WO2016170489A4 - Pharmaceutical compositions of proteasome inhibitor - Google Patents
Pharmaceutical compositions of proteasome inhibitor Download PDFInfo
- Publication number
- WO2016170489A4 WO2016170489A4 PCT/IB2016/052261 IB2016052261W WO2016170489A4 WO 2016170489 A4 WO2016170489 A4 WO 2016170489A4 IB 2016052261 W IB2016052261 W IB 2016052261W WO 2016170489 A4 WO2016170489 A4 WO 2016170489A4
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pharmaceutical composition
- amount
- composition according
- carfilzomib
- solvent
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/40—Cyclodextrins; Derivatives thereof
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- General Chemical & Material Sciences (AREA)
- Gastroenterology & Hepatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Dermatology (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention relates to a stable ready to use pharmaceutical composition comprising the proteasome inhibitor carfilzomib or pharmaceutically acceptable salt thereof.
Claims
1. A non aqueous ready to use liquid pharmaceutical composition comprising:
i. carfilzomib or a pharmaceutically acceptable salt thereof,
li. at least one organic solvent, and
iii. a solubilizer wherein the solubilizer is selected from hydroxypropylbeta cyclodextrin (HPBCD), sulfobutyletherbetacyclodextrin (SBECD) and mixtures thereof.
2. The pharmaceutical composition according to claim 1, wherein the concentration of the carfilzomib ranges from 100 to 1000 mg per 100 ml.
3. The pharmaceutical composition according to claim 1, wherein said organic solvent is selected from at least one protic solvent, at least one aprotic solvent, and mixtures thereof.
4. The pharmaceutical composition according to daim 3, comprising a mixture of a first protic solvent and a second protic solvent.
5. The pharmaceutical composition according to claim 4, wherein the ratio of the first protic solvent to the second protic solvent ranges from 1:0.1-1:5 v/v.
6. The pharmaceutical composition according to claim 3, comprising a mixture of protic solvents and an aprotic solvent.
7. The pharmaceutical composition according to claim 6, wherein the ratio of the protic solvents to the aprotic solvent ranges from 1:0.1-1:5 v/v
8. The pharmaceutical composition according to claim 3, wherein the at least one protic solvent is selected from the group consisting of methanol, ethanol, ethylene glycol, propylene glycol, butylene glycol, glycerin, a polyalkylene glycol selected from polyethylene glycol, polypropylene glycol, polybutylene glycol, and mixtures thereof.
9. The pharmaceutical composition according to daim 3, wherein the at least one aprotic solvent is selected from the group consisting of l-methyl-2-pyrrolidone, 1,3-
dimethyl-2-imidazolidinone, dimethylacetamlde, dimethyl sulfoxide, acetone, tetrahydrofuran, 1,4-dloxane, acetonitrile, dimethyl formamide, propylene carbonate, and mixtures thereof.
10. The pharmaceutical composition according to claim 1, wherein (a) the organic solvent comprises propylene glycol and ethanol, (b) the solubilizer is HPBCD, and (c) the composition further comprises citric acid.
11. The pharmaceutical composition according to claim 1, wherein (a) the organic solvent comprises dimethylacetamlde, propylene glycol and ethanol, (b) the solubilizer is HPBCD, and (c) the composition further comprises citric acid.
12. The pharmaceutical composition according to claim 10 comprising:
a) carfilzomib in an amount of 60 mg, b) anhydrous citric acid in an amount of 58 mg, c) propylene glycol and ethanol in an amount of 12 mL, and d) HPBCD in an amount of 1000 mg.
13. The pharmaceutical composition according to claim 10 comprising:
a) carfilzomib in an amount of 60 mg, b) anhydrous citric acid in an amount of 58 mg, c) propylene glycol and ethanol in an amount of 20 mL, and d) HPBCD in an amount of 1000 mg
14. The pharmaceutical composition according to daim 11 comprising:
a) carfilzomib in an amount of 60 mg,
b) anhydrous citric acid in an amount of 30 mg,
c) dimethylacetamlde in an amount of 0.6 mL
d) propylene glycol and ethanol in an amount of 6 mL, and
e) HPBCD in an amount of 2000 mg
15. The pharmaceutical composition according to claim 10, wherein the weight ratio of citric acid to carfllzomlb is about 1:1 and the weight ratio of HPBCD to carfilzomib is about 16.6:1.
16. A method of preparing the pharmaceutical composition according to claim 1, comprising the steps of:
(a) dissolving 1-100 ml of a first organic solvent with about 8500 mg of cyclodextrin to form a first solution,
(b) dissolving 500 mg of carfilzomib in a second organic solvent in a separate vessel,
(c) dissolving 485 mg of citric acid into the solution of step b to form a second solution
(d) mixing the first and second solutions to form a third solution,
(e) making the volume of the third solution up to 100 ml.
17. The method according to claim 16, wherein the organic solvents are independently selected from at least one protic solvent, at least one aprotic solvent, and mixtures thereof.
18. A container comprising the pharmaceutical composition according to any of daims 1- 15, wherein the container is a vial, ampule, or syringe, and wherein the composition is sterile.
19. A pharmaceutical composition according to any of claims 1-15 for use in the treatment of multiple myeloma.
20. The composition of any of claims 1-15, wherein following storage of the composition at 25 °C for a predetermined time period, the amount of any individual impurity present in the composition is not more than 0.5% relative to the amount of carfilzomib.
21. The composition of claim 20, wherein the predetermined time period is one month or three months.
22. The composition of any of claims 1-15, wherein following storage of the composition at 40 °C for a predetermined time period, the amount of any individual impurity
present in the composition is not more than 0.25% relative to the amount of carfilzomib.
23. The composition of claim 22, wherein the predetermined time period is one week.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN1143DE2015 | 2015-04-24 | ||
| IN1143/DEL/2015 | 2015-04-24 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2016170489A1 WO2016170489A1 (en) | 2016-10-27 |
| WO2016170489A4 true WO2016170489A4 (en) | 2016-12-15 |
Family
ID=56024342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/IB2016/052261 WO2016170489A1 (en) | 2015-04-24 | 2016-04-21 | Pharmaceutical compositions of proteasome inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2016170489A1 (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018138557A1 (en) * | 2017-01-24 | 2018-08-02 | Orbicular Pharmaceutical Technologies Pvt. Ltd. | Ready-to-use carfilzomib compositions |
| WO2019097413A1 (en) * | 2017-11-15 | 2019-05-23 | Intas Pharmaceuticals Ltd. | Stable non-aqueous pharmaceutical compositions |
| JP7422673B2 (en) * | 2017-12-08 | 2024-01-26 | ニューロジーエックス エルエルシー | Synchronized Cell Cycle Gene Expression Testing and Related Therapies for Alzheimer's Disease |
| JP2023522323A (en) * | 2020-04-15 | 2023-05-30 | カシーヴ バイオサイエンシズ，リミテッド・ライアビリティ・カンパニー | Carfilzomib formulation for straight stable dilution |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1745064E (en) | 2004-04-15 | 2011-03-23 | Proteolix Inc | Compounds for proteasome enzyme inhibition |
| PL2261236T3 (en) | 2004-12-07 | 2015-12-31 | Onyx Therapeutics Inc | Composition for proteasome inhibition |
| US9636376B2 (en) * | 2012-09-11 | 2017-05-02 | Innopharma, Inc. | Stable compositions of peptide epoxy ketones |
-
2016
- 2016-04-21 WO PCT/IB2016/052261 patent/WO2016170489A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| WO2016170489A1 (en) | 2016-10-27 |
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