Optimization of harvest and extraction factors by full factorial design for the improved yield of C-glucosyl xanthone mangiferin from Swertia chirata

AbstractSwertia chirata Buch.-Ham. ex C.B. Clarke is an important medicinal plant used in various herbal formulations as it shows significant biological activities such as hepatoprotective, hypoglycemic, anti-inflammatory, antimalarial, antioxidant and anti-parkinson. C-glucosyl xanthone glycoside (mangiferin) is known as bio-marker compound of genus Swertia L. Development of efficient extraction methods of C-glucosyl xanthone mangiferin from Swertia chirata was attempted by optimizing the pre-harvest, post-harvest and extraction techniques by full factorial design. Firstly, a full factorial design was implemented to evaluate the single and interactive effects of pre-harvest (growth stage and plant part), post-harvest (drying condition and storage periods) followed by selection of best extraction technique such as heat reflux extraction (HRE), microwave assisted extraction (MAE) and ultrasound assistant extraction (UAE) at different solvent types on mangiferin yield. HPTLC and HPLC techniques were used for the determination of mangiferin content in extracts generated from different plant samples. In addition, anti-oxidant and anti-diabetic properties were determined by using DPPH assay and percentage inhibition of α‑amylase enzyme. Substantial variation of mangiferin yield, ranged from 1.46 to 4.86% was observed, depending on the growth stage, plant part, drying condition, storage periods and extraction method. Results showed that drying of the leaves of Swertia chirata in the shade harvested at budding stage and stored for not more than 1 month was recommended for obtaining a higher mangiferin yield. Among different extraction techniques, MAE and UAE in 50% aqueous ethanol solvent were found to be efficient and cost-effective with better yield of mangiferin (4.82% and 4.86%, respectively) as compared to HRE (4.14%). Highest DPPH activity and percentage inhibition of α‑amylase was observed in the aqueous ethanol extract of S. chirata leaves harvested at bud-stage of plant followed by flowering stage. The study shows that optimization of various factors by full factorial design was found to be an effective procedure to improve mangiferin yield from Swertia chirata and can be used for extraction of mangiferin.

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Application of 32 Full Factorial Design and Desirability Function for Optimizing The Manufacturing Process for Directly Compressible Multi-Functional Co-Processed Excipient

Current Drug Delivery ◽

10.2174/1567201817666200508094743 ◽

2020 ◽

Vol 17 (6) ◽

pp. 523-539

Author(s):

Jalpa Patel ◽

Dhaval Mori

Keyword(s):

Factorial Design ◽

Spray Drying ◽

Desirability Function ◽

Full Factorial Design ◽

Angle Of Repose ◽

P Value ◽

Independent Variables ◽

Full Factorial ◽

32 Full Factorial Design ◽

Response Variables

Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 32 full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.

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Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and Cassia fistula Seed Gum by QbD Approach

Current Drug Delivery ◽

10.2174/1567201817666200317124022 ◽

2020 ◽

Vol 17 (5) ◽

pp. 422-437

Author(s):

Dixita Jain ◽

Akshay Sodani ◽

Swapnanil Ray ◽

Pranab Ghosh ◽

Gouranga Nandi

Keyword(s):

Drug Release ◽

Factorial Design ◽

Extended Release ◽

Polymer Concentration ◽

Green Manufacturing ◽

Full Factorial Design ◽

Cassia Fistula ◽

Negative Environmental Impact ◽

Seed Gum ◽

Full Factorial

Aim: This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. Background: The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been reported as a solution to this problem. But most of them are found to be composed of synthetic, semi-synthetic or their combination having physiological toxicity as well as negative environmental impact. Therefore, fabrication and formulation of multi-unit extended-release peroral preparations with natural, non-toxic, biodegradable polymers employing green manufacturing processes are being appreciated worldwide. Objective: Lamotrigine-loaded extended-release multi-unit beads have been fabricated with the incorporation of a natural polysaccharide Cassia fistula seed gum in calcium-cross-linked alginate matrix employing a simple green process and 23 full factorial design. Methods: The total polymer concentration, polymer ratio and [CaCl2] were considered as independent formulation variables with two different levels of each for the experiment-design. The extended-release beads were then prepared by the ionotropic gelation method using calcium chloride as the crosslinkerions provider. The beads were then evaluated for drug encapsulation efficiency and drug release. ANOVA of all the dependent variables such as DEE, cumulative % drug release at 2h, 5h, 12h, rate constant and dissolution similarity factor (f2) was done by 23 full factorial design using Design-Expert software along with numerical optimization of the independent variables in order to meet USP-reference release profile. Results: The optimized batch showed excellent outcomes with DEE of 84.7 ± 2.7 (%), CPR2h of 8.41± 2.96 (%), CPR5h of 36.8± 4.7 (%), CPR12h of 87.3 ± 3.64 (%) and f2 of 65.9. Conclusion: This approach of the development of multi-unit oral devices utilizing natural polysaccharides might be inspiring towards the world-wide effort for green manufacturing of sustained-release drug products by the QbD route.

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