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Preparation of nano crystal fibre felt of water-insoluble medicament

A nanocrystal, water-insoluble technology, applied in the direction of drug delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of increasing the difficulty of drug approval work, a large number of carrier materials, and low bioavailability and other problems, to achieve the effect of improving the oral bioavailability of drugs, simple preparation methods, and a wide range of applications

Inactive Publication Date: 2011-01-12
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Those drugs with high pharmacological activity in vitro often cannot fully exert their clinical application value due to solubility problems
The problems that plague poorly soluble pharmaceutical preparations include: ①Due to poor solubility, the absorption of oral administration is incomplete and the bioavailability is low; ②Even if a solubilizer is used, the drug cannot be administered by injection to achieve good curative effect; ③ For those drugs with poor water solubility but certain fat solubility, mixed solvent or microencapsulation technology can be used
However, it also brings problems such as low drug loading, low encapsulation efficiency, and the need to use a large amount of carrier materials, resulting in the failure to obtain the desired therapeutic effect, or increasing the difficulty of drug approval.
④ For drugs with poor water solubility and fat solubility, there is still a lack of effective methods to solve the problem
However, this technology has disadvantages such as long processing time and low product yield.
The method of using a high-pressure homogenizer to prepare drug nano-suspensions is the second generation of technology for preparing drug nano-suspensions by pulverizing. Equipment contamination exists, but nanoparticles often have a wide range of particle sizes and particle sizes
In addition, some researchers have also proposed methods for preparing insoluble drug nanocrystals using supercritical fluid technology, microfluidization technology, etc., but the scope of application is narrow

Method used

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  • Preparation of nano crystal fibre felt of water-insoluble medicament
  • Preparation of nano crystal fibre felt of water-insoluble medicament
  • Preparation of nano crystal fibre felt of water-insoluble medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of ibuprofen-polyvinylpyrrolidone drug-loaded nanofiber mats:

[0042] Dissolve 10 g of ibuprofen in 100 mL of ethanol, then add 20 g of polyvinylpyrrolidone under stirring conditions, continue stirring for 2 hours after the addition, and then use an ultrasonic processor (500W) for ultrasonic degassing for 15 minutes.

[0043] Pour the prepared solution into the solution reservoir (5mL syringe), use the flattened No. 6 injection needle as the capillary for jetting fine flow, connect the positive electrode of the high-voltage power supply, and connect the negative electrode with an aluminum foil receiving plate. Pump control, electrospinning was carried out according to the following conditions: the flow rate was 1.0mL h -1 , the distance between the receiving plate and the spinneret is 15cm, the voltage is 12kV, the ambient temperature is 20°C, and the ambient humidity is 65%.

Embodiment 2

[0045] Preparation of ibuprofen nanosuspension:

[0046] Put the aluminum foil receiving plate receiving the drug-loaded fiber into an electric vacuum drying oven at 35°C and a vacuum of 320Pa to dry for 24 hours, then remove the fiber mat and dissolve it in water.

[0047] Properly dilute the nano-suspension, measurement conditions: T=25°C, λ=633nm, He-Ne excitation light source, incident angle 90°. The particle size and polydispersity index of nanoparticles were measured on a laser particle size analyzer. The result is as figure 2 shown.

Embodiment 3

[0049] Stability investigation of nano-suspension:

[0050] The nano-suspension of Example 2 was kept airtight at room temperature, and the particle size of the nano-suspension was measured within a set time interval. It can be seen from Table 1 that the particle size of the nano-suspension increased from 207.2nm to 227.5nm in the first month, and the polydispersity index (PDI) increased from 0.180 to 0.242, and there was no significant change. It shows that polyvinylpyrrolidone provides greater steric hindrance, and at the same time, the electrostatic repulsion between nanoparticles prevents the agglomeration of nanoparticles, and together maintains the stability of nano-suspension.

[0051] Table 1 Nanosuspension Stability Experimental Results

[0052]

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Abstract

The invention relates to a preparation of a water-insoluble medicine nanocrystal fibrofelt, which comprises that: water-insoluble medicine is dissolved in organic solvent, then polymeric material is added under the stir condition, the stir is continued and ultrasonic degasification is carried out; the prepared solution is poured into a solution storing tank, a flattened injection needle is used as a capillary tube for injecting thin flow, the positive pole of high voltage source is connected, an aluminum foil receiving flat plate is used to connecte with the negative pole, a microinjection pump is used for controlling the solution injection amount, the spinning condition is adjusted, electrostatic spinning is carried out so that nanocrystal fibrofelt is obtained. The method of the invention is simple, the loading action of polymer material can effectively control the administration in a proper releasing rate and a proper amount, the prepared water-insoluble medicine nanocrystal has favorable solubility, the medicine oral administration bioavailability is improved, multiple ways of administration of water-insoluble medicine is realized, and the application range is widened.

Description

technical field [0001] The invention belongs to the field of preparation of medicinal materials, in particular to the preparation of a nano crystal fiber mat of water insoluble medicine. Background technique [0002] Due to the application of high-throughput screening and combinatorial chemistry and the rapid development of bioengineering technology, more and more active substances can be used in the treatment and protection of diseases, but about 40% of them have solubility problems. Those drugs with high pharmacological activity in vitro often cannot fully exert their clinical application value due to solubility problems. The problems that plague poorly soluble pharmaceutical preparations include: ①Due to poor solubility, the absorption of oral administration is incomplete and the bioavailability is low; ②Even if a solubilizer is used, the drug cannot be administered by injection to achieve good curative effect; ③ For those drugs with poor water solubility but certain fat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K45/00A61K47/32
Inventor 朱利民张晓飞申夏夏余灯广
Owner DONGHUA UNIV
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