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Water indissolvable/micro-dissolvable drug sustained release composition

A slow-release composition, poorly water-soluble technology, used in drug delivery, pharmaceutical formulations, nanocapsules, etc., can solve the problems of inconvenient clinical use and poor patient compliance, maintain effective blood drug concentrations, reduce drug delivery Frequency, the effect of convenient life and work

Pending Publication Date: 2017-07-21
AC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation effectively avoids the peak and trough concentration produced by taking the medicine every day, but only a small amount of drug is released on the first day, and then there is a drug release stagnation period of about 3 weeks, so the patient still needs to be treated within 3 weeks after injecting the microspheres. The therapeutic effect can only be achieved by oral administration of common dosage forms, which is inconvenient for clinical use and poor patient compliance

Method used

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  • Water indissolvable/micro-dissolvable drug sustained release composition
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  • Water indissolvable/micro-dissolvable drug sustained release composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] A kind of sustained-release microsphere (sustained-release microsphere A) of this embodiment has no obvious delayed release period or a short delayed release period, and the drug release time is 2-3 weeks, and its preparation raw materials include the following parts by weight Components: 30 parts of poorly water-soluble / slightly soluble drugs, 70 parts of poorly water-soluble polymers; the poorly water-soluble / slightly soluble drugs are risperidone, the poorly water-soluble polymers are PLGA, and the The weight average molecular weight is 20kDa, the viscosity is 0.23dL / g, the molar ratio of lactide to glycolide is 70:30, and it has a carboxyl terminal.

[0064] The preparation method of the slow-release microspheres described in this example is: dissolving the poorly water-soluble / slightly soluble drug and the poorly water-soluble polymer in methylene chloride 10 times the mass to obtain a clear oil inner phase; then the oil The internal phase solution was added to the...

Embodiment 2

[0067] A kind of sustained-release microsphere (sustained-release microsphere A) of the present embodiment has no obvious release delay period and the drug release time is 2 weeks, and its preparation raw materials include the following components by weight: insoluble in water / 35 parts of slightly soluble drugs, 65 parts of poorly water-soluble polymers; the poorly water-soluble / slightly soluble drugs are risperidone, the poorly water-soluble polymers are PLGA, and the weight-average molecular weight of the PLGA is 25kDa, and the viscosity is 0.28dL / g, wherein the molar ratio of lactide to glycolide is 75:25, which has a terminal carboxyl group.

[0068] The preparation method of the slow-release microspheres described in this example is the same as that in Example 1.

[0069] The obtained sustained-release microspheres are round in shape, smooth in surface, and the particle diameter is 24-100 μm. The drug loading rate is 31.94% and the drug encapsulation rate is 91.26%.

Embodiment 3

[0071] A kind of sustained-release microsphere (sustained-release microsphere A) of the present embodiment has no obvious release delay period, and the drug release time is 3 weeks. The raw materials for the preparation of the sustained-release microsphere include the following components by weight: Divide: 35 parts of poorly water-soluble / slightly soluble drugs, 55 parts of poorly water-soluble polymers; the poorly water-soluble / slightly soluble drugs are risperidone, the poorly water-soluble polymers are PLGA, and the weight average of The molecular weight is 30kDa, the viscosity is 0.32dL / g, the molar ratio of lactide to glycolide is 80:20, and it has a terminal carboxyl group.

[0072] The preparation method of the slow-release microspheres A described in this example is the same as that in Example 1.

[0073] The obtained slow-release microsphere A has a round shape, a smooth surface, a particle diameter of 20-95 μm, a drug loading rate of 40.89%, and a drug encapsulation...

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Abstract

The invention relates to a sustained release composition, and particularly relates to a water indissolvable / micro-dissolvable drug sustained release composition. The indissolvable / micro-dissolvable drug sustained release composition comprises more than two indissolvable / micro-dissolvable drug sustained release microspheres with different release behaviors. Through combining more than two drug sustained release microspheres with different release behaviors, the slow release composition of the indissolvable / micro-dissolvable drug is free from obvious release delay period or short delay release period, and also free from sudden release; the composition has good sustained release performance, and can maintain effective blood concentration within several weeks or above, thus the drug applying frequency is effectively reduced, the composition can facilitate patient's life and work; moreover, the composition is good for improving the drug applying compliance and convenience of the patient.

Description

technical field [0001] The invention relates to a slow-release composition, in particular to a slow-water-soluble / slightly soluble drug slow-release composition. Background technique [0002] At present, biodegradable polymer microspheres have become one of the important research fields of new drug delivery systems. The drug delivery system uses microspheres made of polylactic acid (PLA), lactic acid-glycolic acid copolymer (PLGA) and other skeleton materials. It can be used as a carrier for long-acting preparations, and can be administered to humans or animals by intramuscular or subcutaneous injection, and can control the drug release rate and release cycle. Only one administration can maintain an effective drug treatment concentration for a long time, and can be extremely small The total dosage of drugs required for chemotherapy can be improved, and the drug treatment compliance of patients can be improved. [0003] The long-acting antipsychotic drug Risperidal Consta (H...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/34A61K47/10
CPCA61K9/0002A61K9/5146A61K9/5153
Inventor 赖树挺郑阳曹付春连远发刘锋
Owner AC PHARMA
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