Pharmaceutical products are a critical staple of the disease prevention & treatment industry. For example, antibiotics have been commonly available since the 1940s, and have done wonders at saving patients with infections ranging from pneumonia to sexually spread diseases. (1) However, pharmaceutical drugs are not always consistent in their performance, which can affect both customers and pharmaceutical companies. (2) Following are criteria that are impacted by particle size distribution, and which highlight the importance of maintaining its consistency.
Product Performance
- Bioavailability
Bioavailability refers to the fraction of an active drug ingredient that gets absorbed into circulation. A drug product’s bioavailability is directly correlated with its effectiveness; for example, reduced and consistent particle size in hydrophobic drugs increases their oral bioavailability, and thus their ability to achieve the intended function. (3)
- Solubility
Decreased particle size is directly proportional to increased surface area. Drug products containing inconsistent particle size distributions, therefore, also confer inconsistent solubility; if a product cannot be solubilized in the body, its bioavailability will be limited. Homogenizers are one example of lab equipment that can achieve consistent particle size distribution, and ultimately solubility, of consumer drug products.
- Stability
Emulsion stabilization is critical in that it protects against colloid aggregation, or alternatively, phase separation. As with solubility, the level of product stabilization is correlated with the drug’s bioavailability; thus, it is critical that drug manufacturers attain consistent particle size distribution to maximize its stability. (4)
Product Manufacturability
- Direct Compression
Direct compression is a popular method of tablet compression because of its short, simple, and effective method. Its effectiveness is strongly influenced by the ratio of API to excipient, as well as by the amount of moisture and ability to withstand heat. One of the biggest risks of using direct compression is the potential for sifting, which occurs when there is a mixture of small and large particles (AKA, inconsistent particle size). (5)
- Granulation
Granulation is an alternative mode of tablet compression that can be used if the powder’s properties are not suitable for direct compression. Specifically, granulation can tolerate higher quantities of API than direct compression; however, similar to direct compression, consistent particle size distribution is essential to successful granulation. (5)
- Tablet Coating
Manufacturers may choose to coat their drug tablets for reasons such as increased product stability, masked taste, controlled ingredient release, and aesthetic purposes. Consistency (or lack thereof) in particle size distribution can have an effect on the product performance, specifically its bioavailability, stability, and dissolution rate. Product manufacturability may also be affected in its flowability and mixture segregation.
A drug’s ability to have its intended effect can be attributed to a wide variety of factors. In particular, particle size and its consistency in size are high-impact factors that every drug manufacturer should consider. The first step in synthesizing a drug product that confers high bioavailability is purchasing equipment that will achieve consistent particle size distribution.
The Pion High Pressure Homogenizer Advantage
At Pion, we understand the necessity to reduce particles to a stable size repeatedly. That’s why we are proud that our high pressure homogenizers are among few on the market that can achieve particle sizes of 0.1 µm after only one pass.
Our products are trusted by pharmaceutical researchers and lab managers around the world for key benefits, such as production of nano/micro emulsions, dispersions, and suspensions; importantly, this equipment can achieve consistent particle sizes at or below 100 nm, a key benefit for researchers & corporations that synthesize pharmaceutical products.
Learn more here.
