In this study, the ability of pharmaceutical cocrystals on improving solubility and dissolution behaviour of poorly water soluble drug has been studied by a novel technique SDI300 UV imaging surface dissolution system. Pharmaceutical cocrystals of poorly water soluble drug carbamazepine (CBZ) were synthesized, which are 1: 1 carbamazepine - nicotinamide (CBZ-NIC) cocrystal, and 2:1 carbamazepine - succinic acid (CBZ-SUC) cocrystal. Firstly, dissolution and solution mediated phase transformation behaviour (SMPT) of CBZ-NIC cocrystal was studied by in situ techniques of UV imaging and Raman spectroscopy. This study has shown that in situ UV imaging and Raman spectroscopy with a complementary technique of SEM can provide an in depth understanding of cocrystal dissolution processes. It has been found that CBZ-NIC cocrystal including other polymorphs of CBZ III and I and mixture are converting to CBZ DH during dissolution. The influence of surfactants, SLS and Tween 80, on the solubility and dissolution behavior of the CBZ-NIC cocrystal has been studied. Results show that the SMPT of CBZ III and CBZ-NIC cocrystal can be altered by inclusion of a surfactant in dissolution medium. However, CBZ III and CBZ-NIC cocrystal have shown different transformation behavior with different surfactants. The solubility and dissolution behaviour of CBZ-NIC cocrystal, CBZ-SUC cocrystal in four biomedia (simulated gastric fluid, pH1.2 HCl buffer, simulated intestinal fluid, and pH 6.8 PBS buffer) were studied. Results have shown that equilibrium solubility of CBZ samples varied in different media. The two cocrystals dissolution rates show different trends as that of parent drug CBZ III. This can be explained by that the formation of cocrystal change the dissolution ability of CBZ III.
| Identifer | oai:union.ndltd.org:bl.uk/oai:ethos.bl.uk:613566 |
| Date | January 2014 |
| Creators | Qiao, Ning |
| Publisher | De Montfort University |
| Source Sets | Ethos UK |
| Detected Language | English |
| Type | Electronic Thesis or Dissertation |
| Source | http://hdl.handle.net/2086/10201 |
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