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Exenatide oral nanoparticle

A technology of exenatide and nanoparticles, which is applied in the field of exenatide-containing oral nanoparticles and its preparation, which can solve the problems of poor fat solubility, chemical and conformational instability, and large molecular weight

Inactive Publication Date: 2016-02-24
SHANDONG LUYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term injection administration brings great pain to patients, and patients' compliance is poor. Oral route is currently the most widely used and more convenient way of administration. However, due to the low oral bioavailability of protein and polypeptide drugs, most protein and polypeptide drugs Little or no absorption through the gastrointestinal tract, which limits its clinical application, the main reasons are: (1) large molecular weight, poor fat solubility, difficult to pass through the biofilm barrier; (2) there are a large number of peptidases and Proteolytic enzymes can degrade polypeptides and proteins; (3) easily eliminated by the liver after absorption; (4) have chemical and conformational instability problems

Method used

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Examples

Experimental program
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Effect test

Embodiment 1

[0015] The synthesis of embodiment 1CSK polypeptide

[0016] 1. Resin swelling

[0017] Put 100% resin into the reaction tube, add 1500ml dimethylformamide (DMF), and swell for 30min.

[0018] 2. Deprotection

[0019] Remove DMF, add 1500ml 20% piperidine DMF solution, remove after 5min, add 1500ml 20% piperidine DMF solution, 15min.

[0020] 3. Detection

[0021] Take out the piperidine solution, take more than a dozen resins, wash with ethanol three times, add ninhydrin, potassium cyanide (KCN), and one drop of phenol solution, and heat at 105C-110C for 5min.

[0022] 4. Washing

[0023] Wash twice with 1000ml DMF, methanol and DMF respectively.

[0024] 5. Condensation

[0025] According to the amino acid sequence of the required polypeptide, add 10mmol amino-terminal protected amino acid, 30mmol coupling agent 2-(7-azobenzotriazole)-tetramethyluronium hexafluorophosphate (HBTU), use as little DMF as possible Dissolve, add to the reaction tube, and immediately add mo...

Embodiment 2

[0034] The preparation of embodiment 2CSK-chitosan

[0035] 1. Dissolve 100mg of the purified peptide in PBS, soak in ice bath for 15min and set aside.

[0036] 2. Add 200 mg of 1-ethyl-3-(dimethylaminopropyl) carbodiimide hydrochloride (EDC) and 200 mg of N-hydroxysuccinimide (NHS) to the polypeptide PBS solution in 1. ) Low temperature reaction for 1h.

[0037] 3. Add 100 mg of chitosan to the reaction solution, and react for 4 hours.

[0038] 4. Prepare 2000ml of phosphate buffer solution with a pH of 7.4.

[0039] 5. Pack the reaction solution in a dialysis bag and tie it tightly, and dialyze it in the buffer solution for 48 hours.

[0040] 6. Freeze-dry the dialyzed product to obtain CSK-chitosan (1:1).

[0041] Other weight ratios of CSK-chitosan adopt the same method as above, and the required reagents and consumption are shown in Table 1:

[0042] Table 1 prepares the required reagents and consumption of different weight ratios of CSK-chitosan

[0043]

Embodiment 3

[0045] 10ml1mg / ml chitosan solution (dissolved in 0.25% acetic acid), under magnetic stirring, add 0.5ml2mg / mlExenatide solution under gravity with 5ml syringe, add 2.5mg / mlTPP aqueous solution 1.8ml under gravity with 5ml syringe, Stir with a magnetic stirrer at 500 rpm for 50 min, and centrifuge at 3500 rpm for 30 min. Add 0.1 mg of preservative potassium sorbate and 1 mg of sodium malate flavoring agent to the prepared nanoparticle solution to obtain the nanoparticle oral liquid preparation.

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Abstract

The invention provides an exenatide oral nanoparticle and a preparation method thereof. The exenatide oral nanoparticle contains exenatide and CSK-chitosan. The exenatide oral nanoparticle can substantially improve the oral administration absorption effect, improves the bioavailability, and realizes fast blood sugar lowering effect and stable blood sugar.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to oral nanoparticles containing exenatide and a preparation method thereof. Background technique [0002] Diabetes mellitus is a systemic metabolic disease characterized by chronic hyperglycemia, manifested as defects in insulin secretion or impairment of insulin biological action. According to statistics, there are currently about 140 million diabetics in the world, and due to factors such as population aging and increased incidence of obesity, it is estimated that in 2025, global diabetics will reach 300 million. According to pathological features, it can be divided into insulin-dependent (IDDM, type I) and non-insulin-dependent (NIDDM, type II) diabetes. Type I diabetes is characterized by reduced or complete loss of insulin secretion, and clinical treatment requires daily subcutaneous injection of insulin; type II diabetes is characterized by the inability of the hum...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K38/22A61K47/36A61P3/10
Inventor 李想李又欣孙考祥刘万卉王麒麟张方喜
Owner SHANDONG LUYE PHARMA CO LTD
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