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Drug-cyclodextrin nanoparticles and preparation method thereof

A nanoparticle and cyclodextrin technology is applied in pharmaceutical formulations, devices for making medicines into special physical or taking forms, and medical preparations with inactive ingredients, etc. problems such as low rate and bioavailability to achieve continuous operation and reasonable cost

Inactive Publication Date: 2013-01-30
ARISSA PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] The object of the present invention is to provide a new drug-cyclodextrin nanoparticles and preparation method thereof, to overcome the problems of low dissolution rate and bioavailability of existing drug-cyclodextrin products
More importantly, the present invention can overcome the defects that the existing drug-cyclodextrin preparation method is inefficient and cannot be produced on a large scale

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Determine the molecular ratio of drug to cyclodextrin using the mortar and mortar method. As mentioned above, although the mortar method cannot be scaled up for production, it is simple and easy to implement, and it has its unique features in the study of inclusion complexes, especially the molecular ratio of drug to cyclodextrin inclusion complexes. By this method, different molecular ratios of drugs and β-cyclodextrin can be studied, such as: 1:1, 1:2, 1:3, etc. These drugs may include nimesulide, piroxicam, meloxicam, lornoxicam, and indomethacin. Through differential thermal analysis and other detection methods, it is found that when the molecular weight ratio of these drugs to β-cyclodextrin is 1:1 to 1:1.5, their characteristic endothermic peaks (ie, melting point peaks) will change significantly, including peaks position shift, peak shape becomes wider or smaller until all endothermic peaks disappear. For example, when the molecular weight ratio of pyrroxicam a...

Embodiment 2

[0049] On the basis of the above-mentioned Example 1, the feasibility and basic test conditions of the next step of driven media grinding are roughly determined by using small-scale high-energy ball grinding (also known as vibration grinding). Laboratory-scale Retsch MM301, Spex 8000M and other test devices can be used. Take the Retsch MM301 device as an example: add the drug pyrroxicam, β-cyclodextrin and other corresponding grinding auxiliary materials into the stainless steel grinding bottle, including lactose monohydrate, povidone K-30, sodium lauryl sulfate, and then add Grinding media Stainless steel pellets; 9.525 mm in diameter. The total weight of all materials is about 3-5g, and the grinding media is about 4-6 pieces. Set the vibration frequency to 30-40 Hz. Grind in dry powder state for about 3-5 minutes, then add appropriate amount of water (about 30-40% of the total weight of the material), and then continue grinding. Materials were withdrawn at different time ...

Embodiment 3

[0051] On the basis of the above examples 1 and 2, about 450 g of "pyrroxicam-β-cyclodextrin" nanoparticles were produced with a driven media mill, and the mill could be Attritor SD-1 from the Union Process Company of the United States.

[0052] Weighing was as follows: 50 g of pyrroxicam, 200 g of β-cyclodextrin, 160 g of lactose monohydrate, 30 g of povidone K-30, and 10 g of sodium lauryl sulfate. Among them, the molecular weight ratio of pyrroxicam to β-cyclodextrin is 1:1.2. In addition, weigh 9 kg of grinding medium stainless steel balls with a diameter of 9.525 mm.

[0053] The specific steps of grinding are as follows: First, add stainless steel grinding media into the grinding cylinder, and then add the above-mentioned materials into the grinding cylinder one by one. Start the stirring shaft with arm in the cylinder to drive the grinding medium to grind the material. The temperature of the interlayer of the grinding cylinder is controlled at about 20°C by cooling wa...

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Abstract

The invention belongs to the technical field of drug preparation, in particular to drug-cyclodextrin nanoparticles and a preparation method thereof. The drug-cyclodextrin nanoparticle system comprises a drug, cyclodextrin and one or more grinding additives. The manufacturing process is as follows: driving a grinding medium to fully mix and grind the materials under the action of external force; and producing a drug-cyclodextrin inclusion compound and simultaneously greatly reducing the particle size of the drug from the usual micron range to the nanometer range. The method integrates cyclodextrin inclusion and the nano-manufacturing technology into a whole and is the first creation at home and abroad on the modern pharmaceutical preparation technology. Starting from the production and manufacturing point of view, the drug-cyclodextrin nanoparticles have the characteristics of high efficiency, safety and reasonable cost, and are applicable to large-scale production. An oral preparation prepared by the method can be used for significantly improving the dissolution rate and the bioavailability of the water-insoluble drug.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, in particular to a medicine-cyclodextrin nanoparticle and a preparation method thereof. Background technique [0002] How to improve the bioavailability of poorly water-soluble drugs has always been a major problem faced by the pharmaceutical industry, and it is also a research hotspot in the field of drug delivery systems. It is reported that more than 60% of the original chemical drugs in R&D are poorly water-soluble compounds. Due to the low solubility in water and low dissolution rate, these drugs are difficult to be absorbed by the body, so the onset of action is slow, the bioavailability is low and variable, and is often accompanied by the impact of food on absorption. The poor water solubility of the drug will also extend the problem to other aspects, such as the delay in drug efficacy, increased toxicity and side effects (due to increased drug doses), increased research and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K47/48A61J3/00A61K47/69
Inventor 赵履伟
Owner ARISSA PHARMA LTD
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