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Insulin sustained-release oral patch as well as preparation method and application thereof

A technology of insulin and pharmaceutical preparations, which is applied in the direction of pharmaceutical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problems of patients' pain and complications, and achieve prolonged action time and half-life , highly feasible effect

Pending Publication Date: 2022-01-07
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the above reasons, clinical application requires frequent injections, which will cause pain and complications for patients.

Method used

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  • Insulin sustained-release oral patch as well as preparation method and application thereof
  • Insulin sustained-release oral patch as well as preparation method and application thereof
  • Insulin sustained-release oral patch as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Preparation of Insulin Sustained Release Oral Patch

[0063] (1) Polylactic acid-glycolic acid copolymerization (PLGA) solution preparation

[0064] Dissolve 120mg of polylactic acid-glycolic acid copolymer (50:50) in 2ml of dichloromethane to form an organic phase (0.06g / ml);

[0065] (2) Preparation of insulin solution

[0066] Accurately weigh 2 mg of solid insulin powder, dissolve in 190 μl of acetate buffer solution with pH=4, and fully dissolve into a transparent liquid.

[0067] (3) Preparation of insulin dispersion solution

[0068] 190 μl of insulin liquid was evenly dispersed in 250 μl of sodium alginate solution with a mass volume ratio of 0.003% (w / v) to form an internal aqueous phase.

[0069] (4) Preparation of colostrum

[0070] Inject the internal aqueous phase into the organic phase, and perform ultrasonic emulsification for 1 min under ultrasonic conditions of 10-1000w to form colostrum (W / O); the volume ratio of the organic phase to the internal a...

Embodiment 2

[0085] Insulin Nanoparticle Stability Test

[0086] The prepared insulin nanoparticles were subjected to PDI (particle distribution density) detection at the same time on days 1-7. The storage condition of nanoparticles is 4°C, and it is observed whether aggregation or degradation occurs. After detection by Anton Paar LITESIZER 500 particle size analyzer according to the principle of dynamic light scattering (DLS), the PDI value is 0.1-0.3, indicating good dispersion.

[0087] image 3 It is the stability change of the insulin nanoparticle of the present invention; it can be drawn from the figure that the insulin nanoparticle has good stability when stored at 4° C., and no obvious aggregation and degradation phenomenon occurs.

Embodiment 3

[0089] Detection of hypoglycemic activity of insulin lozenges

[0090] The diabetic rat model was induced by intraperitoneal injection of STZ. The established rat models were randomly divided into six groups A, B, C, D, E, and F, with 6 rats in each group, and were fed normally for one week, and fasted for 12 hours before administration.

[0091] Group A blank excipient group (sublingual / buccal patch), group B blank nanoparticle patch group (sublingual / buccal patch), group C insulin nanoparticle patch group (sublingual), group D insulin nanoparticle patch group (buccal patch), E group blank control group, F group positive control group (insulin injection group), after administration, at 0, 15, 30, 45, 60, 90, 120, 150, 180, 210, 240, 300, 360 , 420, and 480 min to take blood from the tail vein, and measure blood sugar with a blood glucose meter and blood glucose test strips. During the experiment, all groups were anesthetized and anesthesia was supplemented appropriately dur...

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Abstract

The invention relates to the field of biomedicines, and particularly relates to an insulin sustained-release oral patch as well as a preparation method and an application thereof. The pharmaceutical preparation is characterized by comprising nanoparticles and pharmaceutical excipients that comprise a filler, an adhesive and a lubricant. The dosage form of the pharmaceutical preparation is an oral patch. According to the invention, insulin is prepared into the sustained-release oral patch, thereby avoiding first-pass effect of gastrointestinal tracts, prolong action time of the medicine, improving curative effect and economic benefit of the medicine, reducing influence of enzymes on the insulin, and relieving pain of patients due to injection. The oral patch of the present invention is high in adhesive capacity, good in release and moderate in dissolution rate.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to an insulin sustained-release oral patch and its preparation method and application. Background technique [0002] Insulin is a protein hormone secreted by the islet β cells in the pancreas when stimulated by endogenous or exogenous substances such as glucose, lactose, ribose, arginine, and glucagon. Insulin is the only hormone in the body that lowers blood sugar, and at the same time promotes the synthesis of glycogen, fat, and protein. Exogenous insulin is mainly used to treat diabetes. It is the main drug for the treatment of type 1 diabetes. The effect is good, but the storage conditions are harsh, easy to inactivate, and unstable. [0003] Due to the above reasons, clinical application requires frequent injections, which can cause pain and complications for patients. It is a complex and arduous task to make it into stable, safe and efficient pharmaceutical preparations. At pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/22A61K47/38A61K47/36A61K47/32A61K47/26A61K47/34A61P3/10
CPCA61K38/28A61K9/2095A61K9/205A61K9/2054A61K9/2027A61K9/2031A61K9/2059A61K9/2018A61K9/006A61P3/10
Inventor 薛建鹏徐寒梅王瑱胡加亮杜南星黄锦辉李则青赵文静来志龙赖文婷
Owner CHINA PHARM UNIV
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