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Handbook Of Pharmaceutical Salts Properties Selection And Use Pdf

handbook of pharmaceutical salts properties selection and use pdf

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Handbook of Pharmaceutical Salts : Properties, Selection, and Use

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Stahl and G. ISBN Because an estimated half of all drug molecules used in medicine are administered as salts, the selection of a suitable salt for a drug candidate is recognized as an essential step in the preclinical phase of drug development. Surprisingly, however, the scientific literature on this topic is rather limited and scattered throughout numerous journals and patents. The majority of medicinal chemists in the pharmaceutical industry whose primary focus is the design and synthesis of novel compounds as future drugs are organic chemists for whom salt formation is often a marginal activity restricted to the short-term objective of obtaining crystalline material.

An Automated Approach to Salt Selection for New Unique Trazodone Salts

Download the May issue in pdf format. CI Homepage. Chemistry International Vol. Stahl and G. ISBN Because an estimated half of all drug molecules used in medicine are administered as salts, the selection of a suitable salt for a drug candidate is recognized as an essential step in the preclinical phase of drug development.

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The properties of the solid-state of drug substances are critical factors that determine the choice of an appropriate salt form for the development of the pharmaceutical formulation. The most relevant properties may affect the therapeutic efficacy, toxicity, bioavailability, pharmaceutical processing and stability. The salt form must fulfil the needs of the targeted formulation, be suitable for full-scale production and its solid-state properties maintained batchwise as well as over time. Comparison of the solid-state properties of different salt candidates may be quite complicated if each salt candidate exist as different solid phases: polymorphs, solvates or amorphous forms. Thermal analysis, microcalorimetry and combined techniques, X-ray diffraction, solubility, intrinsic dissolution, sorption-desorption and stability studies are basic techniques for the characterisation of the salt candidates. Some examples show the role of the salt form as well as the polymorphic form in the characteristics of the solid-state.

handbook of pharmaceutical salts properties selection and use pdf

Unlocking the Use of Lipid-Based Formulations with

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The purpose of this study was to establish an automated approach to salt selection and to search for unique trazodone salts for new applications. Automated procedures were developed on a Biomek automation workstation with stacker and plate reader capabilities. Trazodone was dispensed into well plates, and an automated method was set up to form trazodone salts. Salts were observed under a polarized light microscope to determine crystallinity.

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Characterisation of salts of drug substances

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