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Heparin phospholipid composite suitable for non-injection administration and preparation method thereof

A technology of heparin phospholipids and complexes, applied in the field of medicine, can solve the problem of low oral bioavailability of heparin, and achieve the effects of improving bioavailability, enhancing absorption and high affinity

Inactive Publication Date: 2011-07-20
INST OF BIOPHARM OF SHANDONG PROVINCE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low oral bioavailability of heparin, currently most heparin in clinical application is injection, unfractionated heparin needs intravenous injection, low molecular weight heparin needs subcutaneous injection
Intravenous injection of ungraded heparin usually requires continuous intravenous infusion for 1 week, which brings great pain to the patient and has serious side effects, such as gum bleeding, external auditory canal bleeding, hematuria, melena, etc.; subcutaneous injection of low-molecular-weight heparin generally takes 1 ~2 times, the incidence of the above side effects is low, but there is also a certain risk of bleeding

Method used

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  • Heparin phospholipid composite suitable for non-injection administration and preparation method thereof
  • Heparin phospholipid composite suitable for non-injection administration and preparation method thereof
  • Heparin phospholipid composite suitable for non-injection administration and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1: Low molecular weight heparin sodium lecithin complex and its preparation method

[0050] Its preparation method consists of the following steps:

[0051] (1) Preparation of low molecular weight heparin sodium lecithin complex:

[0052] ① Dissolve 2 g of low-molecular-weight heparin sodium in 100 mL of formamide, and stir in a 60°C water bath until the low-molecular-weight heparin sodium is completely dissolved;

[0053] ② Dissolve 6g of lecithin in 50mL of absolute ethanol;

[0054] ③ Mix the above two solutions ① and ②, and stir evenly to obtain a mixed solution;

[0055] ④ Slowly drop 1.0mol / L CaCl into the above ③ mixture 2Add 20 mL of the solution and stir while adding; after the dropwise addition, continue to stir on a magnetic stirrer for 10 min, centrifuge at 10 000 r / min for 5 min, collect the precipitate, and obtain the crude compound.

[0056] (2) Purification of low molecular weight heparin sodium lecithin complex:

[0057] ①Take the crude low...

Embodiment 2

[0063] Embodiment 2: heparin sodium lecithin complex and preparation method thereof

[0064] Its preparation method consists of the following steps:

[0065] (1) Preparation of heparin sodium lecithin complex:

[0066] ① Dissolve 10 g of heparin sodium in 1000 mL of formamide, and stir in a 60°C water bath until the heparin sodium is completely dissolved;

[0067] ② Dissolve 30g of lecithin in 500mL of absolute ethanol;

[0068] ③ Mix the above two solutions ① and ②, and stir evenly to obtain a mixed solution;

[0069] ④ Slowly drop 1.0mol / L CaCl into the above ③ mixture 2 The solution was 100mL, and stirred while adding; after the dropwise addition, continued to stir on a magnetic stirrer for 10min, centrifuged at 10,000r / min for 10min, collected the precipitate, and obtained the crude compound.

[0070] (2) Purification of heparin sodium lecithin complex:

[0071] ①Take the crude product of heparin sodium lecithin complex, add 400mL of acetone, and stir rapidly for 1.5h...

Embodiment 3

[0077] Embodiment 3: heparin calcium lecithin complex and its preparation method

[0078] Its preparation method consists of the following steps:

[0079] (1) Preparation of heparin calcium lecithin complex:

[0080] ①Dissolve 50g of heparin calcium in 2500mL of formamide, and stir in a 60°C water bath until the heparin calcium is completely dissolved;

[0081] ② Take 200g of lecithin and dissolve it in 1250mL of absolute ethanol;

[0082] ③ Mix the above two solutions ① and ②, and stir evenly to obtain a mixed solution;

[0083] ④ Slowly drop 1.0mol / L CaCl into the above ③ mixture 2 Solution 250mL, stirring while adding;

[0084] After the dropwise addition, continue stirring on a magnetic stirrer for 20 min, centrifuge at 10 000 r / min for 10 min, collect the precipitate, and obtain the crude compound.

[0085] (2) Purification of heparin calcium lecithin complex:

[0086] ①Take the crude product of heparin-calcium-lecithin complex, add 3000 mL of acetone, and stir rapi...

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PUM

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Abstract

The invention provides a heparin and phosphatide compound suitable for non-injection drug administration, which is formed by heparin, phosphatide and calcium ion, wherein, the contents by weight percentage of the heparin, the phosphatide and the calcium ion in the heparin and phosphatide compound respectively are: 1 percent to 60 percent, 40 percent to 95 percent, and 1 percent to 15 percent. After heparin and the phosphatide are formed to be a compound, the fat solubility of the heparin, the absorption of the heparin in the gastrointestinal tract as well as the bioavailability of the oral administration and the external application of the heparin can be improved, ant the heparin and phosphatide compound is suitable for non-injection drug administration.

Description

technical field [0001] The invention relates to a heparin-phospholipid complex suitable for non-injection administration and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Heparin is a mixture of polysaccharide chains with different chain lengths composed of uronic acid (L-iduronic acid; D-glucuronic acid) and hexosamine (α-D-glucosamine). Heparin has a high degree of sulfation, and its molecule is acidic and has a large number of negative charges. This characteristic makes heparin easy to combine with positively charged coagulation factors, which is the basis for its biological activity. Heparin has a variety of pharmacological effects and a wide range of clinical applications. In addition to anticoagulant and antithrombotic, heparin also has anti-inflammation, blood lipid regulation, anti-tumor, anti-virus, and protection of heart, liver, and kidney in patients with atherosclerosis. Heparin is mainly used clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/24A61K31/727A61P7/02A61P29/00A61P31/12A61P35/00A61K47/54
Inventor 凌沛学张治云王凤山张天民荣晓花
Owner INST OF BIOPHARM OF SHANDONG PROVINCE