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Alprostadil injection and preparation method thereof

The technology of dier injection and alprostadil is applied in the direction of medical formula, emulsion delivery, medical preparations containing active ingredients, etc., which can solve the inconvenience of transportation, production, storage and use, and the instability of alprostadil in water , the validity period is only 12 months, etc., to achieve good application prospects, enhance safety and stability, distinct creativity and practicability

Active Publication Date: 2012-09-12
HARBIN PHARMA GROUP BIOLOGICAL ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] But, because alprostadil is unstable when meeting water, in the production process of existing commercially available alprostadil injection products both at home and abroad, the residual probability method (such as sterilizing at 121°C for 8 minutes) terminal sterilization process or no Bacteria production process (trade name: Beichang), the sterility assurance value (SAL) of the product is low, even if the degradation rate of the drug after sterilization exceeds 15%, and it needs to be stored at an unconventional temperature (0-5°C), the validity period is only have 12 months
Product transportation, storage and use are very inconvenient

Method used

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  • Alprostadil injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Add 5mg alprostadil, 12g soybean lecithin (for injection) and 100g soybean oil into the container, and disperse with high shear for 15 minutes to dissolve to form an oil phase; get another container and add 850g water for injection, and 22g glycerin (for injection) ), 0.8g of poloxamer 188 was added and stirred at a low speed for 5 minutes to form a water phase, and the pH value of the water phase was adjusted to 5.5 with 25mM citric acid; After running, slowly add the oil phase, emulsify for 20 minutes to form colostrum, and set the volume to 1000ml. Put the colostrum into the feed port of the high-pressure micro-fluidic nano-disperser, and homogenize it for 3 times under the pressure of 18000-20000Psi. Filling, corking, capping. to a rotary water bath sterilizer, and sterilized at 126°C for 4 minutes (verified sterilization F 0 Value greater than 12, for the overkill method) to obtain.

Embodiment 2

[0058] Add 5mg alprostadil, 18g soybean lecithin (for injection) and 100g soybean oil into the container, and disperse with high shear for 15 minutes to dissolve to form an oil phase; get another container and add 850g water for injection, and 22g glycerin (for injection) ), 2g of Poloxamer 188 was added and stirred at low speed for 5 minutes to form a water phase, and the pH value of the water phase was adjusted to 5.5 with 25mM citric acid; Finally, slowly add the oil phase, emulsify for 20 minutes to form colostrum, and set the volume to 1000ml. Put the colostrum into the feed port of the high-pressure micro-jet nano-disperser, and homogenize it for 3 times under the pressure of 18000-20000Psi. Filling, corking, capping. to a rotary water bath sterilizer, and sterilized at 126°C for 4 minutes (verified sterilization F 0 Value greater than 12, for the overkill method) to obtain.

Embodiment 3

[0060] Add 10mg alprostadil, 18g soybean lecithin (for injection) and 100g soybean oil into the container, and disperse with high shear for 15 minutes to dissolve to form an oil phase; get another container and add 850g water for injection, and 22g glycerin (for injection) ), 2g of poloxamer 188 was added and stirred at a low speed for 5 minutes to form an aqueous phase, and the pH value of the aqueous phase was adjusted to be within 5.5 with 10mM citric acid; the aqueous phase was placed under the working head of a high-shear dispersing emulsifier, After running at high speed, slowly add the oil phase, emulsify for 20 minutes to form colostrum, and set the volume to 1000ml. Put the colostrum into the feed port of the high-pressure micro-fluidic nano-disperser, and homogenize it for 3 times under the pressure of 18000-20000Psi. Filling, corking, capping. to a rotary water bath sterilizer, and sterilized at 126°C for 4 minutes (verified sterilization F 0 Value greater than 12...

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Abstract

The invention relates to an alprostadil injection and a preparation method thereof. The alprostadil injection has a prescription as follows: a, a main drug is alprostadil with concentration of 5mu g-15mu g / ml; b, an oil phase is soybean oil with concentration of respectively 10.0-12.0 percent; c, soyabean lecithin and poloxamer 188 are selected as emulsifying agents and have concentrations of respectively 1.0-1.8 percent and 0.02-0.2 percent; d, citric acid is adopted as a pH regulating agent with concentration of 5nM to 50Mm and pH of 5.0-6.0; e, glycerol is adopted as an osmotic pressure regulating agent with concentration of respectively 2.0-2.5 percent; and f, the balance is injection water.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a safe and stable alprostadil injection and a preparation method thereof. Background technique [0002] Alprostadil aka prostaglandin E 1 (Alprostadil), whose chemical name is: (1R,2R,3R,)-3-Hydroxy 2-[(E)-(3S)-3-hydroxy-1-octenyl]-5-oxocyclopentane Heptanoic acid, chemical structural formula: [0003] [0004] Alprostadil is an endogenous physiologically active substance with various physiological and pharmacological activities. [0005] Specific indications are as follows: [0006] 1. Treat limb ulcers caused by chronic arterial occlusive disease (thromboangiitis obliterans, arteriosclerosis obliterans, etc.) and rest pain in limbs caused by microvascular circulation disturbance. Improve cardiovascular and cerebrovascular microcirculation disorders. [0007] 2. Antithrombotic therapy after organ transplantation to inhibit thrombosis in blood vessels after tran...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5578A61K47/44A61P9/00
Inventor 王孝文李郑武葛存慧李金花陈玉军赵华南李会成王伟权王忠程广伟
Owner HARBIN PHARMA GROUP BIOLOGICAL ENG
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