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The use of beclomethasone dipropionate (BDP) for nebulisation has been limited due to its poor aqueous solubility. A possible method of solving this problem is to complex BDP with a cyclodextrin (CyD) molecule.In order to assess their propensity to complex with BDP, phase solubility studies were conducted over a range of temperatures, with β-CyD, methyl-β-CyD (M-β-CyD), heptakis (2,6-di-o-methyl)-β-CyD...
Rubus pinfaensis has been used in Traditional Chinese Medicine to promote wound healing. Ursene triterpenoids isolated from this source have been examined for antibacterial activity against a range of microorganisms. With the exception of ursolic acid (1), the 28-glucosides, free acids or their derivatives (2-9) do not show significant activity when tested by MIC methods. Minor glycosides 10 and...
Tissue slices have the potential to determine in vitro tissue to unbound drug in plasma partition coefficients (K pu ) that are more consistent with in vivo measurements than homogenates because the cellular architecture of the tissue predominantly remains intact. We have undertaken some fundamental studies with tissue slices to determine the possibilities and limitations of the technique...
Upon exposure to chlordecone (CD), workers in pesticide factories have shown overt signs of toxicity affecting the nervous system, liver and testes. It has been suggested that juveniles are more at risk than adults, hence, a whole body distribution study was undertaken in young and adult F344 rats to determine the relative dermal absorption profiles and subsequent pharmacokinetics of CD. In each...
The development of matrix pellets based on the combination of microcrystalline waxes and starches was described by Zhou et al. The influence of several process parameters on the particle size distribution and drug release profile of the matrix pellets was investigated. Formulations consisting of ibuprofen, microcrystalline wax (Lunacera(R) M/P-ratio: 73) and waxy maltodextrin were used. The critical...
Dopamine (3,4-dihydroxyphenethylamine, DOP) was covalently bond to styrene-maleic anhydride copolymer (SMA) in order to prepare polymeric prodrug SMA-DOP as potentially more stable form of dopamine. The coupling reaction was run under nitrogen atmosphere in dry N,N-dimethylformamide in the presence of sodium dithionite. The remaining anhydride rings were opened with water.The resulting conjugate...
Clinical resistance to natural product cytotoxic drugs represents a major problem in cancer treatment. Multidrug resistance (MDR) has been shown to be mediated by the membrane bound ABC-transporter P-glycoprotein (PGP), which acts as an energy dependent efflux pump for a wide variety of cytotoxic drugs. We recently identified analogs of the class 1c antiarrhythmic agent propafenone as highly effective...
The purpose of this study was to characterize the in-vivo pharmacodynamics of five synthetic opioids by pharmacokinetic-pharmacodynamic modelling, using the EEG descriptors as pharmacological endpoint (0.5-4.5 Hz). The in-vivo pharmacodynamic characteristics were compared with in-vitro receptor binding characteristics.The concentration-EEG effect relationship of the synthetic opioids was determined...
Aromatase (P450 AROM ) catalyses the conversion of androstenedione to oestrone and its inhibitors have been used to suppress growth of metastases in post-menopausal women with oestrogen-dependent breast cancer. Several mechanism-based inactivators with an irreversible action are in the clinic, i.e. 4-hydroxyandrostenedione (4-0HA) and 10-(2-propynl)estr-4-ene-3,17-dione (plomestane)...
The stability of highly concentrated morphine hydrochloride (M) solutions for subcutaneous infusion in terminally ill patients, was investigated. M solutions were prepared in five concentrations: 10, 20, 30, 40 and 50 mg/mL. For each concentration a solution was prepared in water and two isotonic solutions were prepared in the appropriate dilution of NaCl 0.9% and glucose 5%. The solutions were...
We have previously demonstrated the presence of heat-stable complex polysaccharides (glycans) in BCG with marked antineoplastic activity and have shown that these materials are substantially associated with an integument secreted by the living organism in response to environmental stress. Although BCG is normally prepared by surface culture we have found that preparation of cultures in 5-litre vessels...
Kasting proposed a model for transdermal permeation using ideal solution theory whereby the flux of a drug increases exponentially with decreasing melting point. The effects of melting point depression on the transdermal flux of ibuprofen (ibu) were studied by forming eutectic systems between ibu and a range of terpene permeation enhancers (L-menthol, LD-menthol, 1,8-cineole and thymol).Composition/melting...
The arising of human helmintic infestations is very often worldwide and it represents a great health problem. Hydatid disease occupies an outstanding place in many countries. The preferred treatment is surgery. However, drugs application constitutes also a very important therapeutic strategy.Mebendazole is one of the most active agent against the echinoccocus, granulosus, but it has been observed...
The objective of these human studies was to determine the effective permeabilities (Peff) of atenolol, metoprolol, propranolol, desipramine and carbamazepine in the human jejunum using a validated regional perfusion technique (Lennernas et al. Pharm. Res. 9, 1243, 1992). Based on the values of Peff and solubility (S), these drugs will be divided into the following biopharmaceutical drug classes:Each...
Biodegradable polymers, have been utilized for controlled release drug delivery systems. In this study, poly(d,l-lactide)'s and lactide-glycolide copolymers were prepared from d,l-lactide, under various conditions. The model drug, Vancomycin hydrochloride, was encapsulated within the synthesized polymers.Microcapsules were prepared by solvent evaporation method using 3 different polymers: PLA, PGLA...
The amino acid L-histidine buffers in the physiological pH range and is compatible with calcium ions. This is essential in the formulation of protein drugs such as factor VIII. The buffer should preferably stay amorphous during freeze-drying in order to avoid pH shift and possibly also act as stabiliser. Development of a formulation for recombinant factor VIII showed that L-histidine functions...
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