6 research outputs found
Feasibility of transdermal transport of atenolol by combination of iontophoresis and oleic acid pretreatment
Atenolol has a low oral bioavailability and a short elimination half-life. Therefore, alternative route and delivery system is important. Transdermal iontophoresis, i.e. a systemic drug delivery via the skin, implementing a low intensity of electrical current, is one attractive candidate. This study evalu ated feasibility of atenolol transdermal transport when iontophoresis is applied after enhancer pretreatment. There were 4 formulas prepared; 2 implemented iontophoresis for 3 hours (current density: 0.25 mA/cm2) while the others did not use iontophoresis. The enhancer was oleic acid (5 or 10% as a mixture in propylene glycol) with duration of pretreatment of one hour. Transport was evaluated in the diffusion studies across the fresh rat skin in a static-vertical diffusion system. Data were analyzed based on the numeric convolution method to obtain simulated Cp profiles as well as AUC of Cp profiles. Based on the simulated Cp, the best transport was achieved in Formula 3, where iontophoresis is performed across the skin, pretreated with 5% oleic acid for one hour. The value of simulated Cp indicated achievement of therapeutics level of atenolol, suggesting the feasibility of the atenolol delivery by iontophoresis.Key words : atenolol, transdermal, iontophoresis, enhance
PENENTUAN PARAMETER KELARUTAN DAN KOEFISIEN PARTISI SEMU (APPARENT PARTITION COEFFICIENT/APC) SENYAWA YANG TERDUGA MH2011
The Optimum Conditions of Carboxymethyl Chitosan Synthesis on Drug Delivery Application and Its Release of Kinetics Study
In this paper, carboxymethyl chitosan (CMC) was synthesized and studied as a carrier to encapsulate vitamin (as drug model) and controlled release. Chitosan (CS) is a polycationic derivated from chitin, which suitable for active substance carrier system on biomedical function. CS has good properties such as non-toxic, biodegradable, and biocompatible. However, CS insoluble in an aqueous solvent so CS was modified chemically into CMC. CMC was formed by reacting CS and monochloroacetic acid with sodium hydroxide (NaOH) as a catalyst. Optimation was performed by varying the NaOH concentration during alkalizing the CS and the temperature reaction. The functional group and crystallinity of CS and CMC were estimated by FTIR and XRD. The degree substitution of carboxymethylation has an average value of 0.60. The results show optimum temperature reaction and NaOH concentration were 60 °C and 40% (w/v). The nicotinamide (NA), a hydrophilic vitamin, was loaded within CMC matrix system through in vitro precipitation method. To confirm the encapsulation of NA in CMC and the release kinetics of NA from CMC in distilled water was studied through UV-Vis spectrophotometry. The release profile of NA from CMC matrix system carried out for 3 h and 12 h. The rate of NA release from CMC increases with increasing time and the follows a zero order, Higuchi, and Korsmeyer-Peppas kinetics rules