Excipients Used in Parenteral Formulations of Biotech Products

These flashcards encompass key concepts and details from the lecture on excipients used in parenteral formulations of biotech products.

What is the key purpose of excipients in protein formulations?

To enhance therapeutic effectiveness and ensure safe products.

What factor can complicate protein formulations regarding excipients?

The nature of the protein, such as lability and therapeutic use.

Name two examples of solubility enhancers used in protein formulations.

Amino acids (e.g., lysine, arginine) and surfactants (e.g., sodium dodecylsulfate).

What is Tissue Plasminogen Activator (tPA) used for?

To break down blood clots, particularly for treating strokes.

How is tPA produced using biotechnology?

Through recombinant biotechnology techniques, leading to recombinant tissue plasminogen activator (rtPA).

What role does Interleukin 2 (IL-2) play in the immune system?

It regulates the activities of white blood cells responsible for immunity.

What types of interactions can lead to protein aggregation?

Hydrophobic and electrostatic interactions.

What are anti-adsorption agents used for in protein formulations?

To reduce the adsorption of active proteins to interfaces.

What is a common example of a protein that exhibits aggregation?

Insulin.

Which factors influence the equilibrium state of insulin in solution?

pH, insulin concentration, ionic strength, and specific excipients (e.g., Zn2+).

What is the isoelectric point of insulin in the denatured state?

5.3.

What effect do phenolic excipients have on insulin?

They act as antimicrobial agents and stabilize insulin by binding to hexamers.

What are buffer agents used for in parenteral formulations?

To maintain protein solubility and stability by controlling the pH.

What happens to proteins at pH levels above their isoelectric point?

They are predomitantly negatively charged, causing repulsive forces.

What can be done to reduce oxidative degradation of proteins rich in certain amino acids?

Replace oxygen with inert gases or add antioxidants like ascorbic acid.

Why are preservatives added to protein formulations?

To minimize microbial growth in containers designed for multiple injections.

What are osmotic agents and their purpose?

Substances like saline or sugars that adjust tonicity and stabilize protein structure.

What is one method for sterilizing biotech products?

Aseptic manufacturing and final filtration through 0.2 or 0.22 mm pore filters.

Why are there limited oral delivery systems available for proteins?

Due to the hostile environment in the GI tract affecting protein stability and absorption.

What is the significance of the selection of proper pH and ionic strength in protein formulations?

It helps to enhance solubility and reduce aggregation.

What are lyoprotectants used for in biotech product formulations?

To protect proteins during freeze-drying processes.

What does the presence of surfactants do to an interface?

It renders the interface hydrophilic and prevents protein adhesion.

How does albumin function as an anti-adhesion agent?

By competing with therapeutic proteins for binding sites to prevent adhesion.

What is the role of glycerol or NaCl in modern insulin formulations?

To act as isotonic agents and minimize tissue damage upon injection.

Why are concentration levels of preservatives usually bacteriostatic?

To inhibit growth without killing microorganisms.

What can the presence of zinc in insulin formulations promote?

The formation of hexameric complexes that enhance stability.

What is a preferred method for avoiding aggregation during protein formulation?

Maintaining optimal pH to avoid unwanted chemical reactions.

What does the term 'preferential exclusion' refer to in the context of osmotic agents?

The ability of sugars and polyols to hydrate proteins while being excluded from their surface.

What is the significance of thermal stability in protein formulations?

It indicates enhanced structural integrity of the protein in the presence of certain excipients.

Identify a common antioxidant used in protein formulations.

Ascorbic acid.