Abstract
The development of oral tablet formulation for herbal medicines has been restricted by large drug loadings and the poor physicochemical and mechanical properties of dry herbal extracts (DHEs). Herein, statistical experimental designs were applied to herbal tablet formulation development and optimization using Wuzi Yanzong dry extract (WYE). The tablet disintegration time and hardness were identified as the critical quality attributes (CQAs) of the product. The tablet formulation was designed to achieve a high drug loading (50% or higher of WYE), shorter tablet disintegration time (less than 30 minutes), and suitable hardness (6.0 to 7.5 kp). A D-optimal mixture design was used to evaluate the effects of excipients on CQAs to minimize the risk compression failure and improve the tabletability in formulations containing WYE at 50% and 65% by weight. A partial least squares model was used to elucidate the multivariate relationships between a large number of formulation variables and product CQAs, and determine the maximum possible WYE loading. From overlaid plots of the effects of formulation variables on CQAs, it was found that a maximum WYE loading of 67% in tablet formulation satisfied the acceptance criteria of CQAs. In conclusion, this study shows that multivariate statistical tools are useful for developing tablet formulations containing high doses of herbal extracts and establishing control strategies that ensure product quality.
Highlights
Herbal medicines are well-accepted complementary and alternative medicines due to their unique advantages, which include few side effects, affordability, low cost, and widespread availability [1,2]
The aim of this study was to develop a herbal tablet formulation containing a high loading of Wuzi Yanzong dry extract (WYE) (50% or higher of WYE) with an acceptable disintegration time and hardness (6.0 to 7.5 kp)
We found experimental designs using the D-optimal mixture design procedure provided models that predicted the effects of formulation variables on critical quality attributes (CQAs) in tablets containing 50% or 65% WYE well
Summary
Herbal medicines are well-accepted complementary and alternative medicines due to their unique advantages, which include few side effects, affordability, low cost, and widespread availability [1,2]. Convenient, and inexpensive oral solid dosage forms with high physicochemical and microbiological stabilities. The unfavorable physicochemical and mechanical properties of DHEs, such as their hygroscopicity, stickiness, and bulkiness, cause the poor flowability and compressibility in tablet compression process [5]. The incorporation of large amounts of the DHEs into a tablet of acceptable size with appropriate disintegration time and hardness is a major challenge in the formulation of herbal tablets [4,6,7]. In general, the addition of disintegrants to the tablet formulation or high amount of magnesium stearate blended with the granules can promote the tablet integration, and the dry granulation of hygroscopic herbal extracts can improve their poor compressibility [9]
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
