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Insulin flexible particles and preparation thereof

A kind of insulin and flexible technology, which is applied in the field of flexible insulin particles and its preparations, can solve the problems of flexibility and hypoglycemic effect, and limit the development and application of insulin non-injection preparations, and achieve high transmucosal transport capacity and good flexibility Effect

Active Publication Date: 2019-11-19
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] However, further research conducted by the present inventors later found that the "new nanovesicle" in the public document 201410174195.1, because no ionic surfactant was added, its flexibility and hypoglycemic effect were still not ideal, which limited the non-injection of insulin to the preparation. Development and Application

Method used

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  • Insulin flexible particles and preparation thereof
  • Insulin flexible particles and preparation thereof
  • Insulin flexible particles and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1: Insulin / phospholipid complex

[0070] Take 60 mg of insulin, feed the mass ratio of insulin: phospholipid according to 1:3, 1:5, 1:10, 1:20, 1:50, and prepare as follows:

[0071]Dissolve 60 mg of insulin in 6 mL of methanol solution containing 0.1% trifluoroacetic acid; dissolve 180 mg, 300 mg, 600 mg, 1200 mg and 3000 mg of soybean lecithin in 54 mL of dichloromethane, and mix the above two solutions to form a clear solution. The solution was rotary evaporated under reduced pressure at 37°C until the solvent was evaporated to dryness, placed in a vacuum oven, dried and then scraped into a closed container to obtain a series of insulin-phospholipid complexes, labeled as complex I, II, III, IV, V.

Embodiment 2

[0072] Example 2: Using insulin / phospholipid complexes as intermediate carriers to prepare flexible insulin particles

[0073] Take 660 mg of insulin / phospholipid complex III prepared in Example 1, and dissolve it together with 400 mg of Tween20 and 100 mg of sodium deoxycholate in 20 ml of a mixed solvent (chloroform:methanol=3:1) to form a clear solution. The solution was rotary evaporated under reduced pressure at 37°C until the solvent evaporated to dryness to obtain a dry film. Use 20mL of phosphate buffer (0.02mol / L) to hydrate the formed film for 30min. After the hydration is completed, the probe is ultrasonically dispersed (150W, 1min / time, 4 times in total) and passed through the membrane (0.22μm) to obtain Flexible microparticles with insulin / phospholipid complexes as intermediate carriers. The particle size measured by the laser particle size analyzer is 80.57±0.68nm, the PDI is 0.268±0.011, the zeta potential is -25.27±0.85mV, the encapsulation rate is 72.06±1.84%...

Embodiment 3

[0075] Example 3: Using insulin / phospholipid complexes as intermediate carriers to prepare flexible insulin particles

[0076] Take 660 mg of insulin / phospholipid complex III prepared in Example 1 and 400 mg of Tween20 and dissolve them together in 20 mL of dichloromethane to form a clear solution. The solution was rotary evaporated under reduced pressure at 37°C until the solvent evaporated to dryness to obtain a dry film. Dissolve 100 mg of sodium deoxycholate in 20 mL of phosphate buffer (0.02 mol / L) to obtain a phosphate buffer of sodium deoxycholate. Use the phosphate buffer solution of sodium deoxycholate to hydrate the formed film for 30 minutes. After the hydration is completed, the probe is ultrasonically dispersed (150W, 1min / time, 4 times in total) and passed through the membrane (0.22μm) to obtain insulin / phospholipid complex is the flexible particle of the intermediate carrier. The particle size measured by the laser particle size analyzer is 84.57±0.65nm, the ...

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Abstract

The invention discloses insulin flexible particles and a preparation thereof. The insulin flexible particles contain an insulin / phospholipid composite and an ionic surfactant and are vesicles of circular or oval structures, the particle size is 5000nm or below, and the drug encapsulation rate is 60 percent or above. The insulin flexible particles of the invention can further contain a nonionic surfactant, free phospholipid or cholesterol. The insulin flexible particles of the invention differ in composition from insulin contained vesicles or flexible vesicles reported in the prior literatures,is also different from novel insulin contained nanovesicles as reported in the prior literatures, thus having better flexibility and higher transmucosal transport capacity. The insulin flexible particles of the invention can be prepared into clinically acceptable dosage forms by being added with an excipient for insulin parenteral administration delivery including intranasal administration, oraladministration, transdermal administration and pulmonary inhalation.

Description

technical field [0001] The invention relates to a flexible particle of insulin and its preparation, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Since the FDA approved the marketing of recombinant human insulin in 1982, peptide protein drugs have been widely used in the treatment of diseases. Insulin is the mainstay drug for the treatment of diabetes, but limited by its physical and chemical properties, it is almost not absorbed when administered orally, and it is mainly administered by injection in clinical practice. However, long-term frequent injections have poor compliance and bring great pain to patients. Therefore, non-injection administration of insulin has always been a hot topic in the medical field, but there has been no substantial breakthrough so far. The main constraints are due to the large molecular weight of insulin (5800Da), low fat solubility, poor stability, serious enzyme barriers and Membrane barrier an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/127A61K47/24A61P3/10
CPCA61K38/28A61K9/1271A61K9/006A61K47/24A61P3/10
Inventor 刘玉玲夏学军张星徐优
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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