title: Development of a mini-tablet of co-grinded prednisone-Neusilin complex for pediatric use.
abstract: The purpose of this study is to enhance the dissolution rate of prednisone by co-grinding with Neusilin to form a complex that can be incorporated into a mini-tablet formulation for pediatrics. Prednisone-Neusilin complex was co-grinded at various ratios (1:1, 1:3, 1:5, and 1:7). The physicochemical properties of the complex were characterized by various analytical techniques including: differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), scanning electron microscope (SEM), particle size, surface area, solubility, and dissolution rate. The co-grinded prednisone-Neusilin complex (1:7) was blended with other excipients and was formulated into a 2-mm diameter mini-tablet. The mini-tablets were further evaluated for thickness, weight, content uniformity, and dissolution rate. To improve taste masking and stability, mini-tablets were coated by dip coating with Eudragit® EPO solution. DSC and XRPD results showed that prednisone was transformed from crystalline state into amorphous state after co-grinding with Neusilin. Particle size, surface area, and SEM results confirmed that prednisone was adsorbed to Neusilin's surface. Co-grinded prednisone-Neusilin complex (1:7) had a solubility of 0.24 mg/mL and 90% dissolved within 20 min as compared to crystalline prednisone which had a solubility of 0.117 mg/mL and 30% dissolved within 20 min. The mini-tablets containing co-grinded prednisone-Neusilin complex (1:7) exhibited acceptable physicochemical and mechanical properties including dissolution rate enhancement. These mini-tablets were successfully dip coated in Eudragit® EPO solution to mask the taste of the drug during swallowing. This work illustrates the potential use of co-grinded prednisone-Neusilin to enhance solubility and dissolution rate as well as incorporation into a mini-tablet formulation for pediatric use.
authors.affiliation: Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, Tennessee 38163, USA.
authors.forename: H
authors.initials: H
authors.lastname: Lou
authors.forename: M
authors.initials: M
authors.lastname: Liu
authors.forename: L
authors.initials: L
authors.lastname: Wang
authors.forename: S R
authors.initials: SR
authors.lastname: Mishra
authors.forename: W
authors.initials: W
authors.lastname: Qu
authors.forename: J
authors.initials: J
authors.lastname: Johnson
authors.forename: E
authors.initials: E
authors.lastname: Brunson
authors.forename: H
authors.initials: H
authors.lastname: Almoazen
mesh_terms: D017607:Aluminum Compounds / Q000008:administration & dosage / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D002648:Child; D006801:Humans; D017616:Magnesium Compounds / Q000008:administration & dosage / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D010372:Pediatrics; D033362:Powder Diffraction; D011241:Prednisone / Q000008:administration & dosage / Q000737:chemistry*; D017640:Silicates / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D013607:Tablets
chemical_list: D017607:Aluminum Compounds; D017616:Magnesium Compounds; D017640:Silicates; D013607:Tablets; C033065:aluminum magnesium silicate; D011241:Prednisone