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Dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet

A technology of fluorouracil and dextran, which is applied in the field of "dextran-MLDH-fluorouracil" supramolecular assembly type magnetic targeting sustained-release tablets, can solve the problems of short half-life, strong toxic and side effects, and fast metabolism, so as to prolong the half-life in vivo and improve biological Utilization, reduction of acute toxicity level and effect of plasma protein binding rate

Active Publication Date: 2013-10-23
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its half-life in vivo is short, its metabolism is fast, and its toxic and side effects are strong.

Method used

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  • Dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet
  • Dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet
  • Dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]Example 1 The DMF magnetic drug carrier with a fluorouracil content of 20 to 40% was synthesized by the "co-precipitation intercalation-in-situ composite-solvent conversion" method. The specific operation process is as follows:

[0032] Accurately weigh 29.82g FeCl 2 4H 2 O and 13.52 g FeCl 3 ·6H 2 O, add to 500mL N 2 Protect the reactor, add 150mL distilled water 2 Stir to dissolve. Weigh 26.0g of fluorouracil, dissolve it with 100mL of 2M NaOH solution, add it to the mixed salt solution, and stir it evenly. Use 2M NaOH solution as precipitating agent, control the coprecipitation terminal pH to 7.0; 2 Or Ar protection, constant temperature at 60°C and 300r·min -1 The precipitation reaction was completed under the condition of magnetic stirring, and the crystallization was carried out for 45 minutes. Weigh 13.52g dextran, dissolve it with 50mL double-distilled water, add it to the reactor, and react in situ for 35min. Change the solvent with ethanol that was fro...

Embodiment 2

[0033] Embodiment 2 takes the DMF prepared in Example 1 as the drug carrier, and presses the tablet according to the following prescription, and the specific operations are as follows:

[0034] DMF drug carrier (powder)

[0035] Firstly, DMF is solid-phase ground into powder, passed through 80 mesh sieve, hydroxypropyl methylcellulose and chitosan respectively passed through 80 mesh sieve, lactose and magnesium stearate respectively passed through 100 mesh sieve; Each powdery substance is fully mixed by an equal amount incremental method; finally, an appropriate amount of the mixed powder is taken, and the matrix tablet is directly made into a matrix tablet on a single-punch tablet machine with a shallow concave die by the powder direct compression method.

[0036] Embodiment 3 uses the processing method of embodiment 2, compresses tablet by following prescription:

[0037] DMF drug carrier (powder)

[0038] Processing method is with embodiment 2.

[0039]...

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Abstract

The invention relates to a dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet, the sustained release tablet takes dextran-MLDH-fluorouracil DMF as the drug storage and transmission system, and hydrophilic gel auxiliary material as the skeletal material, and the tablet is prepared by direct powder compression. The sustained release tablet has typical in-vitro control release ability, a special and durable in-vivo drug process and prominent magnetic target specificity. Preparation of the DMF magnetic target control release drug delivery system is realized for the first time, a DMF magnetic matrix tablet is prepared by combination of conventional auxiliary materials and DMF, which is a novel inorganic nano drug carrying system, therefore oral medication and magnetic target chemotherapy of fluorouracil, which is a wide-spectrum anti-cancer drug, are provided with a realization way. The dextran-MLDH-fluorouracil supermolecular assembly magnetic targeting sustained release tablet is suitable for the preparation production of magnetic drug control release tablets, which take magnetic layered double hydroxide(MLDH) as the carrier, has the processing advantages of low cost and simple technology, and has the characteristics of integration of magnetic-target and control-release functions, convenient drug delivery, durable effect, stable curative effect, and little toxic and side effects.

Description

technical field [0001] The invention belongs to the category of modern drug delivery system and preparation technology thereof, and specifically relates to a "dextran-MLDH-fluorouracil" supramolecular assembly type magnetically targeted sustained-release tablet, which is suitable for oral administration of anticancer drugs and tablets required for magnetically targeted chemotherapy Agent processing and production. Background technique [0002] Layered double hydroxides (Layered Double Hydroxides, LDH) is an inorganic nanomaterial with intercalation assembly performance. The reversible exchange performance of interlayer anions and the geometric and electrostatic control of the interlayer guest by the laminate make it a new type of material. However, common magnesium-aluminum-based LDH, like other carriers, lacks specific selectivity to lesion sites, which limits the application of LDH-Drugs system in cancer treatment. Magnetic layered double hydroxide (Magnetic Layered Doubl...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/513A61K47/48A61P35/00
Inventor 苟国敬薛冰徐淑芳
Owner NINGXIA MEDICAL UNIV
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