Pharmaceutical science & technology today最新文献

The pharmaceutical industry relies on appropriate in vitro models for the evaluation of drug absorption and metabolism. Despite increasing interest in drug delivery via the lung, there is currently no widely accepted cell culture model of the airway epithelium. This review considers the airway epithelium, the culture of airway epithelial cells and the need for cell lines which can model the airway epithelium. Three of the most promising human bronchial cell lines, 16HBE14o–, Calu-3 and BEAS-2B, are reviewed, with emphasis on their recent application for the study of drug transport, drug metabolism and gene delivery. Current limitations and future directions for the development of these cell lines as models of the airway epithelium are discussed.

Quantitative structure–activity relationships (QSAR) have been applied for decades in the development of new drugs. Although a QSAR does not completely eliminate the trial and error factor involved in the development of a new drug, it certainly decreases the number of compounds synthesized by facilitating the selection of the most promising examples. The success of QSAR has tempted scientists, particularly in the pharmaceutical arena, to investigate relationships of molecular parameters with properties other than activity. The purpose of this two-part review is to provide a broad overview of the development of quantitative structure–property relationships (QSPR) and review the applications in pharmaceutical research. Part one discusses the advantages and limitations of QSPR, and various types of structural descriptors and properties, together with techniques to establish correlations between the two.

Monitor provides an insight into the latest developments in pharmaceutical science and technology through brief synopses of recent presentations, publications and patents, and expert commentaries on the latest technologies. There are two sections: Progress summarizes the latest developments in pharmaceutical process technology, formulation, analytical technology, sterilization, controlled drug delivery systems and regulatory issues; Profiles offers expert commentary on emerging technologies, novel processes and strategic, organizational and logistic issues underlying pharmaceutical R&D.

The stratum corneum, poses a formidable challenge to formulators of drug delivery systems. Several approaches have been utilized to facilitate entry of drugs into the lower skin layers. Traditionally, permeation enhancers were designed to deliver high drug concentrations across the skin into the systemic circulation. The use of many of these agents resulted in unpleasant or toxic side effects. However, in recent years there has been a search for compounds that exhibit low toxicity, and maintain their enhancing activity. More recently, there has been interest in agents that may be used in topical formulations to prevent the passage of active ingredients or excipients into the lower skin layers. These so-called skin retardants have potential uses in many over-the-counter (OTC) skin formulations, such as sunscreens and pesticides, where the site of action is restricted to the skin surface or upper skin layers. Research in the area of permeation enhancement or retardation is yielding valuable insights into the structure–activity relationships of enhancers as well as retardants.

In the practical field of solid pharmaceutical formulations, studies of the physical aging of polymers and the stability of dosage forms are of great importance. Polymers are the additives used to convert pharmacologically active compounds into pharmaceutical dosage forms suitable for administration to patients, and thus a knowledge of the physical aging effects on the stability of final products is essential. In this review, the author attempts to elucidate the fundamental concepts of physical aging in polymers, and correlate the effects of physical aging on the properties with changes in solid dosage form stability.

Anthracyclines such as adriamycin have a broad spectrum of activity in human tumours, but are limited, to an extent, by their non-selective delivery to a host of normal tissues and hence, subsequent toxicity. The development of liposomes has offered a drug delivery system with significant potential to target tumours whilst sparing normal tissues. A significant breakthrough has been achieved by coating the liposome with polyethylene glycol (pegylation), and thus altering the pharmacokinetics of the drug considerably. In this review, the authors discuss the promising data now emerging with pegylated liposomal adriamycin, and also describe possible future applications.

This review provides an overview of the synthesis and application of stable and versatile HPLC chiral stationary phases (CSPs), with emphasis placed on the binding strategies developed to anchor several structurally different chiral selectors to silica-gel microparticles. In addition, selected applications relating to the use of these CSPs for the direct resolution of racemates of biological and pharmaceutical relevance will be described. This review discusses enantioselective molecular recognition and dynamic stereochemistry of stereolabile compounds with reference to receptor-based chiral stationary phases (CSPs) and dynamic HPLC on CSPs, respectively.