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Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof

A technology of hydroxycamptothecin and granule preparation, which is applied in the directions of antitumor drugs, pharmaceutical formulations, and pill delivery, can solve the problems of reducing antitumor activity, leukopenia, and large toxic and side reactions, and achieves improved drug utilization, The effect of stable drug release and high drug loading rate

Inactive Publication Date: 2010-08-04
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the side effects of this drug are relatively large, mainly manifested as bone marrow suppression, leukopenia, gastrointestinal reactions, urinary tract irritation, etc.
At the same time, 10-HCPT is insoluble in water, and the water-soluble preparation used clinically is its sodium salt preparation, which destroys the α-hydroxylactone ring of its anti-topoisomerase I active structure and reduces the anti-tumor activity

Method used

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  • Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof
  • Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof
  • Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: (1) Preparation of drug-loaded microspheres: get HCPT crude drug 100mg, molecular weight is 500mg of polylactic acid of 5000 Daltons, put in beaker and dissolve with 5ml DMF; Under the rotating speed of 100r / min, while stirring Add 5ml of water dropwise until the emulsion is formed; then transfer the emulsion to a dialysis bag, put it in a water bathtub, and replace the water phase in the bathtub every 1h, 4h, and 8h to complete the dialysis; the obtained emulsion is centrifuged at 3500r / min. The precipitates were collected and freeze-dried to obtain drug-loaded microspheres. The yield of HCPT drug-loaded microspheres is over 90%. From figure 1 It can be seen that the surface of the drug-loaded microspheres is round and evenly distributed.

[0027] (2) Preparation of granule preparation: prepare 5ml of acetic acid solution with a concentration of 0.3%, add 37.5mg of chitosan to dissolve; take 175mg of collagen and add it to the above solution, stir until...

Embodiment 2

[0029] Embodiment 2: (1) Preparation of drug-loaded microspheres: get 50 mg of HCPT bulk drug, 500 mg of polylactic acid with a molecular weight of 10,000 Daltons, and dissolve in a beaker with 5 ml of DMF; at a rotating speed of 300 r / min, stir while stirring Add 2.5ml of water dropwise until the emulsion is formed; then transfer the emulsion to a dialysis bag, put it in a water bathtub, and replace the water phase in the bathtub every 1h, 4h, and 8h to complete the dialysis; the obtained emulsion is centrifuged at 3500r / min , collect the precipitate and lyophilize to obtain drug-loaded microspheres; from the ESEM scanning electron micrograph of the resulting microspheres ( figure 2 ) showed that the prepared drug-loaded microspheres were round and well-uniform.

[0030] (2) Preparation of granule preparations: prepare 15 ml of 1% acetic acid solution, add 25 mg of chitosan to dissolve; get 130 mg of collagen and add it to the above solution, stir until it swells; add 25 mg ...

Embodiment 3

[0033] Embodiment 3: (1) Preparation of drug-loaded microspheres: get 50 mg of HCPT bulk drug, 750 mg of polylactic acid with a molecular weight of 5000 Daltons, put it in a beaker and dissolve it with 3 ml DMF; at a rotating speed of 400 r / min, stir while Add 0.6ml of water dropwise until the emulsion is formed; then transfer the emulsion to a dialysis bag, put it in a water bathtub, and replace the water phase in the bathtub every 1h, 4h, and 8h to complete the dialysis; the obtained emulsion is centrifuged at 3500r / min , the precipitate was collected and lyophilized to obtain drug-loaded microspheres.

[0034](2) Preparation of granule preparation: preparation concentration is 20ml of 1% acetic acid solution, add chitosan 20mg to dissolve; get 200mg collagen and join in the above solution, stir until swelling; add water-soluble lecithin 75mg to above-mentioned chitosan etc. Mix well in the mixed solution; stir the above solution and 100mg drug-loaded microspheres until visc...

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Abstract

The invention discloses an implanted dual sustained-release granule preparation of 10-hydroxycamptothecine, an antitumor drug, and a preparation method thereof. The invention relates to pharmaceutical preparation and provides the dual sustained-release granule preparation of 10-hydroxycamptothecine that has long releasing time, stable releasing and high utilization ratio of the drug and the preparation method thereof. The preparation is administrated in the manner of implanting after the operation of tumor nidus, thus realizing local target administration to reduce toxic and side effects on the whole body and prevent the recurrence of the tumor. The ingredients of preparation are drug-loaded microspheres, chitosan, lecithin and collagen. The drug-loaded microspheres contain hydroxycamptothecine and polylactic acid that are dissolved in organic solvent in proportion. Initial latex is prepared by dialysis; deposit is collected by centrifugation; and the drug-loaded microsphere is obtained by freeze drying. Afterwards, the chitosan, the collagen and the lecithin with water solubility are added into acetic acid resolution in proportion; and the drug-loaded microsphere is mixed with the solution. After stamping and drying, solid strip preparation is obtained. And the preparation is cut up and stored according to the specifications of the preparation.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a double slow-release dosage form of 10-hydroxycamptothecin for preventing postoperative recurrence of malignant solid tumors and a preparation method thereof. Background technique [0002] 10-Hydroxycamptothecin (10-HCPT) is a topoisomerase I inhibitor, which can inhibit the enzymatic activity of topoisomerase I, and inhibit topoisomerase from participating in DNA replication, repair, genetic recombination and transcription . 10-HCPT mainly acts on the DNA synthesis phase, and it has an effect on G 0 Phase cells have no effect on G 1 , G 2 , Has slight lethality to cells in M ​​phase. It has a broad anti-tumor spectrum and no cross-resistance with commonly used anti-tumor drugs. Clinically, it is mainly used for the treatment of liver cancer, colorectal cancer, lung cancer and leukemia. However, the side effects of this drug are relatively large, mainly manifested as bone ma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K47/36A61K31/4745A61K47/34A61K9/20
Inventor 张其清侯振清王衍戈韩晶林程宏
Owner XIAMEN UNIV
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