Simultaneous determination of lappaconitine hydrobromide and isopropiram fumarate in rabbit plasma by capillary electrophoresis with electrochemiluminescence detection

Q3 · BIOLOGY

Article

Author: Wang, Shulun ; Zhou, Min ; Liu, Caiyun ; Mi, Juan ; Li, Yujie ; Ma, Yongjun

A CE electrochemiluminescence (CE–ECL) method for simultaneous determination of lappaconitine hydrobromide (LH) and isopropiram fumarate (IF) has been first established, with a chemically modified platinum electrode by europium (III)‐doped Prussian blue analogue film as a working electrode. The conditions for CE separation and ECL detection are discussed and optimized in detail. It has been proved that 20 mmol/L phosphate buffer (pH 8.5) containing 5% (v/v) ACN and 0.17 mol/L SDS could achieve the most favorable resolution, and the high sensitivity of detection was obtained by maintaining the detection potential at 1.23 V. Under optimized conditions, a baseline separation for the two analytes was achieved within 6 min, and the standard curves were linear in the range of 1.0×10−7 ∼ 5.0 × 10−5 g/mL for LH and 4.0 × 10−8 ∼ 1.0 × 10−5 g/mL for IF with the detection limits (3σ) of 6.6 × 10−8 g/mL for LH and 3.7 × 10−8 g/mL for IF, respectively. The precisions of intra‐ and interday measurements for LH and IF were less than 4.21 and 2.61%, respectively. The applicability of the proposed method was illustrated in the determination of LH and IF in rabbit plasma with recoveries between 95.6 and 103.0%.

Arzneimittel-Forschung

2-(Acylamino)pyridine derivatives with morphine agonistic and morphine antagonistic properties

Author: Wollweber, H. ; Schlichting, U. ; Hoffmeister, F. ; Niemers, E. ; Hiltmann, R.

Eighty-one (acylamino)pyridines (I, R = H, 3-, 5-, or 6-Me, or 4-Ph; R1 = Et, H, Me, Pr, Ph, or cyclohexyl, Z = CH2CH2, CHEtCH2, CHMeCH2, CMe2CH2, CHMeCHMe, CH2CHMe, or CH2CMe2; NR2R3 = e.g. NMe2, NEt2, NMeCH2Ph, piperidino, 1-pyrrolidinyl, 1-azepinyl, or morpholino) were prepared by acylation of II.II were obtained either by reaction of 2-bromopyridines with H2NZR2R3 or of 2-aminopyridines with XZNR2R3 (X = Cl or Br).I were tested for morphine antagonistic and morphine agonistic properties.The most active compound was the fumarate of propiram (I, R = H, R1 = Et, Z = CHMeCH2, NR2R3 = piperidino).Also I with NR2R3 = azabicyclos had high analgesic potency with a favorable therapeutic index.Some I showed distinct morphine agonistic but no morphine antagonistic effects.

European Journal of Medicinal Chemistry

Stereochemical studies on drugs. Part 11. Conformation of alkylated 2-acylaminopyridines and their relation with morphine structure

Author: Wollweber, Hartmund ; Geiger, Walter

The conformations of (R,S)-propiram [(±)-I; R = Me, R¹ = R² = R³ = R⁴ = H] [15686-91-6] and 8 analogs I(R and R¹ and R² and R³ and R⁴ = H or Me) and (±)-II [24606-50-6], as well as some enantiomers of I and II, were investigated spectroscopically.The synthesis of some of the compounds is described.Active analgesics are only found among the E-forms of the amides, in which the methylene group of the propionyl substituent hangs over the pyridine ring, which itself stands vertical with respect to the planar amide group.The R-enantiomer of propiram R-I (R = Me, R¹ = R² = R³ = R⁴ = H) [16571-86-1] is morphine-agonistic and corresponds to N-methylmorphinan in its spatial arrangement.

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Indication	Country/Location	Organization	Date
Burns	China	Grand Pharmaceutical (China) Co., Ltd.	-
Neuralgia	China	Grand Pharmaceutical (China) Co., Ltd.	-
Pain, Postoperative	China	Grand Pharmaceutical (China) Co., Ltd.	-

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