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Dipyridamole self-emulsifying medicament administration system and preparation method thereof

A drug delivery system and dipyridamole technology, which are applied in the field of dipyridamole self-emulsifying drug delivery system and its preparation, can solve the problem of no relevant reports on the preparation method, and are suitable for large-scale production and improve bioavailability. , the effect of reducing individual differences

Inactive Publication Date: 2010-07-21
SHENZHEN HEPALINK PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The dipyridamole self-emulsifying drug delivery system involved in the present invention, according to the documents and materials we can retrieve at present, there are no published documents or patents, and there is no relevant report on its preparation method

Method used

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  • Dipyridamole self-emulsifying medicament administration system and preparation method thereof
  • Dipyridamole self-emulsifying medicament administration system and preparation method thereof
  • Dipyridamole self-emulsifying medicament administration system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Prescription composition:

[0028] Dipyridamole 18g

[0029] Oleic acid 120g

[0030] Labrafac lipophile WL 1349 60g

[0031] Solutol HS 15 260g

[0032] Isopropanol 160g

[0033]

[0034] Made 1000 softgels in total

[0035] Preparation Process:

[0036] The excipients in the prescribed amount are weighed, mixed evenly, then the drug in the prescribed amount is added, stirred to dissolve the drug completely, and made into soft capsules, namely dipyridamole self-emulsifying soft capsules.

[0037] The characteristics of the prepared dipyridamole self-emulsifying drug delivery system:

[0038] Physical and chemical properties:

[0039] Particle size determination: Take 50 μl blank self-emulsifying concentrate and dipyridamole self-emulsifying concentrate respectively and add them to a 100ml volumetric flask, dilute to the mark with distilled water, and shake gently to form a clear microemulsion....

Embodiment 2

[0053] Prescription composition:

[0054] Dipyridamole 20g

[0055] Oleic acid 140g

[0056] Labrafac lipophile WL 1349 40g

[0057] Solutol HS 15 240g

[0058] Isopropanol 180g

[0059]

[0060] Made 1000 softgels in total

[0061] Preparation Process:

[0062] The excipients in the prescribed amount are weighed, mixed evenly, then the drug in the prescribed amount is added, stirred to dissolve the drug completely, and made into soft capsules, namely dipyridamole self-emulsifying soft capsules.

Embodiment 3

[0064] Prescription composition:

[0065] Dipyridamole 16g

[0066] Oleic acid 120g

[0067] Labrafac lipophile WL 1349 60g

[0068] Solutol HS 15 260g

[0069] Isopropanol 160g

[0070]

[0071] Made 1000 softgels in total

[0072] Preparation Process:

[0073] The excipients in the prescribed amount are weighed, mixed evenly, then the drug in the prescribed amount is added, stirred to dissolve the drug completely, and made into soft capsules, namely dipyridamole self-emulsifying soft capsules.

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Abstract

The invention discloses a dipyridamole self-emulsifying medicament administration system, which is characterized by comprising the following components in percentage by mass: dipyridamole 0.5-10, an oil phase 20-80, a surfactant 10-70 and an auxiliary surfactant 0-50. The system has the advantages that: self-emulsifying capsules prepared by using the dipyridamole, the oil phase, the surfactant and the auxiliary surfactant change into emulsion by slightly stirring after disintegrating in water or spontaneously change into emulsion in vivo under the action of the peristalsis of the gastrointestinal tracts after being delivered by oral taking, wherein the particle size of the emulsion is 10 to 500 nanometers; the dissolution of the dipyridamole is improved greatly; after the system is taken orally, the absorption of the medicament is improved greatly, the bioavailability is improved and the individual difference is reduced; and the preparation process is simple and is suitable for large-scale production of medical enterprises.

Description

technical field [0001] The invention relates to a dipyridamole self-emulsifying drug delivery system and a preparation method thereof. Background technique [0002] Dipyridamole (DIP) is also known as dipyridamole, and its chemical name is 2,2′,2″,2′″-[(4,8-dipiperidinylpyrimido[5,4-d]pyrimidine -2,6-diyl)bisnitrilo]-tetraethanol. Molecular formula is C 24 h 40 N 8 o 4 , the molecular weight is 504.62. The structural formula is as follows: [0003] [0004] Dipyridamole, yellow crystalline powder, odorless, slightly bitter taste, unstable to light. Soluble in methanol, ethanol, chloroform, slightly soluble in acetone. The drug is weakly alkaline, with a pKa of 6.4, and its solubility in water is pH-dependent, soluble in acidic conditions (such as pH<3), and insoluble in neutral or alkaline conditions. According to the biopharmaceutical classification system, it has been reported that the drug should belong to Class IV (a class of drugs with poor water solubili...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/519A61K9/48A61K9/20A61K9/16A61K9/00A61P9/00A61P9/10A61P11/00A61P31/12A61P17/00A61P31/22A61P27/02A61P7/04A61P11/04A61P1/00
Inventor 钟海军郭锋
Owner SHENZHEN HEPALINK PHARMA GRP CO LTD
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