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Poly acid anhydride for release-controlled medicine carrier and method for producing the same

A technology of polyanhydride and dimer acid, applied in the field of chemically synthesized drug sustained-release materials, to achieve good biocompatibility, slow degradation rate, and long drug release period

Inactive Publication Date: 2004-11-10
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This type of polyanhydride material has not been reported yet

Method used

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  • Poly acid anhydride for release-controlled medicine carrier and method for producing the same
  • Poly acid anhydride for release-controlled medicine carrier and method for producing the same
  • Poly acid anhydride for release-controlled medicine carrier and method for producing the same

Examples

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example 1

[0044] Example 1: Synthesis of poly(dimer acid-lauric acid) copolymer anhydride

[0045] Add 2 grams of lauric acid prepolymer and 2 grams of dimer acid prepolymer into a polymerization tube with a diameter of 2 cm and a length of 20 cm, place it in a silicone oil bath, and stir it electromagnetically. The temperature was raised to 165°C, the vacuum pressure was reduced to 40 Pa, the melt polymerization was carried out for 75 minutes, nitrogen gas was passed for 15 seconds every 15 minutes, and the vacuum was drawn again. After the polymerization is completed, cool down to obtain a pale yellow solid, which is dissolved in dichloromethane, filtered through a G4 sand core funnel, and petroleum ether is precipitated. The precipitate is washed with methyl ethyl ether and dried to obtain a slightly yellow powdery solid. The synthesis of other different prepolymer mass ratios is carried out similarly as above. The FT-IR and physical and chemical properties of 5 different proportion...

example 2

[0055] Example 2: Synthesis of poly(dimer acid-tetradecanedioic acid) copolymer anhydride

[0056] Add 2 grams of dimer acid prepolymer and 3 grams of tetradecanedioic acid prepolymer into a polymerization tube with a diameter of 2 cm and a length of 20 cm, place it in a silicone oil bath, and stir it electromagnetically. The temperature was raised to 170°C, the vacuum pressure was reduced to 45 Pa, the melt polymerization was carried out for 85 minutes, and nitrogen gas was flowed for 10 seconds every 10 minutes, and then vacuumed. After the polymerization is completed, cool down to obtain a pale yellow solid, which is dissolved in dichloromethane, filtered through a G4 sand core funnel, precipitated with cyclohexane, washed with anhydrous ether and dried to obtain a slightly yellow powdery solid. The synthesis of other different prepolymer mass ratios is carried out similarly as above. The FT-IR and physical and chemical properties of 5 different proportions of polyanhydrid...

example 3

[0066] Example 3: Sustained release characteristics of ciprofloxacin hydrochloride in poly(dimer acid-lauric acid) copolymer anhydride-ciprofloxacin hydrochloride sticks

[0067] Mix ciprofloxacin hydrochloride with polyanhydride, grind it in an agate mortar, use the hot-melt method, heat the mixture to about 90 ° C with an infrared lamp to melt, and prepare a drug-loading amount of 20% cylindrical polyanhydride drug rod (φ4mm, length 10mm). The drug sticks were respectively placed in 50 mL of 0.1 mol / L, pH=7.4 phosphate buffer solution, and the degradation experiment was carried out on a constant temperature shaker at 37° C. (rotating speed 60 rad / min). The buffer solution is replaced at regular intervals, and the absorbance of the release medium at a wavelength of 271nm is measured by UV spectroscopy, based on the regression of the measured ciprofloxacin hydrochloride at 271nm in a 0.1mol / L, pH=7.4 phosphate buffer solution Equation A=0.27465ρ-5.133×10-4, where A is the abs...

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Abstract

The invention discloses a process for preparing polyanlydrides, carriers for hydrophilous antiphlogistic drug and antitumor agent by using binary aliphatic acid and dimer acid copolymerization, because the use of diacid with longer carbon chain as monomer, the degradation speed of the polyanlydride material is slow, and the medicinal release cycle is longer, thus is suitable for the local slow release administration treatment for osteomyelitis and solid tumor diseases.

Description

technical field [0001] The invention relates to chemically synthesized drug slow-release materials and methods. The carrier of hydrophilic anti-inflammatory drug and anti-solid tumor drug is prepared by copolymerizing dibasic fatty acid and dimer acid. technical background [0002] Polyanhydrides are a new class of synthetic biodegradable polymer materials discovered by Langer et al. (RosenHB et al.: Bioerodible polyanhydrides for controlled drug delivery. Biomaterials, 1983, 4: 131-133) of the Massachusetts Institute of Technology in the early 1980s. , due to its good biocompatibility, unique surface erosion (surface erosion) degradability, adjustable degradation rate and easy processing and other excellent properties, it will soon be used in medical frontier fields such as controlled drug release. In particular, one type of polyanhydride poly[1,3-bis(p-carboxyphenoxy)propane-sebacic acid][P(CPP-SA)] copolymer, as a new type of matrix-type drug-controlled release material,...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61P37/00C08G67/04
Inventor 郭文迅黄开勋徐辉碧
Owner HUAZHONG UNIV OF SCI & TECH
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