In Vitro and In Vivo evaluation of hydroxypropylmethyl cellulose phthalate capsules

The aim of this study was to develop a novel HPMCP capsule. The HPMCP capsule containing99mTc-DTPA and lactose was evaluated in in vitro and in vivo studies. First of all, the HPMCP capsules were prepared and characterized with lenght and diameter size, brittleness facility, moisture content and microbiological test. In vitro resistance and solubility studies of prepared capsules were tested at pH 1.2 and pH 7.4 buffers. The radiolabeled HPMCP capsules were administrated to fasted volunteers. The disintegration times and positions of capsules were recorded by using gamma scintigraphy. In vitro studies showed that HPMCP capsules were gastro resistant for 2 h at pH 1.2 and dissolved at pH 7.4 in 20-25 minutes. The radiolabeled capsules did not disintegrate in stomach whereas disintegrated in intestines. In conclusion, it was found that, the prepared HPMCP capsules can be an alternative to the hard gelatine capsules and used for intestinal targeting.Keywords: Capsule, hydroxypropylmethylcellulose phthalate (HPMCP), gamma scintigraphy, radiolabelling, technetium-99m

Shake-table testing of a stone masonry building aggregate: overview of blind prediction study

City centres of Europe are often composed of unreinforced masonry structural aggregates, whose seismic response is challenging to predict. To advance the state of the art on the seismic response of these aggregates, the Adjacent Interacting Masonry Structures (AIMS) subproject from Horizon 2020 project Seismology and Earthquake Engineering Research Infrastructure Alliance for Europe (SERA) provides shake-table test data of a two-unit, double-leaf stone masonry aggregate subjected to two horizontal components of dynamic excitation. A blind prediction was organized with participants from academia and industry to test modelling approaches and assumptions and to learn about the extent of uncertainty in modelling for such masonry aggregates. The participants were provided with the full set of material and geometrical data, construction details and original seismic input and asked to predict prior to the test the expected seismic response in terms of damage mechanisms, base-shear forces, and roof displacements. The modelling approaches used differ significantly in the level of detail and the modelling assumptions. This paper provides an overview of the adopted modelling approaches and their subsequent predictions. It further discusses the range of assumptions made when modelling masonry walls, floors and connections, and aims at discovering how the common solutions regarding modelling masonry in general, and masonry aggregates in particular, affect the results. The results are evaluated both in terms of damage mechanisms, base shear forces, displacements and interface openings in both directions, and then compared with the experimental results. The modelling approaches featuring Discrete Element Method (DEM) led to the best predictions in terms of displacements, while a submission using rigid block limit analysis led to the best prediction in terms of damage mechanisms. Large coefficients of variation of predicted displacements and general underestimation of displacements in comparison with experimental results, except for DEM models, highlight the need for further consensus building on suitable modelling assumptions for such masonry aggregates

Labeling of ornidazole with iodine-131

WOS: 000077298200027Ornidazole (1-(3-chloro-2-hydroxypropyl)-2-methyl-5-nitroimidazole) was labeled with iodine-131 by using iodogen method. Quality controls were performed by instant thin layer chromatography (ITLC) and electrophoresis methods. Labeling yield was 91%. Iodination was carried out by substitution of chloride by iodine-131. Structure was confirmed by H-1-NMR

The Release of Isoconazole Nitrate from Different Suppository Bases: In-vitro Dissolution, Physicochemical and Microbiological Studies

PubMed ID: 8583380The influence of the suppository base on the in-vitro release of isoconazole nitrate was studied by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. Vaginal suppository formulations containing 25 mg isoconazole nitrate for local treatment of vaginitis were prepared by a fusion method, using different hydrophilic and lypophilic suppository bases (PEG 6000, PEG 4000, PEG 1500, Witepsol H15, Novata BD and Cremao). In-vitro release rates were examined by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. In the physicochemical investigations the pH indicators (pH 1–14) erythrosin B, thymol blue, bromocresol green, chlorophenol red, phenol red, and alkali blue were added to agar gels. The discs were placed onto the agar gels and 21 h later, the coloured zone diameters were measured. In the microbiological investigations, the discs were put on the inoculated plates with the suspension of Candida albicans (Institute Pasteur 628). The inoculated plates were incubated at 37°C for 3 days, then the diameters of inhibition zones were measured. In the dissolution investigations release rates were in the order PEG 6000 > PEG 4000 > PEG 1500 > > Witepsol H15 > Cremao > Novata BD. The diffusion distance of isoconazole nitrate in the physicochemical investigation was in the order polyethylene glycols > Witepsol H15 > Novata BD. In the microbiological studies release rates were found with polyethylene glycols > Witepsol H15 > Novata BD > Cremao. The findings in the in-vitro studies suggested that polyethylene glycols are suitable bases for vaginal suppositories. 1995 Royal Pharmaceutical Society of Great Britai

The Release of Isoconazole Nitrate From Different Suppository Bases - In-Vitro Dissolution, Physicochemical and Microbiological Studies

WOS: A1995RY38900003PubMed ID: 8583380The influence of the suppository base on the in-vitro release of isoconazole nitrate was studied by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. Vaginal suppository formulations containing 25 mg isoconazole nitrate for local treatment of vaginitis were prepared by a fusion method, using different hydrophilic and lypophilic suppository bases (PEG 6000, PEG 4000, PEG 1500, Witepsol H15, Novata BD and Cremao). In-vitro release rates were examined by dissolution, physicochemical diffusion and microbiological disk-diffusion methods. In the physicochemical investigations the pH indicators (pH 1-14) erythrosin B, thymol blue, bromocresol green, chlorophenol red, phenol red, and alkali blue were added to agar gels. The discs were placed onto the agar gels and 21 h later, the coloured zone diameters were measured. In the microbiological investigations, the discs were put on the inoculated plates with the suspension of Candida albicans (Institute Pasteur 628). The inoculated plates were incubated at 37 degrees C for 3 days, then the diameters of inhibition zones were measured. In the dissolution investigations release rates were in the order PEG 6000 > PEG 4000 > PEG 1500 > > Witepsol H15 > Cremao > Novata BD. The diffusion distance of isoconazole nitrate in the physicochemical investigation was in the order polyethylene glycols > Witepsol H15 > Novata BD. In the microbiological studies release rates were found with polyethylene glycols > Witepsol H15 > Novata BD > Cremao. The findings in the in-vitro studies suggested that polyethylene glycols are suitable bases for vaginal suppositories

Radioactive permeability studies of Doxycycline Hyclate from microemulsion and solution [Doksisiklin Hiklat’ın mikroemülsiyon ve çözelti dozaj şekillerinden radyoaktif permeabilite çalışmaları]

Doxycycline Hyclate (DOX) is an antibacterial drug which is member of the second tetracycline group and the absorption of DOX is reduced about 20% in the presence of skimmed milk. Therefore new drug delivery system can be advisable for DOX to reduce the food and drug interaction and improve the bioavailability. The aim of the present study is to prepare a microemulsion system of DOX which could result in reducing in food interaction and an improvement of oral bioavailability by increasing the drug’s permeability. For this purposes, DOX was radiolabeled with 99mTc. Radiochemical purity was determined with radioactive thin layer chromatography (RTLC) studies. Permeability of DOX from 99mTc-DOX solution (99mTc-DOX-S) and 99mTc-DOX loaded microemulsion (99mTc-DOX-M) was investigated with in vitro cell culture studies by using human colonic adenocarcinoma cell line (Caco-2). The radioactivity of99mTc-DOX-M for the apical to basolateral direction (Papp (A›B)) and basolateral to apical direction (Papp (B›A)) were found higher than 99mTc-DOX-S. Based on the in vitro cell culture studies, this dosage form is a promising formulation as an alternative for oral drug delivery of DOX. © 2016, Marmara University. All rights reserved