Solubility and dissolution rate enhancement of ibuprofen by co-milling with polymeric excipients

Hussain, Amjad; Smith, Geoff; Khan, K. A.; Bukhari, Nadeem Irfan; Pedge, Nicholas I.; Ermolina, I.

doi:10.1016/j.ejps.2018.08.001

Cited by 45 publications

(27 citation statements)

References 34 publications

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“… Typically, amorphous solid dispersions result in a supersaturated solution of the poorly water‐soluble drugs during the dissolution process both in vitro and in vivo , which enhances oral bioavailability . The degree of supersaturation and maintenance of the supersaturated state are dependent on the polymer‐drug interaction (their miscibility) and the ability of the polymer to inhibit the crystallization of drugs . To date, however, selection of an appropriate polymer for the preparation of an amorphous solid dispersion on the basis of structure–activity relationships remains challenging, and the optimal polymer‐to‐drug ratio continues to be determined using empirical data …”

Section: Dissolution Data For Pure Cilostazol and Solid Dispersions Omentioning

confidence: 99%

“…[12][13][14] Typically, amorphous solid dispersions result in a supersaturated solution of the poorly watersoluble drugs during the dissolution process both in vitro and in vivo, which enhances oral bioavailability. [18][19][20][21] To date, however, selection of an appropriate polymer for the preparation of an amorphous solid dispersion on the basis of structure-activity relationships remains challenging, and the optimal polymer-to-drug ratio continues to be determined using empirical data. [18][19][20][21] To date, however, selection of an appropriate polymer for the preparation of an amorphous solid dispersion on the basis of structure-activity relationships remains challenging, and the optimal polymer-to-drug ratio continues to be determined using empirical data.…”

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confidence: 99%

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Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Lee

et al. 2019

Bulletin Korean Chem Soc

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Section: Dissolution Data For Pure Cilostazol and Solid Dispersions Omentioning

confidence: 99%

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confidence: 99%

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Lee

et al. 2019

Bulletin Korean Chem Soc

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“…Although nowadays state of the art mechnanochemical methods such as hot-melt extrusion are exploited for their ability to enhance drug release in conjunction with polymers, there are only a few reports for their application to progesterone, e.g., reservoir systems of progesterone loaded into polymeric matrix for controlled release [5]. Mechano-chemical activation is often applied by dry or wet milling and is used to enhance the solubility and dissolution rate of poorly soluble drugs [3,6]. This is usually applied by co-milling drug with excipients and is commonly used for particle size reduction.…”

Section: Introductionmentioning

confidence: 99%

Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling

et al. 2020

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The aim of this contribution was to evaluate the impact of processing methods and polymeric carriers on the physicochemical properties of solid dispersions of the poorly soluble drug progesterone (PG). Five polymers: hydroxypropyl methylcellulose (HPMC), hydroxypropyl methylcellulose acetate succinate (HPMCAS), microcrystalline cellulose (MCC), polyvinylpyrrolidone (PVP) and silica (SiO2), and two processing methods: solvent evaporation (SE) and mechano-chemical activation by co-milling (BM) were applied. H-bonding was demonstrated by FTIR spectra as clear shifting of drug peaks at 1707 cm−1 (C20 carbonyl) and 1668 cm−1 (C3 carbonyl). Additionally, spectroscopic and thermal analysis revealed the presence of unstable PG II polymorphic form and a second heating DSC cycle, the presence of another polymorph possibly assigned to form III, but their influence on drug solubility was not apparent. Except for PG–MCC, solid dispersions improved drug solubility compared to physical mixtures. For SE dispersions, an inverse relationship was found between drug water solubility and drug–polymer Hansen solubility parameter difference (Δδt), whereas for BM dispersions, the solubility was influenced by both the intermolecular interactions and the polymer Tg. Solubility improvement with SE was demonstrated for all except PG–MCC dispersions, whereas improvement with BM was demonstrated by the PG–HPMC, PG–PVP and PG–HPMCAS dispersions, the last showing impressive increase from 34.21 to 82.13 μg/mL. The extensive H-bonding between PG and HPMCAS was proved by FTIR analysis of the dispersion in the liquid state. In conclusion, although SE improved drug solubility, BM gave more than twice greater improvement. This indicates that directly operating intermolecular forces are more efficient than the solvent mediated.

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“…This can hamper its oral bioavailability and onset of action. Several approached have been employed to increase IB water solubility and oral bioavailability, such as solid dispersion [3], size reduction [4], copolymer [5], and surfactant [6]. Inclusion complex, especially using cyclodextrin (CD), has been widely used to increase the water solubility of poorly water-soluble drugs as well as enhance bioavailability [7].…”

Section: Introductionmentioning

confidence: 99%

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

Purnamasari

Saputra

2020

Int J App Pharm

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Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet). Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result. Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45). Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.

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Solubility and dissolution rate enhancement of ibuprofen by co-milling with polymeric excipients

Cited by 45 publications

References 34 publications

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Solubility Improvement of Progesterone from Solid Dispersions Prepared by Solvent Evaporation and Co-milling

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

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