Sublimation of Drugs from the Site of Application of Topical Products.

Autor:	S G P; Institute for Drug Delivery and Biomedical Research, Bangalore, Karnataka560086, India., Echanur AV; Institute for Drug Delivery and Biomedical Research, Bangalore, Karnataka560086, India., Matadh AV; Institute for Drug Delivery and Biomedical Research, Bangalore, Karnataka560086, India., Rangappa S; Topical Products Testing LLC, Oxford, Mississippi38655, United States., H N S; Institute for Drug Delivery and Biomedical Research, Bangalore, Karnataka560086, India.; KLE College of Pharmacy, Bangalore, Karnataka560010, India., Murthy RN; Topical Products Testing LLC, Oxford, Mississippi38655, United States., V S R; Surgiderma Hospital, Bangalore, Karnataka560043, India., Ureña-Benavides EE; Department of Biomedical Engineering and Chemical Engineering, The University of Texas at San Antonio, San Antonio, Texas78249, United States., Maibach H; Department of Dermatology, University of California, San Francisco, California94115, United States., Murthy SN; Institute for Drug Delivery and Biomedical Research, Bangalore, Karnataka560086, India.; Topical Products Testing LLC, Oxford, Mississippi38655, United States.
Jazyk:	angličtina
Zdroj:	Molecular pharmaceutics [Mol Pharm] 2023 Jun 05; Vol. 20 (6), pp. 2814-2821. Date of Electronic Publication: 2023 Jan 10.
DOI:	10.1021/acs.molpharmaceut.2c00816
Abstrakt:	The objective of the project was to investigate the plausibility of active pharmaceutical ingredients (APIs) to undergo sublimation from topical application following evaporation of solvent. Topical formulations with different APIs were subjected to a sublimation screening test. The APIs in the selected topical products were found to undergo sublimation to a different extent. The salicylic acid topical product was found to undergo a significant loss due to sublimation. The extent of sublimation of salicylic acid was significantly greater at skin temperature compared to room temperature. When the APIs were subjected to the sublimation screening test in their neat form at 32 ± 1 °C, the natural log of the rate of sublimation decreased linearly with the standard enthalpy of sublimation of compound ( R 2 = 0.89). The formulation composition was found to have a significant impact on the extent of sublimation of the representative API, salicylic acid. The sublimation of APIs from the topical product was found to affect the mass balance studies in the case of the salicylic acid ointment. Furthermore, the results of the human studies agreed with the in vitro experimental results demonstrating the plausibility of loss of API due to sublimation from the site of application.
Databáze:	MEDLINE
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