Ibuprofen end group-containing polyethylene glycol medicine macromonomer and synthesis method thereof

A polyethylene glycol and macromonomer technology, which is applied in the directions of drug combinations, pharmaceutical formulations, and medical preparations containing active ingredients, can solve the problems of high price of polyethylene glycol, difficult preparation, and gastrointestinal irritation, etc. Achieve the effect of not easily adhering to the blood vessel wall, mild operating conditions, and long half-life
CN101974150AInactive Publication Date: 2011-02-16EAST CHINA NORMAL UNIV
2 Cites 2 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
EAST CHINA NORMAL UNIV
Publication Date
2011-02-16
Estimated Expiration
Not applicable · inactive patent

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention relates to an ibuprofen end group-containing polyethylene glycol medicine macromonomer and a synthesis method thereof, belonging to the technical field of pharmaceutical chemistry and synthesis thereof. The macromonomer is white powder, is soluble in N,N-dimethylformamide, methylene dichloride, chloroform, dioxane, dimethyl sulfoxide, distilled water or phosphoric acid PBS buffer solution, is not soluble in petroleum ether or aether, and has a structure as shown in the specification, wherein n is an integral number in a interval of 45-224. Under the catalysis condition, polyethylene glycol reacts with ibuprofen acyl chloride to synthesize the crude macromonomer, and then the crude macromonomer is purified to obtain the finished macromonomer, wherein the raw material ibuprofen acyl chloride is synthesized by referencing the known literatures. The macromonomer has the advantages of long half-life period, good water-solubility, little dosage, low toxicity and small thrill on intestines and stomach, contains degradable ester bonds, and is especially suitable for being used as an active component of ibuprofen slow-release drugs.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention relates to a polyethylene glycol drug macromonomer containing ibuprofen end groups and a synthesis method thereof, belonging to the technical field of medicinal chemistry and synthesis thereof. Background technique

[0002] Small-molecule drugs have disadvantages such as short half-life, fast metabolism, and large side effects. Clinical applications often require repeated administration, which increases toxicity and side effects; poor water solubility affects human absorption. In order to solve the above problems, the modification of small molecule drugs has become a research hotspot in recent years. Linking small drug molecules to macromolecules to achieve sustained release or targeting properties can effectively improve their transport and absorption in vivo. Polyethylene glycol is non-toxic, non-teratogenic, non-immunogenic, long half-life, various types, good water solubility and biocompatibility, small molecule drugs modified with i...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More