Publications by authors named "Pingming Tang"

Crisugabalin (HSK16149), a novel VGCC α2δ ligand, has been approved for the treatment of adult diabetic peripheral neuropathic pain (DPNP) and postherpetic neuralgia (PHN). In this study, an LC-MS/MS method was developed for the determination of crisugabalin in rat plasma and tissues homogenate. Samples were extracted by protein precipitation and separated on a Hypersil GOLD aQ column with methanol and 2 mM ammonium acetate in water containing 0.

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Article Synopsis
  • Ciprofol (HSK3486) is a new intravenous drug for general anesthesia, mainly metabolized in humans through glucuronidation and producing various metabolites.
  • The study identified three key hydroxylated metabolites formed in human liver microsomes, primarily by the enzyme CYP2B6, highlighting their individual clearance rates and metabolic pathways.
  • Understanding these metabolic processes is crucial for assessing drug interactions and genetic factors affecting the effectiveness of HSK3486, with a significant role played by glucuronidation by UGT1A9.
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Kappa opioid receptor (KOR) agonists have been promising therapeutic candidates, owing to their potential for relieving pain and treating intractable pruritus. Although lacking morphine-like central nervous system (CNS) effects, KOR agonists do elicit sedation, dysphoria and diuresis which seriously impede their development. Peripherally-restricted KOR agonists have a poor ability to penetrate into the CNS system, so that CNS-related adverse effects can be ameliorated or even abolished.

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In the present work, a novel series of trifluoromethyl-substituted tetrahydropyran derivatives were rationally designed and synthesized as potent DPP-4 inhibitors with significantly improved duration time of action over current commercially available DPP-4 inhibitors. The incorporation of the trifluoromethyl group on the 6-position of the tetrahydropyran ring of omarigliptin with the configuration of (2,3,5,6) not only significantly improves the overall pharmacokinetic profiles in mice but also maintains comparable DPP-4 inhibition activities. Further preclinical development of compound exhibited its extraordinary efficacy and good safety profile.

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Article Synopsis
  • Phosphonamidate 3a, derived from methoxymethylphosphonic acid, shows promise as a delivery method for the drug propofol and other phenolic substances.
  • The study focused on synthesizing and assessing MMPA-based phosphonamidates, demonstrating their effectiveness in transporting various phenolic drugs.
  • In tests with beagle dogs, the oral bioavailability of compound 3a was measured at a high 97.6%, indicating it could be an efficient method for drug delivery.
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Andrographis paniculata (AP) has been widely used in Asian countries to treat many kinds of diseases for several decades. Hutchison Medipharma Ltd. developed an aqueous ethanol extract of A.

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A novel, rapid and sensitive liquid chromatography/quadrupole linear ion trap mass spectrometry [LC-ESI-(QqLIT)MS/MS] method was developed and validated for the quantification of protopanaxadiol (PPD) in rat plasma. Oleanolic acid (OA) was used as internal standard (IS). A simple protein precipitation based on acetonitrile (ACN) was employed.

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