Platinum pharmaceutic preparation as well as preparation method and application thereof

Abstract

The invention relates to a platinum pharmaceutic preparation as well as a preparation method and application thereof. The platinum pharmaceutic preparation is prepared from the following medicinal compositions: (1) 70 to 80 parts of platinum compounds; (2) 0.1 to 0.2 part of alprostadil, and also contains pharmaceutical excipients; according to the preparation method provided by the invention, the platinum compounds and alprostadil are added in tertiary butanol, stirring is performed at the temperature of 30 to 40 DEG C for fully dissolving, isopropyl alcohol is added and uniformly stirred, and then filtering, filling and drying are performed, so as to obtain the platinum pharmaceutic preparation. The platinum pharmaceutic preparation provided by the invention can be applied to antineoplastic drugs, especially can be applied to drugs for treating liver cancer. The platinum pharmaceutic preparation provided by the invention has high curative effect and lower toxicity.

Description

technical field

[0001] The invention relates to the field of medicines, in particular to a platinum drug preparation and its preparation method and application. Background technique

[0002] Since people discovered that cisplatin has anticancer activity, the application and research of platinum-based metal anticancer drugs have developed rapidly. Today, platinum-based drugs have become an indispensable drug in cancer chemotherapy. Platinum antineoplastic drugs currently used clinically include cisplatin, carboplatin, oxaliplatin, nedaplatin, lobaplatin, heptaplatin and the like.

[0003] Miriplatin Hydrate is a new fat-soluble platinum antitumor drug developed by Sumitomo Corporation of Japan. The cultural name is (SP-4-2)-[(1R,2R)-1,2cyclohexanediamine-N,N']bis(tetradecanoic acid-O)platinum hydrate, and the English chemical name is (SP-4-2)-[(1R,2R)-Cyclohexane-1,2-diamine-N,N']bis(tetradecanoatoO)platinummonohydrate, the molecular formula is C 34 h 68 N 2 o 4 Pt H ...

Examples

Embodiment 1

[0050] 1.1 Recipe

[0051]

[0052] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0053] 1.2 Preparation process

[0054] (1) Weighing: take by weighing the rice platinum, alprostadil, tert-butanol and isopropanol of formula quantity;

[0055] (2) Preparation: Add the formula amount of rice platinum and alprostadil to tert-butanol, and ultrasonically stir at a temperature of 30-40°C to dissolve completely, then add the formula amount of isopropanol and stir evenly;

[0056] (3) Filtration: use a 0.22 μm filter membrane to sterilize and filter;

[0057] (4) Filling: After the intermediate is qualified, the liquid medicine is filled in a 40mL vial and half stoppered;

[0058] (5) Freeze-drying: Cool down the empty box of the freeze-drying box to below -40°C, put the sample in the freeze-drying box, pre-freeze at -40°C, and keep it for 3-4h; in the sublimation drying stage, the shelf temperature is 5°C / hour R...

Embodiment 2

[0062] 1.1 Recipe

[0063]

[0064] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0065] 1.2 Preparation process

[0066] With embodiment 1.

Embodiment 3

[0068] 1.1 Recipe

[0069]

[0070] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0071] 1.2 Preparation process

[0072] With embodiment 1.

technical field

[0001] The invention relates to the field of medicines, in particular to a platinum drug preparation and its preparation method and application. Background technique

[0002] Since people discovered that cisplatin has anticancer activity, the application and research of platinum-based metal anticancer drugs have developed rapidly. Today, platinum-based drugs have become an indispensable drug in cancer chemotherapy. Platinum antineoplastic drugs currently used clinically include cisplatin, carboplatin, oxaliplatin, nedaplatin, lobaplatin, heptaplatin and the like.

[0003] Miriplatin Hydrate is a new fat-soluble platinum antitumor drug developed by Sumitomo Corporation of Japan. The cultural name is (SP-4-2)-[(1R,2R)-1,2cyclohexanediamine-N,N']bis(tetradecanoic acid-O)platinum hydrate, and the English chemical name is (SP-4-2)-[(1R,2R)-Cyclohexane-1,2-diamine-N,N']bis(tetradecanoatoO)platinummonohydrate, the molecular formula is C 34 h 68 N 2 o 4 Pt H ...

Examples

Embodiment 1

[0050] 1.1 Recipe

[0051]

[0052] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0053] 1.2 Preparation process

[0054] (1) Weighing: take by weighing the rice platinum, alprostadil, tert-butanol and isopropanol of formula quantity;

[0055] (2) Preparation: Add the formula amount of rice platinum and alprostadil to tert-butanol, and ultrasonically stir at a temperature of 30-40°C to dissolve completely, then add the formula amount of isopropanol and stir evenly;

[0056] (3) Filtration: use a 0.22 μm filter membrane to sterilize and filter;

[0057] (4) Filling: After the intermediate is qualified, the liquid medicine is filled in a 40mL vial and half stoppered;

[0058] (5) Freeze-drying: Cool down the empty box of the freeze-drying box to below -40°C, put the sample in the freeze-drying box, pre-freeze at -40°C, and keep it for 3-4h; in the sublimation drying stage, the shelf temperature is 5°C / hour R...

Embodiment 2

[0062] 1.1 Recipe

[0063]

[0064] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0065] 1.2 Preparation process

[0066] With embodiment 1.

Embodiment 3

[0068] 1.1 Recipe

[0069]

[0070] Note: [1], [2] The final product of the preparation does not appear, and it is removed during freeze-drying.

[0071] 1.2 Preparation process

[0072] With embodiment 1.

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