Methocarbamol composition and related methods
Stable methocarbamol ready to use compositions for parenteral administration including parenteral infusion are provided. In certain embodiments, the compositions are sterile, isotonic, and particulate-matter-free. Further, the compositions reduce or avoid allergic reactions to latex, reduce or avoid extravasation, and permit administration of methocarbamol to subjects having renal pathology. Methods of manufacture and methods of administration are also provided.
1. An injectable methocarbamol solution for intravenous administration comprising:
methocarbamol in an amount from about 1 mg/ml to less than 10 mg/ml;
a tonicity agent; wherein the tonicity agent is selected from the group consisting of sodium chloride, mannitol, sorbitol, dextrose, ethanol, glycerin, sorbitol, propylene glycol, and combinations thereof;
a buffer; and
water,
wherein the solution is isotonic, has a pH of about 3 to about 5, is free of polyethylene glycol (PEG), and contains no more than 2.0% w/w of guaifenesin after storage at ambient temperature for at least 3 months.
2. The solution of claim 1 , wherein the solution is sufficiently stable to allow at least 95 w/v % of the methocarbamol in the composition to remain undegraded and unprecipitated after storage for at least 3 months at 25° C. and 60% relative humidity.
3. The solution of claim 1 , wherein the solution is sufficiently stable to allow at least 95 wt % of the methocarbamol in the composition to remain undegraded and unprecipitated after storage for at least 6 months at 25° C. and 60% relative humidity.
4. The solution of claim 1 , wherein the solution is sufficiently stable to allow at least 95 wt % of the methocarbamol in the composition to remain undegraded and unprecipitated after storage for at least 1 year at 25° C. and 60% relative humidity.
5. The solution of claim 1 , wherein the solution is particulate-matter-free.
6. The solution of claim 1 , wherein methocarbamol is present in an amount from about 1 mg/ml to about 7 mg/ml.
7. The solution of claim 1 , wherein methocarbamol is present in an amount from about 3 mg/ml to about 7 mg/ml.
8. The solution of claim 1 , wherein the solution has an osmotic pressure of about 250-350 mOsmol/Kg.
9. The solution of claim 1 , wherein the solution has a pH of from about 3.5 to about 4.5.
10. The solution of claim 1 , wherein the solution has a pH of about 4.0 to about 4.5.
11. The solution of claim 1 , wherein the solution has about 1.0% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 3 months at 25° C. and 60% relative humidity.
12. The solution of claim 11 , wherein the solution has about 0.5% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 3 months at 25° C. and 60% relative humidity.
13. The solution of claim 1 , wherein the solution has about 1.0% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 6 months at 25° C. and 60% relative humidity.
14. The solution of claim 13 , wherein the solution has about 0.5% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 6 months at 25° C. and 60% relative humidity.
15. The solution of claim 1 , wherein the solution has about 1.0% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 12 months at 25° C. and 60% relative humidity.
16. The solution of claim 15 , wherein the solution has about 0.5% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 12 months at 25° C. and 60% relative humidity.
17. The solution of claim 1 , wherein the solution has about 1.0% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 24 months at 25° C. and 60% relative humidity.
18. The solution of claim 17 , wherein the dosage form has about 0.5% w/w or less of 1-hydroxy-3-(2-methoxyphenoxy)propan-2-yl carbamate after storage for at least 24 months at 25° C. and 60% relative humidity.
19. A method of minimizing an adverse health effect associated with methocarbamol administration to a subject, comprising: intravenously administering a therapeutically effective amount of methocarbamol to the subject in a solution as recited in claim 1 .
20. An injectable methocarbamol solution for intravenous administration comprising:
methocarbamol in an amount from about 1 mg/ml to less than 10 mg/ml;
a tonicity agent, wherein the tonicity agent is selected from the group consisting of sodium chloride, mannitol, sorbitol, dextrose, ethanol, glycerin, propylene glycol, and combinations thereof;
a buffer selected from (I) sodium citrate and citric acid or (II) sodium acetate and acetic acid; and
water,
wherein the solution is isotonic, has a pH of about 3 to about 5, is free of polyethylene glycol (PEG), and contains no more than 2.0% w/w of guaifenesin after storage at ambient temperature for at least 3 months.