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Preparation method of drug microspheres taking hydroxyethyl starch 200/0.5 as carrier

A technology of hydroxyethyl starch and microspheres, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations of non-active ingredients, etc., which can solve the problems of prolonging the action time of drugs on lesion tissues, the effect of drug release behavior, and changes in blood drug concentration Large and other problems, to achieve the effect of safe and reliable drug release stability, good drug release stability, and large drug loading capacity

Active Publication Date: 2018-06-01
HEBEI GUOLONG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In recent years, with the rapid increase of hyperlipidemia, people's demand for lovastatin lipid-lowering drugs is increasing. However, lovastatin has a relatively short half-life in vivo, and the blood concentration of its common preparations changes greatly after taking it. , so that its curative effect is limited to a certain extent, and the slow-release drug microspheres, as a new drug delivery system, can maintain the effective drug concentration in the body for a long time, prolong the action time of the drug on the lesion tissue, and increase the absorption of the drug
At present, the most researched drug microsphere carrier is polyester material (such as PLA, etc.). However, the currently used polyester materials are all artificially synthesized degradable polymer materials. Moreover, the existence of a small amount of impurities in the synthesized polyester product will have a greater impact on the release behavior and curative effect of the drug.

Method used

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  • Preparation method of drug microspheres taking hydroxyethyl starch 200/0.5 as carrier
  • Preparation method of drug microspheres taking hydroxyethyl starch 200/0.5 as carrier

Examples

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Embodiment 1

[0018] A preparation method of drug microspheres using hydroxyethyl starch 200 / 0.5 as a carrier, using lovastatin as a starting material, through H 2 O / O 2 The mixed gas performs plasma chemical modification on the surface of lovastatin, and then coats a layer of hydroxyethyl starch 200 / 0.5 on the surface of lovastatin after surface plasma chemical modification to form hydroxyethyl starch 200 / 0.5 wrapped lovastatin Statin microspheres; the main steps of the preparation method include:

[0019] 1) The plasma chemical modification of the surface of lovastatin is as follows: first, 50 mg of lovastatin is added into the rotatable plasma reaction chamber, and the gas in the plasma reaction chamber is extracted to a pressure of 2Pa; H with a ratio of 1:5 2 O / O 2 Mix the gas to a pressure of 80Pa, repeat the pumping of the gas three times, and finally adjust the pressure in the plasma reaction chamber to 40Pa. Under the conditions of the rotation speed of the plasma reaction chamb...

Embodiment 2～ Embodiment 8

[0022] The difference with Example 1 is that the plasma chemical modification conditions on the surface of lovastatin (shown in Table 1), and hydroxyethyl starch 200 / 0.5 wrapping process on the surface of lovastatin after surface plasma chemical modification Parameters and components (see Table 2).

[0023] Plasma chemical modification conditions on the surface of table 1 Examples 1-8 lovastatin

[0024]

[0025] Table 2 Example 1~8 hydroxyethyl starch 200 / 0.5 on the surface of lovastatin after surface plasmon chemical modification

[0026] Line wrapping process parameters and components

[0027]

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Abstract

The invention discloses a preparation method of drug microspheres taking hydroxyethyl starch 200 / 0.5 as a carrier, and relates to the technical field of organic preparation of drug microspheres. The preparation method adopts lovastatin as a starting material; H2O / O2 mixed gas is used for carrying out plasma chemical modification on the surface of the lovastatin, and the surface of the lovastatin subjected to the surface plasma chemical modification is wrapped with a layer of hydroxyethyl starch 200 / 0.5, so that lovastatin microspheres wrapped with the hydroxyethyl starch 200 / 0.5 can be formed.The preparation method comprises the following main steps: (1) carrying out plasma chemical modification on the surface of the lovastatin; (2) wrapping the surface of the lovastatin subjected to thesurface plasma chemical modification with the hydroxyethyl starch 200 / 0.5. The drug microspheres which are prepared by the method and take the hydroxyethyl starch 200 / 0.5 as the carrier have the advantage of being uniform in particle size distribution, high in drug loading capacity, high in drug encapsulation rate, good in drug release stability, safe, reliable, and the like.

Description

technical field [0001] The invention relates to the technical field of organic preparation of drug microspheres, in particular to a method for preparing drug microspheres with hydroxyethyl starch 200 / 0.5 as a carrier. Background technique [0002] Hydroxyethyl starch 200 / 0.5 (HES 200 / 0.5) is a representative drug of medium-molecular weight and low-substituted hydroxyethyl starch. It is the first plasma substitute developed by Fresenius Kabi Company of Germany. At present, this product has occupied the European market. Market share of more than 70%, and was allowed to enter the Chinese market in 1999. The average molecular weight of this product is 200kDa, and the degree of substitution is 0.43-0.55. It is used as a plasma substitute and has a high volume-expansion strength. The expansion effect of this product is 100%. The effective time of expansion is 4-8 hours, and the half-life is 3-4 hours. It is currently the most widely used artificial plasma substitute in Europe. H...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/22A61K31/366A61K47/36A61P3/06
CPCA61K9/5036A61K9/5089A61K31/22A61K31/366
Inventor 赵雄燕
Owner HEBEI GUOLONG PHARMA CO LTD
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