PMID: 8961161Nov 1, 1996Paper

Terbutaline transdermal delivery: preformulation studies and limitations of in-vitro predictive parameters

The Journal of Pharmacy and Pharmacology
S TenjarlaT Mandal

Abstract

A transdermal dosage form of terbutaline may be useful to prevent nocturnal wheezing by providing prolonged duration of action. It will also improve patient compliance and bioavailability. Controlled input of the drug would be an additional advantage as this will reduce the intersubject variability. Preformulation studies were conducted to determine the feasibility of a transdermal dosage form of terbutaline. The drug solubility in propylene glycol was 6.3 mg mL-1. The apparent partition coefficient (n-octanol/ deionized-water, pH 6.5) of terbutaline was 0.03. A pH-partition coefficient (octanol/buffer) profile indicated that the partition coefficient values were 0.02, 0.05 and 0.4 in buffers of pH 3, 7.4 and 9, respectively. The required drug flux through the human skin to attain therapeutic concentrations in the blood was calculated to be 3.3 micrograms cm-2 h-1 for a 10-cm2 transdermal delivery system. Rabbit, guinea-pig and human skin was tested as the penetration barrier using modified Franz diffusion cells. Terbutaline flux values through the rabbit and guinea-pig skin were 8.3 and 7.7 micrograms cm-2 h-1, respectively. The flux through human full-thickness skin and human epidermis were 0.6 and 3.6 micrograms cm-2 h-1. Az...Continue Reading

References

Mar 1, 1988·Pharmaceutical Research·P V RaykarB D Anderson
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Citations

Dec 17, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·David D N'Da
Mar 25, 2006·Drug Development and Industrial Pharmacy·Miriam López-CervantesEnrique Angeles-Anguiano
Jul 2, 2005·Expert Opinion on Investigational Drugs·G Cevc
Nov 18, 2008·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Ana M Barbero, H Frederick Frasch
Jun 27, 2013·Skin Research and Technology : Official Journal of International Society for Bioengineering and the Skin (ISBS) [and] International Society for Digital Imaging of Skin (ISDIS) [and] International Society for Skin Imaging (ISSI)·Susanne MangelsdorfAlexa Patzelt
Dec 24, 2011·Pharmaceutical Development and Technology·H O AmmarA M Ghoneim
Mar 20, 2015·The Journal of Toxicological Sciences·Tomomi AtobeHirokazu Kouzuki

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