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Nanometer particle target preparation of hydroxycamptothecine, and its preparing method

A hydroxycamptothecin and targeting technology, which is applied in the field of 10-hydroxycamptothecin nanoparticle targeting preparations and its preparation, can solve problems such as drug failure, and achieve improved curative effect, good targeting, and improved curative effect Effect

Inactive Publication Date: 2007-07-25
HUNAN KANGDU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

More than 3.95% of 10-hydroxycamptothecin is combined with serum albumin in the body to form a carboxylate-serum albumin complex, causing more than 95% of the drug to fail
4. Existing 10-hydroxycamptothecin drugs also have adverse reactions such as hematuria, urgency, bone marrow suppression, nausea and vomiting, diarrhea, and rashes

Method used

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  • Nanometer particle target preparation of hydroxycamptothecine, and its preparing method
  • Nanometer particle target preparation of hydroxycamptothecine, and its preparing method
  • Nanometer particle target preparation of hydroxycamptothecine, and its preparing method

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Embodiment 1

[0028] The formula that present embodiment adopts is as follows:

[0029] Gelatin 1.8g;

[0030] 10-Hydroxycamptothecin 1.7g;

[0031] 255ml of tert-butanol;

[0032] Vitamin C 40g;

[0033] Chitosan 0.30g;

[0034] Sodium carboxymethyl cellulose 6.50g;

[0035] Water for injection 765ml.

[0036] The preparation method is as described above.

[0037] Pharmacodynamic experiment verification is as follows:

[0038] Mice models of gastric cancer and head and neck cancer were selected and randomly divided into 20 mice in each group.

[0039] Drug treatment group of the present invention is set as:

[0040] Drug group a of the present invention: 10-hydroxycamptothecin gelatin nanoparticles, the dosage is 1.5 mg / kg, twice a day, intraperitoneal injection, for 21 days.

[0041] Drug group b of the present invention: 10-hydroxycamptothecin gelatin nanoparticles, the dosage is 1.0 mg / kg, twice a day, intraperitoneal injection, medication for 21 days.

[0042] Drug group c of...

Embodiment 2

[0050] The formula that present embodiment adopts is as follows:

[0051] Human serum albumin 4.0g;

[0052] 10-Hydroxycamptothecin 3.2g;

[0053] 520ml tert-butanol;

[0054] Vitamin C 82g;

[0055] Chitosan 0.66g;

[0056] Sodium carboxymethyl cellulose 16g;

[0057] Water for injection 1560ml.

[0058] The preparation method is as described above.

[0059] Pharmacodynamic experiment verification is as follows:

[0060] Mice models of gastric cancer and head and neck cancer were selected and randomly divided into 20 mice in each group.

[0061] Drug treatment group of the present invention is set as:

[0062] Drug group a of the present invention: 10-hydroxycamptothecin human serum albumin nanoparticles, the dosage is 1.5mg / kg, twice a day, intraperitoneal injection, medication for 21 days.

[0063] Drug group b of the present invention: 10-hydroxycamptothecin human serum albumin nanoparticles, the dosage is 1.0 mg / kg, twice a day, intraperitoneal injection, medicat...

Embodiment 3

[0072] The formula that present embodiment adopts is as follows:

[0073] Bovine serum albumin 5.4g;

[0074] 10-Hydroxycamptothecin 4.2g;

[0075] tert-butanol 630ml;

[0076] Vitamin C 120g;

[0077] Chitosan 0.90g;

[0078] Sodium carboxymethyl cellulose 20g;

[0079] Water for injection 1900ml.

[0080] The preparation method is as described above.

[0081] Pharmacodynamic experiment verification is as follows:

[0082] Mice models of gastric cancer and head and neck cancer were selected and randomly divided into 20 mice in each group.

[0083] Drug treatment group of the present invention is set as:

[0084] Drug group a of the present invention: 10-hydroxycamptothecin bovine serum albumin nanoparticles, the dosage is 1.5 mg / kg, twice a day, intraperitoneal injection, medication for 21 days.

[0085] Drug group b of the present invention: 10-hydroxycamptothecin bovine serum albumin nanoparticles, the dosage is 1.0 mg / kg, twice a day, intraperitoneal injection, medi...

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Abstract

A targeting nanoparticle of 10-hydroxy camptothecine for treating tumor is proportionally prepared from gelatin, 10-hydroxy camptothecine, tert-butanol, VC, chitosan, carboxymethyl cellulose sodium, and the water for injection. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a nanoparticle targeting preparation of 10-hydroxycamptothecin and a preparation method thereof. Background technique [0002] 10-Hydroxycamptothecin is a natural alkaloid extracted from the fruit of camptothecin, a DNA topoisomerase I inhibitor, which can be used as a specific anti-tumor drug in the DNA synthesis phase, and its clinical indications are for a variety of solid tumors, Gastrointestinal tumors, non-small cell tumors, ovarian tumors, head and neck tumors, liver cancer, etc. Due to its wide anti-cancer spectrum, sufficient sources, especially the outstanding advantages of no cross-sensitivity with other anti-cancer drugs, if the defects of its existing technology are overcome, its market prospect will be better than paclitaxel, which is resource-constrained. [0003] The defects of the prior art of 10-hydroxycamptothecin are mainly manifested in: 1. Poor water solubility and low bioavailability. [0004] 2. The pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/475A61K47/42A61P35/00
Inventor 蔡海德
Owner HUNAN KANGDU PHARMA
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