Application of a liquisolid technique to Cannabis sativa extract compacts: Effect of liquid vehicles on the dissolution enhancement and stability of cannabinoids

This work describes the application of the liquisolid technique to enhance cannabinoid dissolution from Cannabis sativa L. (CS) compacts. The effects of five vehicles, namely, volatile (ethanol) and nonvolatile (caprylocaproyl macrogolglycerides, polyethylene glycol 400, oleoyl macrogolglycerides and polysorbate 20) liquids, on tablet properties, dissolution and stability were investigated.

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Application of a liquisolid technique to enhance cannabinoid dissolution from Cannabis sativa compacts was described for the first time.

Different vehicles influenced the hardness, disintegration and wettability of Cannabis sativa compacts, as well as cannabinoid dissolutions to different extents.

Liquid vehicles had no effect on the percent remaining cannabinoid content but demonstrated different effects on the dissolution behavior of 90-d-old compacts.

The viscid oleoresin CS extract was mixed with vehicles before being transformed into free-flowing powder by the use of microcrystalline cellulose and silica as carrier and coating materials. Liquid vehicles had a nonsignificant effect on liquid load factor of CS extract. CS liquisolid compacts had acceptable tableting properties in terms of weight variation, friability, hardness, content uniformity and disintegration time. Different vehicles affected the hardness, disintegration, and wettability of CS compacts and thus the dissolution behaviors of cannabinoids to different extents. Dissolutions of cannabinoids from CS compacts were rate-limited by the disintegration process.

Liquisolid formulations using nonvolatile liquids with low polarity or high HLB yielded more than 90% cannabinoid dissolution. Stability studies revealed nonsignificant changes in tablet characteristics, cannabinoid content and dissolutions of CS compacts when stored at 5±3 °C for 3 months. This work presents a general concept of how to successfully formulate CS extract with cannabinoid dissolution enhancement characteristics.

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Article information: Napaphak Jaipakdee, Peera Tabboon, Ekapol Limpongsa, Application of a liquisolid technique to Cannabis sativa extract compacts: Effect of liquid vehicles on the dissolution enhancement and stability of cannabinoids, International Journal of Pharmaceutics, 2021. https://doi.org/10.1016/j.ijpharm.2021.121277.