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Pharmaceutical composition containing human glucagon-like peptide-1 analog administered through oral mucosa

A technology of glucagon and oral mucosa, applied in the direction of drug combination, non-active ingredients of polymer compounds, drug delivery, etc., can solve the problems that are difficult to achieve clinical application effects, and achieve rapid diffusion and penetration, improve bioavailability, Effects of short plasma half-life

Active Publication Date: 2020-06-26
CHENGDU JINKAI BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since Exendin-4 is a macromolecular substance, affected by the structure of the oral mucosa and the physiological environment of the oral cavity, it is not easy to be directly absorbed into the blood circulation through the oral mucosa. Oral mucosal preparations composed of a variety of excipients, but it is found in experiments that it is still difficult to achieve the ideal clinical application effect. Therefore, it is urgent to develop a new dosage form of Exendin-4 administered through the oral mucosa to achieve the desired therapeutic effect. , instead of injectable drug use

Method used

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  • Pharmaceutical composition containing human glucagon-like peptide-1 analog administered through oral mucosa
  • Pharmaceutical composition containing human glucagon-like peptide-1 analog administered through oral mucosa
  • Pharmaceutical composition containing human glucagon-like peptide-1 analog administered through oral mucosa

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1. Exendin-4-containing pharmaceutical composition administered through oral mucosa and preparation method thereof

[0044] Thaw the recombinantly prepared Exendin-4 protein stock solution (purity 98%, concentration 1.5mg / ml) and rhPH20 protein stock solution (purity 98%, activity 500-20000U / ml) at room temperature or 2-8°C, after thawing Store at 2-8°C.

[0045] Accurately weigh the mucosal adsorbent and / or thickener according to the proportions of the ingredients of the pharmaceutical composition A-X in Table 1 below, dissolve them in water for injection and prepare a mixed solution, add the thawed rhPH20 protein stock solution, mix well, and finally Add Exendin-4 protein stock solution, stir and mix well, filter and sterilize with a filter membrane with a pore size of 0.22 μm under sterile conditions to obtain pharmaceutical compositions A-X respectively.

[0046] Table 1. The ratio of each component of the pharmaceutical composition A-X

[0047]

[0...

Embodiment 2

[0050] Example 2 Detection of Active Ingredients in Exendin-4-containing Pharmaceutical Compositions Administered Through the Oral Mucosa

[0051] 1) Detect the biological activity of Exendin-4 in the pharmaceutical composition A-X:

[0052] Adopt cAMP assay method to detect Exendin-4 biological activity in the above-mentioned pharmaceutical composition A-X, high performance liquid chromatography (wherein, chromatographic column adopts Source 5RPC prepacked column (4.6 * 150mm, Amersham Biosciences)) detects the purity of Exendin-4 and concentration.

[0053] Table 2. Exendin-4 biological activity, purity and concentration in pharmaceutical compositions A-X

[0054]

[0055]

[0056] The experimental results are shown in Table 2. The purity of Exendin-4 in the pharmaceutical compositions A-X is above 98%, the biological activity remains at a high level, and the concentration remains basically unchanged.

[0057] 2) Activity test of rhPH20 in the pharmaceutical compositio...

Embodiment 3

[0073] Comparative Example 3 The pharmaceutical composition containing anti-CD20 monoclonal antibody administered through oral mucosa

[0074] Table 6 contains pharmaceutical composition C of anti-CD20 monoclonal antibody

[0075]

[0076] Anti-CD20 monoclonal antibody, such as rituximab, can be prepared by the same method as in Example 1 according to the proportion of each component in composition C in Table 6, if it is to be administered to the oral mucosa. However, to prepare a composition containing such a high concentration of rituximab, the antibody needs to be concentrated, but the concentrated antibody is prone to aggregation, and the activity of the antibody cannot be guaranteed, and after being absorbed through the oral mucosa, it is easy to cause therapeutic antibodies in the body neutralizing antibodies produced during this process can render therapeutic antibodies ineffective. It can be seen that the preparation of the pharmaceutical composition containing ant...

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Abstract

The invention relates to a human glucagon-like peptide-1 analogue containing medicine composition delivered via an oral mucosa. The medicine composition comprises a high-concentration glucagon-like peptide-1 analogue, hyaluronidase, and one or more mucosa absorbents, or further comprises or does not comprise one or more thickening agents. The medicine composition has excellent permeation absorbency and biological activity, and is high in bioavailability and safe and nontoxic in formula. The invention further provides a preparation method of the medicine composition, and application of the medicine composition in preparing a medicine for treating hyperglycemia and / or diabetes mellitus. The medicine composition is convenient to use, has no toxicity or stimulation in a using process, takes effect quickly, and can significantly improve clinical medication compliance of a patient.

Description

technical field [0001] The present invention relates to the field of medicine, and more specifically, the present invention relates to a pharmaceutical composition containing human glucagon-like peptide-1 analogs administered through the oral mucosa and a preparation method thereof, and the pharmaceutical composition is effective in treating high Glycemic and / or diabetic use. Background technique [0002] Diabetes mellitus is a chronic disease that is caused by insufficient insulin secretion or insulin action disorder, resulting in high blood sugar, sugar in urine, and even a series of metabolic disorders. If diabetes cannot be treated in a timely and effective manner, it can also cause complications such as ketoacidosis, cardiovascular disease, renal failure, and retinopathy. Diabetes has become another chronic disease that seriously endangers human life and health after tumors and cardiovascular diseases. At present, the number of diabetic patients in my country has reac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/47A61K38/26A61K9/00A61K47/42A61P3/10
CPCA61K9/006A61K38/26A61K38/47A61K47/42A61K2300/00
Inventor 彭飞魏薇徐小萍李晓鹏何太平张宝华
Owner CHENGDU JINKAI BIOTECH CO LTD
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