17 research outputs found

    Токсикологические свойства корневищ с корнями сабельника болотного

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    РАСТЕНИЯ ЛЕКАРСТВЕННЫЕТОКСИКОЛОГИЯФАРМАКОЛОГИЯЯДЫВРЕДНОДЕЙСТВУЮЩИЕ ВЕЩЕСТВАТОКСИЧЕСКОЕ ВОЗДЕЙСТВИЕ (ВНЕШ)РАСТИТЕЛЬНЫЕ ПРЕПАРАТЫСАБЕЛЬНИК БОЛОТНЫ

    Razvoj i in vitro vrednovanje puferiranog bioadhezivnog vaginalnog gela za miješane vaginalne infekcije

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    An acid buffering bioadhesive vaginal (ABBV) gel was developed for the treatment of mixed vaginal infections. Different bioadhesive polymers were evaluated on the basis of their bioadhesive strength, stability and drug release properties. Bioadhesion and release studies showed that guar gum, xanthan gum and hydroxypropylmethylcellulose K4M formed a good combination of bioadhesive polymers to develop the ABBV gel. Mono sodium citrate was used as an acid buffering agent to provide acidic pH (4.4). The drugs clotrimazole (antifungal) and metronidazole (antiprotozoal as well as antibacterial) were used in the formulation along with Lactobacillus spores to treat mixed vaginal infections. The ex vivo retention study showed that the bioadhesive polymers hold the gel for 12-13 hours inside the vaginal tube. Results of the in vitro antimicrobial study indicated that the ABBV gel had better antimicrobial action than the commercial intravaginal drug delivery systems and retention was prolonged in an ex vivo retention experiment.U radu je opisan razvoj puferiranog biodhezivnog vaginalnog (acid buffering bioadhesive vaginal, ABBV) gela za terapiju miješanih vaginalnih infekcija. Ispitani su različiti bioadhezivni polimeri procijenjena su njihova bioadhezivna svojstva, stabilnost i sposobnost oslobađanja ljekovite tvari. Guar guma, ksantan guma i hidroksipropilmetilceluloza K4M tvore dobru kombinaciju za ABBV gel. Mono natrijev citrat upotrebljen je kao puferirajuća tvar koja omogućava blago kiseli pH (4,4), a kao ljekovite tvari upotrebljeni su klotrimazol (antimikotik) i metronidazol (antiprotozoik i antibakterijsko sredstvo), zajedno sa sporama Lactobacillus. Pripravci su upotrebljeni u terapiji miješanih vaginalnih infekcija. Pokusi ex vivo pokazali su da se bioadhezivni gel zadržava u vagini 12-13 sati. Rezultati in vitro ispitivanja ukazuju na to da ABBV gel ima bolje antibakterijsko djelovanje i dulje zadržavanje od intravaginalnog sustava koji je dostupan na tržištu

    Significance of angular unconformities between Cretaceous and Tertiary strata in the Northwestern Segment of the Zagros Fold-Thrust Belt, Kurdistan Region, Iraq

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    In this study, two angular unconformities are found and analysed for the first time in the Mesozoic–Cenozoic succession in the northwestern segment of the Zagros fold–thrust belt (ZFTB) in the Kurdistan Region. The first unconformity exists between Lower Cretaceous and Paleocene–Eocene rocks and the second between the Campanian Shiranish Formation and the Maastrichtian Tanjero Formation. Each of these unconformities is found in two different localities in the Zagros Imbricate Zone (i.e. the highly deformed zone immediately SW of the Zagros Suture) of the ZFTB of the Kurdistan Region near the border with Iran. The study uses recent geological mapping, structural and stratigraphic analyses in addition to using previous biozonation of the stratigraphic units that bound the two unconformities. The first unconformity was initiated with obduction of the ophiolite and Lower Cretaceous radiolarite onto the passive margin of the Arabian plate. This unconformity formed during an early phase of the Zagros orogeny, which is associated with the developing of a foreland basin, and resulted in the folding of the radiolarites and their uplift to form high-relief land. The erosion of this high-relief land resulted in the formation of the Paleocene–Eocene Red Bed Series and their deposition on the folded radiolarite. The timing of the deformation that caused this unconformity is hard to determine; however, its stratigraphic position may suggest that it possibly is related to post-Cenomanian movements. The second unconformity is between the tilted Campanian Shiranish Formation (hemipelagite) and Tanjero Formation (500 m of conglomerate in the more proximal area). These unconformities indicate that deformation and uplift of the sedimentary units was variable during ophiolite obduction in this part of the ZFTB. We argue that deformation, ophiolite obduction and collision are likely to have varied in space and time along the c. 2000 km long ZFTB

    Purification, refolding, and characterization of recombinant LHRH-T multimer

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    To make the native LHRH immunogenic, a multimer of LHRH interspersed with T non-B peptides (r-LHRH-d2) was expressed as recombinant protein in Escherichia coli. The expression level of the recombinant protein was around 15% of the total cellular protein and it aggregated as inclusion bodies. Inclusion bodies from the bacterial cells were isolated and purified to homogeneity. Instead of high concentrations of chaotropic agents, r-LHRH-d2 was solubilized in 50 mM citrate buffer at pH 3 containing 2 M urea. The protein was refolded by 5-fold dilution (pulsatile) with cold 10 mM citrate buffer at pH 6 in presence of 0.3 M L-arginine. Purification of r-LHRH-d2 was carried out by successive passages on CM-Sepharose column at pH 6.0 which retained extraneous proteins and pH 4.8 at which r-LHRH-d2 bound to the resin. The elution was carried out by using linear salt gradient (0.1-1 M NaCl). The overall yield of the purified r-LHRH-d2 was 40% of the initial inclusion body proteins. The purity and homogeneity were confirmed by a single homogeneous peak on analytical HPLC eluting out at 29.51 min and by single band on SDS-PAGE reactive with polyvalent anti-LHRH antibodies. Mass spectroscopic analysis indicated the protein to be of 16.6 kDa which equals the theoretically expected mass. The N-terminal amino acid analysis of r-LHRH-d2 showed the sequence which corresponded to the designed protein. The CD spectrum of the refolded r-LHRH-d2 showed that the multimer has considerable β sheet structure like the monomeric LHRH protein

    Formulation development and optimization using nanoemulsion technique: A technical note

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    Ramipril nanoemulsion formulations were successfully prepared by the spontaneous emulsification method (titration method). Sefsol 218 was selected as the oil phase for the development of the formulation on the basis of the solubility studies. The differences in the droplet size between the formulations selected from the phase diagram was not statistically significant, although the polydispersity was at a minimum for the formulation containing 20% oil, 27% Smix, and 53% vol/vol aqueous phase. The droplet size was found to be 34.5 nm. Therefore, nanoemulsion, a multipurpose technology, can be exploited in drug delivery for poorly soluble drugs. Nanoemulsions have a higher solubilization capacity than simple micellar solutions, and their thermodynamic stability offers advantages over unstable dispersions, such as emulsions and suspensions, because they can be manufactured with little energy input (heat or mixing) and have a long shelf life. This technical note explains the basis for calculation and construction of pseudoternary phase diagrams and, most important, explains selection of the formulations from the phase diagrams to avoid metastable formulations having minimum surfactant concentration in the least possible time

    Development and Evaluation of Buccal Bioadhesive Tablet of an Anti-emetic Agent Ondansetron

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    The aim of the present study was to develop and evaluate a buccal adhesive tablet containing ondansetron hydrochloride (OH). Special punches and dies were fabricated and used while preparing buccal adhesive tablets. The tablets were prepared using carbopol (CP 934), sodium alginate, sodium carboxymethylcellulose low viscosity (SCMC LV), and hydroxypropylmethylcellulose (HPMC 15cps) as mucoadhsive polymers to impart mucoadhesion and ethyl cellulose to act as an impermeable backing layer. The formulations were prepared by direct compression and characterized by different parameters such as weight uniformity, content uniformity, thickness, hardness, swelling index, in vitro drug release studies, mucoadhesive strength, and ex vivo permeation study. As compared with the optimized formulation composed of OH—5 mg, CP 934—30 mg, SCMC LV—165 mg, PEG 6000—40 mg, lactose—5 mg, magnesium stearate—1.5 mg, and aspartame—2 mg, which gave the maximum release (88.15%), non-bitter (OH) that form namely ondansetron base and complexed ondansetron was used in order to make the selected formulation acceptable to human. The result of the in vitro release studies and permeation studies through bovine buccal mucosa revealed that complexed ondansetron gave the maximum release and permeation. The stability of drug in the optimized adhesive tablet was tested for 6 h in natural human saliva; both the drug and device were found to be stable in natural human saliva. Thus, buccal adhesive tablet of ondansetron could be an alternative route to bypass the hepatic first-pass metabolism and to improve the bioavailability of (OH)
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