Controlled-release injection containing antidiuresis components and preparation method thereof

A slow-release injection and anti-diuretic technology, applied in the field of preparations, can solve problems such as inconvenient clinical use and medication for patients, easy entry of viruses and bacteria into mucous membranes, and frequent administration of injections.

Active Publication Date: 2012-07-18
无锡市恒益健康科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Intranasal administration results in high bioavailability but low patient acceptance
Moreover, intranasal administration may adversely affect the cilia, making it easier for viruses and bacteria to enter the mucosa
Frequent administration of injections is inconvenient for clinical use and medication for patients

Method used

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  • Controlled-release injection containing antidiuresis components and preparation method thereof
  • Controlled-release injection containing antidiuresis components and preparation method thereof
  • Controlled-release injection containing antidiuresis components and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 20mg main drug desmopressin acetate, 80mg PLA, special solvent is 1.5% sodium carboxymethyl cellulose normal saline.

[0020] Its preparation process is as follows:

[0021] Put 80mg of polylactic acid (PLA) into a container, add 100ml of dichloromethane, dissolve and mix well, add 20mg of desmopressin acetate, reshake well, and then vacuum dry to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make sustained-release microparticles containing 20% ​​desmopressin acetate, and then suspended in 5000ml of physiological saline containing 1.5% (percentage by weight) sodium carboxymethylcellulose to prepare Get the corresponding suspension type sustained-release injection.

[0022] 5000 bottles of desmopressin acetate sustained-release injections were prepared in this example, and each bottle contained 4 μg of the main drug (1 ml / bottle). Through the determination of the release degree, the sustained-release effect and clin...

Embodiment 2

[0028] 20mg main drug desmopressin acetate, 80mg PLA, special solvent is 1.5% sodium carboxymethylcellulose and 0.1% Tween 80 normal saline. Its preparation process is as follows:

[0029] Put 80mg of polylactic acid (PLA) into a container, add 100ml of dichloromethane, dissolve and mix well, add 20mg of desmopressin acetate, reshake well, and then vacuum dry to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make slow-release microparticles containing 20% ​​desmopressin acetate, and then suspended in 5000ml containing 1.5% (weight percent) sodium carboxymethylcellulose and 0.1% Tween 80 The corresponding suspension-type sustained-release injection was prepared in normal saline.

[0030] 5000 bottles of desmopressin acetate sustained-release injections were prepared in this example, and each bottle contained 4 μg of the main drug (1 ml / bottle). Through the determination of the release degree, the sustained-release effect an...

Embodiment 3

[0036] 20mg main drug desmopressin acetate, 80mg PLA, the special solvent is 1.5% sodium carboxymethylcellulose, 15% sorbitol and 0.1% Tween 80 normal saline. Its preparation process is as follows:

[0037] Put 80mg of polylactic acid (PLA) into a container, add 100ml of dichloromethane, dissolve and mix well, add 20mg of desmopressin acetate, reshake well, and then vacuum dry to remove the organic solvent. The dried drug-containing solid composition is frozen and pulverized to make slow-release microparticles containing 20% ​​desmopressin acetate, and then suspended in 5000ml containing 1.5% (percentage by weight) sodium carboxymethylcellulose and 15% sorbitol and 0.1 % Tween 80 in normal saline to prepare the corresponding suspension-type sustained-release injection.

[0038] 5000 bottles of desmopressin acetate sustained-release injections were prepared in this example, and each bottle contained 4 μg of the main drug (1 ml / bottle). Through the determination of the release d...

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Abstract

The invention relates to a controlled-release injection containing antidiuresis components and a preparation method thereof. The controlled-release injection contains main drugs of desmopressin acetate, sustained release auxiliary materials, suspending agent and menstruum. The sustained release auxiliary materials are selected from polylactic acid, polylactic acid-co-glycolic acid, ethylene-vinyl acetate copolymer, polifeprosan and the like, which can be used for slowly releasing medicine into disease local parts in a degrading and absorbing process, so that general toxicity reaction is obviously reduced, and simultaneously, the effective medicine concentration can be maintained on the disease local parts; the suspending agent is selected from sodium carboxymethylcellulose, mannitol and the like, which is used for suspending sustained-release granules or microspheres of biological active ingredients; and the menstruum is common menstruum or special menstruum containing the suspending agent, wherein the common menstruum is selected from distilled water, water for injection, physiological lotion, absolute ethyl alcohol or buffer solution prepared by various salts, and the like. According to the controlled-release injection, the action time of the medicine can be prolonged, the dosage times are reduced, the stability of blood drug concentration in vivo is maintained, and the drug toxic and side effects are reduced.

Description

Technical field: [0001] The invention relates to the field of preparations, in particular to a slow-release injection containing antidiuretic components and a preparation method thereof. Background technique: [0002] Desmopressin (Desmopressin) is a synthetic analogue of the natural hormone arginine vasopressin, which has a high degree of anti-urination activity and is used for the treatment of urinary system diseases. Natural human arginine vasopressin is a 9-peptide, the 1st and 6th cysteines are connected by a disulfide bond to form a ring structure, the 1st and 9th positions have an amino group, and the 8th position is L-arginine. Desmopressin has two modifications to the structure of natural molecules, one is to remove the amino group at position 1, and the other is to replace L-arginine at position 8 with D-arginine, namely 1-deamino-8-D - Arginine vasopressin (1-deamino-8-D-arginine vasoprssin, DDAVP). This structural modification greatly enhanced the ability of th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/11A61K9/10A61K47/38A61P7/10A61K38/095
Inventor 姚志勇李新宇支钦
Owner 无锡市恒益健康科技有限公司
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