Inclusion drugs

Aulton, M.E. Abdul-Razzak, M.H. The mechanical properties of hydroxypropylmethylcellulose films derived from aqueous systems, part 2 The influence of solid inclusions. Drug Dev. Ind. Pharm. 1984, 10 (4), 541-561. 

Farmed animals tend to be subjected to compounds that can be classified more easily as drugs. In some cases, animals may encounter compounds in nature that have considerable limitations in inclusion in the diets of farmed animals. An example is the inclusion of zearalenone (Figure 1) and its derivatives in animal diets these have anabolic and oestrogenic properties " and are permitted to be used in some areas of the world but are prohibited from use in others, such as European Union countries. Thus this compound and its reduced isomers (zearalenols, zeranols) improve growth rates in animals but can cause reproductive problems, especially in pigs. Ralgro, which is a commercially prepared derivative of zearalenone, is used as an ear implant in beef cattle as a growth promoter in... 

The barks of Alstoiiia species (Apocyiiaceae) had a considerable reputation throughout the tropics as effective anti-malarial drugs, which led to their inclusion in the British Pharmacopoeia, 1914, and to their chemical examination by various workers. The following is a list of the species examined and of the alkaloids found. The figures in brackets are percentages of total alkaloids. 

As we have seen previously, succinimides containing a quaternary carbon form the basis for a series of anticonvulsant drugs. In the course of research in this series, it was found that the inclusion of additional hetero atoms in the ring was quite compatible with anticonvulsive activity. We consider here the oxa-zolidinediones a discussion of the hydantoins is found later in this section. 

Changing the substitution pattern on the benzimidazole greatly alters the biologic activity. Thus, inclusion of a thia-zole ring affords thiabendazole (70), a drug used for the treatment of helminthiasis. 

Inclusion of fluorine on the pendant aromatic ring and the basic side chain seems to emphasize the anticonvulsant and hypnotic effects of this class of drugs. Thus alkylation of the benzodiazepinone, 24 (prepared from the corresponding substituted aminobenzophenone), with 2-chlorotriethylamine via its sodium salt affords fluazepam. ... 

FIGURE 11.22 Control charts and outliers, (a) pEC50 values (ordinates) run as a quality control for a drug screen over the days on which the screen is run (abscissae). Dotted lines are the 95% c.l. and the solid lines the 99.7% c.l. Data points that drift beyond the action lines indicate significant concern over the quality of the data obtained from the screen on those days, (b) The effect of significant outliers on the criteria for rejection. For the data set shown, the inclusion of points A and B lead to a c.l. for 95% confidence that includes point B. Removal of point A causes the 95% limits to fall below points B, causing them to be suspect as well. Thus, the presence of the data to be possibly rejected affects the criteria for rejection of other data. 

With the development of the polymer field in medicine, great attention has been paid to particulate forms of drugs [82], The most widespread methods for the preparation of particulate drugs are microencapsulation and microgranulation, i.e., the inclusion of BAS into spherical shapes of predetermined dimensions. One form of particulate drugs is microcapsules or artificial cells as they were called by... 

Unit II contains 11 chapters that present the anti-infective drugs, grouped according to classification. These shorter chapters allow for more inclusive coverage of the different types of anti-infectives and the appropriate nursing considerations for each classification. 

These examples of incorporation of a variety of drugs and proteins is meant to be representative, not inclusive, and suggests that the polyanhydrides are capable of delivering a wide range of drugs and proteins for prolonged periods of time from a variety of different dosage forms. 

Only two of the 10 countries have devised specific measures for the benefit of consumers. The Australian dmg regulatory system also provides for the inclusion of consumer group representatives on various drug regulatory committees. The appeals system in the Netherlands is not limited to industry, but is also open to consumers. 

To our knowledge only in a single publication [18] was a better correlation of PSA with drug transport reported after inclusion of S fragments. 

There are other soUd states which sometimes confuse the measurement and definition of solubiUty. The dmg may crystaUize as a hydrate, i.e. under inclusion of water molecules. If the hydrate form is more stable than the pure form it may be difficult to measure the intrinsic solubility of the drug at all. Often drugs tend to precipitate in an amorphous form, often under the inclusion of impurities. As with metastable polymorphs, such amorphous precipitates may lead to erroneously high solubility measurements. CommerciaUy, drugs are often crystallized in salt form, e.g. as the hydrochloride salt, a cation with a chloride anion. In these co-crystallized salts, a much lower solubility than the intrinsic solubility will typi-... 

Biodegradable polyurethanes have been proposed and studied before (9-72). The difference in our study is the inclusion of a phosphoester linkage instead of the commonly used polyester component. This seems to provide more flexibility as the side chain of the phosphate or phosphonate can be varied. For controlled drug delivery applications, drugs can be linked to this site to form a pendant delivery system. Moreover, for certain medical applications, fast degradation rate is obtainable by the introduction of these hydrolyzable phosphoester bonds. With the LDI based polyurethanes, drugs or other compounds of interest can also be coupled to the ester side chain of the lysine portion. 

The topics included in this volume are not intended to be all-inclusive. Our approach has been eclectic, in an effort to bring the reader the most exciting aspects of drug discovery, along with the methods that show the most promise in enhancing the discovery process. 

Because of the resonance stabilization possible in its deprotonated form, the 5-tetrazolyl moiety is actually nearly as acidic (pKa ca. 6) as many carboxylic acids. This has led to its inclusion in many drug series as a carboxyl surrogate. Apparently related in concept to indomethacin (26a), intrazole (26) is a nonsteroidal antiinflammatory agent which also inhibits platelet aggregation, and therefore is of potential value in keeping the contents of the... 

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