Absorption of Solvent-Deposited Weak Electrolytes and Their Salts Through Human Skin In Vitro

Details

• Personal Author:
  Kasting GB ; Miller MA
• Description:
  Permeation of a weak acid (benzoic acid) and a weak base (propranolol) in various stages of ionization through human skin in vitro was measured from 0 to 72 h following solvent deposition of radiolabeled doses ranging from 11 to 11,000 nmol/cm2 and 1.93-1930 nmol/cm2, respectively. For the twenty combinations tested for each compound, mean permeation into the receptor fluid over 72 h ranged from 1.5 to 40.7 percent of dose for benzoic acid and 1.3-35.5 percent of dose for propranolol. For all but the lowest doses, permeation increased with increasing fraction of nonionized permeant in the dose solution. Generally, this trend became stronger as the dose increased. Recovery of radioactivity averaged 94.3 +/- 5.5% for propranolol and was independent of ionization state and dose. Recovery of radioactivity for benzoic acid ranged from 40 to >100%, increasing with fraction nonionized and with dose. These effects can be qualitatively explained in terms of the low permeability of ionized species through stratum corneum, the volatility of free benzoic acid, and a buffer capacity of the stratum corneum deposition region on the order of 10-20 nmol/cm2. [Description provided by NIOSH]
• Subjects:
  Biopharmaceutics Occupational Health Safety Skin Skin Absorption Solvents
• Keywords:
  Author Keywords: Buffer Capacity Dermal Absorption Electrolytes In Vitro Studies Ionization Organic Salts Percutaneous Absorption Pharmaceuticals Skin Absorption Skin Permeability Topical Delivery Weak Electrolytes

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• ISSN:
  0378-5173
• Document Type:
  Text
• Funding:
  Grant
• Genre:
  Journal Article
• Place as Subject:
  Ohio ; OSHA Region 5
• CIO:
  National Institute for Occupational Safety and Health (NIOSH)
• Topic:
  Workplace Safety & Health
• Location:
  North America
• Volume:
  620
• NIOSHTIC Number:
  nn:20067927
• Citation:
  Int J Pharm 2022 May; 620:121753
• Contact Point Address:
  Gerald B. Kasting, The James L. Winkle College of Pharmacy, University of Cincinnati Academic Health Center, Cincinnati, OH 45247-0514, USA
• Email:
  Gerald.Kasting@uc.edu
• Federal Fiscal Year:
  2022
• Performing Organization:
  University of Cincinnati
• Peer Reviewed:
  True
• Start Date:
  20020901
• Source Full Name:
  International Journal of Pharmaceutics
• End Date:
  20130731
• Collection(s):
  National Institute for Occupational Safety and Health
• Main Document Checksum:
  urn:sha-512:4972a1aeabf8aac9ada6aea8fdfc6168b794c83c644bed245ea42e5300140354d6ffbcd76af9bc9a54e50ffb59dcadef88ac0f69fc03efeaade8de0c5c2bf2ee
• Download URL:
  https://stacks.cdc.gov/view/cdc/230161/cdc_230161_DS1.pdf
• File Type:
  [PDF - 661.86 KB ]