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Alprostadil injection

A technology of dil injection and alprostadil, which is used in medical preparations with non-active ingredients, blood diseases, extracellular fluid diseases, etc. The effect of droplet aggregation, prevention of oxidation reaction, and improved safety

Active Publication Date: 2014-12-10
北京德立英捷医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The preparation process of fat emulsion is relatively complicated, and requires the participation of water phase to form a water-in-oil or oil-in-water system, and high-pressure homogenization process will generate local high temperature, these processes will inevitably lead to the degradation of alprostadil and the oxidation of phospholipids , thus affecting the stability of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The alprostadil non-aqueous injection provided by the present embodiment includes:

[0037] Alprostadil 0.001-0.05mg / mL, oil phase 0.01-100mg / mL, phospholipid 10-500mg / mL, and the rest are organic solvents.

[0038] In the above prescription, the phospholipids include at least one of the following: natural phospholipids and synthetic phospholipids.

[0039] The oil phase includes at least one of the following: soybean oil, corn oil, castor oil, olive oil, coconut oil, peanut oil, fish oil, cottonseed oil, glyceryl monostearate, glyceryl monooleate, sesame oil, red Flower Oil, Medium Chain Triglycerides, Ethyl Oleate.

[0040] The organic solvent includes at least one of the following: ethanol, glycerin, propylene glycol, polyethylene glycol.

[0041] The medium chain triglycerides (Medium chain triglycerides, MCT) mentioned in this example refers to the esterification of fatty acids containing 6-12 carbon atoms by glycerol. Wherein preferred MCT refers to saturated c...

Embodiment 2 Embodiment 10

[0063] Following table 1 is the prescription of the alprostadil injection that embodiment two to ten provides.

[0064] The preparation methods of the above-mentioned nine embodiments are basically similar, for example, adding alprostadil to an appropriate amount of absolute ethanol or other organic solvents, and after completely dissolving, add lecithin, soybean oil, oleic acid and the remaining prescription amount of absolute ethanol , stir at room temperature to form a transparent and clear liquid composition after mixing them uniformly, and the order of adding or dissolving each component can be changed according to the actual prescription.

[0065] The alprostadil injection prescription of table 1 embodiment two to ten

[0066]

[0067]

[0068] In the above-mentioned embodiment 2, in clinical application, the injection is diluted 1 to 100 times before use, and the effect is better, and it is more preferable to dilute it 10 times.

[0069] In order to further illus...

Embodiment 11

[0071] Determination of Particle Size of Alprostadil Injection

[0072] experiment method:

[0073] Take 0.1 mL of the injection prepared in Example 2, add purified water (pre-filtered with a membrane with a pore size of 0.22 μm) and dilute it 5000 times, mix well, and use it as the test solution, use a Malvern laser particle size analyzer (Zetasizer 3000HS, Malvem, UK ) to measure the particle size and distribution of the above liquid to be tested at 25°C.

[0074] result:

[0075] Particle size distribution see figure 1 , the average particle size is 146.0nm, and the PDI is 0.177. It can be seen that the injection provided by the invention is suitable for intravenous injection.

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Abstract

The invention belongs to the field of a pharmaceutical preparation, and in particular relates to an alprostadil injection. The injection consists of 0.001-0.05mg / ml of alprostadil, 0.01-100mg / ml of an oil phase, 10-500mg / ml of phospholipid and the balance of an organic solvent. The injection disclosed by the invention is constantly an anhydrous system in storage process, and is used right as long as being ready, so that the injection can prevent oxidization reaction of the phospholipid and degradation reaction of the medicine, and can improve the stability of the alprostadil injection. An alprostadil composition provided by the invention can prepare the alprostadil injection which is excellent in stability, and the preparation process is quite simple.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to alprostadil injections. Background technique [0002] Alprostadil aka prostaglandin E 1 (Alprostadil), abbreviated as PGE 1 , which is a highly active endogenous physiologically active substance, which has obvious activities such as dilating blood vessels and inhibiting platelet aggregation. The first to go on the market is its freeze-dried powder injection. Due to its rapid metabolism in the body, under the action of lung oxidase, 60% to 90% of it will be inactivated every time it passes through the pulmonary circulation. unbearable. [0003] Alprostadil fat emulsion was launched in Japan in 1988, and PGE1 was encapsulated in lipid microspheres with a diameter of 0.2 μm. Lipid microspheres are ideal drug carriers and have special affinity for diseased blood vessels, and can transport PGE1 to specific blood vessels. At the same time, under the barrier protection of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5575A61K47/44A61K47/24A61K47/34A61P7/02
Inventor 吴翠栓马风中曹晴
Owner 北京德立英捷医药科技有限公司
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