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Method for preparing solid dosage forms type microsphere of alcohol soluble protein from source of plants

A plant-derived, gliadin technology, which is applied to medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve problems such as adverse reactions and reduce the frequency of medication, achieve low immunogenicity and improve stability Sex, the effect of improving the sustained-release effect

Inactive Publication Date: 2005-01-12
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be used as a drug carrier for humans and animals to solve the problem of adverse reactions in vivo caused by excessive local concentrations of some drugs. Through the degradation of the carrier in the body, the drug gradually diffuses to achieve a sustained release effect, thereby reducing the frequency of medication. Reduce the peak and valley phenomenon of blood concentration, improve efficacy and safety

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Dissolve 400mg of plant-derived gliadin and 400mg of drugs such as ivermectin in 12ml of 70% ethanol. After the two are dissolved, quickly add 8ml of ultrapure water. After vigorous shaking, the protein and drug concentrations obtained are both 20mg / ml, the weight percentage of protein and drug is 50% of the microsphere suspension, freeze-dried to obtain the microsphere dry powder. Ivermectin was not added to the blank microspheres, and the other treatments were the same, and the diameter of the microspheres was distributed between 0.5-1.2 μm. Weigh 5 mg of freeze-dried drug-containing microspheres, wash with 2 ml of ethyl acetate, vacuum-dry the washing solution and the precipitate, and measure the drug encapsulation efficiency at 245 nm and 280 nm, which is 50 (% w / w).

[0014] Put 0.22g of drug-containing microspheres or 0.18g of blank microspheres into a cylindrical mold with a diameter of 10mm, directly compress, and incubate in a 37°C humid box for 3 days after mo...

Embodiment 2

[0017] Dissolve 100mg of plant-derived gliadin and 1mg of drugs such as ivermectin in 9ml of 70% ethanol. After the two are dissolved, quickly add 6ml of ultrapure water. After vigorous shaking, the obtained protein and drug concentrations are respectively 6.67mg / ml and 66.7μg / ml, the weight percent of protein and drug are respectively 99.01% and 0.99% of the microsphere suspension, after freeze-drying, the microsphere dry powder is obtained. Ivermectin was not added to the blank microspheres, and the other treatments were the same, and the average diameter of the microspheres was 100nm. The method for determining the encapsulation efficiency of the drug is the same as above, and the encapsulation efficiency is 40 (% w / w).

[0018] The process of compressing the obtained microspheres to form a tablet and the determination of drug release kinetics and protein degradation are the same as above.

Embodiment 3

[0020] Dissolve 199mg of plant-derived gliadin and 1mg of drugs such as ivermectin in 6ml of 70% ethanol. After the two are dissolved, slowly add 4ml of ultrapure water and mix evenly while adding. The obtained protein and drug concentration 19.9 mg / ml and 0.1 mg / ml respectively, the weight percent of protein and drug are respectively 99.5% and 0.5% of the microsphere suspension, freeze-dried to obtain the microsphere dry powder. Ivermectin was not added to the blank microspheres, and the other treatments were the same, and the diameter of the microspheres was distributed between 0.5-5 μm. The determination method of drug encapsulation efficiency is the same as above, and the encapsulation efficiency is 70 (% w / w).

[0021] The resulting microspheres were compressed to form tablets, and the drug release kinetics and protein degradation assay procedures were the same as above.

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Abstract

A phytogenous gliadin microsphere solid as the medicine carrier is prepared by phase separation method. It can be mixed with the medicine in the mass ratio of (1-199):1.

Description

technical field [0001] The invention relates to a method for preparing a drug carrier made of plant-derived protein, in particular a method for preparing a solid dosage form of protein microspheres, which is used in the biotechnology field of the drug carrier. Background technique [0002] Substances used as drug sustained-release materials should have good biocompatibility, be non-toxic, be degradable in vivo and not induce antibody reactions. There are very few substances that meet these requirements. Materials currently used for drug sustained release can be roughly divided into synthetic polymers such as polylactic acid, etc. and natural polymers. There are many sugars and proteins in natural polymers. The latter type is more limited, such as ovalbumin, because it needs to use a bridging agent (often toxic) to obtain particles with a size of about 500 nanometers, which is not suitable for human administration; collagen is too soft to be processed into a microparticle s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/7048A61K31/727A61K47/42
Inventor 王瑾晔刘新铭孙庆申
Owner SHANGHAI JIAO TONG UNIV
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