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A kind of phentolamine mesylate injection and preparation method thereof

A technology of phentolamine mesylate and injection, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of alkali damage and oxidative damage instability, and product stability It has the advantages of good effect, low production cost, and prevention of oxidative damage.

Active Publication Date: 2022-02-11
DEYANG HUAKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The dosage forms of phentolamine mesylate on the market include tablets, capsules, suppositories and injections, etc. The application occasions of different dosage forms of phentolamine mesylate are different. Phentolamine mesylate injection is Diagnosis of pheochromocytoma and treatment of hypertensive episodes caused by it, including hypertension during surgical resection, treatment of left ventricular failure, treatment of norepinephrine spillover from intravenous administration, prevention of skin necrosis, etc. Application effect; however, because phentolamine mesylate is extremely unstable to alkali damage and oxidative damage, and it is also unstable under high temperature and light conditions, it is made into phentolamine mesylate injection product The stability is extremely poor and it is difficult to preserve, which has a great impact on the use and promotion of phentolamine mesylate injection

Method used

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  • A kind of phentolamine mesylate injection and preparation method thereof
  • A kind of phentolamine mesylate injection and preparation method thereof
  • A kind of phentolamine mesylate injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Raw materials: 16.32g of phentolamine mesylate, 0.68g of sodium metabisulfite, 3400g of mannitol, add 100ml-120ml of 3.6% dilute acetic acid, adjust the pH value to 3.8-4.0, add water for injection to 68L, and make 40000 sticks, each The size of the bottle is 1.7ml.

[0026] Preparation:

[0027] (1) medicinal solution configuration: a. take by weighing sodium metabisulfite and mannitol of prescription quantity, and dissolve it in the water for injection of 70% of prescription quantity; b. add the phentolamine mesylate of prescription quantity; c. Stir until fully dissolved; d. add water for injection to the prescribed amount; e. adjust the pH value to 3.8-4.0 with 3.6% dilute acetic acid solution; f. feed nitrogen into the prepared medicinal solution;

[0028] (2) Sterilization filling: a. Washing bottle: adopt neutral borosilicate glass ampoule, carry out the mode of dry heat sterilization in the tunnel oven after washing with water for injection, sterilization tempe...

Embodiment 2

[0031] Raw materials: 16.32g of phentolamine mesylate, 0.34g of sodium metabisulfite, 2040g of mannitol, add 2% dilute acetic acid, adjust the pH value to 4.0-4.2, add water for injection to 68L, and make 40,000 sticks, each with a specification of 1.7 ml.

[0032] Preparation:

[0033] (1) liquid medicine configuration: a. take by weighing sodium metabisulfite and mannitol of prescription quantity, and dissolve it in the water for injection of 65% of prescription quantity; b. add the phentolamine mesylate of prescription quantity; c. Stir until fully dissolved; d. add water for injection to the prescribed amount; e. adjust the pH value to 4.0-4.2 with 2% dilute acetic acid solution; f. feed nitrogen into the prepared medicinal solution;

[0034] (2) Sterilization filling: a. Washing bottle: adopt neutral borosilicate glass ampoule, carry out the mode of dry heat sterilization in the tunnel oven after washing with water for injection, sterilization temperature is 300-320 ℃, m...

Embodiment 3

[0037]Raw materials: 16.32g of phentolamine mesylate, 1.02g of sodium metabisulfite, 5440g of mannitol, add 5% dilute acetic acid, adjust the pH value to 3.8-4.2, add water for injection to 68L, and make 40,000 sticks, each with a specification of 1.7 ml.

[0038] Preparation:

[0039] (1) liquid medicine configuration: a. take by weighing sodium metabisulfite and mannitol of prescription quantity, and dissolve it in the water for injection of 60% of prescription quantity; b. add the phentolamine mesylate of prescription quantity; c. Stir until fully dissolved; d. add water for injection to the prescribed amount; e. adjust the pH value to 3.8-4.2 with 5% dilute acetic acid solution; f. feed nitrogen into the prepared medicinal solution;

[0040] (2) Sterilization filling: a. Washing bottle: adopt neutral borosilicate glass ampoule, carry out the mode of dry heat sterilization in the tunnel oven after washing with water for injection, sterilization temperature is 300-320 ℃, ma...

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PUM

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Abstract

The invention provides a kind of phentolamine mesylate injection, comprising phentolamine mesylate, antioxidant, osmotic pressure regulator, pH regulator and water for injection; The pH is 3.8‑4.2. The present invention also provides a preparation method of phentolamine mesylate injection, comprising the steps of: (1) liquid preparation: weighing prescription amount of phentolamine mesylate, antioxidant and osmotic pressure adjustment Dissolve it in water for injection, adjust the pH value to 3.8-4.2 with dilute acetic acid, and fill the mixed solution with nitrogen; (2) Sterilization potting: the mixed solution is filtered with a sterilizing grade filter element After filling and sealing, it is put into storage after passing the test, and it is filled with nitrogen for protection during the filling and sealing process. The phentolamine mesylate injection and the preparation method thereof of the present invention can effectively improve the stability of the phentolamine mesylate injection, so that it can be widely popularized and applied.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a phentolamine mesylate injection and a preparation method thereof. Background technique [0002] Phentolamine Mesylate is a short-acting non-selective α-receptor (α1, α2) blocker, which can antagonize epinephrine and norepinephrine in blood circulation, dilate blood vessels and reduce peripheral Vascular resistance; phentolamine mesylate also has the effect of antagonizing catecholamines, and is used for diagnosis and treatment of pheochromocytoma, but has little effect on blood pressure of normal people or patients with essential hypertension; in addition, phentolamine mesylate It can also reduce peripheral vascular resistance, reduce cardiac afterload, reduce left ventricular end-diastolic pressure and pulmonary artery pressure, increase cardiac output, and can be used to treat heart failure. [0003] The dosage forms of phentolamine mesylate on the market include tablets,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/417A61K47/02A61K47/10A61K47/12A61P9/04A61P35/00
CPCA61K31/417A61K9/0019A61K9/08A61K47/02A61K47/10A61K47/12A61P35/00A61P9/04
Inventor 黄晓平周国虎李开均
Owner DEYANG HUAKANG PHARMA
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