(T1230-05-28) Assessing Impact of Core Components, Coating Formulation and Functional Packaging on Product Quality of Nutraceutical Tablet Dosage Forms

Purpose: It has been reported that the extracts of Active Nutraceutical Ingredient’s (ANI’s) like Bacomind, Garlic, and Ashwagandha offer health benefits (1–3). However, formulating tablet dosage forms with these ANI’s is challenging because of their poor flow and compressibility properties and high moisture sensitivity. This study investigates the potential applications of formulated excipients for producing tablets by direct compression (DC) method for challenging ANIs. The study also examined the effects of film coating applications on the resulting tablets and their stability.

Methods: ANI tablets of Bacomind, Garlic, and Ashwagandha were separately compressed via DC method, utilizing Nutracore Label Friendly Filler and Nutracore Label Friendly Lubricant. Additionally, StarCap was included in the formulation of Bacomind and Ashwagandha to improve the DT of compressed tablets. The ANIs and StarCap were sieved through a #40 mesh, followed by blending with filler using DCM-5 for 10 minutes at 20 rpm, and then a 2–3-minute blending with lubricant in DCM-5 at 20 rpm. Tablet compression was conducted using a singlelayer tablet press. Bacomind tablets were compressed using 15.7 x 9.7 mm oval, plain, D-type, standard concave tooling keeping 600 mg core weight, whereas Garlic and Ashwagandha tablets were produced using 10 mm round, plain, D-type, standard concave tooling keeping 450 mg core weight. The weight of Bacomind tablets is on the higher side (600 mg) due to their higher concentration of Nutracore and StarCap, aimed at improving the DT of tablets. Evaluation of Powder Blend and Core Tablets - The physical properties of ANI and its formulations with Label Friendly Nutracore were assessed. Density was measured using an ETD-1020 density apparatus. Core tablet properties including weight variation, %LOD (Sartorius moisture analyzer MA-35), and crushing strength were determined using a Sotex Tablet Tester. Friability (up to 100 rotations) was evaluated using an Electrolab Friabilator (EF-2), and tablet disintegration in water was tested with a disintegration tester (ED-2l, Electrolab). Film Coating of Tablets - Core tablets, were all coated with Opadry amb II at 3% weight gain with 20% w/w solids in water. The tablet coating process took place in a 10.5-inch perforated coating pan (O’HARA Labcoat™ M5), using the parameters shown in Table 1. Stability Testing - Coated tablets were packaged in 50 CC HDPE bottles with desiccant (SILICAGEL Can, Colorcon), sealed, and screw-capped, then subjected to stability for 1, 3, and 6 months at storage conditions of 30°C/65% RH and 40°C/75% RH. Coated tablets were evaluated for physical appearance, loss on drying (LOD), and disintegration time at predetermined intervals of stability study.

Results: Testing of Physical Properties of Powder Blend - There was a significant improvement in the flow properties of powder blends of all three ANIs compared to respective individual powder forms (Table 1). Testing of Physical Properties of Core and Coated Tablets - On the rotary tablet press, the powder blend of all three nutraceutical formulations demonstrated excellent flow, resulting in core tablets with consistent weight, thickness, desired hardness (9-11kP), and low friability (0.2%). The coated tablets exhibit a smooth appearance (Figure 1). There was no significant difference in the LOD values between core and coated tablets. Both core and coated tablets showed disintegration times of less than 40 minutes (Table 1). Stability Testing - At 1-month stability study, the coated tablets exhibited smooth appearance. The disintegration times were 30-35 minutes for Bacomind tablets, 18-24 minutes for Garlic tablets, and 31-41 minutes for Ashwagandha tablets. There was no change in hardness of the coated tablets from initial to 1 month time point. The above findings indicate that, exposure of coated tablet formulations of all three ANI’s to storage conditions did not show significant differences in physical properties, including LOD, Hardness, Friability, and Disintegration time.

Conclusion: Three ANIs with poor flow and compressibility when blended with Nutracore demonstrated significant improvement in these properties and robust tablets with desired hardness and disintegration along with elegant appearance were achieved. It also helped retain formulation properties when exposed to stability condition indicating the benefit of scientific approach in selection of core component, film coating formulation and appropriate functional packaging.

References: 1. Salve J, Pate S, Debnath K, Langade D. Adaptogenic and Anxiolytic Effects of Ashwagandha Root Extract in Healthy Adults: A Double-blind, Randomized, Placebo-controlled Clinical Study. Cureus. 2019;
2. Fatima U, Roy S, Ahmad S, Al-Keridis LA, Alshammari N, Adnan M, et al. Investigating neuroprotective roles of Bacopa monnieri extracts: Mechanistic insights and therapeutic implications. Biomedicine and Pharmacotherapy. 2022;153.
3. Johnson M, Olaleye O, Kolawole O. Antimicrobial and Antioxidant Properties of Aqueous Garlic (Allium sativum) Extract against Staphylococcus aureus and Pseudomonas aeruginosa. Br Microbiol Res J. 2016;14(1).


Table 1: Coating Process Parameters


Table 2: Physical Properties of Powders and Compressed Tablets


Figure 1: Photographs of Ashwagandha, Garlic and Bacomind Tablets coated with Opadry amb II