Oral sublingual tablet formula and method for preparing oral sublingual tablet by using insulin lipidosome, insulin microsphere (capsule), and insulin nanoparticle (capsule) as raw materials

Abstract

The invention relates to a sublingual tablet formula and a method for preparing the sublingual tablet by using an insulin lipidosome, an insulin microsphere (capsule), and an insulin nanoparticle (capsule) as raw materials. The method is ingenious in conception; various oral sticking agents, oral mucus membrane absorption promoters, oral enzyme inhibitors and the like are scientifically selected and mixed, so that the insulin lipidosome, the insulin microsphere (capsule) and the insulin nanoparticle (capsule) can fast penetrate the oral mucus membrane to enter blood. Through the adoption of the method, a difficult problem that effects of an oral insulin can be reduced by enzymolysis of intestines and stomach enzymes and an first-pass effect of the liver is broken over; the sublingual tablet is safe, effective, controlled in slow release, stable in stability, and excellent in blood sugar reducing effect, and can completely replace an injection; a world-class difficult problem which troubles the medical field for many years can be fundamentally solved, and great convenience is brought to a patient with diabetes.

Description

technical field [0001] The invention relates to a formula and method for preparing oral sublingual buccal tablets using insulin liposomes, microspheres (capsules) and nanoparticle (capsules) as raw materials for treating type I and type II diabetes. It belongs to the field of protein and polypeptide biopharmaceuticals. Background technique [0002] Oral insulin is a world-class problem. For decades, scientists all over the world have racked their brains to find a way to replace insulin injection therapy, but no product has come out yet. The core problem is: because insulin is a protein polypeptide drug with large molecular weight and poor fat solubility, it is not easy to pass through biomembranes; oral administration will be enzymatically hydrolyzed by proteolytic enzymes in the gastrointestinal tract and the first-pass effect of the liver will lose its activity. In order to solve the above problems, many scientists study sublingual administration so that it can directly ...

AI Technical Summary

Problems solved by technology

The core problem is: because insulin is a protein polypeptide drug with large molecular weight and poor fat solubility, it is not easy to pass through biomembranes; oral administration will be enzymatically hydrolyzed by proteolytic enzymes in the gastrointestinal tract and the liver will lose its activity.

However, due to the complex process, low relative bioavailability, poor controllability, and the destructiveness of the penetration enhancer to the sublingual mucosa, it is difficult to guarantee the safety