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Pharmaceutical composition and preparation method and application thereof

A composition and drug technology, applied in the field of medicine, can solve the problems that cancer chemotherapy needs to be greatly improved, and achieve the effect of a good treatment plan

Inactive Publication Date: 2017-01-11
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the means of cancer chemotherapy needs to be greatly improved

Method used

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  • Pharmaceutical composition and preparation method and application thereof
  • Pharmaceutical composition and preparation method and application thereof
  • Pharmaceutical composition and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1 Preparation of Paclitaxel / Hedgehog Signaling Pathway Inhibitor Pharmaceutical Composition Micelles

[0068] Dissolve 150mg of PEG-PLA (2K-2K, or 5K-5K polyethylene glycol polylactic acid diblock copolymer), 20mg of itraconazole and 20mg of paclitaxel in 8mL of acetonitrile, and remove the organic solvent by rotary evaporation at 60°C to obtain The transparent drug-polymer mixed film was hydrated by adding 10 mL of 60°C deionized water, and ultrasonicated for 5 minutes to obtain an aqueous solution containing 2 mg / mL itraconazole and 2 mg / mL paclitaxel polymer drug-loaded micelles (see photo figure 1 ), freeze-dried.

[0069] figure 1 Among them, the meanings of each abbreviation are as follows: IM: itraconazole micelles; PM: paclitaxel micelles; 9I1PM: micelles with a drug loading ratio of itraconazole and paclitaxel of 9 / 1 (w / w); 7I3PM: itraconazole micelles The micelles with the loading ratio of itraconazole and paclitaxel at 7 / 3 (w / w); 5I5PM: the micelles...

Embodiment 2

[0071]Example 2 Preparation of Paclitaxel Analog / Hedgehog Signaling Pathway Inhibitor Composition Micelles

[0072] The paclitaxel analog used in this example is cabazitaxel (CAB), and the hedgehog signaling pathway used is itraconazole (ITA). Dissolve 30mg of PEG-PLA (5K-5K, polyethylene glycol polylactic acid diblock copolymer), 3mg of itraconazole and 3mg of cabazitaxel in 5mL of acetonitrile, and evaporate the organic solvent at 60°C for 20min to obtain a transparent The drug-polymer mixed film was hydrated by adding 3 mL of 60°C deionized water, and sonicated for 5 minutes to obtain an aqueous solution containing 1 mg / mL itraconazole and 1 mg / mL cabazitaxel polymer drug-loaded micelles.

[0073] The photos and particle size detection results of the prepared micelles are as follows: Figure 4 As shown, itraconazole cannot effectively form micelles with uniform particle size distribution, and the film appears turbid immediately after hydration, but when it is combined with...

Embodiment 3

[0074] Example 3 Preparation of Paclitaxel Analog / Kinase Inhibitor Combination Micelle

[0075] The paclitaxel analog selected in this embodiment is cabazitaxel (CAB), the kinase inhibitor selected is sorafenib (SOR) and 40mg PEG-PLA (5K-5K, polyethylene glycol polylactic acid diblock copolymer ), 4 mg of sorafenib and 4 mg of cabazitaxel were dissolved in 5 mL of acetonitrile, evaporated at 60 ° C for 20 min to remove the organic solvent, and obtained a transparent drug-polymer mixed film, added 4 mL of 60 ° C deionized water for hydration, and ultrasonicated for 5 min to obtain 1 mg / mL sorafenib and 1 mg / mL cabazitaxel polymer drug-loaded micelles in water.

[0076] The photos and particle size detection results of the prepared micelles are as follows: Figure 5 As shown, cabazitaxel could not effectively form micelles with uniform particle size distribution, and drug precipitation appeared at the bottom of the bottle after standing at 4°C for 2 hours, and the amount of dru...

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Abstract

The invention provides a pharmaceutical composition and a preparation method and an application thereof. According to the embodiment of the pharmaceutical composition, the pharmaceutical composition comprises two kinds of medicines: 1, taxol or analogue; and 2, a hedgehog signaling pathway inhibitor or a kinase inhibitor. The inventor of the pharmaceutical composition finds that the pharmaceutical composition can be used for treating cancer effectively.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a pharmaceutical composition and its preparation method and use. Background technique [0002] Cancer, also known as malignant tumor, is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. In addition to growing out of control, cancer cells can also locally invade the surrounding normal tissues and even transfer to other parts of the body through the internal circulatory system or lymphatic system. [0003] Cancer cells are characterized by unlimited and endless proliferation, which consumes a large amount of nutrients in the patient's body; cancer cells release a variety of toxins, causing a series of symptoms in the human body; cancer cells can also be transferred to grow and multiply throughout the body, It leads to emaciation, weakness, anemia, loss of appetite, fever, and severe damage to organ function. In contrast, there are benign tum...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/127A61K9/107A61K9/14A61K31/337A61K31/496A61P35/00
CPCA61K9/107A61K9/127A61K9/14A61K31/337A61K31/496
Inventor 钱锋张玲刘淳刘正生刘慧琴
Owner TSINGHUA UNIV
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