Surface-active drugs, properties

Interactions between water vapor and amorphous pharmaceutical solids were evaluated using isothermal microcalorimetry. " The desorption of water from theophylline monohydrate has been investigated using microcalorimetric approaches.The properties of surfactants and surface-active drugs in solution were studied by Attwood et al. " using calorimetry, while titration microcalorimetry has been utilized to elucidate the nature of specific interactions in several pharmaceutical polymer-surfactants systems. " Drug decomposition was evaluated as a function of different... 

The biological and pharmaceutical consequences of the surface activity will be discussed here. The solution properties of these surface active drugs and their mode of association play an important role in their biological efficacy. 

Future research is required for Solubilising agents that increase bio-availability use of co-solvents effect of surfactants on properties of solubilised systems and interaction with components of the body and mixed micelle formation between surface active drugs and surfactants. 

Besides trace metals, adsorptive stripping voltammetry has been shown to be highly suitable for measuring organic compounds (including cardiac or anticancer drugs, nucleic acids, vitamins, and pesticides) that exhibit surface-active properties. 

A summary of how physiological factors affect the dissolution rate is given in Table 21.2. The effective surface area will be affected by the wetting properties of the bile acids and other surface-active agents in the gastrointestinal tract. The dif-fusivity of a drug molecule in the intestinal juice will be altered by changes in viscosity that are induced, for instance, by meal components. An increased dissolution rate could be obtained at more intense intestinal motility patterns or increased... 

Organizational characteristics of surface-active molecules have been studied by several researchers due to their applications in many areas such as personal care, polymerization, catalysis, drug delivery, separation and purification, enhanced oil recovery and lubrication. The structure of supramolecular organized assemblies formed in different solvents, when a critical concentration is exceeded, determines their properties such as solubilization [1-3], catalysis [1,4-6], adsorption [7-11] and flocculation [12,13]. As such, many techniques have been used to determine their structural properties. In this paper, the results obtained using fluorescence probing for properties of assemblies in solution and at solid-liquid interfaces are discussed in detail after a brief review of relevant assemblies formed by them. 

There are drug molecules themselves that resemble surfactant molecules with polar and nonpolar regions exhibiting surface-active properties. These drugs can thus self-associate and fornr small aggregates or micelles. Examples of drugs that are surface active include Dexverapamil-HCI (Surakitbanharn etal., 1995), ibuprofen, and benzocaine. 

There has been considerable recent interest in the self - assembly and surface activity of amphiphilic polymers and copolymers. Their interfacial and bulk solution properties have shown a rich pattern of behavior, and the ability to tailor their properties offers a wide range of potential applications. Their bulk aggregation behavior make them candidates, for example, for dye transportation and drug delivery whereas their surface properties make them useful as colloid stabilisers, anti -foaming agents and emulsifiers. This behavior can be illustrated in Fig. 3.24. 

Although a wide range of polymers have been investigated with various cyclodex-trins, these studies mainly focused on the IC preparation techniques and characterization of solid phases. The solution properties, such as the self - assembly behavior, dissociation, particle size an surface activity, were not commonly reported. These solution properties, especially the assembly and surface behavior, are vital for the potential applications of such systems in biomedical science, such as in controlled drug delivery. 

A new generation of transdermal drug delivery (TDD) system was developed to contain one or more skin permeation enhancers in the surface adhesive coating layers. This TDD system has been found, experimentally, to release the enhancers to the surface of stratum corneum to modify the skin s barrier properties, prior to the controlled delivery of the active drug. The extent of enhancement in skin permeability appears to be dependent upon the chemical structure of drug to be delivered transdermally as well as the type and the concentration of enhancer used. The mechanism of skin permeation enhancement have been explored and are analyzed in this report. 

The properties of the active drug that are most significant are its aqueous solubility and particle size. The particle size needs to be chosen carefully. Smaller particles should dissolve faster because of their greater surface area, but when filled inside a capsule they may aggregate together, and the dissolving liquid may not be able to reach the individual particles (Fig. 6) Thus the available surface area of the active ingredient is more important than the actual surface area. 

In this chapter we will see how the surface activity of a molecule is related to its molecular structure and look at the properties of some surfactants which are commonly used in pharmacy. We will examine the nature and properties of films formed when water-soluble surfactants accumulate spontaneously at liquid/air interfaces and when insoluble surfactants are spread over the surface of a liquid to form a monolayer. We will look at some of the factors that influence adsorption onto solid surfaces and how experimental data from adsorption experiments may be analysed to gain information on the process of adsorption. An interesting and useful property of surfactants is that they may form aggregates or micelles in aqueous solutions when their concentration exceeds a critical concentration. We will examine why this should be so and some of the factors that influence micelle formation. The ability of micelles to solubilise water-insoluble drugs has obvious pharmaceutical importance and the process of solubilisation and its applications will be examined in some detail. 

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