Chemotherapy drug pulse sustained-release implant agent and preparation method thereof

A technology for slow-release implants and chemotherapeutic drugs, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of re-administration, application restrictions, and drugs can only be released once, so as to avoid side damage and prolong Effect of Effective Drug Concentration

Active Publication Date: 2012-09-19
普华赛尔生物医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage is that the drug can only be released once, and when all the drug in the sustained-release formulation is released, it needs

Method used

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  • Chemotherapy drug pulse sustained-release implant agent and preparation method thereof
  • Chemotherapy drug pulse sustained-release implant agent and preparation method thereof
  • Chemotherapy drug pulse sustained-release implant agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1, preparation of gemcitabine hydrochloride microspheres

[0026] Pulverize gemcitabine hydrochloride, pass through a 200-mesh sieve, add PLGA (the number average molecular weight is 6000) in dichloromethane solution (the mass-number ratio of gemcitabine hydrochloride and PLGA is 1:9), stir evenly, evaporate the solvent to dryness, and place in a vacuum Dry in a drying oven (-0.1Mpa, 35°C) for 4 hours, take it out and crush it through an 80-mesh sieve, and then dry it for 24 hours, take out the medicinal material, mix it in a melting and mixing equipment with a constant temperature of 120°C, cool it, and crush it. Sieve, take microspheres between 100 mesh and 120 mesh sieves, and process them with a microsphere processor at 55° C. for 10 minutes to obtain gemcitabine hydrochloride microspheres, marked as sample A.

[0027] Gemcitabine hydrochloride microspheres were prepared according to the same method as above, labeled as sample B and sample C, respectively...

Embodiment 2

[0060] Example 2. Preparation of gemcitabine hydrochloride microspheres

[0061] Gemcitabine hydrochloride microspheres were prepared according to the same method as in Example 1, except that the melt-kneading temperatures were 110° C. and 130° C., respectively, and the prepared microspheres were marked as sample D and sample E, respectively.

[0062] The stability of gemcitabine hydrochloride during melt kneading at 110 ℃, 120 ℃ and 130 ℃ was investigated, and the detection index was related substances of gemcitabine hydrochloride. The results are shown in Table 4.

[0063] Table 4 Limits of related substances for samples D, A and E

[0064]

[0065] It can be seen from Table 4 that the melt-kneading temperature is 110°C to 130°C, and gemcitabine hydrochloride is stable, and the melt-kneading temperature is preferably 120°C.

Embodiment 3

[0066] Example 3. Preparation of gemcitabine hydrochloride microspheres

[0067] Gemcitabine hydrochloride microspheres were prepared according to the same method as in Example 1, except that the microspheres were passed through 80-100 mesh and 120-150 mesh sieves respectively, and the prepared microspheres were marked as sample F and sample G respectively.

[0068] The in vitro release degrees of samples A, F and G were detected, and the results are shown in Table 5 and figure 2 .

[0069] Table 5 Relationship between in vitro release and time of samples A, F and G

[0070]

[0071] From Table 5 and figure 2 It can be seen that the particle size of the microspheres is between 80-100 mesh sieves and 100-120 mesh sieves, and the in vitro release of gemcitabine hydrochloride microspheres can meet the project design requirements. Considering clinical applications, the smaller the particle size, the more convenient, preferably 100-120 mesh microspheres between the sieves. ...

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Abstract

The invention provides a chemotherapy drug pulse sustained-release implant agent and a preparation method thereof. The sustained-release implant agent comprises a chemotherapy drug active component such as any one of gemcitabine, gemcitabine hydrochloride, doxorubicin, 5-fluorouracil, cisplatin, carboplatin and paclitaxel, and an excipient such as a polylactic-glycolic acid copolymer. The preparation method provided by the invention comprises the following steps of: evenly mixing the chemotherapy drug active component with the excipient in a solvent, and then drying the mixture of the chemotherapy drug active component and the excipient in a vacuum after removing the solvent; and then sequentially crushing, sieving, melting and blending the mixture to obtain the sustained-release implant agent. The sustained-release implant agent provided by the invention has the advantages that a second drug release is carried out after tumor growth is controlled by a first drug release for a certain period, and the local effective concentration of a drug is effectively increased, so that the effect of administering once and releasing twice is achieved, and the side injury caused by secondary drug implanting is avoided.

Description

technical field [0001] The invention relates to a chemotherapeutic drug pulse sustained-release implant and a preparation method thereof, belonging to the field of chemotherapeutic drug sustained-release agents and preparation thereof. Background technique [0002] At present, the most widely used in clinical practice is Zhongrenfuan (5-fluorouracil) sustained-release implant produced by Simcere Pharmaceuticals. Achieving a high local concentration and a low systemic blood circulation concentration can reduce the blood circulation drug concentration while maintaining a long-term local effective concentration, so it can play a role in synergizing and reducing toxicity. It has been confirmed in clinical practice that it can prolong the survival period of patients with minimal toxic side effects. Its disadvantage is that the drug can only be released once, and it needs to be re-administered after all the drug in the sustained-release formulation is released. In some abdominal...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61P35/00
Inventor 马洁解亦斌王世亮赵平许健健
Owner 普华赛尔生物医疗科技有限公司
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