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Docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation and preparation method thereof

A docetaxel, self-emulsifying technology, applied in pharmaceutical formulations, emulsion delivery, medical preparations with inactive ingredients, etc. It can improve the bioavailability, improve the dissolution, and reduce the irritation effect.

Active Publication Date: 2019-04-09
KUNMING JIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the shortcomings of the existing docetaxel preparations that only have injections, cannot meet the oral administration of docetaxel, poor patient compliance, and need to be pretreated with hormones before administration, researchers have carried out a lot of research, aiming to improve the multi- Oral bioavailability of docetaxel, but the effect is minimal. The oral bioavailability of docetaxel reported so far is low, which cannot meet the oral needs

Method used

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  • Docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation and preparation method thereof
  • Docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation and preparation method thereof
  • Docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] prescription:

[0079] DTX

1g

CsA

0.5g

MCT

31g

ELP

49g

IMW 742

7g

Absolute ethanol

11.5g

total prescription

100g

[0080] Weigh docetaxel and cyclosporine A according to the above prescription, dissolve them completely with absolute ethanol, then add medium-chain triglycerides, polyoxyethylene 35 castor oil, caprylic capric acid mono-diglyceride, Stir well, dispense and seal with a gland.

[0081] The oral bioavailability of docetaxel of the obtained preparation was measured by the method described in the above test example 2, and the result was 52.5%.

Embodiment 2～8

[0083] Using the same method as in Example 1, the preparations of Examples 2 to 8 were prepared according to the prescriptions in Table 9, and the oral bioavailability of docetaxel was determined, as shown in Table 9.

[0084] Table 9

[0085]

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Abstract

The invention relates to a docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation. The docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation comprises docetaxel, cyclosporin A, an oil phase and an emulsifying agent; the docetaxel and the cyclosporin A are in the weight ratio of 2 to 1. The docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation is a self-emulsifying drug delivery system; the oral bioavailability of the docetaxel can be greatly improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a docetaxel-cyclosporin A co-encapsulated self-emulsifying preparation and a preparation method thereof. Background technique [0002] Docetaxel (Docetaxel) is a taxane drug, by promoting the assembly of microtubule dimers into microtubules, while stabilizing microtubules by preventing depolymerization, arresting cells in G2 and M phases, thereby inhibiting Mitosis and proliferation of cancer cells. The pharmacological effect of docetaxel is stronger than that of paclitaxel, its intracellular concentration is 3 times higher than that of paclitaxel, and its intracellular residence time is longer, and its affinity for microtubules is 2 times that of paclitaxel; in vitro antitumor activity test, it has been confirmed The antitumor activity of docetaxel is 1.3 to 12 times that of paclitaxel. Clinical studies have shown that for anthracycline-resistant breast cancer, docet...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K47/42A61K47/14A61K47/44A61P35/00
CPCA61K47/14A61K47/42A61K47/44A61P35/00A61K9/0053A61K9/107A61K9/1075A61K31/337
Inventor 程晓波陈成军李英吴梅金寅张云王立江
Owner KUNMING JIDA PHARMA