BHS005-6 Drug discovery and development - University of Bedfordshire

Learning Outcome 1: Demonstrate a critical understanding of drug discovery and development and the various processes that underpin drug design, preclinical, clinical and post- licensing development of drugs.

Learning Outcome 2: Critically analyse and evaluate the experimental data and relevant scientific literature to understand current research advancement in the area of drug discovery and development, present and argument information clearly and effectively in the written form.

Students are expected to submit a report based on practical sessions in which they carried out experiments in
Part 1. Determination of Physiochemical properties of drugs and
Part 2. Determination of enzymatic activity of Glutathione - S - Transferase (GST)

Demonstrate the skills necessary to generate, analyse and present laboratory data obtained from a practical exercise in the area of drug discovery and development Produce a written report in the form of a scientific paper that discusses and provides critical analysis of the results of the practical sessions according to expectations described in the assignment brief.

The report is a combined one and should be written based on the two experiments carried out

1. Determination of Physiochemical properties of drugs &
2. Determination of enzymatic activity of Glutathione - S - Transferase (GST)

Clarity of English language and presentation is essential throughout.

Your report should include following sections for each part of the practical. Introduction (300-500 words)

You should summarise the published background literature relevant to this study. You must explain what your experimental
studies were about, and place them in context of the previously published journal research articles and text books.

Aims
Briefly state what you are looking for in the experiment.

Materials and Methods
You should briefly summarise the methods used in the style of a journal. Methods should be written in the past tense and in paragraphs. They should contain sufficient detail to allow someone else to reproduce your experiments, but avoid unnecessary detail. There is no need to restate the contents of the practical handout.

Results
These sections should typically represent approximately 30-40% of each part. Data may be presented in text, tables, graphs, diagrams, or photographs as appropriate for your particular studies. Figures and tables should be separately numbered, and be clearly labelled. You should include written text to explain what your findings are and what is shown in any figures and tables. Results should describe your findings/observations and may state brief conclusions.

Discussion (800-1000 words)
You should interpret your results, explaining what they indicate. You should evaluate the quality of your data and the reliability of the experimental technique. You should identify any problems with the technique or data (if any exist) and suggest possible solutions. You should compare your findings to previously published findings or your expected findings, and should place your results in the context of published scientific literature.

Practical one: partition coefficient

1. You have the concentration and Absorbance for each buffer (Phosphate and Flucanazole).
2. Make a scatter plot using the data collected. Absorbance (y-axis) against concentration of buffer (x-axis) for each buffer phase. Add a trend line and display equation and R squared value on the chart.
3. In the equation derived from the graph below, y = 0.0002x + 0.0191 (these values change for each data set), y is the absorbance and x is the unknown concentration. Using this formula calculate concentration of solute in phosphate buffer and octanol phase from each funnel.
4. Once concentration of solute in each phase calculated, derive partition co-efficient using the formula, P = Corg/Caq. Calculate average partition co-efficient from 4 flasks and standard deviation. Compare the values with the values from literature (Hazare et al., 2009)

Practical two: Calculating pH, pKa and Ka

1. Using the formula, C1V1=C2V2, you will need to calculate the concentration of Sodium acetate and acetic acid (ethanoic acid) in each solution (A, B, C). You have the starting concentration of acetic acid and Sodium acetate (0.1M each).
Eg: Solution A
0.1M Na acetate * 30ml = ? * (Concentration of Na acetate) * 60 ml (total volume of solution A)
= 0.05M Na acetate
Like wise calculate for all the three solutions. Now you have the concentration of acid and base and you can use these concentration values to calculate pKa
2. Once you have pKa, calculate Ka for each solution using the formula mentioned above.
3. Using the formula mentioned in step 1, calculate the concentration of acid and base in solution D. You will get following values.
Concentration of Na acetate (base) = 0.033M
Concentration of acetic acid (acid) = 0.067 M
4. You have pKa, Ka of acetic acid (ethanoic acid) and concentration of acid and base.
5. Use Henderson-Hasselbalch equation (see the formula at the top) to calculate the pH of solution D.
6. Plot graphs of pH against volume of 0.1 M HCl and pH against volume of 0.1M NaOH in the same sheet of graph paper.
7. Change the series name to HCl and NaOH
8. Calculate the buffer capacity of buffer solution upon the addition of 0.1M Hcl or 0.1M NaOH, using the formula mentioned above in a table format
9. From the graph below, calculate the added volume of Hcl that lowered the pH by one unit (pH = 3) and volume of NaOH that increased the pH by one unit (pH = 5). (Note that, lines are not very accurate in this word file)

Attachment:- Drug discovery and development.rar