Crystalline lopinavir/surfactant adducts
View Patent ↗This invention relates to novel crystalline lopinavir/surfactant adducts, methods for their preparation, therapeutic uses of those crystalline lopinavir/surfactant adducts, and pharmaceutical compositions containing them or made from them.
1. A single crystal of crystalline lopinavir/surfactant adduct characterized by an XRPD pattern having peaks at 4.8, 7.3, 8.8, 9.7, 10.3, 12.2, 12.8, 14.7, 16.4, 17.6, 18.6, 20.0, 21.9, 22.5, and 23.0°2θ±0.2°2θ.
2. A single crystal of crystalline lopinavir/surfactant adduct according to claim 1 , wherein the surfactant is selected from at least one of VitE TPGS, a polysorbate, a sorbitan fatty acid ester, a polyoxyethylene ester, a poloxamer or a copolymer of ethylene oxide and propylene oxide, polyglyceryl-3 oleate, a fatty acid, a propylene glycol laurate, a polyoxyethylene hydrogenated castor oil, a polyethoxylated castor oil, and a propylene glycol monocaprylate.
3. A single crystal of crystalline lopinavir/surfactant adduct characterized by an IR spectrum having a peak at 1730 cm −1 .
4. A single crystal of crystalline lopinavir/surfactant adduct characterized by a Raman spectrum having peaks at 3398, 3066, 3042, 2925, 2968, 1660, 1643, 1606, 1585, 1446, 1381, 1346, 1267, 1238, 1209, 1033, 1004, 958, 883, 791, 754, 697, 622, and 532 cm −1 ±1 cm −1 .
5. A single crystal of crystalline lopinavir/surfactant adduct according to claim 1 , wherein the single crystal of crystalline lopinavir/surfactant adduct is substantially pure.
6. A pharmaceutical composition comprising an effective amount of a single crystal of crystalline lopinavir/surfactant adduct according to claim 1 .
7. The pharmaceutical composition of claim 6 , wherein at least 50% of lopinavir in the composition is in the form of the single crystal of crystalline lopinavir/surfactant adduct.
8. The pharmaceutical composition of claim 6 , wherein at least 75% of lopinavir in the composition is in the form of the single crystal of crystalline lopinavir/surfactant adduct.
9. The pharmaceutical composition of claim 6 , wherein at least 95% of lopinavir in the composition is in the form of the single crystal of crystalline lopinavir/surfactant adduct.