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Alprostadil nano granule formulation and preparation thereof

A technology of nano-dil and alprostadil, which is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. Irritant, effect on overcoming chemical and physiological instability

Inactive Publication Date: 2008-12-17
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

None of the above patents involve transdermal dosage forms
And the alprostadil ointment prescription that has been listed on the market is mainly through the alprostadil of α-cyclodextrin inclusion, is directly formulated with vaseline as matrix, does not involve the technology of this application
Currently existing technologies, whether it is fat emulsion injection, liposome injection, cyclodextrin inclusion complex lyophilized powder injection, or alprostadil inclusion complex ointment that is stable in vitro, are used to protect alprostadil , there are certain defects in the treatment of ulcer disease, there is not yet a kind of alprostadil preparation that is chemically and physiologically stable for transdermal administration clinically

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Alprostadil nanoparticle transdermal preparation of the present invention is made up of following raw materials by weight ratio, alprostadil: glyceryl monostearate: soybean lecithin and P188 poloxamer mixture (3: 2): The mixture of polyethylene glycol 4000 and polyethylene glycol 400 according to 3:2: water=0.03g: 10g: 2.5g: 910g: 95g.

[0022] Take glyceryl monostearate, soybean lecithin and P188 poloxamer mixture (3:2) according to the above weight ratio, heat to 60°C to dissolve, add 0.03g of alprostadil, mix well, add the same The temperature of water according to the above ratio is sheared and stirred for 5 minutes under the condition of heat preservation, and then the material is fed into the high-pressure homogenizer, and the pressure is increased to 50MPa and circulated for 5 times. A mixture of ethylene glycol 4000 and polyethylene glycol 400 (3:2), fully stirred to obtain.

[0023] Alprostadil nanoparticles were measured, and the sample 100mg obtained in Exam...

Embodiment 2

[0029] The alprostadil nanoparticle transdermal preparation of the present invention is composed of the following raw materials by weight ratio, alprostadil: tripalmitin: egg yolk lecithin: polyethylene glycol 6000 and polyethylene glycol 400 mixture (2 : 1): water = 0.01g: 1g: 2g: 900g: 95g.

[0030] The preparation method takes the raw materials according to the weight ratios of various raw materials in Example 2, and the preparation method can also be prepared by cooling the milk. Take alprostadil and egg yolk lecithin according to the weight ratio, solidify in liquid nitrogen, and grind them in a ball mill. Grind into particles below 100μm, disperse in water, stir and shear to form colostrum, then put it into a high-pressure homogenizer at room temperature, circulate 5 times in a 20MPa high-pressure homogenizer, discharge the material, and add poly A mixture of ethylene glycol 6000 and polyethylene glycol 400 (2:1), stirred until uniform, packaged, and obtained.

Embodiment 3

[0032] The nanoparticle transdermal preparation of the present invention is composed of the following raw materials by weight ratio, alprostadil: glyceryl behenate: soybean lecithin: carbomer 940: water=0.05g: 0.5g: 0.5g: 700g : 30g.

[0033] In the preparation method, except that the carbomer was hydrated with 5 times of water for 2 hours before feeding, the others were the same as in Example 1.

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PUM

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Abstract

The invention relates to an alprostadil nanoparticle preparation and a preparation method thereof. The preparation is essentially used for transdermal administration and used for treating diseases such as diabetic ulcer, ischemia of extremity end, burn and the like, and belongs to the technical field of medicine. The preparation consists of the raw materials by the following weight ratio that alprostadil:lipid component: emulsifier: excipient matrix: water is 0.01-0.1:0.5-10:0.5-5:550-950:5. The alprostadil nanoparticle preparation has the advantages of overcoming the chemical and physiological instability of the alprostadil, strengthening in vitro stability, reducing degradation of the alprostadil caused by inactivation effect of in vivo pulmonary circulation, enhancing concentration of the preparation on the local affected parts, being more easy to aggregate at the affected part, sustained release and long effect, and reducing irritation of the preparation.

Description

technical field [0001] The invention relates to an alprostadil nanoparticle preparation and a preparation method thereof. The preparation is mainly used for transdermal administration and for treating diseases such as diabetic ulcers, extremity ischemia and burns, and belongs to the technical field of medicines. Background technique [0002] Alprostadil is a vasodilator with definite curative effect and is a human physiological substance, which is widely used in the treatment of coronary heart disease, vasculitis, thrombosis and erectile dysfunction clinically. It also has a good effect on ulcer diseases, such as diabetic ulcers, extremity ischemia, burns, and ulcers caused by trauma. The drug is currently administered mainly in the form of injections, including urethral suppositories and ointments for mucosal administration. Among them, ointment is mainly used to treat diabetic ulcers. The main cause of diabetic ulcer is microcirculatory disturbance. At present, there are...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5575A61K9/14A61K47/32A61K47/34A61K47/38A61P17/02A61P9/00A61K47/10A61K47/12A61K47/14
Inventor 董英杰艾莉邹小峰张乃先
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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