Therapeutic applications

It has been known for more than half a century that antifoams consisting of mixtures of PDMS and hydrophobic silica can be used to dispel excessive gas in the gastrointestinal tract. However, the first use of antifoams in this context was reported by Quin et al. [8] more than 60 years ago and concerned treatment of bloat in ruminants. That the hydrophobed silica is a necessary component of an effective PDMS-based antifoam in vivo was first demonstrated by Birtley et al. [9] using X-ray observation of the stomachs of rats in which foam had been artificially produced. 

Stead et al. [11] that deactivation on inorganic salts like aluminum hydroxide may simply concern adsorption of the antifoam onto the salt, rendering both materials less available. By contrast, tablets based on hydrotalcite as antacid showed stable antifoam and antacid behavior even after storage for 1.8 years at 37°C. If adsorption of simethicone onto the antacid is the cause of deactivation, then it is not, however, obvious why it should not occur on a carbonate clay like hydrotalcite. 

Thus far then there is no convincing explanation for the deactivation of PDMS-hydrophobed silica antifoam when admixed with certain inorganic salts. A possible explanation concerns separation of the hydrophobed silica from the PDMS oil either during admixtnre with the inorganic salt or after storage. This would depend on the 

In the event that simethicone is to be administered in situations without an accompanying antacid, use of an oil-water emulsion stabilized by a suitable aqueous nontoxic surfactant solution would be preferable. However, as we describe in Chapter 6, formation of an emulsion inevitably also causes some deactivation of the antifoam. Such deactivation is, however, usually modest compared with that reported after incorporation in tablets based on certain inorganic salts. 

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CARBmES - SILICON CARBIDE] (Vol4) in therapeutic applications [ENZYME APPLICATIONS - THERAPEUTIC] (Vol 9)... 

E. Theeuwes, Novel Drug Delivey and Its Therapeutic application, John Wiley Sons, Ltd., West Sussex, England, 1989, pp. 323—340. 

The possibility that 11-desoxyprostaglandins might exhibit tissue selectivity in therapeutic applications provided an incentive to develop a short synthetic route to this series (Ref. 1). 

The possible therapeutic applications of these alkaloids as proto-zooicidal agents, coronary dilators and ecbolics, and in nervous diseases, for example in the treatment of post-encephalitic conditions, have been discussed by a number of authors. The alkylharmols, referred to above, form part of an extensive series prepared by Coulthard, Levene and Pyman, and tested by these authors for bactericidal properties and by... 

Design and therapeutic application of matrix metalloproteinase heterocyclic inhibitors 99CRV2735. 

For pharmacology there results a particularly close relationship with chemistry, and the work may lead quite naturally, with no special stress on practicality, to therapeutic application, or (in the case of adverse reactions) to toxicology. 

FIGURE 9.17 Venn diagram consisting of the various possible activities (agonism and antagonism) on two receptor subtypes (a- and P-adrenoceptors). Letters label the areas of intersection denoting joint activity. The table shows possible therapeutic application of such joint activity. 

The growing list of endogenous inhibitors of angiogenesis holds great promise for therapeutic applications (Table 2). Substances most advanced in clinical development include Endostatin, Angiostatin, Interleukin-12, Thrombospondin, and Tumstatin. As... 

Lee DK, George SR, O Dowd BF (2006) Unravelling the roles of Hie apelin system prospective therapeutic applications in heart failure and obesity. Trends Pharmacol Sci 27 190-194... 

Benzodiazepines have found wide therapeutic applications as anxiolytics, sedatives, hypnotics, anticonvulsants, and central muscle relaxants. 

Calpain Tissue specific calpains have been implicated in diabetes, cataracts, multiple sclerosis, and limb-girdle muscular dystrophy type 2A. More than 50 inhibitors of calpain have described which have a potential for therapeutic applications. 

Goudet C, Binet V, Prezeau L et al (2004) Allosteric modulators of class-C G-Protein coupled receptors open new possibilities for therapeutic application. Drug Discov Today Ther Strat 1 125-133... 

BKCa The diversity of BKCa channels can be attributed to the assembly of pore-forming a subunit together with four different auxiliary subunits ((31 -(34). BMS-204352 has been identified as a BKCa channel opener for the treatment of acute ischemic stroke although it has also been shown as an M-channel activator. Therapeutic applications for channel openers include epilepsy, bladder overactivity, asthma, hypertension, and psychosis. Other known BKCa channel openers include NS-8, NS-1619, NS-4, and certain aminoazaindole analogs. 

Magni P, Motta M (2005) Aldosterone receptor antagonists biology and novel therapeutic applications. Curr Hypertens Rep 7 206-211... 

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