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Albumin nanometer particle preparation for soluble injection and preparation method of albumin nanometer particle preparation

A technology for albumin nanoparticles and injections, applied in the field of pharmaceutical preparations, can solve the problems of frequent administration, low oral bioavailability, and increased toxic and side effects, so as to avoid low bioavailability and reduce systemic toxicity Side effects, effects of avoiding gastrointestinal toxic side effects

Inactive Publication Date: 2012-08-08
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, although tinib drugs have many advantages in anti-tumor, the treatment practice shows that they still have the following defects: ① Poor water solubility makes the drug unable to be injected, and the oral bioavailability is not high, and it is prone to gastrointestinal side effects; ②The dosage is large and requires frequent administration, which leads to poor patient compliance; ③The tissue is widely distributed and has no targeting to the tumor site, which weakens its anti-tumor effect to a certain extent and increases systemic side effects
[0009] So far, the basic and applied basic research on tinib drugs has mainly focused on the research on its mechanism of action and the combination of drugs, and there has been no literature report on the effective preparation of albumin nanoparticles into nano-preparations

Method used

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  • Albumin nanometer particle preparation for soluble injection and preparation method of albumin nanometer particle preparation
  • Albumin nanometer particle preparation for soluble injection and preparation method of albumin nanometer particle preparation
  • Albumin nanometer particle preparation for soluble injection and preparation method of albumin nanometer particle preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Prescription process of lapatinib albumin nanoparticles

[0041] Table 1 The proportion of each component in the prescription of albumin nanoparticles containing lapatinib (mg)

[0042]

[0043] Respectively dissolve the lapatinib in the prescriptions 1 to 30 in Table 1 in an appropriate amount of ethanol-water (6:1 to 2:1) mixed solvent or other appropriate solvent, dissolve the phospholipid in an appropriate amount of dichloromethane, and dissolve the two Mix it as the oil phase; dissolve albumin and antioxidants in an appropriate amount of deionized water (water phase), drop the oil phase into the magnetically stirred water phase at room temperature or in an ice-water bath, and continue to stir for a certain period of time, then 40°C The ethanol and dichloromethane are removed by rotary evaporation in a water bath to obtain lapatinib-loaded albumin nanoparticles.

Embodiment 2

[0044] Example 2. Prescription technology of Ariitinib albumin nanoparticles

[0045] Table 2 Proportion (mg) of each component in the prescription of albumin nanoparticles containing eritinib

[0046]

[0047] Dissolve the eritinib in the prescriptions 1-30 of Table 2 in a suitable amount of ethanol-water (6:1~2:1) mixed solvent or other suitable solvents, dissolve the phospholipids in a suitable amount of dichloromethane, and mix the two Then it is used as the oil phase; dissolve albumin and antioxidants in an appropriate amount of deionized water (water phase), drop the oil phase into the magnetically stirred water phase at room temperature or in an ice water bath, and continue to stir for a certain period of time, then water bath at 40°C Rotary evaporation to remove ethanol and dichloromethane to obtain albumin nanoparticles loaded with eritinib.

Embodiment 3

[0048] Example 3. Prescription technology of gefitinib albumin nanoparticles

[0049] Table 3 Proportion (mg) of each component in the prescription of albumin nanoparticles containing gefitinib

[0050]

[0051] Dissolve gefitinib in prescriptions 1-30 in Table 3 in a suitable amount of ethanol-water (6:1~2:1) mixed solvent or other suitable solvents, dissolve the phospholipids in a suitable amount of dichloromethane, and mix the two Then it is used as the oil phase; the albumin and antioxidants are dissolved in an appropriate amount of deionized water (water phase), the oil phase is dropped into the magnetically stirred water phase at room temperature or in an ice water bath, and stirring is continued for a certain period of time. Then, the ethanol and dichloromethane were removed by rotary evaporation in a water bath at 40°C to obtain albumin nanoparticles carrying gefitinib.

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Abstract

The invention belongs to the field of pharmaceutical preparation and relates to an albumin nanometer particle preparation for soluble injection. The albumin nanometer particle, which is formed by combining albumin, indissolvable erlotinib drugs and adding phospholipid for scattering and stabilizing, is prepared into the albumin nanometer particle preparation for soluble injection. The enhancing permeation and detaining effect of nanometer particle to tumor are utilized by the albumin nanometer particle preparation provided by the invention, so that more drugs are passively targeted and gathered on a tumor tissue and the anti-tumor effect is increased. Meanwhile, the bioavailability of injection mode is high, the albumin nanometer particle preparation for soluble injection has a passive targeting function and the dosage is greatly reduced, so that the concentration of the drugs in non-target part is efficiently reduced, the reducing of the toxic side effect of the drugs is boosted and the clinical application prospect is excellent.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a soluble albumin nanoparticle preparation for injection and a preparation method thereof, and in particular to a preparation of a soluble tinib drug into a soluble albumin nanoparticle preparation for injection and a preparation method thereof. Background technique [0002] Malignant tumors are one of the most difficult diseases for human beings to deal with. In recent years, the incidence of tumors has risen sharply, its treatment is difficult and the mortality rate is high, and it has become the second leading cause of human death. According to reports, about 6 million people die from malignant tumors in the world every year. Among them, there are about 4.5 million cancer patients in China with a mortality rate of over 30%, which has become a serious social problem. At present, surgery, chemotherapy, and radiotherapy are commonly used clinically to treat malignant tumors; ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/42A61K45/00A61P35/00
Inventor 高会乐蒋新国曹师磊
Owner FUDAN UNIV
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