When it comes to the $200 billion global pharmaceutical manufacturing market, the real unsung heroes are the excipients – the inactive ingredients that give tablets their form, stability and controlled release properties. While the active drug gets all the attention, excipients are the quiet force enabling medication to be effectively delivered to patients.
“Excipients play an absolutely vital role in drug formulation and manufacturing,” said Dr. Maria Almeida, Principal Scientific Liaison at the International Pharmaceutical Excipients Council (IPEC). “Without the right combination of excipients, many drugs simply couldn’t be produced as viable tablets or capsules.”[1]
As the tablet remains the most popular and patient-friendly dosage form, we take an in-depth look at the top 10 excipients leading the way in solid oral manufacturing based on market usage data, regulatory approval trends, and insights from industry experts.
1. Microcrystalline Cellulose – The Reigning Champion
“Microcrystalline cellulose is the gold standard for tablet binders and diluents. Its versatility and safety record are simply unmatched in the industry.” – Dr. Robert Langer, MIT
Topping the charts at over $1 billion in annual usage is microcrystalline cellulose (MCC).[1] This purified, partially depolymerized cellulose derivative functions as a binder, diluent, disintegrant and adsorbent – making it the true multi-tool for formulators.
“MCC is cost-effective, chemically inert and extremely compressible, which is why it remains the go-to excipient for direct compression tableting,” explained Dr. Langer. “Its exceptional dry binding and disintegration properties allow for very tight control over tablet hardness and dissolution rate.”[2]
2. Croscarmellose Sodium – The Super Disintegrant
When it comes to rapidly breaking apart tablets for fast dissolution and drug release, no excipient does it better than croscarmellose sodium. This cross-linked cellulose polymer ranks as the most widely used superdisintegrant worldwide.
“Croscarmellose has a truly remarkable water wicking and swelling capacity,” noted Dr. Almeida. “Even at low use levels around 2-5%, it facilitates rapid tablet disintegration in the stomach while having no impact on compressibility.”[1]
3. Magnesium Stearate – The Premier Lubricant
Proper lubrication is critical for the manufacturing of robust tablets that can withstand mechanical stress. Magnesium stearate, the salt of stearic acid, is the gold standard lubricant thanks to its superior glidant properties.
“Magnesium stearate allows for lower ejection forces during tableting while preventing sticking and picking of tablet surfaces,” said Terry Schultz, Senior Technical Manager at DuPont Nutrition & Biosciences. “It’s highly hydrophobic which provides additional moisture protection benefits.”[3]
Other Top Excipients:
- Lactose – Cheap filler/diluent with good compressibility
- Starch – Traditional binder and disintegrant
- Povidone (PVP) – Versatile binder used in wet granulation
- Hydroxypropyl Methylcellulose (HPMC) – Controlled release polymer for oral and topical drugs
- Crospovidone – Highly effective disintegrant
- Colloidal Silicon Dioxide – Glidant and anti-caking agent
- Mannitol – Diluent and sweetener for chewable/dispersible tablets
“Choosing the right excipients, and getting their ratios correct, is crucial for optimizing a tablet’s manufacturability, stability and drug release profile,” Dr. Almeida stated. “As new therapeutic compounds emerge, innovative excipients will undoubtedly follow to improve drug delivery.”[1]
With their market valued at over $6 billion and growing steadily, excipients remain a vital component driving the pharmaceutical industry’s success in bringing life-saving medications to market.
Citations:
[1] https://pharmacentral.com/products/25-most-popular-excipients-based-on-search-and-new-product-registration-data/
[2] https://www.drugtopics.com/view/overview-pharmaceutical-excipients-used-tablets-and-capsules
[3] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7662502/
[4] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8745980/
[5] https://pharmacentral.com/learning-hub/technical-guides/pharmaceutical-diluents-and-fillers/
