Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Alprostadil frozen-drying lipid emulsion and preparation method thereof

A technology of alprostadil and lipid emulsion, applied in the field of medicine, can solve the problems of large particles affecting product safety, unfavorable aseptic production, and product instability, so as to reduce the inactivation of pulmonary circulation and blood clearance, and benefit Long-term circulation, beneficial to the effect of tissue distribution

Active Publication Date: 2013-09-18
GRAND LIFE SCI (LIAONING) CO LTD
View PDF2 Cites 21 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the resulting side effects, especially vascular pain, are unbearable for patients
[0003] Existing alprostadil lipid emulsion injection, because alprostadil is very unstable in aqueous solution, makes medicine degrade very quickly, has the shortcomings such as poor drug stability, poor content controllability, short validity period
[0004] Ordinary alprostadil freeze-dried powder for injection has strong vascular irritation and poor chemical stability
[0005] In the preparation method of alprostadil injection-type freeze-dried emulsion disclosed in the existing patent, the method of adding the freeze-drying protective agent is to add after the emulsion is formed, which is not conducive to the dissolution of the freeze-drying protective agent and the uniformity in the emulsion before freeze-drying, and affects the freeze-drying protection agent. The state of emulsion before drying makes the reconstituted product unstable after freeze-drying, the particle size becomes larger, and it is easy to break the emulsion, and the production of large particles affects the safety of the product. At the same time, the process operation is repeated, which is not conducive to aseptic production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Under nitrogen protection, add 20 mg of alprostadil, 15 g of soybean lecithin, 2 g of oleic acid, and 0.5 g of vitamin E to 30 g of soybean oil, heat to 60 ° C, stir and mix well to obtain an oil phase; 2 g of F68, 100 g of sucrose Add 500ml of water for injection, heat to 60°C, stir and mix well to obtain the water phase; slowly pour the above oil phase into the water phase, stir for 10 minutes at 12000rmp / min, set the volume to 1000ml, and adjust the pH value at 4-7 range, get colostrum. The colostrum is transferred to a high-pressure homogenizer, homogenized several times, and then passed through a 0.2 μm microporous membrane, sterilized by filtration, subpackaged, and freeze-dried to obtain a freeze-dried lipid emulsion. The prepared freeze-dried lipid emulsion is added with water as required, and after hydration and shaking, it is restored to a lipid emulsion that can be injected intravenously.

Embodiment 2

[0046] Under nitrogen protection, 20 mg of alprostadil, 15 g of egg yolk lecithin (PC content higher than 98%), 2 g of oleic acid, and 0.5 g of vitamin E were respectively added to 30 g of soybean oil, heated to 60° C., stirred, and mixed uniformly to obtain Oil phase; add 2gF68 and 100g sucrose to 500ml water for injection, heat to 60°C, stir and mix well to obtain the water phase; slowly pour the above oil phase into the water phase, stir at 12000rmp / min for 10 minutes, constant volume to 1000ml, adjust the pH value in the range of 4-7 to obtain colostrum. The colostrum is transferred to a high-pressure homogenizer, homogenized several times, and then passed through a 0.2 μm microporous membrane, sterilized by filtration, subpackaged, and freeze-dried to obtain a freeze-dried lipid emulsion. The prepared freeze-dried lipid emulsion is added with water as required, and after hydration and shaking, it is restored to a lipid emulsion that can be injected intravenously.

Embodiment 3

[0048] Under nitrogen protection, add 20 mg of alprostadil, 15 g of egg yolk lecithin (PC content 80%), 2 g of oleic acid, and 0.5 g of vitamin E into 30 g of soybean oil respectively, heat to 60° C., stir and mix evenly to obtain an oil phase ; Add 2gF68 and 100g sucrose to 500ml water for injection, heat to 60°C, stir and mix to obtain the water phase; slowly pour the above oil phase into the water phase, stir at 12000rmp / min for 10 minutes, and set the volume to 1000ml , adjust the pH value in the range of 4-7 to obtain colostrum. The colostrum is transferred to a high-pressure homogenizer, homogenized several times, and then passed through a 0.2 μm microporous membrane, sterilized by filtration, subpackaged, and freeze-dried to obtain a freeze-dried lipid emulsion. The prepared freeze-dried lipid emulsion is added with water as required, and after hydration and shaking, it is restored to a lipid emulsion that can be injected intravenously.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention provides an alprostadil frozen-drying lipid emulsion and a preparation method thereof. The emulsion comprises the following compositions in percentage by mass: 0.0005-0.01% of alprostadil, 1-10% of oil for injection, 0.01-5% of an emulsifier, 0.02-2% of a stabilizer, 0-0.5% of an antioxidant, 1-20% of a freeze-drying protecting agent, and proper pH regulator and water for injection; the preparation method comprises the steps of: stirring alprostadil and oil for injection, and evenly mixing to obtain an oil phase; stirring freeze-drying protecting agent and water for injection to obtain a water phase; respectively the emulsifier, antioxidant and stabilizer into the water phase or the oil phase according to the solubility; mixing the water phase and the oil phase, carrying out high-speed stirring and dispersion, carrying out constant volume on the water for injection, regulating the pH value to obtain initial emulsion; transferring the initial emulsion into a high-pressure homogenizer for homogenizing for many times, then filtering, subpackaging, freeze-drying to obtain the alprostadil frozen-drying lipid emulsion. The alprostadil frozen-drying lipid emulsion is more stable and more uniform, the preparation technology and method can be simplified, and the economic efficiency can be improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an alprostadil freeze-dried lipid emulsion and a preparation method thereof. Background technique [0002] Alprostadil is also known as prostaglandins (PG). Alprostadil, prostaglandin E1 (PGE1) is one of the highly active physiologically active substances, which can inhibit platelet aggregation, thromboxane A2 generation, atherosclerosis, lipid plaque formation and immune complexes. It can expand peripheral blood vessels and coronary blood vessels, reduce peripheral resistance and blood pressure, protect ischemic myocardium, reduce the size of myocardial infarction, etc. It also has sodium excretion and diuretic effects, and can treat and protect liver, kidney, lung, and stomach lesions. effect, especially for the treatment of elderly cardiovascular disease has a unique effect. However, PGE 1 It is metabolized very quickly in the body, and under the action of pulm...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/19A61K9/107A61K31/5575A61P9/10A61P7/02A61P9/00
Inventor 薛百忠刘伟王宏英薛雁齐琰刘宏大李萍沈文彧刘星孙亮邸伟庆
Owner GRAND LIFE SCI (LIAONING) CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com