Adequate aqueous solubility has been one of the desired properties while selecting drug molecules and other bio-actives for product development. Often solubility of a drug determines its pharmaceutical and therapeutic performance. Majority of newly synthesized drug molecules fail or are rejected during the early phases of drug discovery and development due to their limited solubility. Sufficient permeability, aqueous solubility and physicochemical stability of the drug are important for achieving adequate bioavailability and therapeutic outcome. A number of different approaches including co-solvency, micellar solubilization, micronization, pH adjustment, chemical modification, and solid dispersion have been explored toward improving the solubility of various poorly aqueous-soluble drugs. Dendrimers, a new class of polymers, possess great potential for drug solubility improvement, by virtue of their unique properties. These hyper-branched, mono-dispersed molecules have the distinct ability to bind the drug molecules on periphery as well as to encapsulate these molecules within the dendritic structure. There are numerous reported studies which have successfully used dendrimers to enhance the solubilization of poorly soluble drugs. These promising outcomes have encouraged the researchers to design, synthesize, and evaluate various dendritic polymers for their use in drug delivery and product development. This review will discuss the aspects and role of dendrimers in the solubility enhancement of poorly soluble drugs. The review will also highlight the important and relevant properties of dendrimers which contribute toward drug solubilization. Finally, hydrophobic drugs which have been explored for dendrimer assisted solubilization, and the current marketing status of dendrimers will be discussed.

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Impact of Dendrimers on Solubility of Hydrophobic Drug Molecules

Chiral resolution has achieved an independent identity in the separation sciences and polysaccharide CSPs are viewed as effective and efficient CSPs due to their many unique advantages. The present review article highlights the separations of chiral pharmaceuticals and drugs by liquid chromatographic modalities (high performance liquid chromatography, capillary electro‐chromatography, sub‐ and super critical fluid chromatography and thin layer chromatography) utilizing polysaccharide CSPs. Enantiomeric resolution at analytical and preparative scales and a comparison of coated and immobilized CSPs is discussed. The optimization strategies for enantiomeric separation have also been presented. The possible mechanisms of chiral resolution of racemates were also included. The commercial CSPs of all the Companies i.e., Daicel, Kromasil, Macherey Nagel, Knauer and Sepaserve have been compared and discussed. Finally, the role of these CSPs in chiral drugs development programs has also been identified.

Polysaccharides Chiral Stationary Phases in Liquid Chromatography

The increasing demand for enantiopure drugs has led to the development of a variety of stereoselective separation technologies. Among them, high performance liquid chromatography (HPLC) is well recognized as a powerful, fast and efficient technique, which has been successfully employed for analysis and preparation of enantiomers of drugs. Nowadays, liquid chromatographic techniques are the focus of intensive research, which lead to the rational design and production of highly selective and efficient chromatographic materials. This review focuses on various HPLC methods and related hyphenated techniques (including LC-MS, LC-OR detector, LC-CD detector) for chiral separation of pharmaceuticals, many new developments and applications are introduced in chiral HPLC separations in recent years. In this paper, the usage of new materials as chiral stationary phases (CSPs) in liquid chromatography for enantiomeric discrimination is investigated in detail. Moreover, hyphenated techniques are very useful for chiral separation of HPLC, especially for separation of new pharmaceuticals.

Chiral Separation of Pharmaceuticals by High Performance Liquid Chromatography

Flavonoids as chemosystematic markers in the tribe Cichorieae of the Asteraceae

Enantioseparation of novel chiral sulfoxides on chlorinated polysaccharide stationary phases in supercritical fluid chromatography.

Analytical and semipreparative resolution of enatiomers of albendazole sulfoxide by HPLC on amylose tris (3,5-dimethylphenylcarbamate) chiral stationary phases.

From the whole plant of Tibetan medicinal herb Lagotis ramalana,four phenylpropanoids were isolated for the first time.They were identified as acetoside (1),leucosceptoside A (2),ehinacoside (3) and cistanoside A (4) by means of NMR,and MS spectral data.

Phenylpropanoids from Lagotis ramalana

Xanthone constituents in Gentiana panthaica

Chemical constituents in Ixeridium gramineum

Guanidines have been recognized as one of the most promising receptors for various molecular recognition.Here is a simple introduction about their structure and properties.The molecular recognition and progress of modified guanidines in host-guest chemistry were summarized with 49 references.

Shi Yan-ping

Papers

Analytical and semipreparative resolution of enatiomers of albendazole sulfoxide by HPLC on amylose tris (3,5-dimethylphenylcarbamate) chiral stationary phases.

Phenylpropanoids from Lagotis ramalana

Xanthone constituents in Gentiana panthaica

Chemical constituents in Ixeridium gramineum

Application of Guanidines in Molecular Recognition