RA-chitosan) micelles have been used as novel gene carriers. Uptake of micelles, condensation ability and transfection efficiency of micelle–DNA complexes (miceplexes) in the presence or absence of serum had been investigated on Hela and HepG2 cell lines. Uptake of micelles in Hela cells was faster and more effective than HepG2. After 1.5 hours, micelles were up-taken by Hela cells while no uptake was observed in HepG2 cells. Miceplexes showed lower transfection efficiency in both Hela and HepG2 cells grown in the serum free medium than chitosan polyplexes, with 7.25 × 105 versus 1.47 × 105 RLU.mg-1 and 7.76 × 105 versus 2.16 × 105 RLU.mg-1, respectively. Lower transfection efficiency of miceplexes could be attributed to their stronger complexation. Transfection in the presence of serum increased in both of the cell lines. These properties all together, make RA-chitosan micelles a potential gene carrier for active gene delivery into cells, particularly for transfection in the presence of serum.
[ABSTRACT]   Full text not available  [PDF]
  1,520 166 -
Chemical composition and general toxicity of essential oil extracted from the stalks and flowers of Rheum Ribes L. growing in Iran
Mohammad-Reza Nikbakht, Solmaz Esnaashari, Fariba Heshmati Afshar
July-December 2013, 2(2):165-170
The essential oil of Rheum ribes L. stalks and flowers, growing in Iran, were extracted with hydro-distillation and analyzed by GC-MS. Thirty constituents representing 93.84% of Rheum oil were identified. The oil was found to be rich in hydrocarbons especially long-chain n-alkanes (80.81%). The most abundant components in the oil included tricosane (26.29%), heneicosane (26.07%), pentacosane (10.63%), heptacosane (10.37%) and palmitic acid (3.64%). The essential oil was also evaluated for general toxicity bioassay using brine shrimp lethality method. The toxicity profile of the oil indicated some degree of toxicity in comparison with podophyllotoxin.
[ABSTRACT]   Full text not available  [PDF]
  1,525 158 -
Dispersive liquid-liquid micro-extraction as a sample preparation method for clonazepam analysis in water samples and pharmaceutical preparations
Loghman Miri, Fahimeh Jalali
July-December 2013, 2(2):103-110
Dispersive liquid–liquid micro–extraction (DLLME) technique was successfully used as a sample preparation method for the determination of clonazepam in pharmaceutical preparations and water samples. In this method, a suitable mixture of methanol (disperser solvent) and chloroform (extraction solvent) was injected rapidly into a conical test tube that contained an aqueous solution of clonazepam. After centrifuging, phase separation was performed by sedimenting the fine droplets of the micro–extraction solvent on the bottom of a test tube (about 100 μL) and then the absorbance of the enriched extracted phase was determined at the absorption wavelength of clonazepam (307 nm). Some important parameters such as, the type and volume of extraction and dispersive solvents as well as the extraction time were investigated and optimized. Under the optimum conditions, the calibration graph was linear over the range of 0.95 to 18.94 μg/mL of clonazepam with a limit of detection of 0.06 μg/ml.
[ABSTRACT]   Full text not available  [PDF]
  1,517 158 -
Molecular chaperones, amyloid-binding compounds or antioxidants?: Perspective on their application as possible therapeutic agents in reduction of cytotoxicity of amyloid oligomers
Reza Khodarahmi
July-December 2013, 2(2):205-206
Full text not available  [PDF]
  1,291 167 -