Novel oral delivery composition containing liraglutide derivative and application of novel oral delivery composition
A technology of liraglutide and composition, applied in the field of oral delivery composition, can solve the problems of inconvenient administration frequency and subcutaneous administration, poor patient compliance, short duration, etc., achieve good oral bioavailability efficiency, reduce painful effect
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Embodiment 1
[0042] 1. Synthesis of chemically modified lysine
[0043] 1.1. Weigh 20g of Wang resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DMF, and swell the resin with DMF for 30 minutes, take 9.05g of Fmoc-Lys(Alloc)-OH for use DMF was dissolved, activated by adding 6.65mL DIEA in an ice-water bath, and then added to the above-mentioned reaction column filled with resin. After 2 hours of reaction, 10mL of anhydrous methanol was added to block for 1 hour. Wash 3 times with DMF and 3 times with DCM, then block with anhydrous methanol for 30 minutes, shrink and dry with methanol to obtain Fmoc-Lys(Alloc)-Wang resin, the detection degree of substitution is 0.605mmol / g.
[0044] 1.2. Weigh 10.0g (6.0mmol) of Fmoc-Lys(Alloc)-Wang resin with a substitution degree of 0.605mmol / g, add it to the solid phase reaction column, wash it twice with DMF, and swell Fmoc-Lys(Alloc) with DMF -Wang resin 30 minutes later, add 30mL dichloromethan...
Embodiment 2
[0069] 1. Synthesis of chemically modified lysine
[0070] 1.1. Weigh 20g of Wang resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DMF, and swell the resin with DMF for 30 minutes, take 9.05g of Fmoc-Lys(Alloc)-OH for use Dissolve DMF, activate by adding 6.65mL DIEA in an ice-water bath, add to the above-mentioned reaction column filled with resin, react for 2 hours, add 10mL of anhydrous methanol to seal for 1 hour; wash with DMF for 3 times, DCM for 3 times, and then use After blocking with anhydrous methanol for 30 minutes, the methanol was shrunk and drained to obtain Fmoc-Lys(Alloc)-Wang resin, and the detected substitution degree was 0.605 mmol / g.
[0071] 1.2. Weigh 10.0g (6.0mmol) of Fmoc-Lys(Alloc)-Wang resin with a substitution degree of 0.605mmol / g, add it to the solid phase reaction column, wash it twice with DMF, and swell Fmoc-Lys(Alloc) with DMF -Wang resin 30 minutes later, add 30mL dichloromethane, the...
Embodiment 3
[0096] 1. Synthesis of chemically modified lysine
[0097] 1.1. Weigh 20g of Wang resin with a substitution degree of 1.0mmol / g, add it to a solid-phase reaction column, wash it twice with DMF, and swell the resin with DMF for 30 minutes, take 9.05g of Fmoc-Lys(Alloc)-OH for use Dissolve DMF, activate by adding 6.65mL DIEA in an ice-water bath, add to the above-mentioned reaction column filled with resin, react for 2 hours, add 10mL of anhydrous methanol to seal for 1 hour; wash with DMF for 3 times, DCM for 3 times, and then use After blocking with anhydrous methanol for 30 minutes, the methanol was shrunk and drained to obtain Fmoc-Lys(Alloc)-Wang resin, and the detected substitution degree was 0.605 mmol / g.
[0098] 1.2. Weigh 10.0g (6.0mmol) of Fmoc-Lys(Alloc)-Wang resin with a substitution degree of 0.605mmol / g, add it to the solid phase reaction column, wash it twice with DMF, and swell Fmoc-Lys(Alloc) with DMF -Wang resin 30 minutes later, add 30mL dichloromethane, the...
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