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Nano composition of 9-nitrocamptothecin lipoid and its preparation

A technology of nitrocamptothecin and lipid nanoparticles, which is applied in the field of medicine, can solve the problems of administration and lack of LN finished preparations, and achieve the effects of reducing toxic and side effects, prolonging the circulation time in the body, and improving bioavailability

Inactive Publication Date: 2007-04-25
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, drugs such as camptothecin, zidovudine ester, and doxorubicin ester have been developed into LN as model drugs. Studies have shown that the LN preparations of these model drugs have the characteristics of controlled release, long-acting and targeting ( Yang Shicheng, Zhu Jiabi, Liang Bingwen, etc. Acta Pharmaceutica Sinica, 1999, 34(2): 146-150), but so far no LN finished preparations have been put on the market

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1 Preparation of 9-nitrocamptothecin lipid nanoparticles by solvent diffusion method

[0017] Components:

[0018] 9-NC 2mg

[0019] Dynasan 118 (Triglyceryl Stearate) 100mg

[0020] Miglyol 812 N (caprylic / capric triglyceride) 400μL

[0021] Soy lecithin (PC content > 80%) 100mg

[0022] Myrj 59 200mg

[0023] Ethanol 2mL

[0024] Acetone 8mL

[0025] Water for injection 15mL

[0026] 2% trehalose solution 20mL

[0027] Weigh 9-NC, Dynasan 118, and Miglyol 812 N of the above components, add acetone, heat and dissolve at 70°C; weigh the prescription amount of soybean lecithin, add ethanol and sonicate for 10 minutes, and after dissolution, mix the above two liquids to form an organic phase ; Another prescribed amount of Myrj 59 was dissolved in 15ml of water for injection to form an aqueous phase. Inject the organic phase into the water phase with constant stirring (1000rpm) at 70±2°C with a No. 6 needle, and stir (1000rpm) at 70±2°C for 4 hours until t...

Embodiment 2

[0028] Example 2: Preparation of 9-nitrocamptothecin lipid nanoparticles by solvent diffusion method

[0029] Components:

[0030] 9-NC 2mg

[0031] Dynasan 116 (Triglyceryl Palmitate) 100mg

[0032] Soy lecithin (PC content > 80%) 100mg

[0033] Myrj 59 200mg

[0034] Ethanol 2mL

[0035] Acetone 8mL

[0036] Water for injection 15mL

[0037] 4% trehalose solution 20mL

[0038]Preparation process: Weigh the components of 9-NC and Dynasan 116, add acetone, heat and dissolve at 70°C; weigh the components of soybean lecithin, add ethanol and sonicate for 10 minutes, and after dissolving, mix the above two liquids to form an organic phase; Component amounts of Myrj 59 were dissolved in 15 ml of water for injection to form an aqueous phase. Inject the organic phase into the water phase with constant stirring (1000rpm) at 70±2°C with a No. 6 needle, and stir (1000rpm) at 70±2°C for 4 hours until the organic solvent evaporates completely. The emulsion was rapidly dispersed ...

Embodiment 3

[0039] Example 3 Preparation of 9-nitrocamptothecin lipid nanoparticles

[0040] Components:

[0041] 9-NC 2mg

[0042] Dynasan 118 (Triglyceryl Stearate) 100mg

[0043] Soy lecithin (PC content > 80%) 100mg

[0044] Myrj 59 200mg

[0045] Ethanol 2mL

[0046] Acetone 8mL

[0047] Water for injection 15mL

[0048] 4% trehalose solution 20mL

[0049] Preparation process: Weigh 9-NC and Dynasan 118, add acetone, heat and dissolve at 70°C; weigh the prescription amount of soybean lecithin, add ethanol and sonicate for 10 minutes, and after dissolving, mix the above two liquids to form an organic phase; Component amounts of Myrj 59 were dissolved in 15 ml of water for injection to form an aqueous phase. Inject the organic phase into the water phase with constant stirring (1000rpm) at 70±2°C with a No. 6 needle, and stir (1000rpm) at 70±2°C for 4 hours until the organic solvent evaporates completely. The emulsion was quickly dispersed into 20ml of 4% trehalose solution at ...

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Abstract

A composite 9-nitrocamptothecin lipid nanoparticle used for preparing injection is prepared from 9-nitrocamptothecin, lipid and surfactant.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a 9-nitrocamptothecin lipid nanoparticle composition and a preparation method thereof. Background technique [0002] Camptothecin has good antitumor activity, but due to its high toxicity and side effects, it was developed in the 1970s and was abandoned soon after. Since the 1980s, due to its unique topoisomerase I inhibitory effect, camptothecin has once again attracted domestic and foreign attention. A variety of camptothecin derivatives have been developed abroad. 9-nitro-camptothecin (English name: 9-nitro-camptothecin, hereinafter referred to as 9-NC) is a semi-synthetic derivative of camptothecin, a new generation of anticancer drugs, with a wide range of anticancer activities, especially for Pancreatic cancer and ovarian cancer have remarkable curative effects, and studies have shown that they are less toxic than camptothecins that have been put into clinica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K9/127A61K9/14A61P35/00
Inventor 方晓玲李珺婵沙先谊韩丽妹吴云娟张丽珺白志华韩旻王青松
Owner FUDAN UNIV
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