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A kind of soluble albumin nanoparticle preparation for injection and preparation method thereof

An albumin nanoparticle and injection technology, which is applied in the field of pharmaceutical preparations, can solve the problems of increasing toxic side effects, requiring frequent administration, and low oral bioavailability, avoiding gastrointestinal toxic side effects and avoiding high bioavailability. Low, reduced systemic toxicity

Inactive Publication Date: 2015-10-28
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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  • A kind of soluble albumin nanoparticle preparation for injection and preparation method thereof
  • A kind of soluble albumin nanoparticle preparation for injection and preparation method thereof
  • A kind of soluble albumin nanoparticle preparation for injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1, the prescription process of lapatinib albumin nanoparticles

[0041] Table 1 Ratio (mg) of each component in the albumin nanoparticles formulation loaded with lapatinib

[0042]

[0043] Dissolve lapatinib in prescriptions 1 to 30 in Table 1 in an appropriate amount of ethanol-water (6:1 to 2:1) mixed solvent or other suitable solvents, and dissolve phospholipids in an appropriate amount of dichloromethane. After mixing, 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 40 ° C Ethanol and dichloromethane were removed by rotary evaporation in a water bath to obtain lapatinib-loaded albumin nanoparticles.

Embodiment 2

[0044] Embodiment 2, the prescription process of allitinib albumin nanoparticles

[0045] Table 2 The proportion of each component in the albumin nanoparticle formulation loaded with allitinib (mg)

[0046]

[0047] Dissolve allitinib in prescriptions 1-30 in Table 2 in an appropriate amount of ethanol-water (6:1-2:1) mixed solvent or other suitable solvents, dissolve phospholipids in an appropriate amount of dichloromethane, and mix the two Finally, 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 stirring for a certain period of time, then 40 ° C water bath Ethanol and dichloromethane were removed by rotary evaporation to obtain allitinib-loaded albumin nanoparticles.

Embodiment 3

[0048] Embodiment 3, the prescription process of gefitinib albumin nanoparticles

[0049] Table 3 The ratio (mg) of each component in the albumin nanoparticle prescription loaded with gefitinib

[0050]

[0051] Dissolve gefitinib in prescriptions 1-30 in Table 3 in an appropriate amount of ethanol-water (6:1-2:1) mixed solvent or other suitable solvents, dissolve phospholipids in an appropriate amount of dichloromethane, and mix the two Finally, as the oil phase; dissolve the 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 stirring 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 loaded with 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, in particular to a preparation of insoluble tinib drugs 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 to deal with. In recent years, the incidence of tumor has risen sharply, and its treatment is difficult and its mortality rate is high. It has become the second leading cause of human death. According to reports, about 6 million people die of malignant tumors in the world every year, among which about 4.5 million cancer patients in China, the mortality rate exceeds 30%, which has become a serious social problem. At present, surgery, chemotherapy, and radiotherapy are usually used to treat malignant tumors clinically; for early-stage tumors, surgica...

Claims

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Application Information

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