Liquisolid technique as a tool for the enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties
| Autor: | Yousef Javadzadeh, Mohammad Reza Siahi, Solmaz Asnaashari, Ali Nokhodchi |
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| Jazyk: | angličtina |
| Rok vydání: | 2007 |
| Předmět: | |
| Zdroj: | Acta Pharmaceutica Volume 57 Issue 1 |
| ISSN: | 1846-9558 1330-0075 |
| Popis: | The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was investigated. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of aging on the dissolution behaviour of indomethacin liquisolid compacts was investigated. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, X-ray powder diffraction (XPD) and differential scanning calorimetry (DSC) were used. Dissolution test was carried out at two different pH, 1.2 and 7.2, to simulate the stomach or intestine fluid, respectively. The results showed that liquisolid formulations exhibited significantly higher drug dissolution rates at pH 1.2 and 7.2 compared to compacts prepared by the direct compression technique. The enhanced rate of indomethacin dissolution from liquisolid tablets was, due to an increase in wetting properties and surface area of drug particles available for dissolution. In order to investigate the effect of aging on the hardness and dissolution rate of liquisolid compacts, the formulations were stored at 25 oC/75% relative humidity for a period of 12 months. The results showed that aging had no significant effect on dissolution profiles of liquisolid tablets. Liquisolid compacts containing propylene glycol as vehicle produced higher dissolution rates in comparison with liquisolid compacts containing PEG 400 or Tween 80 of the same concentration. The DSC and XPD results showed no changes in crystallinity of the drug and interaction between indomethacin and excipients (Avicel and silica) during the process. U radu je ispitivan učinak tekućinsko-čvrstih sustava na poboljšanje oslobađanja u vodi netopljivih tvari (indometacina). Koristeći različita nehlapljiva otapala pripravljeno je nekoliko tekućinsko-čvrstih tableta, a zatim je proučavan učinak starenja na oslobađanje indometacina. Moguće interakcije između indometacina i drugih komponenata praćene su difrakcijom rentgenskih zraka na praškastom uzorku (XPD) i diferencijalnom pretražnom kalorimetrijom (DSC). Oslobađanje je praćeno pri dva različita pH, 1,2 i 7,2, simulirajući uvjete u želučanoj ili crijevnoj tekućini. Rezultati pokazuju da je profil oslobađanja iz tekućinsko-čvrstih pripravaka značajno bolji pri pH 1,2 ili 7,2, u usporedbi s pripravcima dobivenim kompresijom. Poboljšanje oslobađanja indometacina iz tekućinsko-čvrstih pripravaka posljedica je povećanog vlaženja površine čestica ljekovite tvari. Da bi se proučio učinak starenja na čvrstoću pripravaka i oslobađanje ljekovite tvari, tekućinsko-čvrsti pripravci su uskladišteni 12 mjeseci na 25 oC/75% relativne vlažnosti. Rezultati ukazuju da starenje nema značajni učinak na profil oslobađanja. Pripravci s propilenglikolom imaju bolji profil oslobađanja nego pripravci s istom koncentracijom PEG 400 ili Tween 80. DSC i XPD pokazuju da nije došlo do promjene kristaliničnosti niti do interakcije između indometacina i pomoćnih tvari (Avicel i silikagel) za vrijeme izrade pripravaka. |
| Databáze: | OpenAIRE |
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