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In an effort to determine the stereochemical requirements for pharmacological activity among the series of nonclassical cannabinoids synthesized at Pfizer, we have studied the conformational properties of the parent bicyclic analog CP-47,497. For this study, we have used a combination of solution NMR and theoretical computational approaches. The(More)
A new cellulose-based tabletting excipient, hereinafter referred to as UICEL, has been developed by treating cellulose powder with an aqueous solution of sodium hydroxide (conc. > or = 5N) and subsequently precipitating it with ethyl alcohol. UICEL is similar in structure to Avicel PH-102, a commercial direct compression excipient commonly referred to as(More)
We have studied the interactions of the anaesthetic steroid alphaxalone and its inactive isomer delta 16-alphaxalone with model membrane bilayers using differential scanning calorimetry, small angle X-ray diffraction and solid state NMR. Our data show that the anaesthetic steroid broadens the membrane phase transition and increases the ratio of gauche to(More)
We have studied in detail the effects of the anesthetic steroid alphaxalone and its inactive analog delta 16-alphaxalone on the thermotropic properties of model membranes using differential scanning calorimetry (DSC). The results obtained showed that, for model membranes from hydrated dipalmitoylphosphatidylcholine (DPPC), dioleoylphosphatidylcholine(More)
We have previously studied and compared the location of (-)-delta 8-tetrahydrocannabinol (delta 8-THC) with that of O-methyl-delta 8-THC (Me delta 8-THC) in the membrane using partially hydrated dimyristoylphosphatidylcholine (DMPC) bilayers ((Mavromoustakos et al. (1990) Biophys. Acta 1024, 336-344; Yang et al. (1993) Life Sci. 53, 117-122). delta 8-THC(More)
The effects of (-)-delta 8-tetrahydrocannabinol (delta 8-THC) and its biologically inactive O-methyl ether analog on model phospholipid membranes were studied using a combination of differential scanning calorimetry (DSC), small angle X-ray diffraction and solid state 2H-NMR. The focus of this work is on the amphipathic interactions of cannabinoids with(More)
This work describes a melt granulation technique to improve the dissolution characteristics of a poorly water-soluble drug, griseofulvin. Melt granulation technique is a process by which pharmaceutical powders are efficiently agglomerated by a meltable binder. The advantage of this technique compared to a conventional granulation is that no water or organic(More)
The effects of (-)-delta 9-tetrahydrocannabinol (delta 9-THC) on model phospholipid membranes were studied using solid-state 2H and 13C nuclear magnetic resonance spectroscopy. Aqueous multilamellar dispersions of dipalmitoylphosphatidylcholine with specific 2H- and 13C-labels as endogenous probes at the C7, methylene and the carbonyl groups, respectively,(More)
The solubility of camptothecin (CPT), a highly potent antineoplastic agent, as a function of different concentrations of cyclodextrins (alpha-cyclodextrin, alpha-CD; beta-cyclodextrin, beta-CD; and gamma-cyclodextrin, gamma-CD; hydroxypropyl-beta-cyclodextrin, HP-beta-CD; and randomly substituted dimethyl-beta-cyclodextrin, RDM-beta-CD, and(More)
In a previous publication, we have described in detail how we used small angle x-ray diffraction to determine the topography of (-)-delta 8-tetrahydrocannabinol (delta 8-THC) in dimyristoylphosphatidylcholine (DMPC) bilayers, and to deduce the conformation of the THC side chain by using the iodo-analog (5'-I-delta 8-THC) in the model membrane. We have now(More)