Injection medicine composition containing glucocorticoid and NOS (nitric oxide synthase) inhibitor

Abstract

The invention discloses an injection medicine composition containing glucocorticoid and NOS (nitric oxide synthase) inhibitor, containing glucocorticoid which is used as an active ingredient, NOS inhibitor, and one or more pharmaceutical excipients suitable for injection.

Description

technical field

[0001] The invention relates to a pharmaceutical composition, an injection pharmaceutical composition containing corticosteroids and NOS inhibitors. Background technique

[0002] Glucocorticoids have anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and are widely used in the treatment of allergic and autoimmune inflammatory diseases. Such as connective tissue disease, active rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, severe dermatitis, ulcerative colitis, acute leukemia, etc. It is also used for some serious infections, poisoning, and malignant lymphoma. treat. Although glucocorticoids are widely used, they are likely to cause many side effects when used for a long time or in large doses, such as Cushing's syndrome, osteoporosis, aseptic femoral head necrosis, and the induction and aggravation of infection.

[0003] NO is an inorganic small molecule with a wide range of biological function...

Examples

Embodiment 1

[0020] Embodiment 1, the preparation of glucocorticoid cyclodextrin increasing solution

[0021] Example number

[0022] Dissolve 6g of cyclodextrin in 100ml of 95% ethanol at room temperature, add 1g of glucocorticoid under nitrogen protection, stir to dissolve, stir for another 30 minutes, filter, add 50ml of water for injection, stir for 5 minutes, concentrate under reduced pressure, evaporate Remove ethanol to obtain glucocorticoid / cyclodextrin solution for later use.

Embodiment 2

[0023] Embodiment 2, the preparation of NOS inhibitor cyclodextrin solubilization solution, the obtained cyclodextrin solubilization solution

[0024] Example number

[0025] Dissolve 5 g of cyclodextrin in 100 ml of 95% ethanol at room temperature, add 1 g of NOS inhibitor under nitrogen protection, stir, stir for another 30 minutes, filter, add 50 ml of water for injection, stir for 5 minutes, concentrate under reduced pressure, evaporate ethanol, The NOS inhibitor / cyclodextrin liquid was obtained and kept under nitrogen protection for later use.

Embodiment 1

[0026]Formulation Example 1 (injection containing cyclodextrin)

[0027] Active ingredient:

[0028] Hydrocortisone Cyclodextrin Solubilization Solution (1-5) Equivalent to Hydrocortisone 10.0g

[0029] Aminoguanidine hydrochloride cyclodextrin solubilization solution (2-7) equivalent to aminoguanidine 1g

[0030] Accessories:

[0031]

[0032] Take the prescribed amount of hydrocortisone cyclodextrin solubilization solution, aminoguanidine hydrochloride cyclodextrin solubilization solution, propylene glycol, sodium pyrosulfite, and sodium chloride and dissolve them in part of the water for injection, and use disodium hydrogen phosphate, dihydrogen phosphate Adjust the pH of the sodium buffer solution to 6.8, add water for injection to 1000ml, sterilize, and pack aseptically. Obtaining injection dosage is hydrocortisone 10mg / ml, aminoguanidine 1mg / ml.

technical field

[0001] The invention relates to a pharmaceutical composition, an injection pharmaceutical composition containing corticosteroids and NOS inhibitors. Background technique

[0002] Glucocorticoids have anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and are widely used in the treatment of allergic and autoimmune inflammatory diseases. Such as connective tissue disease, active rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, severe dermatitis, ulcerative colitis, acute leukemia, etc. It is also used for some serious infections, poisoning, and malignant lymphoma. treat. Although glucocorticoids are widely used, they are likely to cause many side effects when used for a long time or in large doses, such as Cushing's syndrome, osteoporosis, aseptic femoral head necrosis, and the induction and aggravation of infection.

[0003] NO is an inorganic small molecule with a wide range of biological function...

Examples

Embodiment 1

[0020] Embodiment 1, the preparation of glucocorticoid cyclodextrin increasing solution

[0021] Example number

[0022] Dissolve 6g of cyclodextrin in 100ml of 95% ethanol at room temperature, add 1g of glucocorticoid under nitrogen protection, stir to dissolve, stir for another 30 minutes, filter, add 50ml of water for injection, stir for 5 minutes, concentrate under reduced pressure, evaporate Remove ethanol to obtain glucocorticoid / cyclodextrin solution for later use.

Embodiment 2

[0023] Embodiment 2, the preparation of NOS inhibitor cyclodextrin solubilization solution, the obtained cyclodextrin solubilization solution

[0024] Example number

[0025] Dissolve 5 g of cyclodextrin in 100 ml of 95% ethanol at room temperature, add 1 g of NOS inhibitor under nitrogen protection, stir, stir for another 30 minutes, filter, add 50 ml of water for injection, stir for 5 minutes, concentrate under reduced pressure, evaporate ethanol, The NOS inhibitor / cyclodextrin liquid was obtained and kept under nitrogen protection for later use.

Embodiment 1

[0026]Formulation Example 1 (injection containing cyclodextrin)

[0027] Active ingredient:

[0028] Hydrocortisone Cyclodextrin Solubilization Solution (1-5) Equivalent to Hydrocortisone 10.0g

[0029] Aminoguanidine hydrochloride cyclodextrin solubilization solution (2-7) equivalent to aminoguanidine 1g

[0030] Accessories:

[0031]

[0032] Take the prescribed amount of hydrocortisone cyclodextrin solubilization solution, aminoguanidine hydrochloride cyclodextrin solubilization solution, propylene glycol, sodium pyrosulfite, and sodium chloride and dissolve them in part of the water for injection, and use disodium hydrogen phosphate, dihydrogen phosphate Adjust the pH of the sodium buffer solution to 6.8, add water for injection to 1000ml, sterilize, and pack aseptically. Obtaining injection dosage is hydrocortisone 10mg / ml, aminoguanidine 1mg / ml.

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