Croda presents new high purity excipients
Oleic Acid drug delivery excipients, claimed to enhance active
pharmaceutical ingredient (API) and formulation stability.
The excipients, presented at CPhI 2005, are designed specifically for pharmaceutical applications and manufactured via the company's unique purification technology, involving their flash chromatography process.
"Many excipients add impurities to drug products, which can interact with and cause instability of the API, or the dosage form of a drug," Rodolphe Bedel, head of Pharmacy and Nutrition, Croda, told In-PharmaTechnologist.com.
"It is very important that nothing harms the activity of the API," he said.
One of the industry's greatest challenges in dosage design is formulating a product that maintains the integrity of the API.
PEGs
Super Refined PEG 300, 400 and 600 are highly purified polyethylene glycols, offering pharmaceutical formulators the benefits of high purity excipients.
This is achieved through Super Refining, a technique that removes polar impurities, such as peroxide species, aldehydes and ketones.
Removal of these polar impurities eliminates their adverse interaction with APIs, thereby enhancing the stability of the drug. "Stability increases 2-3 times," Bedel said.
In accelerated stability trials (50°C), Super Refined PEG 400 demonstrated a peroxide value at least 50 per cent lower than a standard pharmaceutical grade PEG, both initially and after four weeks. Formaldehyde values after four weeks were at least 60% lower.
In addition to increasing stability, Super Refining of PEGs also minimises the potential for gelatin cross-linking by removing the impurities that cause this problem.
Cross-linking impairs dissolution, causing erratic drug release and can cause the capsule to harden and crack, shortening shelf life.
Polyethylene glycols are widely used as excipients in a variety of pharmaceutical products, including topical, oral and parenteral preparations.
Oleic acid
Croda's Super Refined Oleic Acid is a high purity lipid designed to aid drug delivery may provide reduced skin damage compared with an equivalent formulation.
By removing polar impurities, including primary and secondary oxidation products, Super Refining of oleic acid ensures drug formulations have greater stability and reduced potential for cellular irritation, the company claims.
In vitro testing with Super Refined Oleic Acid, as compared with a standard, has shown a clear reduction in intercellular leakage - an indicator of skin irritation potential
Oleic acid aids transdermal drug delivery by enhancing skin penetration and is also employed in pulmonary and nasal delivery systems.
Super Refined Oleic Acid can be used as an absorption enhancer in topical, transdermal and oral dosages, an excipient in nasal and pulmonary metered dose inhalers (MDIs), and as a component of self emulsifying drug delivery systems (SEDDS).
