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A kind of exenatide nasal cavity administration preparation and preparation method thereof

A technology for nasal administration preparations and exenatide, which is applied in the field of pharmaceutical preparations and pharmaceutical preparations of pharmaceutical engineering, can solve the problems of easy degradation and poor stability of exenatide, and achieves weight reduction, poor stability, and improved stability. Effects on quality of life

Active Publication Date: 2021-05-04
HEBEI NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of exenatide nasal cavity administration preparation, to overcome chitosan and sodium glycerophosphate temperature-sensitive hydrogel solution preparation poor long-term storage stability and exenatide easy to be degraded in solution state Shortcomings

Method used

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  • A kind of exenatide nasal cavity administration preparation and preparation method thereof
  • A kind of exenatide nasal cavity administration preparation and preparation method thereof
  • A kind of exenatide nasal cavity administration preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of Exenatide Nasal Administration Preparation

[0028] Dissolve chitosan in 0.1 M lactic acid. After fully dissolving, add the mixed aqueous solution of inorganic salt and sodium glycerophosphate dropwise under ice bath conditions, stir at 200 rpm for 15 minutes, and mix well; then, add For exenatide, adjust the pH of the mixed solution to 4.0-6.0 with 0.1M sodium hydroxide and 0.1M hydrochloric acid, stir at 200 rpm for 15 minutes, mix well, and dispense into 1 ml EP tubes or vials. After pre-freezing at -80°C for 12 hours, vacuum freeze-drying with a lyophilizer for 12 hours to obtain a lyophilized powder preparation for nasal administration containing exenatide.

[0029] Viscosity measurement method: put the solution in a small beaker with an interlayer, keep the temperature of the solution in the beaker constant by controlling the temperature of the interlayer, and use the NDJ-8S rotational viscometer to measure the rotational viscosity of the ...

Embodiment 2

[0034] Dissolve chitosan (molecular weight: 80,000-120,000) in 0.1M lactic acid, add magnesium chloride / α,β-sodium glycerophosphate dropwise to it under ice bath conditions, adjust the pH to 6.0 with NaOH, 200 Stir at rpm for 15 minutes. The concentrations of chitosan, α,β-sodium glycerophosphate and magnesium chloride in the solution are shown in Table 1. The prepared chitosan / α,β-sodium glycerophosphate / magnesium chloride mixed solution is subpackaged, and freeze-dried powder is obtained after vacuum freeze-drying treatment, and deionized water is added to redissolve, and the volume of the solution is the same as that before freeze-drying. The influence of the concentration of each substance in the system on the resolubility of the lyophilized powder, the formation of hydrogel at 4 ℃, 20 ℃ and 37 ℃ and the long-term storage stability of the lyophilized powder were investigated.

[0035]The experimental results are shown in Table 1. Whether the chitosan / α,β-sodium glyceropho...

Embodiment 3

[0038] Dissolve chitosan in 0.1M lactic acid, add calcium chloride / α,β-sodium glycerophosphate dropwise to it in an ice bath, adjust the pH to 6.0 with NaOH, and stir at 100 rpm for 15 minutes . The concentrations of chitosan, α,β-sodium glycerophosphate and calcium chloride in the solution are shown in Table 2. The mixed chitosan / α,β-sodium glycerophosphate / calcium chloride mixed solution was subpackaged, and the freeze-dried powder was obtained by vacuum freeze-drying, and redissolved in deionized water. The volume of the solution was the same as before freeze-drying. The effect of the concentration of each substance in the lyophilized powder on the resolubility of the lyophilized powder, the formation of hydrogel at 4 ℃, 20 ℃ and 37 ℃, and the long-term storage stability of the lyophilized powder.

[0039] The experimental results are shown in Table 2. Whether the redissolution of the chitosan / α,β-sodium glycerophosphate / calcium chloride hydrogel system is affected by the ...

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Abstract

The invention discloses an exenatide nasal cavity administration preparation, which is in the form of freeze-dried powder. The active ingredients in the reconstitution solution include chitosan, sodium glycerophosphate, magnesium chloride or calcium chloride, and exenatide. Its preparation method is: (1) dissolving chitosan or its derivatives at room temperature; (2) slowly adding sodium glycerophosphate and inorganic salt mixed solution under ice-bath conditions, and stirring; (3) adding For exenatide, adjust the pH value of the solution to 4.0-6.0, and freeze-dry to obtain the finished product. The lyophilized powder reconstitution solution can be stored in the form of a solution for more than two weeks at room temperature or in a refrigerator, and forms a hydrogel within 8 to 123 minutes at body temperature to achieve sustained release of exenatide and promote exenatide recovery. Through the penetration, improve the bioavailability of exenatide. The reconstituted Exenatide Nasal Administration Solution can be used for nasal administration to help obese people reduce their body weight and improve their quality of life.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a freeze-dried powder nasal administration preparation containing exenatide, which belongs to the pharmaceutical preparation technical field of medical engineering. Background technique [0002] Exenatide is an agonist of glucagon-like peptide receptors, which can promote the proliferation of pancreatic β cells, promote insulin secretion, increase the body's sensitivity to insulin, and delay gastric emptying. Exenatide injection was approved by the US Food and Drug Administration in 2005 for the adjuvant treatment of type 2 diabetes. Clinical studies in recent years have shown that exenatide can also be used to reduce the weight of type 2 diabetic patients and non-diabetic obese people, and is used for weight loss treatment of obese people. However, the current route of administration of exenatide is injection. Because of its short half-life, it needs to be administered twice a da...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/22A61K9/19A61K47/36A61K47/10A61K47/02A61P3/04
CPCA61K9/0002A61K9/0019A61K9/0034A61K9/0043A61K9/19A61K38/22A61K47/02A61K47/10A61K47/36
Inventor 贺进田武广昊袁园李莹王改珍
Owner HEBEI NORMAL UNIV
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