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Drug sustained release composition sparingly soluble or slightly soluble in water, and preparation method thereof

A slow-release composition and water-insoluble technology, which can be used in drug delivery, pharmaceutical formulations, non-active ingredients of polymer compounds, etc., can solve the problems of inconvenient clinical use and poor patient compliance, and achieve effective blood drug concentration, Good stability, avoiding the effect of delayed release platform

Inactive Publication Date: 2017-06-13
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method avoids the initial burst release phenomenon, it causes a delayed release of about 5 days, which is inconvenient for clinical use and poor patient compliance

Method used

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  • Drug sustained release composition sparingly soluble or slightly soluble in water, and preparation method thereof
  • Drug sustained release composition sparingly soluble or slightly soluble in water, and preparation method thereof
  • Drug sustained release composition sparingly soluble or slightly soluble in water, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076]An embodiment of the poorly water-soluble / slightly soluble drug sustained-release composition of the present invention, the non-solvent preparation raw materials of the poorly water-soluble / slightly soluble drug sustained-release composition in this embodiment contain the following components in mass percentage : Poorly water-soluble / slightly soluble drug: Entecavir 25%, poorly water-soluble polymer: PLGA 74.9%, release modifier: mixture of stearic acid and PEG6000 0.1%.

[0077] Wherein, the molar ratio of lactide to glycolide in the PLGA is 90:10, the weight average molecular weight of the PLGA is 25kDa, the viscosity is 0.24dL / g, and the PLGA has a terminal ester group; the hard In the mixture of fatty acid and PEG6000, the mass percent content of PEG6000 in the release regulator is 70%.

[0078] The poorly water-soluble / slightly soluble drug sustained-release composition described in this example is prepared by the following method:

[0079] (1) The poorly water-sol...

Embodiment 2

[0084] An embodiment of the poorly water-soluble / slightly soluble drug sustained-release composition of the present invention, the non-solvent preparation raw materials of the poorly water-soluble / slightly soluble drug sustained-release composition in this embodiment contain the following components in mass percentage : Poorly water-soluble / slightly soluble drug: aripiprazole 27%, poorly water-soluble polymer: PLGA 72.5%, release modifier: mixture of behenic acid and PEG4000 0.5%.

[0085] Wherein, the molar ratio of lactide to glycolide in the PLGA is 95:5, the weight average molecular weight of the PLGA is 30kDa, the viscosity is 0.29dL / g, and the PLGA has a terminal ester group; In the mixture of sputic acid and PEG4000, the mass percent content of the PEG4000 in the release modifier is 60%.

[0086] The poorly water-soluble / slightly soluble drug sustained-release composition described in this example is prepared by the following method:

[0087] (1) Dissolve the poorly wa...

Embodiment 3

[0092] An embodiment of the poorly water-soluble / slightly soluble drug sustained-release composition of the present invention, the non-solvent preparation raw materials of the poorly water-soluble / slightly soluble drug sustained-release composition in this embodiment contain the following components in mass percentage : Poorly water-soluble / slightly soluble drug: risperidone 30%, poorly water-soluble polymer: PLA 69.2%, release regulator: behenic acid 0.8%.

[0093] Wherein, the weight average molecular weight of the PLA is 35Da, the viscosity is 0.31dL / g, and the PLGA has a terminal ester group.

[0094] The poorly water-soluble / slightly soluble drug sustained-release composition described in this example is prepared by the following method:

[0095] (1) Dissolve the poorly water-soluble polymer in the organic solvent toluene, then add the poorly water-soluble / slightly soluble drug and the release regulator, and obtain the internal oil phase after dissolving; wherein, the poo...

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Abstract

The present invention discloses a drug sustained release composition sparingly soluble or slightly soluble in water, comprising non-solvent based raw material: a releasing conditioning agent. In the composition, the releasing conditioning agent is added into preparation raw materials and can be used for effectively adjusting the releasing speed of the drug sustained release composition sparingly soluble or slightly soluble in the water, so that a phenomenon of obvious releasing delaying period and burst releasing of the drug sustained release composition sparingly soluble or slightly soluble in the water is avoided, the good sustained release performance is obtained, the therapeutic plasma concentration can be kept for several weeks or even more, the stabilization is relatively good, and the releasing behavior of the drug can be maintained after long-time storage. At the same time, the present invention also discloses a preparation method of the drug sustained release composition sparingly soluble or slightly soluble in the water.

Description

technical field [0001] The invention relates to a sustained-release pharmaceutical composition and a preparation method thereof, in particular to a slow-water-soluble / slightly soluble pharmaceutical sustained-release composition and a preparation method thereof. Background technique [0002] In the past ten years, biodegradable polymer microspheres have become one of the important research fields of new drug delivery systems, which combine polylactide (PLA), lactide-glycolide copolymer (PLGA) and so on. The microspheres made of the skeleton material can be used as the carrier of long-acting preparations, which can be administered to humans or animals by intramuscular or subcutaneous injection, which can limit the release rate and cycle of the drug, and can maintain the effective drug for a long time with only one administration. Therapeutic drug concentration can minimize the total drug dosage required for treatment, and can improve the patient's drug treatment compliance. ...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/12A61K47/10A61K47/32A61K47/42A61K47/18
CPCA61K9/1647A61K9/1682A61K31/522A61K31/496A61K31/519A61K31/551A61K31/4196A61K31/445A61K9/0002A61K9/5123A61K9/5138A61K9/5146A61K9/5169
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC PHARMA CO LTD
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