A Comparison of the Solubility of Danazol in Human and Simulated Gastrointestinal Fluids

In: Pharmaceutical Research · 2000 · vol. 17(7) , pp. 891–894 · doi:10.1023/a:1007576713216 · PMID:10990211 · W25021539
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This study characterized the solubility of danazol in human gastrointestinal fluids and compared it to solubility in simulated fluids.

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This paper compared the solubility of danazol when exposed to human gastrointestinal fluids versus simulated gastrointestinal fluids, using dissolution/solubility testing in different media representative of the stomach and intestine. The key finding was that danazol solubility differed depending on whether human or simulated fluids were used, indicating that simulation media do not fully replicate the solubilizing properties of actual human GI fluids. A major limitation is that results are specific to danazol and to the particular fluid compositions and simulation approaches employed, so generalization to other drugs or GI conditions may be limited. The paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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REFERENCES A. Lindahl, A. L. Ungell, L. Knutson, and H. Lennernäs. Characterization of fluids from the stomach and proximal jejunum in men and women. Pharm. Res. 14:497–502 (1997). B. L. Pedersen, H. BrØ ndsted, H. Lennernäs, F. N. Christensen, A. Müllertz, and H. G. Kristensen. Dissolution of hydrocortisone in human and simulated intestinal fluids. Pharm. Res. 17:183–189 (2000). H. Tomida, T. Yotsuyanagi, and K. Ikeda. Solubilization of Steroid Hormones by Polyoxyethylene Lauryl Ether. Chem. Pharm. Bull. 26:2832–2837 (1978). V. Bakatselou, R. C. Oppenheim, and J. B. Dressman. Solubilization and wetting effects of bile salts on the dissolution of steroids. Pharm. Res. 8:1461–1469 (1991). L. J. Naylor, V. Bakatselou, N. Rodriguez Hornedo, N. D. Weiner, and J. B. Dressman. Dissolution of steroids in bile salt solutions is modified by the presence of lecithin. Eur. J. Pharm. Biopharm. 41:346–353 (1995). T. Schersten. Formation of lithogenic bile in man. Digestion 9:540–553 (1973). N. Robinson. Review article: Lysolecithin. J. Pharm. Pharmacol. 13:321–354 (1961). K. Larsson. On phospholipids and hydrophobicity of the gastric wall. J. Disp. Sci. Tech. 15:353–357 (1994). M. Efentakis and J. B. Dressman. Gastric juice as a dissolution medium: Surface tension and pH. Eur. J. Drug Metab. Pharmacokinet. 23:97–102 (1998). J. B. Dressman, R. R. Berardi, L. C. Dermentzoglou, T. L. Russell, S. P. Schmaltz, J. L. Barnett, and K. M. Jarvenpaa. Upper gastroin-testinal (GI) pH in young, healthy men and women. Pharm. Res. 7:756–761 (1990). P. Finholt, H. Gundersen, A. Smit, and H. Petersen. Surface tension of human gastric juice. Medd. Nor. Farm. Selsk. 41:1–14 (1978). J. B. Dressman, G. L. Amidon, C. Reppas, and V. P. Shah. Dissolution testing as a prognostic tool for oral drug absorption: immediate release dosage forms. Pharm. Res. 15:11–22 (1998). FIP Guidelines for Dissolution Testing of Solid Oral Products. Dissolution Technologies 4:5–14 (1997). J. R. Crison, N. D. Weiner, and G. L. Amidon. Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. J. Pharm. Sci. 86:384–388 (1997). Author information Authors and Affiliations Rights and permissions About this article Cite this article Pedersen, B.L., Müllertz, A., Brøndsted, H. et al. A Comparison of the Solubility of Danazol in Human and Simulated Gastrointestinal Fluids. Pharm Res 17, 891–894 (2000). https://doi.org/10.1023/A:1007576713216 Issue date: DOI: https://doi.org/10.1023/A:1007576713216

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