Injectable antibiotic formulations and their methods of use
This invention relates to a composition, including penethamate (PNT) or a pharmaceutical equivalent thereof; and at least one oily vehicle.
1. An injectable, ready-to-use, oil-based, non-aqueous veterinary pharmaceutical composition comprising as the only antibiotic in the composition, penethamate (PNT) hydroiodide, and at least one oily vehicle selected from one or more of the group consisting of ethyl oleate, medium chain triglycerides, and triacetin, wherein the ratio of the PNT hydroiodide to the at least one oily vehicle is 1:1 to 1:4 w/v, wherein the concentration of PNT hydroiodide is between 15-55% w/v, and wherein the viscosity of the composition is below 3000 mPas at a temperature of 20° C. and a shear rate of 1/s when measured with a cup cylinder method, and wherein the penethamate hydroiodide shows substantially no degradation after storage of the composition over 180 days at 30 degrees Celsius.
2. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the concentration of penethamate (PNT) hydroiodide in the composition is between 20-35% w/v.
3. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the at least one oily vehicle is triacetin.
4. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the composition is in liquid form.
5. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the particle diameter d 50 of the penethamate (PNT) hydroiodide is between 8-30 microns.
6. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the composition further includes a surfactant.
7. The non-aqueous veterinary pharmaceutical composition of claim 6 wherein the surfactant is polysorbate 80.
8. The non-aqueous veterinary pharmaceutical composition of claim 1 wherein the non-aqueous veterinary pharmaceutical composition further includes a preservative.
9. The non-aqueous veterinary pharmaceutical composition of claim 8 wherein the preservative is benzyl alcohol.
10. The non-aqueous veterinary pharmaceutical composition of claim 1 further comprising an emulsifier or dispersing agent.
11. The non-aqueous veterinary pharmaceutical composition of claim 6 wherein the surfactant is selected from a compound with a hydrophobic-lipophilic balance (HLB) of between 7 to 16.
12. A syringe containing the non-aqueous veterinary pharmaceutical composition of claim 1 .
13. The syringe of claim 12 wherein the syringe comprises 5 g of penethamate hydroiodide.
14. A method of treating an animal with the non-aqueous veterinary pharmaceutical composition of claim 1 for the treatment of a microbial infection, wherein the method includes intramuscular or subcutaneous injection of the non-aqueous veterinary pharmaceutical composition to the animal in need thereof.
15. The method of claim 14 wherein the microbial infection is pre-clinical or clinical mastitis.
16. The method of claim 14 wherein the method of treatment includes a dosage regime of 5 g penethamate hydroiodide per day repeated for approximately three days.
17. The method of manufacturing the non-aqueous veterinary pharmaceutical composition of claim 6 , including
a) preparing the at least one oily vehicle by either (i) providing the at least one oily vehicle, or (ii) mixing the at least one oily vehicle and a surfactant in a container to form a homogenous oil mixture: and
b) dispersing the penethamate hydroiodide in the at least one oily vehicle.
18. The method of manufacturing of claim 17 wherein a preservative is added to the at least one oily vehicle in a).
19. The method of manufacturing of claim 17 wherein high shear dispersion equipment is used in b).
20. The non-aqueous veterinary pharmaceutical composition of claim 1 , further comprising at least one non-thickening anti-caking agent.
21. The non-aqueous veterinary pharmaceutical composition of claim 1 , wherein the viscosity of the at least one oily vehicle is 2.0 to 100.0 mPa at 25° C.
22. The non-aqueous veterinary pharmaceutical composition of claim 1 , wherein the at least one oily vehicle is ethyl oleate.
23. The non-aqueous veterinary pharmaceutical composition of claim 22 , further comprising at least one non-thickening anti-caking agent.
24. The composition of claim 22 , further comprising lecithin.
25. The composition of claim 1 , further comprising lecithin.
26. The composition of claim 1 , which achieves a WHP in milk of less than 72 hours.