COMPARATIVE OPEN-LABEL BIOEQUIVALENCE TRIAL OF VITAMIN D3 60 K FORMULATIONS: ULTRA NANO VS. NANO SOLUTION AND CONVENTIONAL FORMULATION

Prof. Dr. D. Gokul Raj MBBS MS (Ortho) FIGOF(Germany) Arthroplasty fellowship USA, *Dr. Anish Desai and Dr. Manish R. Garg

ABSTRACT

Background: Vitamin D supplementation plays a significant role in addressing vitamin D deficiency/ insufficiency. Various conventional and nanoformulations of 60k Vitamin D3 are available in the market to cater to this requirement. The ultra nano oral solution formulated with patented En-Infi™ nanotechnology comes with ultra nano vitamin D3 particles. The main objective of this study was to determine the bioequivalence of ultra nano oral solution (test formulation) with nano solution and conventional capsule (reference formulation - R1, R2, respectively). Method: This was an open-label, balanced, randomized, single-dose, three-treatment, single-period, parallel bioequivalence study of test formulation with reference formulations R1 and R2. Subjects (n=30) were supplemented with a single dose of one of these formulations. Their blood sample was assessed for the maximum observed drug concentration (Cmax), the area under the concentration-time curve up to 144 h (AUC0–144h), and the time to reach maximum drug concentration (Tmax) for the metabolite 25-HydroxyvitaminD3 [25(OH)D3]. Result: Among the 30 participants, the Cmax of serum 25(OH) D from the test formulation was higher than that of R2 by 14.94%. The area under the concentration-time curve up to 144 h (AUC0-144h) of serum 25(OH)D3 from the test formulation was higher than that of R2 by 20.52%. The Cmax and AUC0-144h of serum 25(OH)D3 levels from the test formulation were comparable to that of R1. Thus, the test formulation is bioequivalent to R1 and shows a trend of superiority over R2. Tmax of 25(OH)D3 was found to be 8.3602 hr, 6.4674 hr, and 7.3419 hr for test formulation, R1, and R2 respectively. The test formulation was safe and well tolerated, as no adverse events were reported. Conclusion: The test formulation, formulated with En-Infi™ nanotechnology, exhibited higher Cmax and AUC0-144h compared to the R2, and showed bioequivalence to the R1, and was well tolerated. These elevated metabolite levels (serum 25(OH)D) are likely attributed to the superior rate and extent of absorption of vitamin D3 from the test compared to R2. The comparable data confirms the advantages of En-Infi™ nanotechnology and underscores the benefits of ultra-nanoparticles utilized in the test formulation.

Keywords: Cholecalciferol; vitamins; vitamin D deficiency; Administration, Oral; Area Under Curve; Healthy Volunteers.