Hot Melt Extrudates Formulated Using Design Space: One Simple Process for Both Palatability and Dissolution Rate Improvement

Malaquias, Lorena F.B.; Schulte, Heidi Luise; Chaker, Juliano Alexandre; Karan, Kapish; Dürig, Thomas; Marreto, Ricardo Neves; Gratieri, Taís; Gelfuso, Guilherme M.; Cunha-Filho, Marcílio

doi:10.1016/j.xphs.2017.08.014

Cited by 25 publications

(9 citation statements)

References 33 publications

(34 reference statements)

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“…Indeed, an important fraction of the new drug candidates emerging from drug discovery programs have poor water solubility. It is estimated that 75% of drug candidates and approximately 40% of currently marketed drugs are poorly water soluble [2,3]. This unsatisfactory physicochemical property of APIs leads to poor absorption and poor bioavailability and the need for high drug dosage to be administered, leading to increased side effects [4].…”

Section: Introductionmentioning

confidence: 99%

Physical formulation approaches for improving aqueous solubility and bioavailability of ellagic acid: A review

Nyamba

Lechanteur

Semdé

et al. 2021

European Journal of Pharmaceutics and Biopharmaceutics

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Section: Introductionmentioning

confidence: 99%

Physical formulation approaches for improving aqueous solubility and bioavailability of ellagic acid: A review

Nyamba

Lechanteur

Semdé

et al. 2021

European Journal of Pharmaceutics and Biopharmaceutics

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“…Intermediate precision was evaluated according to a complete factorial design 2 3 , in which the factors were the day of analysis, analyst, and chromatograph apparatus in triplicate using PPN solutions in the nominal concentration (Gui et al, 2020). Model validation was performed using analysis of variance (ANOVA) (Malaquias et al, 2018). All calculations were performed using Design‐Expert software version 11 (Stat‐Ease, Minneapolis, MN, USA).…”

Section: Methodsmentioning

confidence: 99%

Development of a reversed‐phase high‐performance liquid chromatographic method for the determination of propranolol in different skin layers

Cunha-Filho

Rocha

Duarte

et al. 2020

Biomedical Chromatography

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The aim of this work was to develop and validate an analytical method using HPLC for the determination of propranolol in the different layers of the skin to be used in kinetic studies of skin permeation. The development of the method was based on the suitability of the chromatogram, and the validation followed the international health regulation for bioanalytical methods. In addition, the method was tested in an in vitro permeation assay using porcine skin. The drug was determined using an RP‐C18 column at 30°C, a mobile phase comprising acidic aqueous phase:acetonitrile (75:25 v/v), at a flow rate of 1.0 mL min−1, and UV detection at 290 nm. The method was demonstrated to be selective against skin contaminants, linear in a wide range of concentrations (3–20 μg mL−1), sensitive enough to quantify less than 0.1% of the drug dosage in skin matrices, and precise regardless of analysis variations such as day of analysis, analyst, or equipment. In addition, the method presented a high drug extraction capacity greater than 90% for all skin layers (stratum corneum, hair follicle, and remaining skin). Finally, the method was successfully tested in skin permeation assays, proving its value in the development of topical formulations containing propranolol.

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“…A simplex centroid mixture design with three components without constraints was used in order to determine the ideal combination of excipients to improve CE properties ( Table 1 ) [ 14 ]. The responses obtained for the flowability, dispersibility, contact angle and dissolution rate were analyzed using the software Design Expert 8.0 (Stat-Ease, Minneapolis, MN, USA).…”

Section: Methodsmentioning

confidence: 99%

“…Meanwhile, the use of this technology surpasses the limitations of more traditional methods that also produce drug solid dispersions, such as lyophilization or spray-drying. Samples are rapidly processed by HME in a continuous single step without requiring the use of organic solvents, and production is easily scaled up [ 14 ].…”

Section: Introductionmentioning

confidence: 99%

Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

et al. 2018

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The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME were evaluated using morphologic, chromatographic, thermic, spectroscopic, and diffractometric assays. The flow, wettability, and dissolution rate of HME powders were also assessed. Both CE and its marker theobromine proved to be stable under heating according to thermal analysis and Arrhenius plot under isothermal conditions. Physicochemical analysis confirmed the stability of CE HME preparations and provided evidence of drug–polymer interactions. Improvements in the functional characteristics of CE were observed after the extrusion process, particularly in dissolution and flow properties. In addition, the use of a mixture design allowed the identification of synergic effects by excipient combination. The optimized combination of polymers obtained considering four different aspects showed that a mixture of the Soluplus, Plasdone S630, and Eudragit E in equal proportions produced the best results (flowability index 88%; contact angle 47°; dispersibility 7.5%; and dissolution efficiency 87%), therefore making the pharmaceutical use of CE more feasible.

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Hot Melt Extrudates Formulated Using Design Space: One Simple Process for Both Palatability and Dissolution Rate Improvement

Cited by 25 publications

References 33 publications

Physical formulation approaches for improving aqueous solubility and bioavailability of ellagic acid: A review

Physical formulation approaches for improving aqueous solubility and bioavailability of ellagic acid: A review

Development of a reversed‐phase high‐performance liquid chromatographic method for the determination of propranolol in different skin layers

Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

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