From Frustration to Formulation: Miglyol 812 N
After not having much luck with long-chain triglycerides, I began testing several medium chain triglycerides (MCTs), this week. When I tried Miglyol 812 N – I could hardly contain my excitement! Although I was trying my best to keep my calm, you better believe I was jumping with joy on the inside!
The Miglyol 812 N + TMZ solution was highly soluble, since Miglyol is also lipophilic like TMZ. Furthermore, Miglyol’s lipophilicity ensures its stability in the nasal cavity, while its insolubility in water is an added advantage, given that TMZ is highly unstable in water. AND, the formulation sprayed more like a mist than any other combination I had tried up until this point, due to Miglyol’s low viscosity.
Miglyol 812 N – a medium chain triglyceride ester, is formed when a plant-derived glycerol molecule is chemically bonded with caprylic acid (C8) and capric acid (C10) which are derived from saturated coconut and palm kernel oil and combined in a 58:41 ratio.
But, “high solubility” and “better sprayability” aren’t the only reasons Miglyol 812 N is an ideal primary solvent for my nasal spray composition. It also offers:
- Excellent Stability: under thermal and oxidative stress, which is crucial for meeting the FDA’s 2-year shelf life requirement.
- Miglyol has shown excellent stability in long-term studies and at elevated temperatures (including the 6-month accelerated studies required by the FDA) when evaluated under ICH (The International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use) guidelines.
- High Safety: Miglyol is certified low in impurities and made from renewable, vegetable raw materials, such as palm kernel and coconut oil. By mimicking natural fats, it is readily biodegradable in the body, lowering the risk of adverse effects
- Increased Efficiency: Higher absorption and quicker metabolism than long chain triglycerides, improves the onset of action.
- Improved Patient Compliance: Being a clear, colorless liquid, with neutral odor and taste will improve patient acceptance and compliance.
However, I wasn’t satisfied with just Miglyol 812 N as my base solution/ solvent system. I wanted to go all the way through standard protocol to determine a solvent for lipophilic molecules, and continue to look for ways to improve the solubility.
Miglyol’s compatibility with a wide range of pharmaceutical excipients and APIs, was a huge stress buster at this point, as it gave us the liberty to create complex formulations and try many inactive ingredients, without worrying too much about compromising the stability of the formulation.
But, I don’t want to steal the show from Miglyol 812 N today… so to find out which inactive pharmaceutical ingredients, excipients, and cosolvents we end up adding to complement our primary solvent, Miglyol 812 N, and finalize our base solution, you’ll have to come back next week!
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