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Thermosensitive non-steroidal anti-inflammatory drug solid dispersion and instant tablet and preparation method thereof

A non-steroidal anti-inflammatory drug and solid dispersion technology, which is applied in the direction of medical preparations, anti-inflammatory agents, and pharmaceutical formulations of non-active ingredients, and can solve the problem of poor, slow release of non-steroidal anti-inflammatory drugs. and other issues, to achieve the effect of improved compressibility, strong interaction, increased fluidity and compressibility

Active Publication Date: 2020-06-02
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The present invention solves the technical problems of slow drug release and poor solubility of non-steroidal anti-inflammatory drugs in the prior art, and provides a solid dispersion of temperature-sensitive non-steroidal anti-inflammatory drugs and instant tablets and its preparation method

Method used

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  • Thermosensitive non-steroidal anti-inflammatory drug solid dispersion and instant tablet and preparation method thereof
  • Thermosensitive non-steroidal anti-inflammatory drug solid dispersion and instant tablet and preparation method thereof
  • Thermosensitive non-steroidal anti-inflammatory drug solid dispersion and instant tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Synthesis and NMR Characterization of Thermosensitive Excipients

[0048] 1. Synthesis and NMR characterization of poly(N-isopropylacrylamide)

[0049] Dissolve 6 g of N-isopropylacrylamide (NIPAM) crystals in a three-necked bottle filled with 50 mL of deionized water, drum N 2 After 30 minutes, it was heated and stabilized in a constant temperature water bath at 60°C under magnetic stirring, and then injected into 5 mL of aqueous solution containing 30 mg of ammonium persulfate, and reacted for 7 hours. After the reaction was completed, the reaction solution was transferred to a dialysis bag (MWCO: 3500) for dialysis for 3 days, and the product was collected after freeze-drying. Dissolve the sample in heavy water to prepare a solution with a concentration of 20mg / mL, and measure its H NMR spectrum after constant temperature at 25°C for 10min, as shown in figure 1 As shown, it was confirmed that PNIPAM was synthesized successfully.

[0050] 2. Synthesis an...

Embodiment 2

[0054] Example 2: Preparation and structural characterization of thermosensitive ibuprofen solid dispersion

[0055] 1. Preparation and characterization of poly(N-isopropylacrylamide)-ibuprofen solid dispersion

[0056] The PNIPAM-ibuprofen solid dispersion is prepared by an anti-solvent co-precipitation method, specifically a preparation method in which an organic solvent is removed by dialysis. Dissolve 100mg of poly(N-isopropylacrylamide) (PNIPAM) and 91mg or 182mg of ibuprofen in 30mL of dimethyl sulfoxide (DMSO), and transfer to a dialysis bag (MWCO: 3500) after complete dissolution. 1 L of deionized water with a pH of about 3 was dialyzed. Change the water every 3 hours for the first 12 hours, and every 6 hours for the next 36 hours. After the dialysis, the solution in the dialysis bag was centrifuged at 3000 rpm for 10 min, the precipitate was discarded, and the solution was freeze-dried to obtain a PNIPAM-ibuprofen solid dispersion.

[0057] The content of ibuprofen...

Embodiment 3

[0070] Example 3: Research on thermosensitive behavior and in vitro release of ibuprofen solid dispersion

[0071] 1. The average hydrated particle size and intuitive temperature sensitivity of ibuprofen solid dispersion

[0072] Utilize dynamic light scattering to measure the hydration diameter of ibuprofen solid dispersion 3, solid dispersion 4 below its phase transition temperature (room temperature) and above (37 ℃) respectively, as Figure 4As shown, the temperature-sensitive carrier dextran-g-poly(N-isopropylacrylamide) (Dex-g-PNIPAM) has a particle size of about 20nm at room temperature, and when the temperature rises to 37°C, the solution forms a particle size of 100nm micelles. After the drug is entrapped, the system appears as an emulsion at room temperature. After the temperature rises, the particle size decreases from 260nm to about 140nm, and the particle size change is reversible. This shows that when the temperature is lower than the lower critical solution te...

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Abstract

The invention discloses a temperature-sensitive non-steroid anti-inflammatory medicine solid dispersed agent and a rapidly dissolving tablet, and a preparation method thereof, and belongs to the fieldof medicine dosage form. The temperature-sensitive non-steroid anti-inflammatory medicine solid dispersed agent contains a non-steroid anti-inflammatory medicine and a temperature-sensitive carrier at a mass ratio of 1: (1-10). According to the preparation method, anti-solvent method is adopted for co-deposition of the non-steroid anti-inflammatory medicine and the temperature-sensitive carrier,and separation freeze drying is adopted for preparation. The interaction effect of the non-steroid anti-inflammatory medicine and the temperature-sensitive carrier is high, the temperature-sensitive non-steroid anti-inflammatory medicine solid dispersed agent is excellent in stability; after entering into the body and contact with digestive juice, under hydration effect, temperature sensitive change of the temperature-sensitive carrier is caused, system phase separation is caused, and rapid medicine release is achieved; and in addition, after adjusting of the temperature-sensitive non-steroidanti-inflammatory medicine solid dispersed agent with an accessory material, micro nano grade solid dispersion particles can be obtained, system fluidity and compressibility are improved, solid dispersed agent direct powder tabletting is realized. The temperature-sensitive non-steroid anti-inflammatory medicine solid dispersed agent possesses oral administration quick effect achieving effect, andis capable of increasing the relative bioavailability of non-steroid anti-inflammatory medicines.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical dosage forms, and in particular relates to a temperature-sensitive non-steroidal anti-inflammatory drug solid dispersion capable of exerting quick-acting effects. Background technique [0002] At present, many potential drugs are shelved due to their low solubility, which seriously affects the absorption in the body, resulting in low bioavailability, resulting in great waste. According to rough statistics, nearly 70% of the drugs with good clinical application prospects are insoluble drugs. The solubility and dissolution rate of poorly soluble drugs directly affect their bioavailability. With the continuous development of new drugs, improving the solubility of poorly soluble drugs and improving the physical and chemical properties of poorly soluble drugs is a research hotspot in the international pharmaceutical community. the daunting task before them. [0003] The solubilization of poorl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/32A61K47/36A61K47/38A61K47/34A61K47/58A61K47/61A61K47/60A61K47/10A61K47/08A61K47/12A61K47/04A61K47/20A61K9/20A61K31/192A61K31/196A61K31/635A61P29/00
CPCA61K9/19A61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2059A61K9/2095A61K31/192A61K31/196A61K31/635A61K47/08A61K47/10A61K47/32A61K47/34A61K47/36A61K47/38A61K47/58A61K47/60A61K47/61A61P29/00
Inventor 谭松巍高雪琴邹晨明尹明星张伟王利群
Owner HUAZHONG UNIV OF SCI & TECH
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