Influence of melting point and hydrophilic/lipophilic balance on the release of salbutamol sulfate from lipid matrices

  • A. Esquisabel
  • , A. San Vicente
  • , M. Igartua
  • , R. M. Hernández
  • , A. R. Gascón
  • , M. B. Calvo
  • , J. L. Pedraz*
  • *Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

10 Citations (Scopus)

Abstract

Salbutamol is a drug with a short elimination half life, and is thus a possible candidate for the development of sustained release formulations. We developed sustained release lipid matrices using Gelucires. Three different release profiles were observed : fast release, in the case of Gelucires 33/01, 35/10, 37/02, 42/12 and 44/14, with a mean dissolution time (Td50) of 6, 16, 3, 40 and 12 min; a sustained release for Gelucires 48/09, 50/13 and 53/10 with a mean dissolution time of 186, 147 and 168 min; and a slow release for Gelucires 46/07 and 50/02, with a mean dissolution time of 310 and 621 min, respectively. The percentages of salbutamol released with Gelucires 46/07 and 50/02 were below 60% of the dose. Multiple regression analysis of the hydrophilic/lipophilic balance (HLB), melting point (MP), dissolution constant (K1) and mean dissolution time (Td50) yielded the following equations: K1 = 3.13 - 0.262*HLB - 0.0648*MP + 0.00556HLB*MP, (R2 =0.88), and Td50 = - 1485 + 105*HLB + 43.2*MP - 3.03 HLB*MP, (R2 = 0.91).

Original languageEnglish
Pages (from-to)365-369
Number of pages5
JournalS.T.P. Pharma Sciences
Volume6
Issue number5
Publication statusPublished - Sept 1996
Externally publishedYes

Keywords

  • Capsules
  • Gelucire
  • Hydrophilic/lipophilic balance
  • Melting point
  • Release kinetics
  • Salbutamol
  • Sustained release

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