Alprostadil and vitamin F millimicroball composite medicine and its preparation method

An alprostadil and vitamin technology, applied in the field of nanosphere combination medicine and preparation thereof, can solve the problems of unacceptable to patients, low bioavailability, short elimination half-life, etc., and achieves reduced vascular irritation, excellent curative effect, and good targeting effect of action

Inactive Publication Date: 2008-01-09
蔡海德
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The prodrug vitamin F of alprostadil can generate alprostadil in the human body, make oral preparation evening primrose oil capsules for oral administration, overcome the defects of alprostadil injection pain and short half-life, but due to evening primrose The side effect of oil capsules diarrhea is still unacceptable to patients, and the efficacy of the medicine is limited due to diarrhea and low bioavailability

Method used

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  • Alprostadil and vitamin F millimicroball composite medicine and its preparation method
  • Alprostadil and vitamin F millimicroball composite medicine and its preparation method
  • Alprostadil and vitamin F millimicroball composite medicine and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] The formula adopted in the preparation of blank nanospheres in this embodiment is as follows:

[0053] Gelatin mixed with casein and human gamma globulin in any proportion 200g

[0054] Hydroxypropyl-β-cyclodextrin 500g

[0055] Pluronic F68 15g

[0056] Soybean oil and ethyl acetate weight ratio 3:1 mixed oil 1000g

[0057] Ethanol 8000g

[0058] Add water for injection to 1000ml

[0059] The method steps for preparing blank nanospheres are as follows:

[0060] (1) Dissolve the mixture of the amount of gelatin, casein and human gamma globulin in any proportion in the amount of water for injection, dissolve completely under stirring, maintain the solution temperature at 55 ± ℃, and add the amount of cyclodextrin, Pluronic F68 and PEG6000 mixture, completely dissolved;

[0061] (2) Cool the solution prepared in step (1) to room temperature, add it to an equal volume of vegetable oil and ethyl acetate mixture, emulsify, and continue cooling the formed emulsion to 5-...

Embodiment 2

[0085] Preparation of blank nanosphere recipe:

[0086] Gelatin mixed with casein and human gamma globulin in any proportion 300g

[0087] γ-cyclodextrin 200g

[0088] Mixture of Pluronic F68 and polyethylene glycol 6000 in any proportion 30g

[0089] The mixture of peanut oil and ethyl acetate 3:1 weight ratio 2000g

[0090] Ethanol 10000g

[0091] Water for injection 2000g

[0092] The preparation steps and method are the same as in Example 1.

[0093] Preparation method of nanosphere carrier drug:

[0094] Blank nanospheres prepared above 150g

[0095] Alprostadil or vitamin F mixture in any proportion 5g

[0096] Tween80 4g

[0097] Vitamin C 20g

[0098] The mixture of N-(2-mercaptopropionyl)-glycine and cysteine ​​with a weight ratio of 2-4:1 40g

[0099] Add water for injection to 2000ml

[0100] The preparation steps and method are the same as in Example 1.

[0101] Drug efficacy verification test:

[0102]A rat model of renovascular hypertension was used....

Embodiment 3

[0104] Preparation of blank nanosphere recipe:

[0105] Gelatin mixed with casein and human gamma globulin in any proportion 260g

[0106] Mixture of hydroxypropyl-β-cyclodextrin and γ-cyclodextrin in any proportion 140g

[0107] Mixture of Pluronic F68 and polyethylene glycol 6000 in any proportion 22g

[0108] The mixture of soybean oil, peanut oil and ethyl acetate in a weight ratio of 3:1 1680g

[0109] Ethanol 7000g

[0110] Water for injection 1660g

[0111] The preparation steps and method are the same as in Example 1.

[0112] Preparation method of nanosphere carrier drug:

[0113] Blank nanospheres prepared above 130g

[0114] Alprostadil or vitamin F mixture in any proportion 3g

[0115] Tween80 3g

[0116] Vitamin C 16g

[0117] The mixture of N-(2-mercaptopropionyl)-glycine and cysteine ​​with a weight ratio of 2-4:1 32g

[0118] Add water for injection to 1600ml

[0119] The preparation steps and method are the same as in Example 1.

[0120] Drug effic...

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Abstract

The present invention relates to a millimicrosphere composite medicine containing mixture of alprostadil and vitamin F and its preparation method. The invented medicine can greatly prolong the half-life time in vivo and has good target action for tumor.

Description

technical field [0001] The invention relates to a nanosphere combination drug of alprostadil and vitamin F and a preparation method thereof. Background technique [0002] Alprostadil used to be called microprostaglandin E1, and vitamin F is also called γ-linolenic acid, both of which are unsaturated fatty acids, and vitamin F is the precursor of alprostadil. Both are cardiovascular and cerebrovascular drugs, drugs for the treatment of viral hepatitis and anti-liver cancer, drugs for the treatment of diabetes and its complications. [0003] Existing alprostadil preparations have the fat emulsion of alprostadil, the freeze-dried injection that the cyclodextrin of alprostadil contains, but the fat emulsion of alprostadil and the freeze-dried injection that the cyclodextrin contains enter the body and release immediately, eliminate The half-life is very short, only 10-30 minutes. At the same time, the patient's pain was unbearable during the injection, which affected the use o...

Claims

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Application Information

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IPC IPC(8): A61K31/5575A61K31/201A61K31/375A61K9/14A61P9/00A61P1/16A61P31/12A61P35/00A61P3/10
Inventor 蔡海德
Owner 蔡海德
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