Cbe 4404a – Downstream Processes in Pharmaceutical Manufacturing

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The University of Western Ontario Department of Chemical and Biochemical Engineering

CBE 4404a – Downstream Processes in Pharmaceutical Manufacturing

Assignment 2

Giordano Festa – 250 675 865 – gfesta@uwo.ca

Prof. Lauren Anne Briens

Date Submitted: September 29th, 2016

1. Cialis

Cialis is a film-coated pill that is used to treat erectile dysfunction. The excipients used are added to achieve rapid therapeutic onset, hardness, low friability and to promote easy dosing i.  

The active component is tadalafill and is available in 2.5mg, 5mg, 10mg and 20 mg dosages. This constituent is not water soluble, but instead only in very basic pH’s. Sodium laurilsulfate is added to act as a solubilising agent; the excipient is commonly found in detergents and is known to encourage a basic pH ii. It is most likely incorporated to successfully dissolve the active and so, relatively speaking, there probably does not need to be a large amount of sodium laurilsulfate (needed to dissolve only a = small amount of active). Some excipients that might be present in larger amounts, relatively speaking, would be fillers or buffers and include lactose monohydrate and microcrystalline cellulose.  

Lactose Monohydrate, commonly referred to as ‘milk sugar’, has widespread use in the pharmaceutical industry as a filler or diluent. This is so because the excipient is economical (cheap and available), compatible with many other commonly used excipients and has a bland taste. Additionally, milk sugar exhibits favorable workability characteristics, for example low hydroscopicity and excellent compressibility. Microcrystalline cellulose, like milk sugar, is commonly used in pharmaceuticals as a filler. The two excipients will therefore be present in relatively large amounts.

Other excipients include binders and lubricants.  Hydroxypropylcellulose (HPC) is the primary binder used in Cialis manufacturing. It is a polymer (saccharide) that enables the providers of Cialis to supply tiny pills, in order to facilitate dosing, that possess sufficient mechanical strength, to ensure the pills remain intact until ingestion. Cialis makes use of two very widely used lubricants. The first being magnesium stearate (of vegetable origin) and the other being Opadry Yellow II. As lubricants they are both present in relatively small amounts, and are incorporated due to high lubrication potential, stability and cost effectiveness.  Additionally, Opadry Yellow II is pH independent iv. The final excipient is croscarmellose sodium, which acts as a superdisintegrant and is therefore also present in relatively small amounts v.