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Published on: September 24, 2020
Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle
Yonggang Wei1, Guanpeng Qiu1, Bailin Lei1
1Haisco Pharmaceuticals Group Co. Ltd. , 136 Baili Road, Wenjiang District, Chengdu, 611130, China.
Abstract:
Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (1) and l-alanine ethyl ester was found to be an efficient scaffold for the oral delivery of compound 1. The synthesis and evaluation of MMPA based phosphonamidates of compound 1, HSK3486 (2), and other phenolic drugs revealed the general application of MMPA as the effective delivery vehicle for phenolic drugs. On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97.6% and 34.1%, respectively.
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