diplomska naloga
Neža Benedik (Author), Janez Kerč (Mentor), Miha Homar (Co-mentor)

Abstract

Vgradnja slabo topnih učinkovin v samomikroemulgirajoče sisteme, kjer se učinkovina nahaja že v raztopljeni obliki, je ena izmed možnosti povečanja topnosti in hitrosti raztapljanja učinkovine v vodi. V okviru diplomske naloge smo raziskovali primernost izdelave tablet iz suhih mikroemulzij, ki smo jih izdelali s postopkom sušenja z razprševanjem. Kot modelno učinkovino smo izbrali kompetitivni inhibitor HMG CoA reduktaze simvastatin, ki je slabo topen in dobro permeabilen. Pri izdelavi suhih mikroemulzij smo uporabljali različne trdne nosilce. Trdni nosilec, s katerim smo dosegli najboljše rezultate, smo uporabili za nadaljne eksperimentalno delo. Z izvedbo eksperimentalnega načrta, načrtovanega s statističnim orodjem DoE (Design of Experiments), smo določili korelacije med razmerjem sestave suspenzije za razprševanje ter lastnostmi nastalega granulata (vsebnost simvastatina, pretočnost, stisljivost) oziroma tablet. (enakomernost mase, trdnost, razpadnost) Modela v večini primerov ni bilo mogoče postaviti, ugotovili pa smo, da se z večanjem deleža Pharmacoata® 606 veča izkoristek procesa in manjša relativna standardna deviacija mase izdelanih tablet. Iz granulata s sestavo, ki je izkazoval najboljše lastnosti, smo izdelali tablete in primerjali hitrost sproščanja učinkovine s tabletami originatorja Zocor®. Učinkovina se je iz naše tablete sproščala hitreje kot iz tablete originatorja predvsem v prvih petnajstih minutah testa, kasneje razlika ni bila značilna. Rezultati diplomske naloge kažejo, da so samomikroemulgirajoči sistemi primerni za vgradnjo v tablete. Učinkovina simvastatin pri vgradnji v testirana samomikroemulgirajoča sistema ne izkazuje zadostne stabilnosti pri sobni temperaturi, za stabilizacijo bi bili potrebni dodatni pristopi.

Keywords

biofarmacija;mikroemulzije;topnost učinkovin;izdelava tablet;simvastatin;stabilnost učinkovin;

Data

Language: Slovenian
Year of publishing:
Source: Ljubljana
Typology: 2.11 - Undergraduate Thesis
Organization: UL FFA - Faculty of Pharmacy
Publisher: [N. Benedik]
UDC: 544.351.3+615.014+615.454
COBISS: 3635057 Link will open in a new window
Views: 906
Downloads: 253
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Other data

Secondary language: English
Secondary title: Formulation optimization of peroral drug delivery system based on microemulsions
Secondary abstract: Incorporation of poorly soluble drugs into self emulysifying drug delivery systems, where the substance is in a solubilized form, is one of the many possibilities for enhancing solubility. The aim of the study was to evaluate the possibility of tablet production from dry microemulsions, produced with spray drying process. Simvastatin, a HMG CoA reductase inhibitor, was used as a model substance, due to its poorly aqueous solubility and good permeability. Various solid carriers were used to produce dry microemulsions, the sample with best results was chosen for further experiments. Experimental design was conducted with statistical tool DoE (Design of Experiments). The aim of the experimental design was to evaluate correlation between composition of suspension for spray drying and quality of dry emulsions (simvastatin content, granules flowability and compressibility) or tablets (mass, hardness and disintegration uniformity). It was impossible to construct a model in most of the cases, but it was shown, that higher Pharmacoat® 606 content leads to higher efficiency of spray drying process and lower relative standard deviation in tablets mass uniformity test. Tablets were compressed from granules with the best characteristics. The dissolution rate of prepared tablets was higher compared to the original Zocor® tablets, especially in the first 15 minutes of the dissolution test. The results of the present work suggest that it is appropriate to incorporate self microemulsifying drug delivery systems into tablets. Sivastatin, incorporated into tested self microemulsifying drug delivery systems, is not stable at room temperature, further methods are needed to enhance its stability.
Type (COBISS): Undergraduate thesis
Pages: 64 f.
ID: 12053337