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Liposomes sodium morrhuate

A technology of sodium morrhuate and body fish, which is applied in the field of medicine, can solve the problems of affecting the normal tissue function around, increasing the pain of children, side effects, etc., and achieves easy mastery and industrial production, good inhibitory therapeutic effect, good stability and The effect of encapsulation rate

Inactive Publication Date: 2012-09-05
XI AN JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, 5% sodium morrhuate is usually injected directly into the tumor, but there are many problems in the use of traditional dosage forms of sodium morrhuate. For example, after sodium morrhuate is injected into the hemangioma, it disperses with the blood flow and is difficult to enter the tumor. To form an effective concentration concentration, repeated injections are often required to achieve the effective concentration in the tumor body. After injection, the local side effects are severe, which prolongs the treatment cycle, increases the pain of the child, increases the economic burden, and even causes local ulceration. Infection and other complications, and the lesions are prone to relapse, excessive dosage or drug extravasation will cause tissue necrosis, and there is a risk of massive bleeding
Especially in the maxillofacial area, obvious scar tissue is left behind after healing, which affects the facial appearance and brings psychological harm to the patient at the same time
Common dosage forms can also affect the function of surrounding normal tissues
At present, most of the clinical drugs have been partially degraded or eliminated before reaching the site of action in the body, which reduces the potency of the drug; in addition, after the drug enters the body, it not only acts on the target tissue, but also acts on non-target tissues, causing toxicity effect

Method used

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  • Liposomes sodium morrhuate
  • Liposomes sodium morrhuate
  • Liposomes sodium morrhuate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Example 1: Liposomal drug product containing 1% sodium morrhuate

[0079] Liposomal Drug Prescription:

[0080] name

[0081] Weigh EPC and CHO according to the prescription amount and place them in a test tube, add 4ml of chloroform and shake to dissolve them completely. In a water bath at 60°C, blow off the chloroform with nitrogen gas. After all the chloroform is about to be removed, quickly vacuum to form a flocculent film , continue vacuuming for 3h to completely remove chloroform. Weigh 100mg of sodium morrhuate powder and dissolve it in 10ml of PBS (pH6.84), oscillate to dissolve it completely, suck it into a disposable syringe, and slowly drop into the sodium morrhuate solution while oscillating the vacuum-pumped test tube. It must be slow until all the solution is dripped out (the whole process is about 15 minutes), and the test tube forms a yellow-white emulsion and continues to shake for 45 minutes, that is, multi-lamellar liposomes (MLV) are forme...

Embodiment 2

[0082] Example 2: 2.5% sodium morrhuate in liposomal drug product

[0083] Liposomal Drug Prescription:

[0084] name

[0085] The above-mentioned raw materials were weighed according to the prescription quantity, and the preparation process was the same as in "Example 1", to obtain liposomal sodium morrhuate with an average particle diameter of 108.4nm ± 39nm.

Embodiment 3

[0086] Example 3: Liposomal drug product containing 5% sodium morrhuate

[0087] Liposomal Drug Prescription:

[0088] name

[0089] The above-mentioned raw materials were weighed according to the prescription quantity, and the preparation process was the same as in "Example 1", that is, liposomal sodium morrhuate with an average particle diameter of 103.6nm ± 32nm was obtained.

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Abstract

The invention discloses a liposome-encapsulated sodium morrhuate, which is prepared from the following active ingredients (vol.%) sodium morrhuate 1-10, lecithin 4.31-10, cholesterol 0-2.19, vitamin E 0-0.03 and PBS buffer in balancing amount. The sodium morrhuate is used as an encapsulated active ingredient and is a sodium salt mixture of multiple fatty acids with eicosapentaenoic acid (EPA) anddocosahexaenoic acid (DHA) as main components, wherein the unsaturated fatty acids include from fatty acids with 18 carbon atoms and 3 olefinic bonds to fatty acids with 22 carbon atoms and 6 olefinic bonds. The liposome encapsulation technology completely solves the acute toxicity problem of sodium morrhuate used as a hardener, so that the drug has good passive targeted drug delivery function and reduced toxic and adverse effects caused after the drug enters the systemic blood circulation system. The inventive liposome-encapsulated sodium morrhuate can be used for treating hemangioma and vascular malformations.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a local sclerosing preparation for the clinical treatment of hemangioma and vascular malformation, in particular to liposome sodium morrhuate. Background technique [0002] Hemangioma is a benign tumor commonly seen in infants and young children, with an incidence rate of about 3% to 8%. Hemangiomas occurring in the oral and maxillofacial areas account for about 60% of the whole body. Hemangiomas are mainly characterized by the proliferation of endothelial cells and the formation of microvessels, and there are obvious proliferative and regression phases, but the mechanism of their proliferation and regression is still not very clear. Although most hemangiomas can regress on their own, their regression cycle is long, incomplete, and local sequelae remain after large areas of hemangiomas regress, which brings great difficulties to clinical diagnosis and treatment. Make hemangioma a hotspot i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/20A61K9/127A61K47/24A61P35/00A61P9/10
Inventor 杨壮群屠军波宋勇兰海龙王正辉傅经国
Owner XI AN JIAOTONG UNIV
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