Monika Balcerkiewicz, Edmund Grześkowiak, Pascal Le Corre, Maja Ratajczak-Enselme, Anna Wolc, Karol Szlufik
Biofarmaceutyczna ocena bupiwakainy inkorporowanej w postaci mikrosfer polimerowych
2009-03-25
Aim: Bupivacaine is an amide type local anesthetics widely used in surgery and obstetrics for sustained central and peripheral nerve blockade. However, its use is limited by its systemic toxicity related to high drug plasma concentrations resulting from a fast systemic absorption. Improvement of regional administration of local anesthetic formulations could be obtained by their incorporation in controlled delivery systems such as implants, liposomes, drug complexes with cyclodextrins and microspheres. The aim of the present study was to determine the reduced systemic absorption leading to high plasma concentrationa related to central nervous and cardiovascular toxicity and prolong the duration of action of bupivacaine through the modification of this pharmacokinetics by its application as polymeric microspheres. Results: We evaluated in rabbits the bupivacaine pharmacokinetics: in first stage after 15 minutes intravenous infusion of 5 mg bupivacaine solution and after intravenous injections of 5 mg bupivacaine-loaded microspheres (type I), in second stages after intramuscular injections of 5 mg bupivacaine in solution and after intramuscular injections of 5 mg bupivacaine-loaded microspheres (type I and II). Blood samples were collected at several time points. Plasma concetration of BP were measured by HPLC with hydrochloride ropivacaine as internal standard. Conclusion: Obtained data indicates that bupivacaine is realeased from microspheres in prolonged and controlled way that is characterized by beneficial bioaccess parameters for anesthetics locale.Keywords: microspheres, bupivacaine, anesthetics locale, PLGA
Biofarmaceutyczna ocena bupiwakainy inkorporowanej w postaci mikrosfer polimerowych
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21 grudnia 2017