Bioavailability of tetracycline hydrochloride capsules (an in vivo study)]

Blood absorption of tetracycline hydrochloride of various dispersity levels from capsules containing tetracycline alone or in combination with additives, such as magnesium carbonate and calcium salts was studied on humans. It was found that higher dispersity levels of tetracycline hydrochloride powder in capsules was not accompanied by increased blood absorption of the antibiotic. Addition of magnesium carbonate and calcium salts to the antibiotic in the process of capsulation markedly retarded the blood absorption. Clear correlation between the antibiotic dissolution rate in vitro and intensity of its blood absorption in volunteers was shown.     

Effect of fluoride on cariogenic oral microorganisms (an in vitro study)

The effect of sodium fluoride and sodium monofluorophosphate at concentrations of 1, 5, 10, 50, 100 and 1000 mg/l in phosphate buffer (pH 6.5) as well as in UHT milk were studied on cultures and suspensions of Streptococcus mutans, Lactobacillus acidophilus and Candida albicans. Using serial tenfold dilutions up to 10(-7) of 24-48 hour cultures, a subsequent 0, 60 and 120 min incubation caused no decrease in the number of CFUs. Growth kinetic studies in the Bioscreen biophotometer (Labsystem, Finland) revealed that sodium fluoride in different concentrations (from 0.875 mg/l up to 500 mg/l) influenced the growth dynamics of S. mutans and C. albicans: the exponential phase flattened out at the highest fluoride concentrations (500 mg/l) present in the growth media. The lag phase of C. albicans became longer. The results of these experiments indicate that sodium fluoride administered at higher concentrations than the usual caries preventive dosage made the generation time of cariogenic oral bacteria and fungi longer, slowing down their multiplication.     

Differentiation of the degree of bioavailability of peroral drug forms of tetracycline hydrochloride in experiments on laboratory animals]

Difference in the levels of bioavailability of 4 types of tetracycline hydrochloride tablets was shown on rabbits and guinea pigs. The rates of the antibiotic absorption into the blood of the laboratory animals and volunteers were the same. Relation between the rate of disintegration of various types of tablets of tetracycline hydrochloride and the antibiotic blood levels in the rabbits after administration of the same tablets was found.     

Effect of tetracycline hydrochloride on the physical and chemical properties of Heliothis virescens larvae

1. The effects of various levels of tetracycline hydrochloride on the feeding habits, larval growth, and the metabolism of lipids, carbohydrates and proteins of Heliothis virescens were studied.2. Regression analysis showed that larval weight, fatty acids and glycogen decreased exponentially with increasing concentration of antibiotic, whereas protein showed a linear decrease.3. Larval feeding was initially decreased when antitiotics were added to the diet but there was no difference after 24 hr.     

Polymethyl-methacrylate-sorbitol-based capsules as local drug delivery vehicles: an in vitro antibiotic elution study

A PMMA (polymethyl-methacrylate)-sorbitol-based capsule system was recently developed, and the permeability of 16 types of capsules with different wall thicknesses and sorbitol contents tested. By optimizing these two parameters, we showed that capsule permeability could be controlled. Promising preliminary data obtained using BPB (Bromophenol Blue) as diffusion marker prompted us to further investigate the antibiotic release of capsules showing the most appropriate release characteristics. PMMA-sorbitol capsules were prepared with wall thickness of 0.5 or 0.6 mm and 60 or 70 w/w% (weight percent) of sorbitol content. In vitro gentamicin, amikacin, tobramycin releases were determined by using a microbiological agar plate diffusion assay. Capsules released 70-100% of their gentamicin load, substantially superior to Septopal, and showed preferable, extended release profiles when compared with the beads. The release kinetics of amikacin and tobramycin closely resembled those of gentamicin. PMMA-sorbitol capsules have been developed and tested, which make them promising devices for local antibiotic delivery.     

A physicochemical study of the tetracycline coordination to oxovanadium(IV)

The interaction of tetracycline and oxovanadium(IV) in aqueous solution was studied by potentiometric and spectrophotometric methods. Oxovanadium(IV) ions form both a positively charged 1:1 and a neutral 2:1 metal-ligand complex with tetracycline. When a 1:1 ligand-to-metal ratio mixture is used at about pH 4.5 the 1:1 species predominates, being replaced at pH 6 by the binuclear complex. The binuclear complex has been isolated and fully characterised. Infrared and EPR studies suggest the existence of two distinct vanadyl binding sites. Our results indicate that the first vanadium coordinates to the BCD-ring system and the second one to the A-ring. Biological implications of the existence of a neutral complex at physiological pH are briefly discussed.     

Nickel bioavailability in an ultramafic toposequence in the Vosges Mountains (France)

A serpentinised harzburgite outcrop located in the Vosges Mountains hosts a population of the Ni-hyperaccumulator Thlaspi caerulescens J. & C. Presl. A complete study was undertaken to relate the variability of Ni availability along the ultramafic toposequence to pedogenesis, soil mineralogy and functioning with X-Ray Diffraction, Transmission Electron Microscope observations coupled with Isotopic Exchange Kinetics and diethylenetriamine pentaacetic acid extraction of Ni. The soil profiles ranging from Dystric Cambisol to Hypermagnesic Hypereutric Cambisol were distributed unevenly along the toposequence probably due to geochemical variability of the bedrock and also complex quaternary erosion features. The richest soils were characterised by slight mineral weathering leading to Ni, Cr and Fe accumulation in the B horizons whereas the lowest saturated soils had very low-metal contents. Most soil minerals were inherited from the parent materials and there were only few traces of formation of secondary minerals. Primary minerals (e.g. serpentine, chlorite) contained low Ni concentrations (0.2%) whereas neoformed goethite, mainly in the B horizons of the richest soils, contained up to 4.3% Ni. Ni was probably sorbed onto amorphous Fe oxy−hydroxide particles (oxalate extraction) rather than incorporated within the crystal lattice of goethite. Ni availability in the B horizon of Hypereutric Cambisols was extremely high and so was the oxalate extractable Fe. At the toposequence level, there was a high level of Ni availability in the least weathered soils and a very low-availability level in the more intensively weathered soils (strongly acidic pH). Ni availability was unexpectedly positively correlated to pH and was controlled by soil mineralogy and Ni-bearing mineral phases. Ni hyperaccumulation (above 1,000 mg kg⁻¹) by native T. caerulescens was only reached in the Ni-rich soils as a consequence of the local edaphic factors. Ni uptake by T. caerulescens is strongly regulated by Ni availability in soils and therefore related to pedogenesis.     

Effect of organogel components on in vitro nasal delivery of propranolol hydrochloride

The purpose of this research was to evaluate in vitro transnasal sustained-release ability of sorbitan monostearate (SMS) organogels in isopropyl myristate (IM). Organogels were prepared containing SMS (2.5%–20%) and water (5%–25%) in IM and analyzed microscopically for phase behavior. The effect of Tween surfactants on gel strength and in vitro nasal diffusion of propranolol is reported. The in vitro nasal release retardant effect of SMS and Tween 20 was investigated using factorial design. The microscopic changes in structure of organogel during in vitro nasal diffusion were studied. The water-holding capacity of SMS organogels in IM increased with SMS concentration. The release retardant effect with incorportation of cosurfactant was of the order of Tween 80> Tween 60> Tween 20. Gel strengthening and increased viscosity were evident with increased concentration of SMS and Tween 20. The 3-dimensional network of SMS molecules controls the diffusional drug release. The organogel system on nasal mucosa during diffusion is dynamic in nature and changes continuously with the time of diffusion. The water penetration in the organogel network results in percolation and emulsification of organogel, thus affecting the release. Organogels provided an effective barrier for diffusion of propranolol. The surface epithelium lining and the granular cellular structure of treated nasal mucosa were intact.     

Comparative study of the biological activity of tetracycline hydrochloride and morphocycline by using reverse turbidimetry]

The method of back turbidimetry was used for determination of the biological activity of the antibiotics, since high turbidity of the nutrient medium with Staph. aureus as the testculture prevented from direct measurements. Broth containing phosphate buffer, Staph. aureus and definite concentrations of the antibiotic was used as the reference solution. The experiments showed that the differences in the biological activities of tetracycline hydrochloride and morphocycline may be found with the method of back turbidimetry 6-8 hours after the microbe cultivation on media with the antibiotics.