PubMed · 7619595
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R M Wylie. 1995. Reducing benzodiazepine usage.. https://pubmed.ncbi.nlm.nih.gov/7619595/
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Poorly soluble drugs are often a challenging problem in drug formulation, especially when the drug is not soluble in either aqueous media or organic solvents. Attempts to overcome the solubility problem are, e.g. solubilisation with mixed micelles or forming a complex using cyclodextrines, but these approaches are of limited success. Another problem with new high potential drug is that these drugs often show bioavailability problems. One tried to improve the in vivo performance of poorly soluble drugs by reducing the particles size of the drug thus leading to an increased surface area and an increased dissolution velocity (Müller et al., 1994, 1999). Some of these problems occurred with tarazepide and therefore it was tried to create a formulation with this drug as nanosuspension which is suitable for intravenous administration.
Insomnia, or the dissatisfaction with the quantity, quality or timing of sleep, is a common complaint. Because the definition of "normal" sleep is not well established, the estimates of the prevalence and severity of insomnia vary widely. Insomnia is often secondary to underlying psychiatric and medical conditions, and these should be evaluated and treated as a first measure. Nonpharmacological interventions for insomnia including sleep hygiene manoeuvres and exercise are recommended, although the success of these interventions has not been well documented. Benzodiazepines have been the pharmacologic agents of choice for the treatment of insomnia, but there is reason to exercise caution with their use; their overall benefit compared with placebo appears to be minor, and they are often associated with adverse cognitive effects. Unfortunately, no other class of drugs has proven to be superior to the benzodiazepines in terms of benefit:risk ratio. Given the importance of sleep for health and normal daily functioning the diagnosis, prognosis and treatment of insomnia should be a research priority.
A radioreceptor binding assay was used to guide the isolation of four chemical constituents in the organic solvent extracts of Scutellaria baicalensis Georgi capable of binding to the benzodiazepine site (BZD-S) of the GABAA receptor: wogonin (Ki = 2.03 +/- 0.24 microM), baicalin (Ki = 77.10 +/- 4.79 microM), baicalein (Ki = 5.69 +/- 0.95 microM), and scutellarein (Ki = 12.00 +/- 1.27 microM). All four compounds contain the flavonoid phenylbenzopyrone nucleus. Based on BZD-S binding, the order of affinity among these four compounds was wogonin > baicalein > scutellarein > baicalin.