A kind of oral preparation containing polypeptide drug self-nanoemulsion and preparation method thereof

Abstract

The present invention discloses a polypeptide drug-containing self-nano-emulsion oral preparation and a preparation method thereof. According to the present invention, a polypeptide drug is added to an auxiliary surfactant, stirring is performed until the polypeptide medicine is wet to obtain a solution A, the solution A is added to an oil phase solution to dissolve and uniformly mix to obtain a solution B, a surfactant is added to the solution B, uniform mixing is performed to obtain a polypeptide drug-containing self-nano-emulsion, and the polypeptide drug-containing self-nano-emulsion is encapsulated in an enteric soft capsule from the nanoemulsion to obtain the polypeptide drug-containing self-nano-emulsion oral preparation. According to the present invention, the preparation method is simple, the obtained nanometer micro-emulsion has characteristics of small particle size, easy absorption, high bioavailability and good stability, wherein the particle size of 99.3% of the emulsion droplets is less than 44 nm, the Zeta potential is -6.4 mv, and the nano Milk with better stability.

Description

technical field [0001] The invention relates to an oral preparation, in particular to an oral preparation containing polypeptide drug self-nanometer emulsion and a preparation method thereof. Background technique [0002] With the development of biotechnology and genetic engineering, more and more peptide drugs are used in clinical treatment. Most peptide drugs are biologically active and unstable to heat, enzymes and other factors, so they are often administered by injection. However, long-term injections not only bring great pain and inconvenience to patients, but also cause various adverse reactions such as lipoatrophy, and require special injection techniques and equipment, which are costly and expensive. Therefore, pharmaceutical workers at home and abroad have been devoting themselves to the research of non-injection routes of polypeptide drugs, such as nasal cavity, rectal, oral, lung, eye, transdermal absorption and other routes of administration. Among the above ro...

AI Technical Summary

Problems solved by technology

There are many studies on the oral administration of polypeptide drugs such as insulin (INS). The earlier ones include liposomes, emulsions, enteric-coated preparations, etc., but the bioavailability is still lower than 5%. In recent years, there are microspheres, microemulsions, Nanoparticles, etc. But the results are still not ideal

Although there are currently studies on INS self-emulsifying oral preparations, the results are still not suitable for clinical use due to failure to develop the best combination of oil phase, surfactant, and co-surfactant species and their ratios suitable for INS. So far there is no oral INS self-emulsifying formulation on the market

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