Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing
|Title:||Tigecycline compositions and methods of preparation|
|Abstract:||The present invention relates to novel tigecycline compositions with improved stability in both solid and solution states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid or buffer.|
|Inventor(s):||Fawzi; Mahdi B. (Morristown, NJ), Zhu; Tianmin (Monroe, NY), Shah; Syed M. (Delray Beach, FL)|
|Assignee:||Wyeth LLC (New York, NY)|
1. A composition consisting of tigecycline, lactose, and an acid, wherein the molar ratio of tigecycline to lactose is between about 1:1.6 to about 1:3.3, and the pH of the
composition in a solution is between about 4.0 and about 5.0, wherein the acid is hydrochloric acid, and the composition further comprises tigecycline epimer in an amount that is not more than 2.56% as measured after storage of the composition at about
40.degree. C. and 75% relative humidity for not more 39 days.
2. The composition of claim 1, wherein the composition is lyophilized.
3. The composition according to claim 1 further comprising a pharmaceutically acceptable diluent.
4. The composition according to claim 3, wherein the pharmaceutically acceptable diluent is water, a saline, Lactated Ringer's Injection solution, or dextrose solution.
5. The composition of claim 1, wherein the pH of the composition in a solution is between 4.2 and about 4.8.
6. A composition prepared in accord with a process comprising combining lactose with tigecycline and water to form a solution; reducing the pH of the solution with hydrochloric acid to between about 4.0 and about 5.0; and lyophilizing the solution to dryness to prepare a lyophilized composition; wherein the lactose is capable of reducing epimer formation of tigecycline whereby the lyophilized composition further comprises tigecycline epimer in an amount that is not more than 2.56% as measured after storage of the lyophilized composition at about 40.degree. C. and 75% relative humidity for not more 39 days, and the molar ratio of tigecycline to lactose is between about 1:1.6 to about 1:3.3.
7. The composition of claim 6 further comprising combining the composition with a saline, Lactated Ringer's Injection solution or dextrose solution.
8. The composition of claim 6, wherein a solid is formed.
9. The composition of claim 6, wherein the pH of the solution is reduced to between about 4.2 and about 4.8.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.