Details for Patent: 8,536,155

Title:	Process for preparing malathion for pharmaceutical use
Abstract:	The present invention provides a process for preparing a highly pure form of malathion having a reduced level of toxic impurities. In addition, the malathion prepared by the process of this invention is storage stable. The level of toxic impurities in the malathion, e.g., isomalathion, O,O,S-trimethyl phosphorodithioate (MeOOSPS), O,O,S-trimethyl phosphorothioate (MeOOSPO), O,S,S-trimethyl phosphorodithioate (MeOSSPO), malaoxon, isomalathion, diethyl fumarate, methyl malathion, dimethyl malathion, O,O-methyl,ethyl-S-(1,2-dicarboethoxy)ethyl-phosphorodithioate are lower than that of any other commercial preparation of malathion that may be used for pharmaceutical purposes.
Inventor(s):	Gutman; Daniella (Rishon Lezion, IL), Baidussi; Wael (Hamisholash, IL)
Assignee:	Taro Pharmaceuticals North America, Inc. (Grand Cayman, KY)
Filing Date:	Sep 22, 2011
Application Number:	13/239,750
Claims:	1. A topical pharmaceutical formulation comprising at least 70% (w/w) isopropyl alcohol, and terpineol, dipentene, pine needle oil, and pharmaceutical grade malathion, said pharmaceutical grade malathion containing 0.1% or less (w/w) MeOOSPO, 0.1% or less (w/w) MeOSSPO, 0.2% or less (w/w) MeOOSPS, less than 0.1% (w/w) methyl malathion, 0.1% or less (w/w) malaoxon and 0.1% or less (w/w) isomalathion. 2. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion has a purity greater than 98.5% (w/w). 3. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion has a purity of greater than 99% (w/w). 4. The topical pharmaceutical formulation of claim 1 wherein the pharmaceutical grade malathion contains 0.05% or less (w/w) MeOOSPO. 5. The topical pharmaceutical formulation of claim 1 wherein the pharmaceutical grade malathion contains 0.04% or less (w/w) MeOOSPO. 6. The topical pharmaceutical formulation of claim 1 wherein the pharmaceutical grade malathion contains 0.02% or less (w/w) MeOSSPO. 7. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains not more than about 0.1% (w/w) of any other detectable impurity. 8. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains 0.08% or less (w/w) methyl malathion. 9. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains 0.06% or less (w/w) methyl malathion. 10. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains 0.05% or less (w/w) isomalathion. 11. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains 0.02% or less (w/w) isomalathion. 12. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains 0.2% or less (w/w) diethyl fumarate and 0.2% or less (w/w) dimethylmalathion. 13. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains less than 0.05% (w/w) malaoxon. 14. The topical pharmaceutical formulation of claim 1 wherein the pharmaceutical grade malathion contains 0.1% or less (w/w) MeOOSPS. 15. The topical pharmaceutical formulation of claim 1, wherein the amount of isomalathion in the pharmaceutical grade malathion is not more than 0.1% (w/w), after storage for 3 months at 25.degree. C. and 60% relative humidity. 16. The topical pharmaceutical formulation of claim 1, comprising at least 0.5% (w/w) pharmaceutical grade malathion. 17. The topical pharmaceutical formulation of claim 1, comprising 0.65% (w/w) of the pharmaceutical grade malathion. 18. The topical pharmaceutical formulation of claim 1, wherein the pharmaceutical grade malathion contains less than 0.1% (w/w) MeOOSPO, less than 0.1% (w/w) MeOSSPO, and less than 0.1% malathion carboxylic acids. 19. The topical pharmaceutical formulation of claim 1, comprising at least 12% (w/w) terpineol, at least 10% (w/w) dipentene, and at least 0.28% (w/w) pine needle oil. 20. The topical pharmaceutical formulation of claim 1 wherein the formulation is a lotion. 21. The topical pharmaceutical formulation of claim 1 wherein the formulation is a gel. 22. The topical pharmaceutical formulation of claim 1 wherein the formulation is a cream.