Method for oral delivery of proteins
A protein and matrix technology, applied in the field of oral release of protein, can solve the problem of lack of available release carriers
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Embodiment 1
[0042] pH-dependent release of P(MAA-g-EG) hydrogel contents
[0043] The ability of P(MAA-g-EG) hydrogels to serve as release vehicles for three compounds of different sizes: theophylline (MW 180.2), vancomycin (MW 1485.7) and insulin (MW 5733.2) was investigated.
[0044] P(MAA-g-EG) hydrogels were prepared by radical solution polymerization of methacrylic acid and poly(ethylene glycol) monomethacrylate at 37 °C, and the resulting oligomer chains were combined with dimethylmethacrylate Tetraglycerides cross-linked. The resulting hydrogel was rinsed in deionized water for one week to remove unreacted monomers and un-crosslinked oligomer chains, vacuum dried and ground into a powder with an average particle diameter of 100-150 μm.
[0045]Drug incorporation experiments were performed using theophylline (MW 180.2), vancomycin (MW 1485.7) and insulin (MW 5733.2). Each drug was dissolved in pH 7.4 phosphate buffer and P(MAA-g-EG) hydrogel was added to the drug solution to load ...
Embodiment 2
[0049] In vitro mucoadhesion studies
[0050] P(MAA-g-EG) hydrogels were fabricated into thin films using solution polymerization technique. The hydrogels were swollen and equilibrated in DMGA buffered saline at pH = 3.2 and 7.4. The swelled hydrogel was cut into disks with a diameter of 20 cm and placed in a tensile tester at 25°C and 90% RH. Whereas the gelled bovine submandibular mucin sample was fixed in the lower port with adhesive, the polymer sample was adhered to the upper handle of the detector using cyanoacrylate medical adhesive. The two mouths were pulled together for 15 minutes and then separated at a speed of 1 mm / min. The separation force was measured as a function of displacement. Work of separation, equal to the work of bioadhesion calculated by the area under the curve.
[0051] Since P(MAA-g-EG) hydrogel can block the effect of protease inhibitors, and can be attached to the intestinal wall mucosa, making close contact and thus facilitating the absorptio...
Embodiment 3
[0058] In Vivo Study of Insulin Administration in Rats
[0059] Graft copolymers were prepared by free-radical solution polymerization of methacrylic acid and poly(ethylene glycol) monomethacrylate. The resulting hydrogel was rinsed in deionized water for 7 days to remove unreacted monomer and un-crosslinked oligomer chains, and the hydrogel was vacuum dried and ground into a powder. The powder is filtered to obtain granules with an average particle diameter of 100-150 μm. Crystalline porcine insulin (26.9 U / mg) was loaded by balanced distribution. The drug-loaded particles were filtered and washed to remove surface drug and vacuum dried.
[0060] Male Wistar rats (200 g) were fasted for 24 hours. Rats were fixed in the supine position, and insulin-loaded polymer gelatin capsule microparticles were administered, and the gelatin capsules dissolved immediately in the stomach. Blood samples were collected from the jugular vein in 0.2 ml aliquots for serum glucose before the e...
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