A kind of oral exenatide nanoparticle preparation and its preparation method and application
A technology of exenatide and nanoparticles, which is applied in the field of biomedicine, can solve the problems of low oral bioavailability, large molecular weight of exenatide, loss of activity, etc., and achieve high-efficiency maintenance of drug activity, good hypoglycemic effect, The effect of controlling blood sugar
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Embodiment 1
[0050] Example 1 Preparation of exenatide-loaded nanoparticles and enteric-coated microcapsule preparations using FNC technology
[0051] 1. Preparation of tannic acid (TA) and exenatide (EXE) nanocomposite cores
[0052] TA was dissolved in deionized water at a concentration of 0.1-0.9 mg / mL. EXE was dissolved in 0.2% acetic acid solution (HAc), and then the pH value was adjusted to different pH values (5.5-6.8) with NaOH solution, and the concentration of EXE solution was 0.3 mg / mL. The TA solution is distributed in the first and second channels, and the EXE solution is distributed in the third and fourth channels, such as figure 1 As shown, the four channels have the same flow rate, adjust the channel flow rate, 5 mL / min, 10 mL / min, 20 mL / min, 30 mL / min, 40 mL / min, 50 mL / min, make the two solutions pass through four The channel reaches the vortex mixing zone for mixing to obtain the nanocomposite core (NC) of TA and EXE.
[0053] figure 2 Shown is the effect of flow ...
Embodiment 2
[0065] Example 2 In vitro drug release experiment
[0066] Three preparations of NC, NP and E-NP were prepared under optimal conditions using RITC-labeled EXE for use. The E-NP preparation was placed in the HCl solution of pH = 2.5, at 37 o C, incubate in a shaker at 150 rpm, centrifuge at 10,000 rpm for 10 min every 2 h, take the supernatant, and measure the concentration of EXE in it. Figure 10 When the pH=2.5, the EXE release curves of E-NP prepared with different concentrations of Eudragit can be seen from the figure, when the concentration of Eudragit is 0.9 mg / mL, 1.2 mg / mL, and 1.5 mg / mL, within 2 hours 50%, 18% and 7% of EXE were released respectively, which shows that when the concentration of Eudragit is low, a large amount of EXE is released, which cannot effectively protect EXE from passing through the strong acid environment of the stomach. When the concentration of Eudragit increases to At 1.5 mg / mL, it can effectively protect EXE from rapid release in the aci...
Embodiment 3
[0068] Example 3 Small Intestine Permeability Test of Exenatide-loaded Nanoparticles
[0069] Two preparations of NC and NP were prepared under optimal conditions using RITC-labeled EXE for use. The SD rats were fasted for 12 hours, and after anesthesia, the duodenum, jejunum, and ileum of the small intestine of the rats were surgically removed with a length of 5 cm each, and then the rats were sacrificed. The two ends of the small intestine in different parts were ligated, and 1 mL of EXE solution, NC particle suspension, and NP particle suspension were injected, and then the small intestine was placed in 10 mL of krebs ringer buffer, 37 o C, dialyze in a shaking table at 150rpm, take out 1mL of dialysate every 0.5h, measure the concentration of EXE in it, and use the formula (3-3) to calculate the apparent permeability coefficient (PAPPvalue) of different EXE preparations.
[0070]
[0071] in, is the flux of fluorescently labeled nanoparticles or EXE permeating throug...
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