インドメタシンとリドカイン複合体の経皮吸収の検討  [in Japanese] Investigation of the Percutaneous Absorption of a Novel Molecular Complex between Indomethacin and Lidocaine  [in Japanese]

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Abstract

<p>The purpose of this study is to develop new ointments containing the complex of indomethacin (IDM) and lidocaine (LDC) for alleviation of the pain of post-herpetic neuralgia. Methylcellulose-based hydrogel ointment was prepared with a molar ratio of LDC to IDM of 1 or 10.5. The concentration of IDM was fixed at 1% (w/w). The skin permeation of IDM and/or LDC was evaluated using hairless mouse skin with the flow-through-cell method. The amount of IDM permeating from the IDM/LDC (1:1) ointment was about 6-fold higher than that from the ointment containing IDM alone. This can be attributed to the fact that the solubilities of IDM in octanol and water increase in the IDM/LDC (1:1) ointment compared to the ointment containing IDM alone due to the formation of a complex. The amount of IDM permeating from the IDM/LDC (1:10.5) ointment was about 2.2-fold higher than that from the IDM/LDC (1:1) ointment. In contrast, the amount of LDC permeating from IDM/LDC (1:1) ointment decreased to 40% compared to the ointment containing LDC alone (0.65% (w/w)) which was equivalent to the amount used in IDM/LDC (1:1) ointment. However, as the molar ratio of LDC in IDM/LDC ointment was increased from 1 to 10.5 (LDC: 6.9% (w/w)), the amount of LDC permeating from IDM/LDC (1:10.5) ointment was nearly equal to that from the ointment containg LDC alone (6.9%) which is equivalent to the amount used in clinical practice. In such a novel IDM/LDC ointment is a potential formulation to alleviate the pain of post-herpetic neuralgia.</p>

Journal

  • Journal of Pharmaceutical Science and Technology, Japan

    Journal of Pharmaceutical Science and Technology, Japan 69(5), 384-391, 2009-09-01

    The Academy of Pharmaceutical Science and Technology, Japan

References:  25

Codes

  • NII Article ID (NAID)
    10025720815
  • NII NACSIS-CAT ID (NCID)
    AN00266708
  • Text Lang
    JPN
  • Article Type
    ART
  • ISSN
    03727629
  • Data Source
    CJP  J-STAGE 
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