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Formulation studies on ibuprofen sodium-cationic dextran conjugate: effect on tableting and dissolution characteristics of ibuprofen.
Drug Dev Ind Pharm. 2016 Jan; 42(1):39-59.DD

Abstract

The effect of electrostatic interaction between ibuprofen sodium (IbS) and cationic diethylaminoethyl dextran (Ddex), on the tableting properties and ibuprofen release from the conjugate tablet was investigated. Ibuprofen exhibits poor flow, compaction (tableting) and dissolution behavior due to its hydrophobic structure, high cohesive, adhesive and viscoelastic properties therefore it was granulated with cationic Ddex to improve its compression and dissolution characteristics. Electrostatic interaction and hydrogen bonding between IbS and Ddex was confirmed with FT-IR and DSC results showed a stepwise endothermic solid-solid structural transformation from racemic to anhydrous forms between 120 and 175 °C which melted into liquid form at 208.15 °C. The broad and diffused DSC peaks of the conjugate granules as well as the disappearance of ibuprofen melting peak provided evidence for their highly amorphous state. It was evident that Ddex improved the flowability and densification of the granules and increased the mechanical and tensile strengths of the resulting tablets as the tensile strength increased from 0.67 ± 0.0172 to 1.90 ± 0.0038 MPa with increasing Ddex concentration. Both tapping and compression processes showed that the most prominent mechanism of densification were particle slippage, rearrangement and plastic deformation while fragmentation was minimized. Ddex retarded the extent of dissolution in general, indicating potentials for controlled release formulations. Multiple release mechanisms including diffusion; anomalous transport and super case II transport were noted. It was concluded that interaction between ibuprofen sodium and Ddex produced a novel formulation with improved flowability, tableting and dissolution characteristics with potential controlled drug release characteristics dictated by Ddex concentration.

Authors+Show Affiliations

a Leicester School of Pharmacy, De Montfort University , The Gateway , Leicester , United Kingdom.a Leicester School of Pharmacy, De Montfort University , The Gateway , Leicester , United Kingdom.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25826253

Citation

Abioye, Amos Olusegun, and Adeola Kola-Mustapha. "Formulation Studies On Ibuprofen Sodium-cationic Dextran Conjugate: Effect On Tableting and Dissolution Characteristics of Ibuprofen." Drug Development and Industrial Pharmacy, vol. 42, no. 1, 2016, pp. 39-59.
Abioye AO, Kola-Mustapha A. Formulation studies on ibuprofen sodium-cationic dextran conjugate: effect on tableting and dissolution characteristics of ibuprofen. Drug Dev Ind Pharm. 2016;42(1):39-59.
Abioye, A. O., & Kola-Mustapha, A. (2016). Formulation studies on ibuprofen sodium-cationic dextran conjugate: effect on tableting and dissolution characteristics of ibuprofen. Drug Development and Industrial Pharmacy, 42(1), 39-59.
Abioye AO, Kola-Mustapha A. Formulation Studies On Ibuprofen Sodium-cationic Dextran Conjugate: Effect On Tableting and Dissolution Characteristics of Ibuprofen. Drug Dev Ind Pharm. 2016;42(1):39-59. PubMed PMID: 25826253.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation studies on ibuprofen sodium-cationic dextran conjugate: effect on tableting and dissolution characteristics of ibuprofen. AU - Abioye,Amos Olusegun, AU - Kola-Mustapha,Adeola, Y1 - 2015/03/31/ PY - 2015/4/1/pubmed PY - 2017/3/31/medline PY - 2015/4/1/entrez KW - Granulation KW - ibuprofen–Ddex conjugate KW - inter-particulate bonding KW - mechanism of compaction KW - mechanism of release SP - 39 EP - 59 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 42 IS - 1 N2 - The effect of electrostatic interaction between ibuprofen sodium (IbS) and cationic diethylaminoethyl dextran (Ddex), on the tableting properties and ibuprofen release from the conjugate tablet was investigated. Ibuprofen exhibits poor flow, compaction (tableting) and dissolution behavior due to its hydrophobic structure, high cohesive, adhesive and viscoelastic properties therefore it was granulated with cationic Ddex to improve its compression and dissolution characteristics. Electrostatic interaction and hydrogen bonding between IbS and Ddex was confirmed with FT-IR and DSC results showed a stepwise endothermic solid-solid structural transformation from racemic to anhydrous forms between 120 and 175 °C which melted into liquid form at 208.15 °C. The broad and diffused DSC peaks of the conjugate granules as well as the disappearance of ibuprofen melting peak provided evidence for their highly amorphous state. It was evident that Ddex improved the flowability and densification of the granules and increased the mechanical and tensile strengths of the resulting tablets as the tensile strength increased from 0.67 ± 0.0172 to 1.90 ± 0.0038 MPa with increasing Ddex concentration. Both tapping and compression processes showed that the most prominent mechanism of densification were particle slippage, rearrangement and plastic deformation while fragmentation was minimized. Ddex retarded the extent of dissolution in general, indicating potentials for controlled release formulations. Multiple release mechanisms including diffusion; anomalous transport and super case II transport were noted. It was concluded that interaction between ibuprofen sodium and Ddex produced a novel formulation with improved flowability, tableting and dissolution characteristics with potential controlled drug release characteristics dictated by Ddex concentration. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/25826253/Formulation_studies_on_ibuprofen_sodium_cationic_dextran_conjugate:_effect_on_tableting_and_dissolution_characteristics_of_ibuprofen_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2015.1024684 DB - PRIME DP - Unbound Medicine ER -