DARU, Journal of Pharmaceutical Sciences
Volume:10 Issue: 2, Summer 2002

Abstract: Humanized monoclonal antibody U36 and its F(ab'')2 fragment, radio labeled with 125I, were tested for tumor localization in nude mice bearing a squamous cell carcinoma xenograft line derived from a head and neck carcinoma. Monoclonal antibody IgG or F(ab'')2 fragment were injected in parallel and at days 1, 2 and 3, mice were dissected for determination of isotope biodistribution. IgG as well as F(ab'')2 showed highly specific localization in tumor tissue. The mean tumor uptake (n=3) is expressed as the percentage of the injected dose per gram of tumor tissue (%ID/g). %ID/g of IgG was 11.7% at day 1 and decreased to 10.9% at day 3 whereas %ID/g of F(ab'')2 was 2.9% at day 1 and decreased on following days. Tumor to blood ratios (T/B) at day 1 were 0.86 for IgG and 1.32 for F(ab'')2 and reached a maximum at day 3 with values of 4.41 and 1.84 respectively. These findings suggest that the superior tumor to non-tumor ratios in the day of 1 render the F(ab'')2 fragment more qualified for specific targeting radioisotopes to tumor xenografts in this exprimental setting.

Abstract: The use of secondary metrics has become special interest in bioequivalency studies. The applicability of partial area method, truncated AUC and Cmax/AUC has been argued by many authors. This study aims to evaluate the possible superiority of these metrics to primary metrics (i.e. AUCinf, Cmax and Tmax). The suitability of truncated AUC for assessment of absorption extent as well as Cmax/AUC and partial AUC for the evaluation of absorption rate in bioequivalency determination was investigated following administration of same product as test and reference to 7 healthy volunteers. Among the pharmacokinetic parameters obtained, Cmax/AUCinf was a better indicator or absorption rate and the AUCinf was more sensitive than truncated AUC in evaluation of absorption extent.

Abstract: Matricine of flowers of cultivated Matricaria chamomilla L. was isolated and identified by TLC, IR, UV and ¹H-NMR and quantified by HPLC. One of the lopophylic materials of this plant (matricine) has been used as antispasmodic and anti-inflammatory. Retention of matricine by microencapsulation technique was one of the objectives of this study. Encapsulation was carried out by cold dehydrating liquid method and effects of the various process parameters on retention of the matricine were evaluated. To achieve high retention values it was necessary to employ low core to shell material ratio, high solid concentration, high viscosity of the emulsion continuous phase, the use of absolute ethanol as desiccant, short contact times between capsules and desiccant, and low air pressure in the formation of microcapsules. Results suggested that the process might be much more efficient if continuous coextrusion of the emulsion and desiccant were used.

Abstract: A dicholoromethane extract of the roots of Valeriana sisymbriifolia Vahl. afforded a new valepotriate. I-α-aceisovaltrate and a new valepotriatehydrine, acetoxydesiovaleroxy-1-α-acetoxy-isovaleroxy isovaltratehydrine together with a known compound, valtrate. Structural assignments of the compounds were based on spectroscopic methods (UV, IR, MS, ¹H-NMR and ¹³C-NMR). Keywords: Valeriana sisymbriifolia, Valepotriate, 1-α, -Aceisovaltrate, Iranian valerian

Abstract: The chemical compositions of the essential oils and the volatile concentrate of Mentha piperita L. (Labiatae) obtained by supercritical carbon dioxide extraction (SFE) at 35°C and 100 atm were compared using GC/MS. Whereas twenty four components were identified in the essential oil, only seven compounds, including the main compounds of the peppermint oil were isolated by the SFE. The percent of major components of the oil and the extract were: Menthol (31.53 and 48.39), Menthone (23.37 and 26.68) and Isomenthone (11.11 and 6.58), respectively. From these results it may concluded that the SFE method supply a selective essential oil extract.

Abstract: Natural sterols are potential raw materials for the prepartion of pharmacologically active steroid products. This paper details preparation of testosterone, one of the steroidal hormones, through microbial metabolism of cholesterol followed by chemical reduction. The side chain of cholesterol was selectively cleaved by Mycobacterium smegmatis PTCC 1307, and then selective reduction of resulting 17-keton group of androst-4-ene-3, 17-dione (AD), the main product of microbial transformation, with sodium borohydride at -10°C gave testosterone in high yeild (90%). Assignment of structures were made by IR, NMR, Mass, and UV spectroscopic data.

Abstract: The purpose of this study was to evaluate the efficacy of the topical use of 0.2% oral mouth wash of essential oil of zataria multiflora in the control of recurrent aphthous stomatitis (RAS). In this double-blind, randomized study each of 60 patients with RAS was assigned to one of the 2 management modalities. Those in group Areceived an oral rinse solution of Zataria multiflora essential oil, 3 times a day for 4 weeks and those in group B received placebo 3 times a day for 4 weeks. The patients were monitored two times weekly. A statistical Chi-Square test was performed to analyze the data. Zataria multiflora oral rinses was shown to be more efficacious than placebo in the treatment of patients with RAS.

Abstract: In this study, 278 species from 37 families of native Iranian plants were screened for in vitro antifungal activity against 19 fungal strains. Initially, the crude extracts in concentration of 100 μg/ml were tested. Among 278 plant extracts, 201(71.27%) of them showed antifungal activity against at least one fungal strain. A wide range of total extracts of different species were shown to have potentially noticeable antifungal effects. The outstanding species were: Mentha longifolia, Saliva multicaulis, Thymus transcaspicus, Zataria multiflora, Glycyrrhiza glabra, Hulthemia persica, Heracleum persicum, Pimpinella anisum, Pragnos ferulacea, Pragnos uloptera, and Viola odorata.