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Method for increasing solubility of 10-hydroxycamptothecin, product prepared by the method and applications of the product

A technology of hydroxycamptothecin and water solubility, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, drug combinations, etc., which can solve the problem of reducing the anti-tumor activity of drugs, prolonging the administration time, and toxic and side effects Major problems, to achieve the effect of reducing the time and frequency of clinical administration, shortening the course of treatment, and simple methods

Inactive Publication Date: 2014-12-17
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the low solubility of HCPT, HCPT is mainly used in clinical practice as sodium salt injection and sodium salt powder injection.
HCPT sodium salt injection has a short half-life, and it is necessary to prolong the administration time or the course of treatment in clinical practice, resulting in serious side effects
In addition, the sodium salt form also destroys the lactone ring structure of hydroxycamptothecin, which reduces the antitumor activity of the drug

Method used

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  • Method for increasing solubility of 10-hydroxycamptothecin, product prepared by the method and applications of the product
  • Method for increasing solubility of 10-hydroxycamptothecin, product prepared by the method and applications of the product
  • Method for increasing solubility of 10-hydroxycamptothecin, product prepared by the method and applications of the product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Screening of 10-hydroxycamptothecin-seven-membered cucurbit inclusion complex process conditions

[0019] (1) Determine the optimal feed ratio (also known as the stoichiometric ratio) between the seven-membered cucurbitan and 10-hydroxycamptothecin

[0020] In four 100mL round-bottomed flasks, add about 0.5g seven-membered cucurbitan ring respectively, then add a certain amount of 10-hydroxycamptothecin respectively, so that the metering ratio (n Q[7] :n HCPT ) were 1:1, 2:1, 3:1, 4:1, respectively, and finally about 85mL of hydrochloric acid solution with a pH of 2.0 was added and fully stirred for 4 hours at a constant temperature of 40~45°C. After the reaction was completed, the solution in the round bottom flask was filtered while hot to remove undissolved precipitates to obtain a clear and translucent yellow-green filtrate. Then the filtrate was concentrated and dried at 40-45°C, scraped out and weighed, and the yield and inclusion rate were calcula...

Embodiment 2

[0032] Example 2: Preparation of 10-hydroxycamptothecin-seven-membered cucurbit ring solid inclusion complex by co-evaporation

[0033] Weigh a certain amount of seven-membered cucurbit ring and hydroxycamptothecin (the stoichiometric ratio n Q[7] / n [HCPT] =3:1 Put it into a 100mL round bottom flask, add about 85mL of hydrochloric acid solution with a pH of 2.0, and stir fully at a constant temperature of 40~45°C for 4h. After the reaction was completed, the solution in the round bottom flask was filtered while hot to remove undissolved precipitates to obtain a clear and translucent yellow-green filtrate. Then the filtrate was evaporated to dryness by rotary evaporation, dried at 40-45°C, scraped off and weighed to obtain the seven-membered cucurbitanyl-hydroxycamptothecin solid inclusion compound.

Embodiment 3

[0034] Example 3: Preparation of 10-hydroxycamptothecin-seven-membered cucurbit ring solid inclusion compound by grinding method

[0035] Weigh the stoichiometric ratio (n Q[7] :n HCPT ) with a ratio of 3:1 of Q[7] and HCPT solids were placed in an agate mortar, added about 1 mL of hydrochloric acid solution with a pH of 2.0, ground for 1 hour, and then dried in an oven at 40-45 °C to obtain .

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Abstract

The invention relates to methods of preparing medicaments by a medicine inclusion technology, belongs to the field of pharmaceutical preparation technology, and particularly relates to a method for increasing solubility of 10-hydroxycamptothecin, a product prepared by the method and applications of the product. The invention discloses a solid inclusion compound 10-hydroxycamptothecin (HCPT) / cucurbit[7]uril (Q[7]) formed by including 10-hydroxycamptothecin and cucurbit[7]uril. By dissolving the solid inclusion compound in water, the solubility of the 10-hydroxycamptothecin is increased by 1642-2565 times. Preparation methods of the solid inclusion compound comprise A. a co-evaporation method, B. a grinding method and C. a freeze-drying method. The preparation methods for the inclusion compound are simple and the solubility of the 10-hydroxycamptothecin in water can be greatly increased, thus reducing medicine dosage, reducing medicine taking duration and frequency, shortening courses of treatment and reducing medicine toxic and side effects for patients who take the 10-hydroxycamptothecin for treatment.

Description

technical field [0001] The drug inclusion technology is a new form of pharmaceutical preparation, which belongs to the technical field of pharmaceutical preparations, specifically a method for increasing the solubility of 10-hydroxycamptothecin in water and the preparation and application of the product. Background technique [0002] Drug inclusion technology is a new form of drug preparation, which means that drug molecules as guest molecules are embedded in the cavity structure of host molecules to form molecular capsules. After the drug is included, its physical properties change, which can not only increase the solubility, dissolution rate, and oral bioavailability of the drug, but also improve the stability of the drug and prevent the volatilization of volatile components. At present, the commonly used drug inclusion host molecules are cyclodextrin and its derivatives, such as ibuprofen cyclodextrin inclusion compound, which can increase the solubility of ibuprofen by n...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K31/4745A61P35/00
Inventor 董南吕妍颜丽芬
Owner GUIZHOU UNIV
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