LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet and preparation method thereof

An aspirin and supramolecular technology, applied in the field of LDH supramolecular assembled aspirin sustained-release tablets and preparation, can solve problems such as disintegration, LDH easy to erode, and failure to achieve sustained-release effects, etc., to improve sustained-release performance, transport and The release process is particularly durable and the effect of improving biocompatibility

Inactive Publication Date: 2013-03-27
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Scholars at home and abroad have been engaged in the research of LDH-Drug sustained and controlled release systems for many years. The results show that LDH is easily eroded under acidic conditions, resulting in rapid "disintegration" of oral LDH-Drug preparations in the gastric juice environment, and the sustained release effect cannot be achieved; while There is an obvious "burst release" phenomenon in the independent LDH-Drug secondary assembly

Method used

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  • LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet and preparation method thereof
  • LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet and preparation method thereof
  • LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: The prescription of "DET-LDH-ASP" supramolecular sustained release tablet is as follows

[0027]

[0028] The method for preparing the DET-LDH-ASP drug-carrying system is as follows: 40.82g MgCl 2 ·6H 2 O, 24.30g AlCl 3 ·6H 2 O and 72.83g ASP are dropped into the reactor of 2000mL three-neck bottle assembly respectively, add 800mL water and dissolve to clarification, in N 2 Add 2.0mol L dropwise under the conditions of protection, 80°C constant temperature and 300rpm magnetic stirring -1 NaOH solution, control the pH of the co-precipitation end point to be 10.06, and make the LDH-ASP secondary complex slurry; add 200 mL of dextran aqueous solution with a mass concentration of 16% after in-situ crystallization for 45 min, and keep the N 2 Protection, 80°C constant temperature and 300rpm stirring conditions remain unchanged, and the in-situ reaction is performed for 40 minutes to make a DET-LDH-ASP tertiary compound slurry; transfer the prepared hot slur...

Embodiment 2

[0030] Example 2: The preparation prescription of "DET-LDH-ASP" supramolecular sustained-release tablets is as follows

[0031]

[0032] The method for preparing the DET-LDH-ASP supramolecular drug carrier is the same as that in Example 1. Tablet preparation method: weigh a certain amount of "DET-LDH-ASP" powder (80 mesh), hypromellose (80 mesh), and sodium alginate (80 mesh) according to the prescription ratio, mix the three fully, and pour A small amount of talc powder (100 mesh) is added to the mixed raw materials, mixed evenly, and the tablet is directly compressed using a die with a diameter of 8 mm to obtain a sustained-release tablet with a hardness of about 4.5 kg and a tablet weight of 0.12 to 0.16 g.

Embodiment 3

[0033] Example 3: "DET-LDH-ASP" supramolecular sustained-release tablets were prepared according to the following prescription

[0034]

[0035]

[0036] The method for preparing the "DET-LDH-ASP" supramolecular drug carrier is the same as in Examples 1-2. Tablet preparation method: Grind raw materials such as DET-LDH-ASP, hydroxypropylmethylcellulose, sodium alginate and talcum powder into powder respectively, pass the DET-LDH-ASP powder through a 80-mesh sieve, and hydroxypropylmethylcellulose Pass through an 80-mesh sieve, pass through a 80-mesh sieve for sodium alginate, pass through a 100-mesh sieve for talcum powder, and grind until it can be completely sieved; mix the powder raw materials according to the prescription ratio, grind and disperse evenly with a mortar, and then use a shallow concave with a diameter of 8mm The tablet can be directly compressed by the die to obtain a sustained-release tablet with a diameter of 8 mm, a hardness of about 4.5 kg, and a tab...

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Abstract

The invention relates to an LDH (Layered Double Hydroxides) supermolecular assembly type aspirin sustained release tablet, wherein three levels of supermolecules consisting of dextran, layered double hydroxides and aspirin are used as a medicine barrier, hydroxypropyl methylcellulose is used as a material of a gel skeleton, and the sustained release tablet is prepared by carrying out direct tablet compressing on powder. Auxiliary materials adopted by the LDH supermolecular assembly type aspirin sustained release tablet are good in liquidity, the sustained release tablet can be prepared by carrying out direct tablet compressing on the powder, the process is simple and fast and the cost is low; DET (Dextran)-LDH (Layered Double Hydroxides)-ASP (Aspirin) three-level supermolecule assembly isadopted to overcome the defects of acid dissolution and easiness in sudden release of LDH-ASP so that the system biocompatibility is improved, and by cooperative control of HPMC (Hydroxypropyl Methylcellulose)-DET-LDH, the sustained release performance is obviously improved; and compared with traditional aspirin sustained release tablets with organic auxiliary materials, the LDH supermolecular assembly type sustained release tablet has special cytobiology advantages, relatively high bioavailability, obvious releasing effect and specially sustained transferring and releasing process.

Description

technical field [0001] The invention relates to the fields of assembly chemistry and pharmaceutical preparation of layered double hydroxides (Layered Double Hydroxides, LDH) for medicine, in particular to an LDH supramolecular assembled aspirin sustained-release tablet and a preparation method. Background technique [0002] Oral sustained and controlled release preparations have become an important direction for the development of the modern pharmaceutical industry at home and abroad due to the advantages of short development cycle, low investment, low risk, and significant increase in added value with the increase in technical content. The development of modern pharmacy is inseparable from the development and utilization of new materials, and the inorganic layered carrier LDH has a certain application prospect in the field of sustained and controlled release preparations. [0003] Since the 19th century, aspirin (ASP) has been widely used clinically for anti-inflammation, a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/22A61K31/616A61K47/38A61K47/36A61K47/02A61P29/00A61P7/02A61P9/10
Inventor 苟国敬焦林
Owner NINGXIA MEDICAL UNIV
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