DARU, Journal of Pharmaceutical Sciences
Volume:11 Issue: 4, Winter 2003

Abstract: Using pharmacologic approach, neurokinin receptor-mediated bronchoconstrictor responses in anesthetized guinea-pigs was characterized. Thus, the bronchospastic effects of substance P (SP) and SP fragments (all administrated intravenously) before and after giving vehicle or selective neurokinin receptor antagonists were compared. Ranking order of potency of SP or SP fragments for induction of bronchoconstriction was: SP4-11 >> SP5-11 = SP3-11 = SP2-11 > SP = SP6-11 (the number of amino acid in the sequence of SP fragments are shown by superscript). The neurokinin 1 (NK1) receptor antagonists (CP 96,345 or CP 99,994, 3 mg kg-1, iv) did not change baseline values of pulmonary flow resistance (RL) and dynamic pulmonary elastance (EL) and did not eliminate bronchopulmonary responses to these peptides but decreased changes in RL and EL in response to SP and SP fragments. The neurokinin 2 (NK2) receptor antagonist SR 48,968 (1 mg kg-1, iv) failed to induce a rightward shift in dose-response curves to SP or SP fragments except to SP4-11. Combinations of NK1 and NK2 receptor antagonists shifted dose-response curves to SP and SP fragments more than that of NK1 receptor antagonists alone. These findings reveal that SP-induced bronchoconstriction is mediated by its C-terminal sequence and this response is mainly via NK1 receptors. Moreover, bronchopulmonary responses to SP and its C-terminal fragments are complex and there may be interactions between NK1 and NK2 receptors in the lungs.

Abstract: Albumin microspheres (AMS) have found many applications in the diagnosis and treatment in recent years and more than 100 diagnostic agents and drugs have been incorporated into AMS. In the present study Bovine Serum Albumin (BSA) based microspheres bearing propranolol hydrochloride were prepared by an emulsion-internal phase stabilization technique. The prepared microspheres were studied for particle size distribution, drug loading, release characteristics, bioadhesion and in-vitro controlled diffusion across the rat intestine. The microspheres had mean diameters between 1-25 mm of which more than 50 percent were below 5 mm. The encapsulated drug was found to be about 9% w/w of that initially added to microspheres and the superficial drug was 25% of the total amount of the encapsulated drug. Also AMS were noted to possess good bioadhesion in such a way that about 70% of microspheres remained adherent on the surface mucosa of rat jejunum.The drug release from albumin microspheres was mainly controlled by diffusion and showed a biphasic pattern with a high initial release (burst effect), followed by a more gradual terminal release. The total amount of drug released from microspheres after 12h was 70%. In vitro experiments on the rat intestinal segments revealed that the microspheres could effectively pass their content through intestinal membrane.

Abstract: Granule capability is defined in terms of the strength of individual granule and friability of granulation batch to withstand breaking, abrasion and compactibility. Binder(s) are added to perform the above properties. The common methods to asses their capability are to test crushing strength of the granules directly and to make statistical analysis and /or testing the friability of bulk granulation. In this work four substrate models including polymethylmetacrylate beads(PMMA),glass powder, acetaminophen, and para-aminobebzoic acid were chosen. The binder models were corn starch, gelatin, methylcellulose (MC) and hydroxypropylmethylcellulose (HPMC). After massing the substrates with the binder solutions, discs were produced by the mean of the mold technique. The discs were dried and conditioned and then tested for tensile strength while the failed areas were scanned by SEM. Various granulations were made and the results of friability and crush strength were compared with the discs strength. The bond areas in the SEM showed the trend with the binder concentration. A comparison of the standard deviation shows that discs have much lower level of the strength than granules. The resulting discs showed a higher performance which is related to the stems for the discs shape. In conclusion, this method is a simple and is applicable to differentiate efficacy of binder under studies.

Abstract: Lead as one of the environmental pollutants can threats the life of living creatures in many ways. In this study, hematological effects of chronic toxicity of the lead acetate in adult male rats through measurement of the lead concentration in the blood of animal’s heart by atomic absorption as well as hematological analyses and differential cell count were investigated. Results showed that lead concentration in the treatment group was significantly higher than that of the control groups (P<0.001), and basophilic stippling, Howell-Jolly bodies, decreased RBC count (anemia), increased leukocyte count (leukocytosis), monocytosis, eosinopenia, neutrophilia, and thrombocytosis were observed in the test group (P<0.001). It is concluded that microcytic hypochromic anemia can be attributed to the interaction of lead with iron and copper metabolism and increased leukocyte count may be linked to the inflammatory effects of lead on lymphatic organs.

Abstract: In the present in vitro study, using superfusion technique, the pharmacological responsiveness of the excisional wound granulation tissue myofibroblasts to a variety of agents were compared with those of normal connective tissue taken from the superficial fascia. Bolus doses of angiotensin II (0.1 to 1000nM), mepyramine (1 to 128µM), calcium chloride (75 to 300µM) and potassium chloride (100 to 400µM) were added to the superfusate solution and the responses were recorded on Narco chart recorder. The results showed that both types of tissues have qualitatively similar characteristic responsiveness to potassium and calcium ions, mepyramine and angiotensin II. However, quantitatively, they were distinctly different, the myofibroblasts from granulation tissues produced greater contractile responses to mepyramine and angiotensin II, whilst they lost most of their responsiveness to potassium and calcium ions. The present study demonstrated that these tissues respond to pharmacological manipulation, but the responses they produce are distinct from smooth muscle cells and need to be considered further in experiments involving wound healing.

Abstract: The use of plants in treatment of burns, dermatophytes, and infectious diseases is common in traditional medicine of Iran. Based on ethno pharmacological and taxonomic information, antibacterial activities of methanol extracts of some medicinal plants of Iran were determined by In Vitro bioassays using agar diffusion-method against standard strains of Pseudomonas aeruginosa, P. fluorescens, Bacillus subtilis, B. cereus and B. pumilis at 20 mg/ml. From 180 plant species of 72 families, 78 species (43.3%) in 42 families (58.3%) showed antibacterial activities against B. cereus (88.4%), B. subtilis (39.7%), B. pumilis (37.1%), P. fluorescens (37.1%) and P. aeruginos (10.2%). The most active plant families were Apiaceae, Compositae and Labiatae with 9, 8 and 7 active plant species respectively. Minimum inhibitory concentrations (MIC) of the active plants were determined using two fold serial dilutions. Most active plant against Bacilli was Myrtus communis L. with MIC of 1.87 mg/ml. For Pseudomonas species, Dianthus caryophyllus L. and Terminalia chebula (Gaertner) Retz. were more active with the MIC of 0.46 mg/ml for P. fluorescens and of 1.87 mg/ml for P. aeruginosa respectively.

Abstract: Lilium ledebourii (Baker) Boiss.(Liliaceae), locally named “Susan -e Chelcheragh” is a native and rare species grown on the heights of Damash region (ca. 2100 m) in Gilan province, north part of Iran.The microscopic and anatomical features and the composition of oils of flower and corm of this unique plant were studied. The microscopic study has shown the main characteristic elements of leaf, stem, corm and flower of this plant. The composition of essential oils of flower and corm were determined by coupled GC-MS analysis. The yields of oils of flower and corm were 0.71 % and 1.65 % (v/w) respectively. The major components of flower’s oil were isopulegol (55.15 %), pentacosane (18.1%), 3-methyltricosane (9.97%), tricosane (5.35%), 2-methylpentacosane (4.35%), docosane (4.28%) and linalool oxide (2.20%). The components of corm’s oil were almost fatty acids. No aromatic volatile compound was found in the corm oil. Primary qualitative phytochemical tests of stem, leaf, corm and flower showed positive results for alkaloid and flavonoid (one plus) in stem and for saponin (4 plus) in corm and (2 plus) in the flower. Tests for tannin in all parts were negative. Further phytochemical and botanical studies on this unique plant is of importance.

Abstract: A new guaianolide, 3β, 4β –epoxy-8α–isobutyryloxyguaia – 1(10), 11(13) – dien – 12,6α–olide (Carlaolide) (1) from Tanacetum fruticulosum was isolated, and it’s structure was elucidated on the basis of spectroscopic data. Keywords: Tanacetum fruticulosum, Compositae, Sesquiterpene lactone, Guaianolide.