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

A self-nanoemulsion, oral preparation technology, applied in the field of oral preparations, can solve the problems of not being suitable for clinical use, unsatisfactory results, bioavailability lower than 5%, etc., to improve bioavailability, shorten contact time, and formulate composition. simple effect

Active Publication Date: 2020-01-10
GUANGDONG GENERAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 determines that insulin (INS) self-microemulsion system optimal prescription

[0035] (1) Test of INS solubility

[0036] ①Preparation of different test samples: Weigh 50mg / part of INS raw material drug (Tonghua Dongbao Pharmaceutical Co., Ltd.), and put it into a 5mL graduated centrifuge tube with stopper. Add 5 mL each of different oil phases, co-surfactants, and surfactants, seal, and vortex to mix. Place at 4±1°C, vortex, and dissolve for 60h. Centrifuge at 4000r / min for 10min. Take the supernatant, filter it with a 0.45μm microporous membrane, accurately measure 0.2mL of the filtrate, add 1.8mL of HCl solution with a concentration of 0.01mol / L, vortex (the vortex in front, please be consistent) for 10min, and centrifuge at 4000r / min After 10 minutes, remove the lower layer, filter it with a 0.45 μm microporous membrane, take 0.1 mL of the filtrate, add 0.9 mL of 0.01 mol / L HCl solution, and mix well to obtain the test product. Three repetitions wer...

Embodiment 2

[0070] (1) According to the best combination determined in Example 1, add INS to propylene glycol, stir, and wait for the INS to be moistened to obtain solution A; add solution A to medium-chain triglycerides, stir and dissolve to obtain solution B; Add polyoxyethylene hydrogenated castor oil to solution B, and mix well to obtain an insulin self-nanometer emulsion containing INS, medium-chain triglycerides, propylene glycol, and polyoxyethylene hydrogenated castor oil (hereinafter referred to as: INS self-nanometer emulsion), which is packed in a sealed Store in sealed vials at 2-8°C.

[0071] Formula composition: Medium-chain triglycerides, polyoxyethylene hydrogenated castor oil and propylene glycol in a ratio of 0.22:0.55:0.23 by volume, and INS is 0.9 mg per mL of medium-chain triglycerides-polyoxyethylene hydrogenated castor oil-propylene glycol Add to. At the same time, the blank control is set from the nanoemulsion, that is, no INS is added.

[0072] (2) Determination...

Embodiment 3

[0086] Investigation on Appearance and Emulsification Rate of INS Self-nanometer Emulsion

[0087] Aspirate 3 parts of INS self-nanoemulsion prepared in step (1) of Example 2, 0.1 mL for each part, and quickly add 10 mL of ultrapure water respectively. The emulsification is complete when a stable clear transparent nanoemulsion with blue opalescence is formed, observe the appearance change of the emulsification process and the appearance of the formed nanoemulsion, and record the emulsification time (starting from adding water). Results: The appearance change order of the emulsification process is: clear, turbid, clear and blue at the same time, the appearance of the formed nanoemulsion is: clear, transparent, blue opalescent, after the emulsification is complete, timing, the emulsification time is 40 ±0.1s.

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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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/28A61K9/48A61K9/107A61K47/10A61K47/14A61K47/44A61P3/10
CPCA61K9/0053A61K9/1075A61K9/4858A61K38/28A61K47/10A61K47/14A61K47/44
Inventor 梁丽梅
Owner GUANGDONG GENERAL HOSPITAL
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