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Urapidil hydrochloride injection and preparation method thereof

A technology of urapidil hydrochloride and injection, which can be applied to pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. It can improve the stability, reduce the probability of deterioration, and promote the effect of large-scale industrial production.

Inactive Publication Date: 2022-01-04
SHIJIAZHUANG NO 4 PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the pharmaceutical preparations mainly include injections, freeze-dried powder injections, tablets, capsules, etc., and the tablets and capsules are all oral preparations, because the first The effect of the drug is reduced due to over-effect; the freeze-dried powder injection needs to be reconstituted before use, which is inconvenient for clinical use and has the risk of cross-contamination
In order to improve the curative effect, urapidil hydrochloride can be made into injection, thereby avoiding the first-pass effect, but urapidil hydrochloride has problems such as poor stability, easy decomposition and deterioration in the injection solution, and these problems seriously limit the injection of urapidil hydrochloride. Wide application of liquid

Method used

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  • Urapidil hydrochloride injection and preparation method thereof
  • Urapidil hydrochloride injection and preparation method thereof
  • Urapidil hydrochloride injection and preparation method thereof

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Embodiment 1

[0033] The embodiment of the present invention provides a kind of urapidil hydrochloride injection, and every 1000mL of urapidil hydrochloride injection contains the following raw materials: 5 g of urapidil hydrochloride, 100 g of polyethylene glycol, 0.3 g of citric acid and 2.6 g of sodium citrate g, the pH value of the urapidil hydrochloride injection is 6.2.

[0034] The preparation method of above-mentioned urapidil hydrochloride injection comprises the following steps:

[0035] Step 1: weighing each component according to the above-mentioned raw material ratio;

[0036] Step 2: Cool down the water for injection of 60% of the total volume of the preparation to 50° C., under nitrogen protection, add urapidil hydrochloride, polyethylene glycol, citric acid and sodium citrate, dissolve evenly and add at a temperature of The remaining water for injection at 50°C was adjusted to a pH value of 6.2, filtered through a polyethersulfone filter element with a pore size of 0.45 μm ...

Embodiment 2

[0039] The embodiment of the present invention provides a kind of urapidil hydrochloride injection, and every 1000mL of urapidil hydrochloride injection contains the following raw materials: 5 g of urapidil hydrochloride, 100 g of polyethylene glycol, 0.3 g of citric acid and 3.3 g of sodium citrate g, the pH value of the urapidil hydrochloride injection is 6.3.

[0040] The preparation method of above-mentioned urapidil hydrochloride injection comprises the following steps:

[0041] Step 1: weighing each component according to the above-mentioned raw material ratio;

[0042] Step 2: The water for injection of 80% of the total volume of the preparation is cooled to 30°C, under the protection of nitrogen, add urapidil hydrochloride, polyethylene glycol, citric acid and sodium citrate, and add the temperature after dissolving evenly. For the remaining water for injection at 45°C, adjust the pH value to 6.3, filter through a polyethersulfone filter element with a pore size of 0....

Embodiment 3

[0045] The embodiment of the present invention provides a kind of urapidil hydrochloride injection, and every 1000mL of urapidil hydrochloride injection contains the following raw materials: 5 g of urapidil hydrochloride, 100 g of polyethylene glycol, 0.3 g of citric acid and 2.3 g of sodium citrate g, the pH value of the urapidil hydrochloride injection is 6.1.

[0046] The preparation method of above-mentioned urapidil hydrochloride injection comprises the following steps:

[0047] Step 1: weighing each component according to the above-mentioned raw material ratio;

[0048] Step 2: Cool down the water for injection of 70% of the prepared total volume to 35° C., under nitrogen protection, add urapidil hydrochloride, polyethylene glycol, citric acid and sodium citrate, dissolve evenly and add at a temperature of For the remaining water for injection at 40°C, adjust the pH value to 6.1, filter through a polyethersulfone filter element with a pore size of 0.45 μm and a polyethe...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses an urapidil hydrochloride injection and a preparation method thereof. In the urapidil hydrochloride injection, every 1000 mL of the urapidil hydrochloride injection comprises the following raw materials: 5 g of urapidil hydrochloride, 100 g of an osmotic pressure regulator and an acid-base buffer pair, and the pH value of the urapidil hydrochloride injection is 5.9-6.5. According to the invention, citric acid-sodium citrate, acetic acid-sodium acetate, citric acid-disodium hydrogen phosphate or phosphoric acid-sodium phosphate are used as acid-base buffer pairs, and the pH value of the injection is adjusted to 5.9-6.5, so that the stability of the injection is remarkably improved. In the preparation process of the injection, the adding and mixing sequence of the main drug urapidil hydrochloride and other auxiliary materials is adjusted, and the temperature in the preparation process is controlled to be lower than 60 DEG C, so that the deterioration probability of urapidil hydrochloride is effectively reduced, and the stability of the injection is remarkably improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to urapidil hydrochloride injection and a preparation method thereof. Background technique [0002] Urapidil hydrochloride is a uracil derivative substituted by phenylpiperazine. It is currently an effective and safe vasodilator for the treatment of hypertensive crisis, severe hypertension, control of hypertension during surgery, and treatment of congestive heart failure. It is a national essential drug. In addition, urapidil hydrochloride generally does not cause reflex tachycardia while lowering blood pressure. [0003] At present, the pharmaceutical preparations mainly include injections, freeze-dried powder injections, tablets, capsules, etc. Among them, tablets and capsules are all oral preparations, and the drug efficacy is reduced due to the unavoidable first-pass effect; freeze-dried powder injections need to be reconstituted after reconstitution. Reuse ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/513A61K47/02A61K47/10A61K47/12A61P9/04A61P9/12
CPCA61K31/513A61K9/08A61K9/0019A61K47/12A61K47/02A61K47/10A61P9/12A61P9/04
Inventor 王立江李丽王恰茹王晖李鑫燕磊李翠芸
Owner SHIJIAZHUANG NO 4 PHARMA
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