UCL School of Pharmacy
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UCL School of Pharmacy
29/39 Brunswick Square
London WC1N 1AX
United Kingdom
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New methods for exquisite control and quantification of amorphous pharmaceuticals

Project Description

The physical form of an active pharmaceutical ingredient (API) will impact solubility, dissolution rate and, as a consequence, bioavailability. APIs commonly exist as a number of polymorphs; metastable polymorphs generally have higher solubilities and so greater bioavailability. In the limit, the form with the greatest solubility will be the amorphous form. It follows that formulation of poorly soluble APIs in the amorphous state has the potential to produce the most efficacious final product. However, the amorphous state is also the most thermodynamically unstable state. Relaxation with time, and eventual conversion to a crystalline form, will dramatically reduce solubility and the performance of the drug product may be lost. Even though it is widely studied, the amorphous state is still poorly understood. Successful formulation of amorphous drug products therefore requires fundamental understanding of the short-range molecular ordering that must be present in amorphous matrices, correlation of this ordering with the method of manufacture and knowledge of the temporal conversion to long-range, crystalline, structure.

This project will use the novel method of vapour-phase deposition onto low temperature substrates for generating amorphous forms of APIs with minimal short-range order. It will then develop a range of spectroscopic, diffraction and calorimetric analyses with the specific aims of i) characterising the degree of short-range order, ii) determining the rate of change in order with time and iii) quantifying the amorphous content.

Main Methods and Techniques to be employed

The project will initially involve the use of vapour phase deposition to prepare amorphous forms of drugs; characterisation will then be undertaken using X-ray diffraction, differential scanning calorimetry, and Raman spectroscopy. Subsequently, the project will use pair-distribution function analysis to gain a detailed characterisation of molecular ordering in the amorphous state, and use the results to develop methods for quantifying amorphous content. Finally, the changes the molecular ordering occuring as a function of time and temperature will be probed using synchtrotron radiation.

Further information

This studentship is limited to students with Home/ EU tuition fee status and the preferred start date is October 2013.

The successful applicant will be expected to have a UK Bachelor’s degree in Pharmacy, Chemistry or Materials Science, awarded with first or upper second-class Honours, or an overseas qualification of an equivalent standard from a recognised higher education institute, or a recognised taught Master’s degree is required.

Applications must include CV, personal statement plus the contact details of two referees and should be sent to Victor Diran.

For any academic queries please contact the lead supervisors:

Dr Simon Gaisford

Dr Gareth Williams

Dr Christoph Salzmann

Closing date of application is 31st May 2013.

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