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OBJECTIVE To develop appropriate formulation and process design for hot melt extrusion (HME) of poorly soluble drug posaconazole with aid of rheology and discriminatory dissolution. METHODS The viscoelastic properties of polymer matrices were assessed for oscillation shear strain on a rotation disc rheometer within temperature of 14-180 ℃ and angular frequency of 100-0.1 rads·s-1, respectively. A paddle method and an open flow cell method were developed alternatively to screen key critical quality attributes. RESULTS The selected polymer carrier showed storage modulus (G') >loss modulus (G″) with loss factor Tan(delta) <1 within the assessed temperature range, for better HME processability. Oscillation-frequency assessments further demonstrated that G'and G″ were more shear stable with angular strain at 140 ℃ compared with the increasing modulus trends at 150 and 160 ℃. Based on quality by design, discriminatory dissolution helped in defining if need to add excipient hydroxypropylcellulose in the process, as well as in designing HME granule size for formulation drug T. DSC, XRPD, Raman and optical microscopy characterization showed that the morphology of API changed from multicrystalline state to amorphous molecule dispersion after extrusion. CONCLUSION The drug release in vitro and in vivo of formulation drug posaconazole T is in bioequivalence with that of reference listing drug.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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