Development of a mini-tablet of co-grinded prednisone-neusilin complex for pediatric use

H. Lou, M. Liu, L. Wang, S. R. Mishra, W. Qu, J. Johnson, E. Brunson, Hassan Almoazen

Research output: Contribution to journalArticle

11 Citations (Scopus)

Abstract

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.

Original languageEnglish (US)
Pages (from-to)950-958
Number of pages9
JournalAAPS PharmSciTech
Volume14
Issue number3
DOIs
StatePublished - Sep 1 2013

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prednisone
Prednisone
Tablets
Pediatrics
Solubility
solubility
Powder Diffraction
Differential Scanning Calorimetry
grinding
differential scanning calorimetry
scanning electron microscopes
Particle Size
X-Ray Diffraction
particle size
surface area
powders
physicochemical properties
X-radiation
Electrons
Excipients

All Science Journal Classification (ASJC) codes

  • Agronomy and Crop Science
  • Pharmaceutical Science
  • Drug Discovery

Cite this

Development of a mini-tablet of co-grinded prednisone-neusilin complex for pediatric use. / Lou, H.; Liu, M.; Wang, L.; Mishra, S. R.; Qu, W.; Johnson, J.; Brunson, E.; Almoazen, Hassan.

In: AAPS PharmSciTech, Vol. 14, No. 3, 01.09.2013, p. 950-958.

Research output: Contribution to journalArticle

Lou, H, Liu, M, Wang, L, Mishra, SR, Qu, W, Johnson, J, Brunson, E & Almoazen, H 2013, 'Development of a mini-tablet of co-grinded prednisone-neusilin complex for pediatric use', AAPS PharmSciTech, vol. 14, no. 3, pp. 950-958. https://doi.org/10.1208/s12249-013-9981-x
Lou, H. ; Liu, M. ; Wang, L. ; Mishra, S. R. ; Qu, W. ; Johnson, J. ; Brunson, E. ; Almoazen, Hassan. / Development of a mini-tablet of co-grinded prednisone-neusilin complex for pediatric use. In: AAPS PharmSciTech. 2013 ; Vol. 14, No. 3. pp. 950-958.
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