Liquisolid systems represent an emerging approach in the preparation of solid dosage forms with liquid lipophilic drug or poorly water-soluble drug solution/suspension in suitable liquid vehicle. This study addresses the lack of data regarding the compaction behavior of liquisolid systems, with the aim to investigate the influence of liquid load, carrier to coating ratio, carrier type (microcrystalline cellulose vs. spray dried calcium hydrogen phosphate, anhydrous (Fujicalin®)) on flowability and compaction properties of liquisolid systems and to determine the optimum liquid loads. Liquisolid admixtures with Fujicalin® showed notably better flowability than those with microcrystalline cellulose. An increase in carrier to coating ratio led to enhanced flowability of the admixtures. Compacts with Fujicalin® had good mechanical properties up to 24.7% liquid, while those with microcrystalline cellulose had acceptable mechanical strength up to 16.2% liquid. Liquisolid systems with Fujicalin® showed similar tabletability profiles as those with microcrystalline cellulose, despite having higher liquid content. The ejection stress values indicated that the addition of lubricant might be needed in the case of liquisolid systems with Fujicalin®. Superior properties of Fujicalin® as a carrier for liquisolid tablets were revealed, and dynamic compaction analysis was found to be a valuable tool for the assessment of compaction behavior of liquisolid systems.
The processing of liquisolid systems (LSS), which are considered a promising approach to improving the oral bioavailability of poorly soluble drugs, has proven challenging due to the relatively high amount of liquid phase incorporated within them. The objective of this study was to apply machine-learning tools to better understand the effects of formulation factors and/or tableting process parameters on the flowability and compaction properties of LSS with silica-based mesoporous excipients as carriers. In addition, the results of the flowability testing and dynamic compaction analysis of liquisolid admixtures were used to build data sets and develop predictive multivariate models. In the regression analysis, six different algorithms were used to model the relationship between tensile strength (TS), the target variable, and eight other input variables. The AdaBoost algorithm provided the best-fit model for predicting TS (coefficient of determination = 0.94), with ejection stress (ES), compaction pressure, and carrier type being the parameters that influenced its performance the most. The same algorithm was best for classification (precision = 0.90), depending on the type of carrier used, with detachment stress, ES, and TS as variables affecting the performance of the model. Furthermore, the formulations with Neusilin® US2 were able to maintain good flowability and satisfactory values of TS despite having a higher liquid load compared to the other two carriers.
Liquisolid systems are a novel, promising platform for the production of solid dosage forms with a high liquid content, i.e. dispersion of the drug in a suitable, hydrophilic, non-volatile liquid vehicle or liquid drug. This technology requires conventional, but highly porous excipients (carrier and coating material in the appropriate ratio) able to absorb/adsorb liquid medication, resulting in both good flowability and acceptable compression properties. This approach has shown great potential to improve the dissolution rate and bioavailability of poorly soluble drugs, and has been recognized as a good alternative to common, more complex and expensive techniques. A variety of applications of this simple technique have been investigated recently, including the preparation of: modified release tablets, orally disintegrating tablets, solid dosage forms with liquid herbal extracts, etc. This emerging technology has numerous advantages, and the most important are: simplicity, cost-effectiveness, applicability in large scale production and environmental friendliness. However, it is accompanied by certain challenges as well, such as limited applicability in the case of highly dosed drugs. This article aims to give a comprehensive overview of recent progress regarding the potential applications of this technology, as well as to give an insight into the new liquisolid-based techniques intending to further support its commercial applicability.
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