Insulin intranasal inhalation powder spray

A technique for inhaling powder and aerosol insulin, which is applied in the field of nasal insulin preparations, can solve the problems of poor physical stability, achieve rapid onset of action, reduce the risk of nasal irritation, and have high bioavailability

Inactive Publication Date: 2009-05-13
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Now through experimental investigation, it is found that lecithin and poloxamer are used as emulsifiers, because the HLB values ​​of the two are quite different (lecithin HLB is 5-6, and poloxamer HLB is 25), the physical stability of the obtained system Poor, although both have good safety and are widely used in the preparation of fat emulsions, the particle size of the resulting emulsion is often greater than 100nm

Method used

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  • Insulin intranasal inhalation powder spray
  • Insulin intranasal inhalation powder spray
  • Insulin intranasal inhalation powder spray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0093] Get 75mg of chitosan and dissolve it with 1ml0.1mol / l hydrochloric acid for subsequent use;

[0094] Take 1.6g of lecithin, 2.0ml of caprylic acid glyceride, 0.4g of tween80 and 40mg of vitamin E, dissolve at 60°C to obtain the oil phase;

[0095] Pour the oil phase into distilled water at the same temperature at 60°C, stir to obtain colostrum, and circulate the colostrum under a high-pressure milk homogenizer at a pressure of 800 bar for 6 times to obtain 60ml of blank microemulsion. The average particle size of oil droplets is About 45nm;

[0096] Mix 3.0 g of insulin with the above microemulsion, add chitosan solution, add 0.3 ml of 3mol / l HCl dropwise to dissolve insulin; add 3.0 g of mannitol, adjust pH to 4.0 with 0.1 mol / l NaOH, and freeze-dry to obtain insulin nanoemulsion dry powder, freeze-drying procedure:

[0097] -40°C 4h, -15°C 12h, -5°C 4h, 5°C 4h, 20°C 2h, the lowest eutectic point is -9.4°C; the dry powder is sieved and mixed with the mixture of manni...

Embodiment 2

[0099] Get chitosan 75mg and dissolve it with 1ml 0.1mol / l hydrochloric acid for subsequent use;

[0100] Take 1.6g of lecithin, 2.0ml of caprylic acid glyceride, 0.4g of tween80 and 40mg of vitamin E, dissolve at 60°C to obtain the oil phase;

[0101] Pour the oil phase into distilled water at the same temperature at 60°C, stir to obtain colostrum, and circulate the colostrum under a high-pressure homogenizer at a pressure of 600 bar for 6 times to obtain 60ml of blank microemulsion. The average particle size of oil droplets is About 60nm;

[0102] Take 3.0g of insulin and mix it with the above microemulsion, add chitosan solution, add dropwise 0.3ml 3mol / l HCl to dissolve insulin; add 3.0g mannitol, adjust the pH to 4.0 with 0.1mol / l NaOH, freeze-dry to obtain insulin nano Dry powder of milk, freeze-drying procedure: -40°C 4h, -15°C 12h, -5°C 4h, 5°C 4h, 20°C 2h, the lowest eutectic point is -9.6°C; Crystalline cellulose mixed, mannitol:microcrystalline cellulose=1:1, weig...

Embodiment 3

[0104] Get chitosan 75mg and dissolve it with 1ml 0.1mol / l hydrochloric acid for subsequent use;

[0105] Take 1.6g of lecithin, 2.0ml of caprylic acid glyceride, 0.4g of tween80 and 40mg of vitamin E, dissolve at 60°C to obtain the oil phase;

[0106] Pour the oil phase into distilled water at the same temperature at 60°C, stir to obtain colostrum, and circulate the colostrum under a high-pressure homogenizer at a pressure of 400 bar for 6 times to obtain 60ml of blank microemulsion. The average particle size of oil droplets is About 95nm;

[0107] Take 3.0g of insulin and mix it with the above microemulsion, add chitosan solution, add dropwise 0.3ml 3mol / l HCl to dissolve insulin; add 3.0g mannitol, adjust the pH to 4.0 with 0.1mol / l NaOH, freeze-dry to obtain insulin nano Dry powder of milk, freeze-drying procedure: -40°C 4h, -15°C 12h, -5°C 4h, 5°C 4h, 20°C 2h, the lowest eutectic point is -9.8°C; Crystalline cellulose mixed, mannitol:microcrystalline cellulose=1:1, weig...

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Abstract

The invention provides insulin nasal dry powder inhalation which comprises the following components by contents (weight percentages): 1% to 100% of insulin freeze-dry powder with self emulsifying effect and 0% to 99% of carrier. In the insulin nasal dry powder inhalation, the dosage of grease is determined according to the surface area and the grain size of grease drops, and a large quantity of animal experiments prove that under the condition and in the proportion, the optimal drug treatment effect can be achieved. Compared with the liquid preparation, the stability of the dry powder is increased, and the dry powder can be automatically re-dissolved into nano-sized emulsion after being in contact with water; after the drug-containing compound enters the nasal cavity, the nano-size emulsion easily passes by the barrier of the nasal mucosa and enters the body via the rich capillaries and lymphatic vessels in the nasal mucosa to exert the efficacy, thereby remarkably improving the bioavailability of the drug and being rapidly absorbed, without stimulation to the nasal mucosa; in addition, the adoption of bio-adhesive increases the retention time of the drug-containing powder on the nasal mucosa, so that the absorption and the utilization of the drug are more complete.

Description

technical field [0001] The invention relates to an insulin nasal preparation, in particular to an insulin nasal inhalation powder mist and a preparation method thereof. Background technique [0002] Insulin is a polypeptide hormone consisting of 51 amino acids with a molecular weight of approximately 5800, which is produced in the beta cells of the pancreatic islets of normal individuals (non-diabetic). Insulin mainly plays a role in regulating glucose metabolism and lowering blood sugar levels; the lack of insulin will lead to diabetes. Many diabetics require long-term frequent administration of insulin to maintain acceptable blood sugar levels. [0003] Insulin is most commonly given as an injection under the skin, usually into the abdomen or upper thigh. To maintain acceptable blood sugar levels, insulin injections are usually required at least once or twice a day, supplemented with rapid-acting insulin injections as necessary. Injection administration of insulin bring...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K38/28A61K47/38A61P3/10
Inventor 金方雷伯开闻聪
Owner SHANGHAI INST OF PHARMA IND CO LTD
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