Liquisolids as a platform for the formulation of cannabis tablets

液固体系作为大麻片剂制剂的平台

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Abstract

Mesoporous silica-based liquisolids offer an effective method for transforming liquid or sticky actives, such as cannabis extracts, into free-flowing powders. This approach broadens the formulation strategies available for these actives, which are typically limited to liquid formulations or soft gelatin encapsulation, by facilitating the formulation of tablets. However, tableting liquisolids is challenging due to issues including low tensile strength, capping and delamination. Overcoming these challenges requires careful selection of excipients and tableting parameters to produce tablets with sufficient tensile strength while also maintaining high Overall Liquid Load. In our study, we utilized a 65/35 volumetric ratio of 0.75 mL/g liquid loaded Syloid® XDP 3050 silica and Vivapur® 101 as a binder/filler to formulate cannabis liquisolid tablets with a target THC dose of 10 mg per tablet. Findings indicated that a 4% concentration of Kollidon® CL-F was optimal for disintegration, while 0.5% magnesium stearate proved to be the most effective lubricant concentration. Utilizing a rotary press compaction cycle on a StylOne® compaction simulator, we found precompression around half the main compaction pressure allowed for maximizing tableting speed while maintaining high tensile strength and keeping tablet defects to a minimum. The resulting cannabis liquisolid tablets demonstrated a tensile strength of 1.58 N/mm(2) and a high Overall Liquid Load of 38.4% (V/V). They exhibited acceptable disintegration time, friability, dissolution behavior and were proven to remain stable for 30 days at 40 °C and 0% humidity. Under refrigerated conditions, stability is predicted to be >3 years.

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