Development and Evaluation of Cannabidiol Orodispersible Tablets Using a 23-Factorial Design

Abstract

Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from Cannabis sativa used in the treatment of Lennox–Gastaut and Dravet syndromes. The tablets were obtained using an eccentric tableting machine and 9 mm punches. To develop CBD ODTs, the following parameters were varied: the Poloxamer 407 concentration (0 and 10%), the type of co-processed excipient (Prosolv® ODT G2—PODTG2 and Prosolv® EasyTab sp—PETsp), and the type of superdisintegrant (Croscarmellose—CCS, and Soy Polysaccharides—Emcosoy®—EMCS), resulting in eleven formulations (O1–O11). The following dependent parameters were evaluated: friability, disintegration time, crushing strength, and the CBD dissolution at 1, 3, 5, 10, 15, and 30 min. The dependent parameters were verified according to European Pharmacopoeia (Ph. Eur.) requirements. All the tablets obtained were in accordance with quality requirements in terms of friability (less than 1%), and disintegration time (less than 180 s). The crushing strength was between 19 N and 80 N. Regarding the dissolution test, only four formulations exhibited an amount of CBD released higher than 80% at 30 min. Taking into consideration the results obtained and using the Modde 13.1 software, an optimal formulation was developed (O12), which respected the quality criteria chosen (friability 0.23%, crushing strength of 37 N, a disintegration time of 27 s, and the target amount of CBD released in 30 min of 99.3 ± 6%).

Structural Characterization and Optimization of a Miconazole Oral Gel

“…The statistical parameters used to evaluate the proposed model are the coefficient of determination R 2 , which indicates the variance in the response variable as explained by the model, and Q 2 , which indicates the variation of the response as predicted by the model, model validity, and reproducibility. Based on the statistical data, the software develops an equation from which the influence of the independent variables on the response can be evaluated [43][44][45]. The goal is to optimize the independent variables to achieve the desired values of the dependent parameters [46].…”

Phytocannabinoids: Exploring Pharmacological Profiles and Their Impact on Therapeutical Use

“…A 10 mg CBD orodispersible tablet (CBD-ODT) has been developed using Quality by Design (QbD) principles to optimize formulation parameters such as disintegration time, crushing strength, friability, and the release profile of the API at different intervals (Figure 3). Independent variables, including the choice of solid carriers, were carefully considered [84,85]. However, a significant challenge encountered in developing ODT with CBD is the in vitro dissolution test, owing to the API s low solubility in water-based media.…”

“…To address this issue, varying amounts of surfactants (such as sodium lauryl sulfate or Tween 20) were incorporated to establish an appropriate dissolution medium. Notably, no further in vivo evaluation results have been reported for these two CBD-ODT studies [85,86].…”

Analytical strategies for herbal Cannabis samples in forensic applications: A comprehensive review

“…For instance, in Belgium, a maximal limit of 0.2 w/w% of the total THC content is stated (Royal Decree, 2017). Czech Republic and Austria allow a THC content <0.3 w/w% and Switzerland, as a non‐EU nation, even tolerates Cannabis products containing THC ≤1.0 w/w% before they are covered by the narcotics legislation (Hädener, Gelmi, et al, 2019; Kadkhodaei et al, 2021; Vlad et al, 2020). Important to mention is that it is often unclear whether the regulated % THC contains the total THC concentration, that is, THC and THCA, or the THC content only.…”