PHARMACEUTICAL SCIENCES
Year:2005 | Volume:- | Issue:3|Papers Count:15

Objectives: Solvents are one of the most important ingredients in the preparation of hygienic and cosmetic products. Nowadays the adverse effects of the sun light on the skin such as stinging, erythema and finally skin cancer have been known. Therefore the use of anti preparations is common. In this study we tried to evaluate the effect of the solvents in altering of absorption amount and λmax of UVB for the chemical substance of products. METHODS: For this mean anti solar materials were solved in solvents i.e. water, sorbitol, ethanol, propylene glycol and glycerin. Then spectra and absorption intensities of them were measured in 5 nm intervals using by spectrophotometer instrument. Finally according to them maximum absorption. Shift amount, area under the curve and relative efficacy of the anti solar substance were calculated. RESULTS: The results showed that the type of solvent had significantly effect on lmax. It should be considered that in the formulations containing Parsol 5000, using water and sorbitol as a solvent is not reasonable. Because these solvents will shift the lmax sunscreen and the efficacy of the preparation will be lost Most of the solvents altered the lmax the benzophenon toward lower wave lengths. It was showed that PABA and Parsol HS had low sensitivity to the type of solvent among other sunscreens. Then it is possible to use most of the solvents in formulations as sunscreen products. It is necessary to say that the SPF of the product may be changed because of altering the lmax and absorption intensity of the anti solar substance by the solvents. CONCLUSION: Then it is possible to choose proper solvent for the each of above anti solar materials.

OBJECTIVES: Terfenadine, as an antihistaminic agent. is widely used to control seasonal allergy such as rhinitis. Terfenadine is in fact a prodrug and is rapidly absorbed from the gastrointestinal tract It undergoes extensive first-pass metabolism in the liver to its active metabolite the carboxylic acid derivative fexofenadine. Sustained or controlled- release dosage forms favor the strategy of therapy by minimizing the side effects via reducing terfenadine plasma concen1ration which is the main cause of its cardiotoxicity as well as maximizing the patient compliance. However, few studies have been conducted to formulate the controlled-release dosage forms. Thus, in the current investigation in an attempt to formulate oral controlled-release terfenadine. METHODS: We have directly compressed terfenadine with a designated mixture of hydroxypropyl methylcellulose (HPMC) and magnesium stearate using 13.5, 54.0 and 67.5 MPa compression pressure. Also two conventiona tablets (home and foreign made) as well as the drug powder were included in the release studies. The content uniformity of the matrices and the tablets were assessed. Further, the release profiles of the prepared matrices were evaluated exploiting various classical kinetics models i.e., Weibull, Hixon-Crowell cube root, Higuchi square root of time, probability linear and log linear, first-order, zero-order and polynomial model comprising erosion and diffusion terms. Among the models used, the data was fitted best to the polynomial model with lag time. RESULTS: No significant difference was detected for content uniformity. The release of the drug from the matrices was markedly dependent on the compression pressure, that is the higher the pressure the lower is the release rate and hence the longer the complete release time. The complete release times were 480, 510 and 570 min for the compression pressure of 13.5, 54.0 and 67.5 MPa, respectively. The conventional tablets and the drug powder exhibited rapid dissolution compared to matrices. CONCLUSION: Based upon our results, it appears that the terfenadine HPMC matrix provides reliable sustained characteristics from release rate point of view.

OBJECTIVES: Citrullus colocynthis (Handal) is a medical plant have been used for the treatment of diabetes in Iran from a long time ago. METHODS: The antidiabetic effect of hydromethanolic (70%) extracts of Handal on the plasma glucose levels were investigated in diabetic rabbits. The rabbits were randomly divided to 3 groups, the first group as a control the second and the third as a test 100 mg/kg and 200 mg/kg of extracts were administrated orally to group 2 and group3 for 6 days respectively.RESULTS: The first day, oral administration of 100 mg/kg of C. colocynthis, produced non significant reduction in plasma glucose levels after 2 and 6h and significant reduction after 12 h in comparison with the first group (p<0.05). Every 3 time, the dose of 200 mg/kg was due to significant blood glucose reduction in comparison with the control group. Mean blood glucose levels decreased in both test groups during the third and the fifth day of study, However, it was significant only in group 2 the fifth day (p<0.000) All the rabbits of group 3 died of diarrhea in the sixth day of experiment. CONCLUSIONT: he results suggest that although hydromethanolic extract of the pulp of C. colocynthis can decrease plasma glucose levels in diabetic rabbits, further studies are necessary for finding the effective and safety dose.

OBJECTIVES: Ibuprofen was the first non-steroidal anti-inflammatory drug (NSAID) which was commonly used for the treatment of pain and inflammation. Ibuprofen can cause serious gastrointestinal, renal and cardiovascular side effects especially when used in high doses and/or over long periods of time. NSAIDs have been combined with other drugs, including opioid analgesic agents and glucosamine in order to achieve an effective degree of analgesia with lower dosage of the NSAID. These combination products exhibit a variety of effects on the level of analgesia, which may be sub-additive (inhibitory), additive or super additive (synergistic). Contrastive pharmacological results have been obtained in co-administration of ibuprofen and glucosamine. The reason for these contrastive results is unknown. In this study, we tried to understand the reason of these contradictions. METHODS: For this mean, solubility dissolution rate protein binding and partition coefficient of ibuprofen alone and in combination with glucosamine were studied. RESULTS: The results showed that glucosamine increased solubility and dissolution rate of ibuprofen. In preparations with 1:1 or higher ratios of ibuprofen to glucosamine the protein binding of ibuprofen was increased. The peak of melting point was altered in DSC thermogriun that can indicate to formation of complex between ibuprofen and glucosamine during process. Partition coefficient of drug decreased in combination form with glucosamine. This is an important phenomenon in permeability of drug through mucus membrane. CONCLUSION: The Above results may be helpful to explain the contrastive results that obtained from studies.

OBJECTIVES: Anti-lymphocyte globulin (ALG) is a polyc1onal anti human lymphocyte surface markers which is produced in rabbits. ALG is one of the potent immunosuppressive agents which is currently used for preventing organ allograft rejection, treatment of aplastic anemia and some autoimmune disorders. ALG causes elimination of human lymphocytes from the peripheral blood circulation, regulation of cytotoxic activities and apoptosis. The goal of this project was urification of ALG by a simple, rapid and inexpensive method, ion exchange chromatography. METHODS: ALG riched serum of immunized rabbit with human lymphocytes was diluted with phosphate-buffered saline (PBS, pH 7.4) in a ratio of 1:1 and precipitated with ammonium sulfate in the final concentration of 50%. The precipitant was rewashed with 50% ammonium sulfate, dialyzed against tris-phosphate pH=8.1 and applied to ion-exchange chromatography on DEAE-Sepharose 6B.ALG riched fraction was eluted with starting buffer; Tris-Phosphate (PH=8.1) and final buffer; Tris-Phosphate containing 50 mM NaCl (PH=8.1). RESULTS: The purity of ALG with high percent purity was confirmed by SDS-PAGE, and efficiency of it by histocompatibility assay. CONCLUSION: This preparation is comparable in purity to those of commercially available standard ALG in the benefit of self sufficiency. The 1/80 dilution of purified ALG can lyse human lymphocytes properly in histocompatibility testing which verifies its high efficiency.

OBJECTIVES: Perioperative hypothermia occurs due to dysfunction of thermoregulatory system because of anaesthetic drugs and patients contact with the cold environment of an operative room. It can produce some complications such as post anesthesia shivering. Post anesthesia shivering can produce adverse haemodynamic, metabolic sequelae and prolong hospital admission.This study was designed to evaluate the effect of hydrocortisone and dexamethasone pretreatment on the rate and severity of shivering. Methods: A randomized, double-blind, placebo-controlled study was done. 150 patients undergoing selective general surgery were studied. Patients were randomly divided into three equal groups. Patients of group I received dexamethasone, group II received hydrocortisone and group III received a placebo on normal salin before induction of anesthesia. The rate and severity of post anesthesia shivering and haemodynamic variables were recorded. Results: In this study, 58 patients experienced shivering. The rate of post anesthesia shivering recorded in group I (24%), group II (28%) and group III (64%) (p<0.05). Also severity of shivering in both group I and II was mild but it was recorded moderate and severe in group III.Conclusion: The Results of this study showed that hydrocortisone and dexamethasone pretreatment could significantly decrease the rate and severity of post anesthesia shivering. The effects of these drugs are dispensed through anti inflammatory mechanisms and reduction of central and skin gradient.

OBJECTIVES: Multipotent mesenchymal stem cells (MSc) are known for a long period of time. These cells are adherent, clonogenic and fibroblastic and can be isolated from bone marrow stroma of postnatal organisms. Under appropriate conditions, these cells can give rise to the broad spectrum of fully differentiated connective tissues including cartilage, bone, adipose tissues and muscle cells. Upon isolating of cells in vitro, these cells tend to differentiate and it is very difficult to direct these cells into self-renewal in order to get more Multipotent MSc for medical purposes. In the previons study, the effect of leukemia inhibitory factor (LIF) on MSc was investigated and it was shown that in the presence of LIP, MSc have more proliferation ability and the self renewal ability of cells increases. Also it was shown that these cells tend to differentiate into bones. In this study the effect of Mitogen Activated Protein Kinase Inhibitor (MAPKI) on MSc was investigated. METHODS: Bone marrow stroma cells were extracted from 2-month-old mice. These cells were cultured in a medium containing 25 micro moles MAPKI. After formation of colonies, cells were stained by methylen blue. The activity of alkaline Phosphatase was also investigated. To study the effect of both LIP and MAPKI simultaneously on colony formation ability of MSc, cells were cultured in a culture containing 25 micro moles MAPKI and 500 U/ml LIF. The number and size of colonies was studied. Results: In the presence of MAPKI the number and the size of colonies (CFU-F) formed in the culture was significantly decreased. The number of CFU-ALP+ in the culture containing MAPKI was decreased according to the decrease of CFU-F number. Adding MAPKI to a medium containing LIF neutralized the effect of LIP on MSc. Conclusion: The presence of MAPKI in the culture affects the number of colonies. This factor, despite LIP, does not affect the expression of alkaline phosphatase in Mesenchymal Stem Cells. UF increases the self renewal and proliferative ability of cells. Adding MAPKI factor to a culture containing LIP neutralizes the proliferative effect of LIF.

OBJECTIVES: Aluminum (AI) is a toxic metal at high levels and has been involved as a causative factor in several diseases, therefore, its determination in different samples is very important. METHODS: In this study a method based on cloud point extraction (CPE) technique in mixed micellar medium was applied for the extraction and preconcenttation of Al in different samples. For the CPE of Al, an aliquot of 25 ml solution containing appropriate amounts of Al, acetate buffer, morin and surfactant (Tttiton X-114 + SDSN) were kept in the thermostatic bath at 50ºC. Thus, two phases were appeared and separation of these phases was achieved by centrifugation. After cooling in ice-bath the surfactant-rich phase became viscous and the upper aqueous phase decanted. The fluorescence intensity of chelate in the micellar phase (after addition of 2.5 ml of ethanol-water mixture) was measured at 512 nm with the excitation set at 442 nm. RESULTS: The parameters affecting complication and phase separation were studied and optimized. Under the optimum experimental conditions, the detection limit of Al for the preconcenttation of 25 ml of solution was 0.52 µg 1-1 . The calibration graph was linear within a range of 2-200µg 1-1 AI. The relative standard deviation (RSD) of 5 replicated determinations of 10 µg 1-1  of AI was 2.1%. CONCLUSION: The method was successfully applied to the determination of Al in water samples and parenteral solutions.

Objective: Benzoyl peroxide (BPO) is commonly used in topical formulations for the treatment of acne. Skin irritation is a common side effect, and it has been shown that controlled release of BPO from a delivery system to the skin could increase patient compliance and reduce the side effect while reducing percutaneous absorptioo. Method: In this study, MMA/EGDM copolymer was prepared by monomers methyl methacrylate and ethylene glycol dimethaaylate. After impregnating copolymer MMA/EGDM, microsponges were evaluated in respect to morphology, particle size, volume, pore size and molecular weight characteristics. Releases of drug from microsponges were investigated using Cell-Franz with dialysis membrane and drug release was determined by HPLC. Results: The results showed that the cumulative amount of release increased with an increase in the concentration of the active ingredient in the formula. The amount of drug released at the first hour was higher compared to its released amount at 2ndh. This could be due to the presence of non encapsulated BPO in these formulations. When the free BPO was released, the flux remained constant for the next 7 hrs. CONCLUSION: This flux represents the release of entrapped drug from microsponges. Released BPO in different dosage forms was respectively lotion < gel < cream. The topical microsponge delivery system can clearly maximize the amount of time that an active ingredient presents on the skin surface within the epidermis, therefore, into the body.

OBJECTIVES: This study was designed to increase the dissolution rate of poorly water soluble anti rheumatic agent, indomethacin, preparing solid dispersion with different with polyethylene glycoles of different molecular weights, and to study the mechanism of enhanced dissolution properties. Methods: PPEG2000, PEG4000, PEG6000 and PEG20000 were used as carriers and the solid dispersions were prepared by modified solvent method. Evaluation of solid dispersion properties was performed using solubility measurements, dissolution studies, Fourier-transform infrared spectroscopy and X-ray powder diffractometery (PXRD). Result: The results from solubility measurement indicated that, the solubility of indomethacin increased as the concentration and the molecular weight of PEG increased. The dissolution data revealed that these carriers can enhance the in vitro dissolution rate of indomethacin in both SGF (Simulated Gastric Fluid) and SIP (Simulated Gastric Fluid) media. The results of infrared spectroscopy together with those from x-ray diffraction showed no drug-carrier interactions and indomethacin was still detectable in its solid state in all solid dispersions. Conclusion: An increased dissolution rate of indomethacin at pH 1.2 and 7.2 was observed when the drug was dispersed in these carriers. The solubilization effect of polyetbylene glycoles as well as the reduction of particle aggregation and an alteration of the surface properties of the drug particles might be responsible for the enhanced dissolution rate.

OBJECTIVES: The present study was performed to investigate the role of 5-HT 1A Receptors in dorasal and median raphe nuclei on the withdrawal syndrome of morphine and acceleration the restraint of opioides. METHODS: Experiments were performed on adult male wistar weighing between 225 and 275 g. The control group (n=8)bad 9 days s.c. injections of morphine (5, 10, 10, 15, 15, 20, 20. 25, 25mg/kg12h) and the last day, 60 minutes after first injection of  morphine 5mg/kg naloxone was injected (i.p.) and sips of withdrawal syndrome were recorded until 60 minutes. In the sham and test group following inductionanoesthesia, rats were secured in a stereotaxic frame with ear and incisor bars. Then a guide cannuls was implanted into the DRN and MRN in the separated groups (0=8). After five days recovery of animals, injections of morphine began and the 9th day, 55 minutes after first s.c. injection of morphine, 1µ/2min of 1-(2-methoxypbeoyl)-4-[4-(2-pthalimmido) butyl] piperazine hydrobromidc (NAN-190) vehicle was injected into the nuclei in the sham group. But in the test groups 1.5, 3.0 and 6.0 µg/µl/2min of NAN-190 (antagonist of 5-HT1A receptors) was injected Do the nuclei, and then naloxone was injected (i.p.).RESULTS: Data sips were analyzed by one way ANOVA and Tukey post test. The results this study showed a significant decrease in some of the recorded morphine withdrawal sips (jumping p<0.05, writhing p<0.01 and wet-dog shakes p<0.001) in test groups in comparison with the control group. CONCLUSION:  The results confirmed the important role of 5-HT1A receptors in raphe nucleuses on some of the morphine withdrawal signs and may dissolve problems of opioides addiction.

OBJECTIVES: The importance of using sunscreens is not unknown nowadays. Mean while the adverse reactions of some synthetic chemical or physical sunscreens and successful researches done on using natural ingredients from plants and animals, extended the way of studying on natural compounds of which Artemia is one new example. The aim of this investigation was to study the sunscreen effects of total extracts of Artemias and their fractions. METHODS: For achieving this aim, two main steps were taken including preparation of different extracts and fractionating them and then studying their UV spectra. The dried Artemia powder was extracted with hexane for 24h, and then the remained powder was extracted with dichloromethane. Extraction with dichloromethane caused remarkable decoloration of Artemia powder. Final extraction was done by several solved systems including methanol, ethanol am hydro alconholic solution (70: 30 water- ethanol).The liquid extracts were dried by rotary evaporator at ambient temperature and reduced pressure and standard solutions were prepared from dried extracts. For preparing of standard solutions, a distinct weight of dry extracts was dissolved in equal volwne of solvent. The UV spectra of the solutions were recorded in the range 190-400 nm. Then fractionation of these extracts was done f<r more accurate aualysis of active sunscreen ingredients included in them. For this purpose, the total extracts were chromatographed over a column of Sephadex LH-20 using MeOH. RESULTS: The collected fractions were aualyzed by UV spectrophotometer individually and the same samples were combined with each other for determining the main fractions. After evaluation of fractions, the best sunscreen fraction was selected based on UV absorption characteristics. The second fraction of hydro alcoholic (70:30) and the third fraction of methanol extract had the best results in UV-B region. CONCLUSION: The Results of the present study showed that the hydroalcoholic and methanol extract of Artemia urmiana as well as Artemia salina can be used as sunscreen in topical preparations but it would be suggested to use hydro ethanolic fraction in formulating sunscreen products because of disadvantages of methanol application in topical formulation.