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Semaglutide contained oral prolonged-release preparation and preparation method thereof

A sustained-release preparation, semaglutide technology, applied in medical preparations containing active ingredients, medical preparations with non-active ingredients, pill delivery, etc., can solve the problem of high cost for patients

Inactive Publication Date: 2018-10-02
南京星银药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the oral dosage form of semaglutide requires 300 times the dose of active ingredient than the subcutaneous injection, that is, 40 mg of semaglutide is taken orally every day, which will cause the patient to spend too much

Method used

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  • Semaglutide contained oral prolonged-release preparation and preparation method thereof
  • Semaglutide contained oral prolonged-release preparation and preparation method thereof
  • Semaglutide contained oral prolonged-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Prescription for oral sustained-release preparations containing semaglutide (content per tablet)

[0033]

[0034] Pass the raw materials and auxiliary materials through 80-mesh sieves respectively, set aside, and configure the prescription quantity of 1000 samples.

[0035] ① Weigh semaglutide, metformin, cellulose acetate, ethyl cellulose, and polyethylene glycol according to the prescription amount; dissolve polyethylene glycol, semaglutide, and metformin in 1 mL of water as the internal water phase W1 ; Dissolve cellulose acetate in 10mL of dichloromethane as the organic phase O; dissolve polyvinyl alcohol in 50mL of water as the external aqueous phase W2;

[0036] ② Add the internal water phase W1 to the organic phase O, and ultrasonically emulsify with a power of 250W for 10 minutes to form a uniform colostrum W1 / O;

[0037] ③ Add colostrum W1 / O to the external water phase W2, and ultrasonically emulsify with a power of 250W for 10 minutes to form double emuls...

Embodiment 2

[0043] Prescription for oral sustained-release preparations containing semaglutide (content per tablet)

[0044]

[0045] Pass the raw materials and auxiliary materials through 80-mesh sieves respectively, set aside, and configure the prescription quantity of 1000 samples.

[0046] ① Weigh semaglutide, ciglitazone, cellulose acetate, polyethylene, and Tween-80 according to the prescription amount; dissolve Tween-80, semaglutide, and ciglitazone in 2 mL of water, and prepare Inner water phase W1; cellulose acetate and polyethylene were dissolved in 10 mL of dichloromethane as the organic phase O; polyvinyl alcohol was dissolved in 100 mL of water as the outer water phase W2;

[0047] ② Add the internal water phase W1 to the organic phase O, and ultrasonically emulsify with a power of 300W for 8 minutes to form a uniform colostrum W1 / O;

[0048] ③ Add colostrum W1 / O to the external water phase W2, power 300W ultrasonic emulsification for 8 minutes to form double emulsion W1 / ...

Embodiment 3

[0054] Prescription for oral sustained-release preparations containing semaglutide (content per tablet)

[0055]

[0056] Pass the raw materials and auxiliary materials through 80-mesh sieves respectively, set aside, and configure the prescription quantity of 1000 samples.

[0057] ① Weigh semaglutide, pioglitazone, ethyl cellulose, polyethylene, and mannitol respectively according to the prescription quantity; dissolve mannitol, semaglutide, and pioglitazone in 2 mL of water as the inner water phase W1; 1. Dissolve polyethylene in 10mL of dichloromethane as organic phase O; dissolve polyvinyl alcohol in 100mL of water as external water phase W2;

[0058] ②Add the internal water phase W1 into the organic phase O, and ultrasonically emulsify with a power of 350W for 7 minutes to form a uniform colostrum W1 / O;

[0059] ③ Add colostrum W1 / O to the external water phase W2, and ultrasonically emulsify with a power of 350W for 7 minutes to form double emulsion W1 / O / W2;

[0060] ④...

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Abstract

The invention relates to a semaglutide contained oral prolonged-release preparation and a preparation method thereof. The semaglutide contained oral prolonged-release preparation is characterized in that a drug active component is semaglutide as a GLP-1 analogue and is also prepared from a sulfonylurea, biguanide or thiazolidinedione blood sugar lowering drug which has the synergistic effect withthe semaglutide; the drug active component is wrapped with a sustained release carrier to prepare a sustained release microsphere, and then the sustained release microsphere is mixed and pressed witha pharmaceutically acceptable auxiliary material to form a tablet with a certain shape for orally use, so that the long-term sustained release effect is exerted. By adopting the prepared oral prolonged-release preparation, the conventional administration way of a polypeptide drug is changed, the action time of the polypeptide drug is prolonged, the medication compliance of a patient with diabetesmellitus is obviously improved, and the therapeutic effect is improved.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to an oral sustained-release preparation containing semaglutide and a preparation method thereof. Background technique [0002] With the development of the global economy and the improvement of living standards, changes in lifestyle and population aging, the prevalence of diabetes is on the rise worldwide, becoming another chronic disease that seriously endangers public health after cardiovascular and cerebrovascular diseases and tumors. non-communicable diseases. The main types of diabetes include type Ⅰ diabetes, type Ⅱ diabetes, gestational diabetes and other special types of diabetes. Among them, type Ⅱ diabetes accounts for about 95%. At present, there are mainly four types of drugs that can be used to reduce blood sugar levels in patients with type 2 diabetes: sulfonylurea hypoglycemic drugs, such as gliquidone, glimepiride, and gliclazide; biguanide hypo...

Claims

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Application Information

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IPC IPC(8): A61K9/26A61K47/38A61K47/32A61K47/06A61K47/18A61K38/26A61P3/10A61K31/425A61K31/4439A61K31/155
CPCA61K9/0002A61K9/0053A61K9/2013A61K9/2027A61K9/2054A61K9/2077A61K31/155A61K31/425A61K31/4439A61K38/26A61K2300/00
Inventor 刘铠豪赵文华
Owner 南京星银药业集团有限公司
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