Preparation and Evaluation of Directly Compressible Orally Disintegrating Tablets of Cannabidiol Formulated Using Liquisolid Technique

This study demonstrated the implementation of a liquisolid technique to formulate directly compressible orally disintegrating tablets (ODTs). Cannabidiol (CBD), a hydrophobic cannabinoid, was prepared as a liquisolid powder using microcrystalline cellulose–colloidal silicon dioxide as a carrier–coating material. Different liquid vehicles differing in their volatility, hydrophilicity, and viscosity were investigated. Each of the CBD–ODTs comprised CBD liquisolid powder (10 mg CBD), superdisintegrant, flavors, lubricant, and filler. The physical mixture (PM) ODT was prepared as a control. Ethanol-based ODTs (CBD–EtOH–ODTs) had comparable tablet properties and stability to CBD–PM–ODTs.

ODTs with nonvolatile-vehicle-based liquisolid powder had lower friability but longer disintegration times as compared with CBD–PM–ODTs and CBD–EtOH–ODTs. Compression pressure influenced the thickness, hardness, friability, and disintegration of the ODTs. With a suitable compression pressure to yield 31-N-hardness-ODTs and superdisintegrant (4–8%), CBD–ODTs passed the friability test and promptly disintegrated (≤25 s). Times to dissolve 50% of CBD–PM–ODTs, CBD–EtOH–ODTs, and nonvolatile-vehicle-based CBD–ODTs were 10.1 ± 0.7, 3.8 ± 0.2, and 4.2 ± 0.4–5.0 ± 0.1 min, respectively. CBD–EtOH–ODTs exhibited the highest dissolution efficiency of 93.5 ± 2.6%. Long-term and accelerated storage indicated excellent stability in terms of tablet properties and dissolution. Nonvolatile-vehicle-based CBD–ODTs exhibited a higher percentage of remaining CBD. This study provides useful basic information for the development of ODT formulations using a liquisolid technique application.

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Materials

The cannabidiol (CBD, CBD isolate, 99%) was received as a gift from the Medical Cannabis Research Institute, College of Pharmacy, Rangsit University (Mueang, Pathum Thani, Thailand). Microcrystalline cellulose (MCC; Avicel PH102) and croscarmellose sodium (CCS, Ac-Di-Sol) were received from Onimax Co., Ltd. (Bangkok, Thailand). Colloidal silicon dioxide (CSD, Aerosil 200) was received from Maxway Co., Ltd. (Bangkok, Thailand). Absolute ethyl alcohol (EtOH) was obtained from QRëC (Auckland, New Zealand). Caprylocaproyl macrogolglycerides (CM, Labrasol, Gattefossé SAS (Saint-Priest, French)), diethylene glycol monoethyl ether (DEGEE, Transcutol P, Gattefossé SAS (Saint-Priest, French)), oleoyl macrogolglycerides (OM, Labrafil M 1944 CS, Gattefossé SAS (Saint-Priest, French)), mannitol USP/EP (Mannogem EZ spray-dried mannitol), sodium starch glycolate (SSG, Explotab, JRS Pharma), and sodium stearyl fumarate (Lubripharm, SPI Pharma) were sourced from Rama Production, Co., Ltd. (Bangkok, Thailand). Glycerin and propylene glycol (PG) were supplied by RCI Labscan Ltd. (Bangkok, Thailand). Polyethylene glycol 400 (PEG) and polyoxyethylene sorbitan monolaurate (Polysorbate 20, P20) were purchased from Sigma-Aldrich (Missouri, MO, USA) and AppliChem GmbH (Darmstadt, Germany), respectively. Formic acid was obtained from KemAus (Cherrybrook, Australia). HPLC-grade methanol and acetonitrile were purchased from Fisher Scientific (Loughborough, UK). Spray-dried lactose (FlowLac 100) was provided by Meggle GmbH & Co. KG (Wasserburg am Inn, Germany). Stevioside or stevia powder was received from Krungthepchemi Co., Ltd. (Bangkok, Thailand). Menthol and peppermint oil were supplied by Thai-China Flavours and Fragrances Industry Co., Ltd. (Bangkok, Thailand). All chemicals were used as received.

Limpongsa, E.; Tabboon, P.; Pongjanyakul, T.; Jaipakdee, N. Preparation and Evaluation of Directly Compressible Orally Disintegrating Tablets of Cannabidiol Formulated Using Liquisolid Technique. Pharmaceutics 2022, 14, 2407. https://doi.org/10.3390/pharmaceutics14112407