Artemether-Soluplus Hot-Melt Extrudate Solid Dispersion Systems for Solubility and Dissolution Rate Enhancement with Amorphous State Characteristics

Table 1

 Comparative evaluation of ARTM and its HME formulations in terms of aqueous solubility, solubility in dissolution medium.

Batch	Formulation type	Ratio	Extrusion temp.; (°C)	Batch size; (gm)	Solubility in water; (μg/mL)	Solubility in disso. medium; (μg/mL)
Drug	Pure ARTM	—	—	—	0.0183±1.3	0.254±1.34
F1	ARTM : SOL : PEG 400	1 : 1.8 : 0.2	82-83	30	88.52±1.54	221.2±1.54
F2	ARTM : SOL : PEG 400	1 : 2.8 : 0.2	82-83	30	94.78±1.12	222.9±1.08
F3	ARTM : SOL : PEG 400	1 : 3.8 : 0.2	82-83	40	98.14±1.69	216.2±1.85
F4	ARTM : SOL : LF127	1 : 1.8 : 0.2	79-80	25	74.95±1.47	210.2±1.15
F5	ARTM : SOL : LF127	1 : 2.8 : 0.2	79-80	30	79.84±1.29	213.3±1.41
F6	ARTM : SOL : LF127	1 : 3.8 : 0.2	79-80	30	86.25±1.36	218.4±1.52
F7	ARTM : SOL : LF68	1 : 1.8 : 0.2	76-77	40	70.25±1.12	219.2±1.71
F8	ARTM : SOL : LF68	1 : 2.8 : 0.2	76-77	30	76.54±1.24	218.3±1.16
F9	ARTM : SOL : LF68	1 : 3.8 : 0.2	76-77	30	85.15±1.56	220.6±1.92
F10	ARTM : SOL	1 : 4	83-84	20	78.98±1.24	213.8±1.39
F11	ARTM : SOL	1 : 5	83-84	25	87.33±1.71	217.2±1.34
F12	ARTM : SOL	1 : 6	83-84	30	98.23±1.39	219.4±1.2
F13	ARTM : SOL	1 : 7	82-83	40	115.8±1.45	222.8±1.67
F14	ARTM : SOL	1 : 8	82-83	40	131.9±1.85	224.3±1.88
F15	ARTM : SOL	1 : 9	82-83	40	137.2±1.05	231.7±1.54

Artemether: ARTM, Soluplus: SOL, Polyethylene Glycol 400: PEG 400, Lutrol F127: LF127, and Lutrol F68: LF68 (mean ± SD (𝑛=3)).