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Alprostadil injection and preparation method thereof

A technology of dil injection and alprostadil, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and drug delivery, can solve the problems of demulsification, inconvenient operation, high viscosity, etc., and achieves high content of the main drug. , good stability, less related substances

Active Publication Date: 2014-02-26
SICHUAN KELUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the study of dosage forms, lipid emulsion (lipid microspheres) is the most successful, but this technology still has the defect of instability of the main drug; on this basis, a sterile filtration method is proposed, such as application number: 200810064654.5; 200910091207.3 , but the emulsion requires a particle size of about 200 nanometers. At this time, the viscosity is relatively high, and filtration is difficult. Even if it is heated and filtered, it will inevitably break the emulsion. At the same time, bacteria may also squeeze through, and the sterility level is difficult to guarantee; No.: 200510028341.0; 201210065141.2) proposed freeze-dried milk. In addition to the previous filtration problems and the difficulty in ensuring sterility, due to the increase in the freeze-drying process and the addition of a freeze-drying protective agent, the freeze-dried milk particles are easy to grow and break. Clinical application requires Reconstitution is not only inconvenient to operate, but also increases the cost of the preparation, and at the same time increases the clinical risk accordingly
It is also reported in the literature that by adding excipients (such as application number: 200910058187.X; 201110104824.X) poloxamer, etc., poloxamer itself is a surfactant, which increases the chance of hemolysis and also brings safety hazards, not applicable Human application

Method used

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  • Alprostadil injection and preparation method thereof
  • Alprostadil injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] 1) Add 18g of lecithin, 2.4g of oleic acid and 5mg of alprostadil into 100g of soybean oil, heat to 70±2°C and stir to dissolve, as the oil phase;

[0029] 2) Add 22.5 g of isotonic agent glycerin and pH regulator sodium hydroxide to water, heat to 65±2°C, stir and mix, filter, and use as water phase, the volume of the prepared water phase is 9 times that of the oil phase;

[0030] 3) Stir and mix the water phase and the oil phase to form colostrum, and add water for injection to 1000ml. Then homogenize under high pressure, filter and sterilize.

Embodiment 2

[0032] 1) Add 18g of lecithin, 2.4g of oleic acid and 5mg of alprostadil into 100g of soybean oil, heat to 70±2°C and stir to dissolve, as the oil phase;

[0033] 2) Add 22.5g of isotonic agent glycerin and pH regulator sodium hydroxide into water, heat to 65±2°C, stir and mix, filter, and use as water phase, the volume of the prepared water phase is 8 times that of the oil phase;

[0034] 3) Stir and mix the water phase and the oil phase to form colostrum, and add water for injection to 1000ml. Then homogenize under high pressure, filter and sterilize.

Embodiment 3

[0036] 1) Add 18g of lecithin, 2.4g of oleic acid and 5mg of alprostadil into 100g of soybean oil, heat to 70±2°C and stir to dissolve, as the oil phase;

[0037] 2) Add 22.5g of isotonic agent glycerin and pH regulator sodium hydroxide to water, heat to 65±2°C, stir and mix, filter, and use it as the water phase, the volume of the prepared water phase is 7 times that of the oil phase;

[0038] 3) Stir and mix the water phase and the oil phase to form colostrum, and add water for injection to 1000ml. Then homogenize under high pressure, filter and sterilize.

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Abstract

The invention provides an alprostadil injection. Every 1000ml of alprostadil injection comprises the following raw materials: 5mg of alprostadil, 90-110g of soybean oil, 15-20g of phosphatide, 2-3g of oleic acid, 22.1-25g of isoosmotic agent, and appropriate pH modifier, wherein the content of the pH modifier is enough to regulate the pH of the injection to be 5.0-6.0. The invention also provides a preparation method for the alprostadil injection. Compared with the prior art, the alprostadil injection prepared by the method has higher encapsulation efficiency and content of main drug, contains fewer related substances, has good stability, and provides safety guarantee for clinical medication.

Description

technical field [0001] The invention relates to an alprostadil injection and a preparation method thereof. Background technique [0002] Alprostadil (PGE1), its structural formula is as follows: [0003] [0004] It is a bioactive substance widely present in the body and can treat diabetic neuropathy. [0005] It can be seen from its compound structure that the compound is extremely sensitive to heat and unstable in aqueous solution, so there are reports or patents (patent application number: 200310102253.1), which require the preparation of alprostadil for injection at a temperature below 45°C or by adding cyclodextrin. Inclusion. [0006] However, the inactivation time of alprostadil powder for injection in the body is very fast, the dosage is large, and the side effects are obvious. Therefore, scientists continue to explore how to improve the curative effect and reduce side effects. In the study of dosage forms, lipid emulsion (lipid microspheres) is the most succe...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/5575A61K47/44A61P3/10A61P25/00
Inventor 欧苏陈香梅朱志新
Owner SICHUAN KELUN PHARMA CO LTD
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