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Study on the Degradable Poly (Ether-anhydride) Photocrosslinked Gel for Hydrophobic Drugs

Author: YangJi
Tutor: WangZheng
School: Tianjin University
Course: Pharmacy
Keywords: Photo-crosslinkable Poly (ether - anhydride) Gel Indomethacin Drug solubilization
CLC: R94
Type: Master's thesis
Year: 2007
Downloads: 69
Quote: 0
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Abstract


Some water insoluble drugs lead to low bioavailability because of its poor solubility, absorption is not completely serious impact on its clinical application to become a major problem faced by the preparation field. Many scholars at home and abroad dedicated to the solubilization of insoluble drugs and achieved certain results, such as made of solid dispersion and cyclodextrin inclusion complexes, soluble prodrug, but are present in varying degrees shortcomings, such as the storage instability. To solve this problem, this paper proposes a package containing a biodegradable three-dimensional optical cross-linked network gel insoluble drugs and achieve the idea of ??drug solubilization and storage stability. This selection of the FDA approved the polyethylene glycols PEG of biocompatible material for the human body, sebacic acid, SA, etc. as a skeleton composed of the gel network, the introduction of hydrophilic PEG polyanhydride segment so that two The advantage of the material to be fully reflected. PEG derivatives and sebacic acid by a double capped biocompatible initiator, 2,2 - dimethoxy - 2 - phenyl acetophenone initiator, UV irradiation free radical polymerization reaction, the formation of biodegradable poly (ether - anhydride) three-dimensional optical cross-linked network gel, Structure Characterization by FTIR and 1H NMR and swelling and degradation of performance measurement. Together with the in situ method and after the package are two ways of poorly water-soluble model drug indomethacin package contained in the gel, to meet the different purpose of the medication. Determination of the presence of drug morphology and storage stability, made of two methods of drug-loaded gel the indomethacin are amorphous or molecular state distribution, and after 8 months of storage, still maintaining the original through the X-ray and DSC morphology, no precipitation of crystals; drug in vitro dissolution test show that the packet contained in the poly (ether - anhydride) of the drug in the network have a more crystalline bulk drug faster dissolution rate and the amount of cumulative dissolution, and by adjusting the affinity, hydrophobic the molecular monomer ratio may delay the drug release. Poly (ether - anhydride) in the gel network, the introduction of the polyethylene glycol may effectively increase the surface wettability of poorly soluble drugs, the distribution state of amorphous or molecular form able to increase the surface area of ??the drug contact with the media, the three-dimensional network can be effectively inhibit drug crystallization, this method is expected to solve the problem of poorly water-soluble drug solubility and dissolution rate is low and unstable drug physical form preparation easy crystallization aging, poorly soluble drug solubilization put forward a new idea to the field of pharmaceutical preparations The overall development has a certain significance.

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