Predmetom príspevku je hodnotenie liberácie liečiva alaptid z gélov a jeho permeácia cez rôzne typy permeačných membrán. Pripravili sa gély na báze troch rôznych polymérov (3 % chitosan; 2,5 % hydroxypropylcelulóza; 3 % hydroxyetylcelulóza) v rôznej koncentrácii s prísadou humaktantov (5 %; 15 % propylénglykol a 0 % glycerol) a konzervantu 0,3 % Sepicide HBR a liečiva 1 % alaptid a gély bez liečiva. Prestup liečiva z gélov do akceptorového roztoku sa hodnotil cez nasledovné membrány: celofán, kuracia koža, zvlečená hadia koža a stena tenkého čreva. Z výsledkov merania bolo zistené najväčšie percento uvoľneného alaptidu cez stenu tenkého čreva, menej cez kuraciu kožu a najmenej sa uvoľnilo cez hadiu kožu. V práci sa hodnotili aj reologické vlastnosti pripravených hydrogélov. Pseudoplastický tok bol zistený iba v prípade hydrogélu na báze hydroxypropylcelulózy. Naopak to bolo pri hydrogéloch na báze chitosanu a hydroxyetylcelulózy, ktoré vykazovali výrazný tixotropný charakter a miera tixotropie sa s časom zväčšovala. Na základe výsledkov merania pH boli vzorky na báze chitosanu a hydroxypropylcelulózy vyhodnotené ako nevyhovujúce, nakoľko dosahovali nižšie hodnoty pH a mohli by spôsobiť podráždenie pokožky. Fyziologickým hodnotám pH kože zodpovedal hydrogél na báze hydroxyetylcelulózy a to i po 14. dňoch po príprave.

The paper evaluates the liberation of alaptide from gels through various types of permeable membranes. The gels were prepared on the basis of three different polymers (3% chitosan; 2.5% hydroxypropyl cellulose; 3% hydroxyethyl cellulose) in different concentrations with additions of humectants (5 %; 15% propylene glycol and 10% glycerol) and the preserving agent, 0.3% Sepicide HBR with 1% alaptide, and finally without the drug. The permeation of the drug from gels into the acceptor solution was evaluated with the use of the following membranes: the hydrophilic membrane from Chemosvit, the chicken skin, the stripped snakeskin, and the wall of the small intestine. The measurements showed that the highest percentage of the drug penetrated through the small intestine, a smaller percentage through the chicken skin, and the smallest amount through the snakeskin. Rheological properties of the prepared hydrogels were evaluated as well. The pseudo-plastic flow was only confirmed for the hydrogel prepared on the basis of hydroxypropyl cellulose. An utterly opposite situation was with the hydrogels prepared on the basis of chitosan and hydroxyethyl cellulose. They showed a significant thixotropic character and the degree of thixotropy increased with time. Based on the results of the pH measurement, the samples prepared on the basis of chitosan and hydroxypropyl cellulose have been shown to be inconvenient because they reached a lower pH and had a potential of causing skin irritation. The hydroxyethyl cellulose hydrogel matched the physiological values of skin pH even after 14 days since its preparation.

Univerzita Komenského Bratislava Farmaceutická fakulta Katedra galenickej farmácie

Influence of membranes on alaptide permeation from hydrogels

Lit.: 14