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Solubility of Pharmaceutical Ingredients in Natural Edible Oils.
Mol Pharm. 2020 Jul 06; 17(7):2499-2507.MP

Abstract

Natural edible oils (NEOs) are common excipients for lipid-based formulations. Many of them are complex mixtures comprising hundreds of different triglycerides (TGs). One major challenge in developing lipid-based formulations is the variety in NEO compositions affecting the solubility of active pharmaceutical ingredients. In this work, solubilities of indomethacin (IND), ibuprofen (IBU), and fenofibrate (FFB) in soybean oil and in coconut oil were measured via differential scanning calorimetry, high-performance liquid chromatography, and Raman spectroscopy. Furthermore, this work proposes an approach that mimics NEOs using one key TG and models the API solubilities in these NEOs based on perturbed-chain statistical associating fluid theory (PC-SAFT). Key TGs were determined using the 1,2,3-random hypothesis, and PC-SAFT parameters were estimated via a group-contribution method. Using the proposed approach, the solubility of IBU and FFB was modeled in soybean oil and coconut oil. Furthermore, the solubilities of five more APIs (IND, cinnarizine, naproxen, griseofulvin, and felodipine) were modeled in soybean oil. All modeling results were found in very good agreement with the experimental data. The influence of different NEO kinds on API solubility was examined by comparing FFB and IBU solubilities in soybean oil and refined coconut oil. PC-SAFT was thus found to allow assessing the batch-to-batch consistency of NEO batches in silico.

Authors+Show Affiliations

Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Str. 70, D-44227 Dortmund, Germany.Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Str. 70, D-44227 Dortmund, Germany.Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Str. 70, D-44227 Dortmund, Germany.Laboratory of Thermodynamics, TU Dortmund University, Emil-Figge-Str. 70, D-44227 Dortmund, Germany.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32369379

Citation

Brinkmann, Joscha, et al. "Solubility of Pharmaceutical Ingredients in Natural Edible Oils." Molecular Pharmaceutics, vol. 17, no. 7, 2020, pp. 2499-2507.
Brinkmann J, Rest F, Luebbert C, et al. Solubility of Pharmaceutical Ingredients in Natural Edible Oils. Mol Pharm. 2020;17(7):2499-2507.
Brinkmann, J., Rest, F., Luebbert, C., & Sadowski, G. (2020). Solubility of Pharmaceutical Ingredients in Natural Edible Oils. Molecular Pharmaceutics, 17(7), 2499-2507. https://doi.org/10.1021/acs.molpharmaceut.0c00215
Brinkmann J, et al. Solubility of Pharmaceutical Ingredients in Natural Edible Oils. Mol Pharm. 2020 Jul 6;17(7):2499-2507. PubMed PMID: 32369379.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solubility of Pharmaceutical Ingredients in Natural Edible Oils. AU - Brinkmann,Joscha, AU - Rest,Frauke, AU - Luebbert,Christian, AU - Sadowski,Gabriele, Y1 - 2020/05/15/ PY - 2020/5/6/pubmed PY - 2020/5/6/medline PY - 2020/5/6/entrez KW - PC-SAFT KW - lipid-based drug delivery systems KW - oils KW - solubility SP - 2499 EP - 2507 JF - Molecular pharmaceutics JO - Mol. Pharm. VL - 17 IS - 7 N2 - Natural edible oils (NEOs) are common excipients for lipid-based formulations. Many of them are complex mixtures comprising hundreds of different triglycerides (TGs). One major challenge in developing lipid-based formulations is the variety in NEO compositions affecting the solubility of active pharmaceutical ingredients. In this work, solubilities of indomethacin (IND), ibuprofen (IBU), and fenofibrate (FFB) in soybean oil and in coconut oil were measured via differential scanning calorimetry, high-performance liquid chromatography, and Raman spectroscopy. Furthermore, this work proposes an approach that mimics NEOs using one key TG and models the API solubilities in these NEOs based on perturbed-chain statistical associating fluid theory (PC-SAFT). Key TGs were determined using the 1,2,3-random hypothesis, and PC-SAFT parameters were estimated via a group-contribution method. Using the proposed approach, the solubility of IBU and FFB was modeled in soybean oil and coconut oil. Furthermore, the solubilities of five more APIs (IND, cinnarizine, naproxen, griseofulvin, and felodipine) were modeled in soybean oil. All modeling results were found in very good agreement with the experimental data. The influence of different NEO kinds on API solubility was examined by comparing FFB and IBU solubilities in soybean oil and refined coconut oil. PC-SAFT was thus found to allow assessing the batch-to-batch consistency of NEO batches in silico. SN - 1543-8392 UR - https://www.unboundmedicine.com/medline/citation/32369379/Solubility_of_Pharmaceutical_Ingredients_in_Natural_Edible_Oils L2 - https://doi.org/10.1021/acs.molpharmaceut.0c00215 DB - PRIME DP - Unbound Medicine ER -
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