Development of a formulation of Pirodavir using 2-hydroxypropyl-β-cyclodextrin

被引：0
|
作者：
Jef Peeters
Peter Neeskens
Marcus Eli Brewster
机构：
[1] Johnson and Johnson,
[2] Chemical and Pharmaceutical Research,undefined
[3] Pharmaceutical Sciences,undefined
来源：
Journal of Inclusion Phenomena and Macrocyclic Chemistry | 2007年 / 57卷
关键词：
Pirodavir; Solubility; Cyclodextrins; Complexation capacity; Nasal formulation;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
Pirodavir, 4-[2-[1-(6-Methyl-3-pyridazinyl)-4-piperidinyl]ethoxy]benzoic acid ethyl ester, is an antiviral compound which has low aqueous solubility (<0.01 mg/ml). The compound is a weak base (pKa 5.8) with high lipophicity (logP 4.44). Ionization of the compound increases the solubility in acidic medium to 2.3 mg/ml at pH 2.4. However, a low pH is not acceptable for nasal application as this would induce irritation.
引用
收藏
页码：137 / 139
页数：2
相关论文
共 50 条
  • [1] Development of a formulation of Pirodavir using 2-hydroxypropyl-β-cyclodextrin
    Peeters, Jef
    Neeskens, Peter
    Brewster, Marcus Eli
    JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2007, 57 (1-4) : 137 - 139
  • [2] Development and testing of an improved parenteral formulation of phenytoin using 2-hydroxypropyl-β-cyclodextrin
    Blanchard, J
    Ugwu, SO
    Bhardwaj, R
    Dorr, RT
    PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, 2000, 5 (03) : 333 - 338
  • [3] Silylation of 2-hydroxypropyl-β-cyclodextrin
    M. K. Grachev
    A. V. Popkov
    I. I. Levina
    G. I. Kurochkina
    Russian Journal of General Chemistry, 2017, 87 : 1536 - 1541
  • [4] Silylation of 2-hydroxypropyl-β-cyclodextrin
    Grachev, M. K.
    Popkov, A. V.
    Levina, I. I.
    Kurochkina, G. I.
    RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2017, 87 (07) : 1536 - 1541
  • [5] Comparison between 2-hydroxypropyl-β-cyclodextrin and 2-hydroxypropyl-γ-cyclodextrin for inclusion complex formation with danazol
    Thao Do Thi
    Koen Nauwelaerts
    Luc Baudemprez
    Michiel Van Speybroeck
    Jan Vermant
    Patrick Augustijns
    Pieter Annaert
    Johan Martens
    Jan Van Humbeeck
    Guy Van den Mooter
    Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2011, 71 : 137 - 147
  • [6] Comparison between 2-hydroxypropyl-β-cyclodextrin and 2-hydroxypropyl-γ-cyclodextrin for inclusion complex formation with danazol
    Thao Do Thi
    Nauwelaerts, Koen
    Baudemprez, Luc
    Van Speybroeck, Michiel
    Vermant, Jan
    Augustijns, Patrick
    Annaert, Pieter
    Martens, Johan
    Van Humbeeck, Jan
    Van den Mooter, Guy
    JOURNAL OF INCLUSION PHENOMENA AND MACROCYCLIC CHEMISTRY, 2011, 71 (1-2) : 137 - 147
  • [7] Enhancement of zona binding using 2-hydroxypropyl-β-cyclodextrin
    Parinaud, J
    Vieitez, G
    Vieu, C
    Collet, X
    Perret, B
    HUMAN REPRODUCTION, 2000, 15 (05) : 1117 - 1120
  • [8] Designing a Formulation of the Nootropic Drug Aniracetam Using 2-Hydroxypropyl-β-Cyclodextrin Suitable for Parenteral Administration
    Goldsmith, Sebastian D.
    McDowell, Arlene
    PHARMACEUTICS, 2018, 10 (04):
  • [9] 2-Hydroxypropyl-β-cyclodextrin encapsulates dimethyl disulfide producing a controlled release formulation
    Hao, Baoqiang
    Ren, Lirui
    Huang, Bin
    Tang, Xiujun
    Cheng, Hongyan
    Yan, Dongdong
    Li, Yuan
    Cao, Aocheng
    Ouyang, Canbin
    Wang, Qiuxia
    SCIENCE OF THE TOTAL ENVIRONMENT, 2021, 773
  • [10] Inclusion complexes of sulfanilamide with β-cyclodextrin and 2-hydroxypropyl-β-cyclodextrin
    Ana Tačić
    Ivan Savić
    Vesna Nikolić
    Ivana Savić
    Snežana Ilić-Stojanović
    Dušica Ilić
    Slobodan Petrović
    Mirjana Popsavin
    Agnes Kapor
    Journal of Inclusion Phenomena and Macrocyclic Chemistry, 2014, 80 : 113 - 124
12345