In vitro and in vivo evaluation of the transdermal iontophoretic delivery of sumatriptan succinate
| Autor: | Yogeshvar N. Kalia, Ashutosh Das Sharma, Hui Zhong, Sonal R. Patel |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Swine
Chemistry Pharmaceutical Drug Compounding Skin Absorption Pharmaceutical Science Pharmacology Administration Cutaneous Subcutaneous injection Organ Culture Techniques Pharmacokinetics Sumatriptan Succinate In vivo Serotonin Receptor Agonists/administration & dosage/blood/chemistry/pharmacokinetics medicine Animals Transdermal Dosage Forms ddc:615 Iontophoresis Sumatriptan business.industry Sumatriptan/administration & dosage/blood/chemistry/pharmacokinetics General Medicine Hydrogen-Ion Concentration Serotonin Receptor Agonists Rectal administration Diffusion Chambers Culture Feasibility Studies Female business Biotechnology medicine.drug |
| Zdroj: | European Journal of Pharmaceutics and Biopharmaceutics, Vol. 66, No 2 (2007) pp. 296-301 |
| ISSN: | 0939-6411 |
| DOI: | 10.1016/j.ejpb.2006.11.001 |
| Popis: | The objective was to evaluate the transdermal delivery of the 5-HT(1B/1D) agonist, sumatriptan from an iontophoretic patch system, in vivo. Initial in vitro experiments were conducted to optimize formulation parameters prior to iontophoretic delivery in Yorkshire swine. It was found in vitro that increasing drug load in the patch from 9.7 to 39 mg had no statistically significant effect on cumulative delivery (cf. 305.6+/-172.4 vs. 389.4+/-80.4 microg cm(-2), respectively). However, for a given drug load (39 mg) increasing formulation pH from pH 4.7 to 6.8 significantly increased the cumulative amount of sumatriptan delivered across the skin (389.4+/-80.4 vs. 652.4+/-94.2 microg cm(-2)). A biphasic current profile comprising intensities of 1.8 mA from t=0 to t=180 min and 0.8 mA from t=181 min to t=360 min was used for the in vivo experiments. Drug levels in the blood were 13.7+/-4.5 and 53.6+/-10.2 ng ml(-1) at the 30 and 60 min time-points, rising to 90-100 ng ml(-1) during the 90-180 min time-period. The in vivo results show that the pharmacokinetics following transdermal iontophoretic delivery are comparable to those after oral, nasal or rectal administration, but do not match those upon subcutaneous injection. |
| Databáze: | OpenAIRE |
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