You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 4,997,651


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 4,997,651
Title: Pharmaceutical formulations
Abstract:The present invention relates to a new two-component pharmaceutical formulation of melphalan in which the two components comprise (a) freeze-dried mephalan hydrochloride and (b) a solvent-diluent comprising a citrate, propylene glycol and ethanol. Substantially pure melphalan, substantially pure melphalan hydrochloride and methods for preparing them are also described.
Inventor(s): Poole; Stephen W. (Dartford, GB2), Stanley; Timothy P. (Dartford, GB2), Divall; Geoffrey (Dartford, GB2), Packham; Terence W. (Dartford, GB2), Knight; Joseph (Dartford, GB2)
Assignee:
Application Number:07/273,227
Patent Claims: 1. A pharmaceutical formulation of melphalan comprising as two separate components

(a) freeze-dried melphalan hydrochloride, and

(b) a solvent-diluent comprising a citrate, propylene glycol and ethanol.

2. A pharmaceutical formulation according to claim 1 wherein component (a) includes a non-hydroxylated matrix-forming agent.

3. A pharmaceutical formulation according to claim 2 wherein the non-hydroxylated matrix-forming agent is polyvinylpyrrolidone.

4. A pharmaceutical formulation according to claim 1 wherein the citrate is an alkali metal citrate.

5. A method for preparing a pharmaceutical formulation of melphalan which comprises formulating as two separate components

(a) freeze-dried melphalan hydrochloride and

(b) a solvent-diluent comprising a citrate, propylene glycol and ethanol.

6. A pharmaceutical formulation according to claim 1, wherein the melphalan hydrochloride is in substantially pure form.

7. A pharmaceutical formulation according to claim 6, wherein the substantially pure melphalan hydrochloride is prepared by heating a mixture of melphalan and hydrogen chloride in a C.sub.2-4 alkanol for up to five minutes and cooling to effect crystallization of melphalan hydrochloride.

8. A pharmaceutical formulation according to claim 6, wherein the melphalan hydrochloride is prepared by reacting ethyl N-phthaloyl-p-amino-L-phenylalnine or an acid addition salt thereof with ethylene oxide such that the reaction temperature does not exceed 35.degree. C. followed by the steps of chlorination and hydrolysis and conversion into the hydrochloride salt.

9. A pharmaceutical formulation according to either claim 2 or claim 3, wherein the matrix-forming agent constitutes 20-95% by weight of component (a).

10. A pharmaceutical formulation according to claim 4, wherein the alkali metal citrate is selected from sodium and potassium citrate.

11. A pharmaceutical formulation according to claim 1, wherein component (b) contains 40-80% by volume of propylene glycol.

12. A pharmaceutical formulation according to claim 1, wherein component (b) contains 0.1-10% by volume of ethanol.

13. A pharmaceutical formulation according to claim 1, wherein component (b) contains 0.05-5% w/v of the citrate.

14. A pharmaceutical formulation according to claim 1, in the form of a unit dose containing from 1-100 mg of melphalan and from 1-50 ml of solvent-diluent.

15. A pharmaceutical formulation according to claim 14, containing 10 mg of melphalan and 10 ml of solvent-diluent.

16. A pharmaceutical formulation according to claim 14, containing 50 mg of melphalan and 10 ml of the solvent-diluent.

Make Better Decisions: Try a trial or see plans & pricing

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 verification 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.