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Medicine releasing system of aliphatic polylactone mixture

A polylactone and aliphatic technology, applied in the field of drug release system, can solve the problems of poor drug permeability, slow degradation rate, and inability to achieve constant drug release.

Inactive Publication Date: 2003-01-29
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the disadvantage is that when polylactide homopolymer is used as the drug carrier, because polylactide has poor drug permeability and slow degradation rate, it is prone to two-stage release behavior, that is, it needs to go through a period of initial stagnation During the period, the drug molecules are slowly released after the carrier begins to degrade (Makoto Miyajima et al., J. Controlled Release, 61, 295-304 (1999)); while polycaprolactone homopolymer is used as the drug carrier, then Because polycaprolactone has good drug permeability, it is prone to serious initial burst release (Bei Jianzhong et al., Chinese J.Polym.Sci., 13, 154-161 (1995)), these are clinical The application is not desired, so neither PLA nor PCL can be used as a drug carrier to achieve a constant release rate of the drug

Method used

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  • Medicine releasing system of aliphatic polylactone mixture
  • Medicine releasing system of aliphatic polylactone mixture
  • Medicine releasing system of aliphatic polylactone mixture

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] The molecular weight is 1×10 3 , 2×10 3 , 5×10 3 , 8×10 3 , 1.7×10 4 , 4.9×10 4 , 1×10 5 , 2.1×10 5 and 3.3×10 5 After dissolving 0.1g of each of the nine polylactide homopolymers with different molecular weights in 20ml of dichloromethane, add 0.1g of 5-fluorouracil (5-Fu), and make it uniformly dispersed in the solution by grinding, and wait for the solvent to volatilize After completion, a 5-Fu tablet with a diameter of 10 mm and a thickness of about 1 mm was prepared by molding at 180° C. with a mold. The tablet was subjected to an in vitro drug release test in a phosphate buffer solution of pH 7.4 at 37° C., and the amount of drug released was detected by an ultraviolet spectrophotometer (λ=266nm). The pharmaceutical preparation has no initial stagnation period in the release process, and the initial burst release is very small, and the constant release time is six months.

Embodiment 2

[0020] 7g has a molecular weight of 2.1×10 4 3 g of polylactide and a molecular weight of 1.7 x 10 4 After the polycaprolactone homopolymer was dissolved in 200ml of dichloromethane, 1g of 5-fluorouracil (5-Fu) was added, and it was evenly dispersed in the above solution by grinding. ℃Prepare 5-Fu tablets with a diameter of 10mm and a thickness of about 1mm by compression molding. The tablet was subjected to an in vitro drug release test in a phosphate buffer solution of pH 7.4 at 37° C., and the amount of drug released was detected by an ultraviolet spectrophotometer (λ=266nm). Although the pharmaceutical preparation has a relatively obvious initial burst release (about 10%) during the release process, the sustained release time at a constant rate can still be maintained for more than one month.

Embodiment 3

[0022] 0.5g molecular weight is 1.9×10 4 0.3 g of polylactide and a molecular weight of 5.6 x 10 4 After the polyhydroxybutyrate homopolymer was dissolved in 20ml of dichloromethane, 0.1g of 5-fluorouracil (5-Fu) was added, and it was uniformly dispersed in the solution by grinding. After the solvent was completely evaporated, a 5-Fu tablet with a diameter of 10 mm and a thickness of about 1 mm was prepared by molding at 180° C. with a mold. The tablet was subjected to an in vitro drug release test in a phosphate buffer solution of pH 7.4 at 37° C., and the amount of drug released was detected by an ultraviolet spectrophotometer (λ=266nm). This pharmaceutical preparation has no obvious initial burst release during the release process, and the sustained release time at a constant rate is as long as twelve months.

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Abstract

An aliphatic polylactone intermingled material as medicine releasing system contains hydrophilic medicine (1-30 wt. portions) and medicine carrier (100 wt. portions). The mentioned hydrophilic medicine may be 5-fluorouracil, streptomycin, growth factor, etc.. The mentioned carrier is the mixture of PLA, PGA, PCL, PHB, or PHV. Its advantage is constant-speed sustained releasing.

Description

Technical field: [0001] The invention relates to a drug release system using a blend of biodegradable aliphatic polylactone homopolymers as a hydrophilic drug carrier. Background technique: [0002] For a long time, matrix pharmaceutical preparations have been the most commonly used drug delivery system, such as ordinary tablets and drug capsules. The matrix pharmaceutical preparation is generally prepared by uniformly dissolving or dispersing the drug in the drug carrier, and has the characteristics of simple molding method, easy production, and low price. However, this type of drug preparation usually exhibits a "first-order" release behavior, that is, whether it is a tablet preparation, a cylindrical dosage form, or a spherical preparation, there is a burst of drug release at the initial stage, and then the drug release rate continues to decrease. release behavior. This is because matrix pharmaceutical preparations are generally diffusion-controlled drug release dosage ...

Claims

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Application Information

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IPC IPC(8): A61K47/34
Inventor 王身国蔡晴贝建中
Owner INST OF CHEM CHINESE ACAD OF SCI
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