diplomska naloga
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: |
2011 |
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
|
Views: |
906 |
Downloads: |
253 |
Average score: |
0 (0 votes) |
Metadata: |
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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 |