HER-2 humanized monoclonal antibody long-acting sustained-release preparation and preparation method thereof

A HER-2 and monoclonal antibody technology, applied in the field of medicine, can solve the problems of low drug utilization rate, poor patient compliance, tumor recurrence in situ, etc., and achieve the effect of reducing tumor recurrence rate and drug toxicity and side effects.

Pending Publication Date: 2020-01-03
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once-weekly pulsed intravenous administration has low drug utilization, frequent administration, and poor patient compliance
[0004] At the same time, considering that the existing clinical treatment of breast cancer is mainly surgical treatment, and an important problem after clinical surgery is the tumor recurrence in situ

Method used

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  • HER-2 humanized monoclonal antibody long-acting sustained-release preparation and preparation method thereof
  • HER-2 humanized monoclonal antibody long-acting sustained-release preparation and preparation method thereof
  • HER-2 humanized monoclonal antibody long-acting sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] An amphiphilic block copolymer. Weigh 30g of PEG 1500 in a 250mL three-neck bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3h under mechanical stirring. Then cool down to 100°C with argon, add 40g of D,L-lactide and 8g of glycolide, stir well; add toluene solution containing 60mg of stannous octoate, vacuumize for 15min to remove toluene, then heat up to 150°C under argon The reaction was carried out under gas protection for 12h. Then lower the temperature to 110°C and vacuumize for 3 hours to remove unreacted monomers, then wash the initial product three times with 80°C deionized water, and freeze-dry to obtain the final product, obtaining the BAB type triblock polymer PLGA-PEG-PLGA, The yield is about 80%. The properties of the block polymer were measured, and the results are shown in Table 1. The number-average and weight-average molecular weight (M n ,M w ) are 5550 and 6330 respectively, molecular weight distribution coeffi...

Embodiment 2

[0056] An amphiphilic block copolymer. Weigh 30g of PEG 1500 in a 250mL three-neck bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3h under mechanical stirring. Then cool down to 100°C with argon, add a total of 48g of D-lactide and glycolide with a molar ratio of 1:1, and stir thoroughly; add toluene solution containing 60mg of stannous octoate, vacuumize for 15min to remove toluene and then raise the temperature React at 150°C for 12h under the protection of argon. Then lower the temperature to 110°C and vacuumize for 3 hours to remove unreacted monomers, then wash the initial product three times with 80°C deionized water, and freeze-dry to obtain the final product to obtain the BAB type triblock polymer PDLGA-PEG-PDLGA, The yield is about 87%. The properties of the block polymer were measured, and the results are shown in Table 1. The number-average and weight-average molecular weight (M n ,M w ) are 5100 and 6320 respectively, molec...

Embodiment 3

[0058] An amphiphilic block copolymer. Weigh 20g of PEG 1000 in a 250mL three-neck bottle, seal each port with vacuum ester, and remove water under vacuum at 130°C for 3h under mechanical stirring. Then cool down to 100°C with argon gas, add 46.6g of D,L-lactide and 9.4g of glycolide, stir well; add toluene solution containing 60mg of stannous octoate, vacuumize for 15min to remove toluene, then heat up to 150°C The reaction was carried out under the protection of argon for 12h. Then lower the temperature to 110°C and vacuumize for 3 hours to remove unreacted monomers, then wash the initial product three times with 80°C deionized water, and freeze-dry to obtain the final product, obtaining the BAB type triblock polymer PLGA-PEG-PLGA, The yield is about 80%. The properties of the block polymer were measured, and the results are shown in Table 2. The number-average and weight-average molecular weight (M n ,M w ) are 5590 and 7040 respectively, molecular weight distribution c...

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Abstract

The invention discloses a HER-2 humanized monoclonal antibody long-acting sustained-release preparation. The preparation comprises 2-50 wt% of an amphiphilic block copolymer mixture, 0.05-10 wt% of anHER-2 humanized monoclonal antibody and 40-88 wt% of a menstruum, and the storage modulus and the loss modulus of an amphiphilic block copolymer mixture aqueous solution have an intersection point at0-55 DEG C. By utilizing the dual action of the diffusion of the HER-2 humanized monoclonal antibody along with drugs and gel degradation, the stable and slow release is realized, so that tumor recurrence is inhibited, and the drug utilization rate is increased; within the dosage range of 0.05-10 wt%, the cardiotoxicity of the preparation can be remarkably reduced; and moreover, the release kinetics of the drugs can be effectively regulated and controlled by changing the mixing ratio of a block copolymer carrier, and the administration frequency can be effectively reduced. Besides, the invention further discloses a preparation method of the HER-2 humanized monoclonal antibody long-acting sustained-release preparation, and the method is simple in condition and high in practicability and has good market application potential.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a long-acting sustained-release preparation of a HER-2 humanized monoclonal antibody. Background technique [0002] Breast cancer accounts for a quarter of all cancers in women, yet its survival rate is only 29.8%. Studies have found that 20%-25% of breast cancer patients have overexpression of epidermal growth factor 2 (HER-2). Such patients have high tumor malignancy, early metastasis and recurrence, poor prognosis, and are not sensitive to chemotherapy and hormone therapy. Herceptin (trastuzumab) is a human monoclonal antibody approved by the Food and Drug Administration of the United States in 1998 for use against the HER-2 antigen and to increase the chemotherapy sensitivity of HER-2 positive breast cancer patients. Its principle of action is to target and inhibit the P13K and MAPK signaling pathways of cancer cells, prevent angiogenesis and DNA repair, thereby promoting...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/34A61K39/395A61P35/00A61K31/704A61K31/337
CPCA61K9/0024A61K9/06A61K47/34A61K39/395A61K31/704A61K31/337A61P35/00C07K16/32C07K16/2863A61K2039/505A61K2300/00
Inventor 俞麟陈晓斌丁建东
Owner FUDAN UNIV
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