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Taxol double-layer soft capsule oral preparation medicament

An oral preparation, paclitaxel technology, applied in the field of medicine, can solve the problems of reducing bioavailability, unable to take continuous medication, affecting the curative effect, etc., to achieve the effect of adjusting the dosage and time, solving the problems of toxicity and curative effect, and easy to take the dosage and time.

Active Publication Date: 2009-08-26
辽宁奥佳生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although paclitaxel and docetaxel have been proved to be the best drugs for current chemotherapy, there are still some insurmountable shortcomings in the current injection dosage forms
One is the high toxicity and side effects. Paclitaxel itself has certain toxicity and side effects. In addition, the solvent castor oil used in the injection also has strong toxicity and side effects. It must be neutralized by another drug.
Second, the dosage form is single. The only dosage form of paclitaxel is injection, which is relatively complicated to produce and use, and the toxic and side effects are more prominent.
The third is to affect the curative effect
With injections, the serum concentration of paclitaxel is higher than the toxic concentration in a short period of time. Due to the high toxicity and side effects, continuous medication cannot be used, which will affect the therapeutic effect. Therefore, paclitaxel cannot be fully absorbed, which also affects the curative effect to a certain extent.
[0003] Oral paclitaxel alone has so far not been used for two reasons of reduced bioavailability

Method used

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  • Taxol double-layer soft capsule oral preparation medicament
  • Taxol double-layer soft capsule oral preparation medicament
  • Taxol double-layer soft capsule oral preparation medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Paclitaxel-based double-layer soft capsule oral preparation drug, the inner layer is paclitaxel anticancer drug soft capsule, and the outer layer is cyclosporin A semi-solid capsule; figure 1 As shown, from inside to outside are paclitaxel anticancer drug 1, inner soft capsule 2, cyclosporin A semi-solid 3 and outer capsule 4.

[0028] The preparation method of paclitaxel double-layer soft capsule oral preparation medicine is as follows:

[0029] 1) Preparation of paclitaxel anticancer drugs:

[0030] Dissolve 1.5 grams of paclitaxel in 10 grams of D-α-polyethylene glycol 1000 succinate (TPGS, D-alpha-tocopheryl polyethylene glycol 1000 succinate), add 5 grams of caprylic macrogol glyceride and caprylic macrogol in turn A mixture of alcohol glycerides, 3 grams of Sorbitan monooleate, 0.2 grams of Ascorbylpalmitate, and 1 gram of absolute ethanol. This formulation is blended in an amount of 100 unit doses.

[0031] 2) Wrap paclitaxel anticancer drugs in the inner soft...

Embodiment 2

[0037] Different from Example 1, only the paclitaxel anticancer drug in the inner layer and its preparation method are different:

[0038] Preparation of paclitaxel anticancer drugs: Dissolve 1.5 grams of paclitaxel in 10 grams of D-α-polyethylene glycol 1000 succinate (TPGS, D-alpha-tocopheryl polyethylene glycol 1000 succinate), and then add 3 grams of polyoxyethylene oleic acid in turn Glyceride (LabraWl M 1944CS, polyoxyethylated oleic glycerides), 5 grams of polyethylene glycol 400 (PEG 400: polyethylene glycol 400), 0.2 gram of ascorbyl palmitate (Ascorbylpalmitate) and 1 gram of absolute ethanol. This formulation is mixed in an amount of 100 unit doses.

Embodiment 3

[0040] Preparation of paclitaxel anticancer drugs: dissolve 0.5 g of docetaxel in 3 g of D-α-polyethylene glycol 1000 succinate (TPGS, D-alpha-tocopheryl polyethylene glycol 1000 succinate), and then add 1 g of polyoxyethylene Glyceryl oleate (LabraWl M 1944CS, polyoxyethylated oleic glycerides), 1.5 grams of polyethylene glycol 400 (PEG 400: polyethylene glycol 400), 0.1 gram of ascorbyl palmitate (Ascorbylpalmitate) and 0.4 gram of absolute ethanol. This formulation is mixed in an amount of 100 unit doses.

[0041] Preparation of cyclosporine A semi-solid: Mix 7 grams of polyoxyethylene castor oil diglyceride, 7 grams of polyoxyethylene, 7 grams of sorbitan glyceride, 7 grams of poloxamer, and 12 grams of polyethylene glycol-4000, Heat to 60-70°C to dissolve. Add 10 g of cyclosporine A and mix well to dissolve. Cool to room temperature and solidify into a semi-solid. This formulation is in the amount of 100 unit doses.

[0042] The preparation process of the inner layer ...

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Abstract

The invention relates to a taxol double-layer soft capsule oral preparation medicament. The taxol double-layer soft capsule oral preparation medicament adopts the technical proposal that an inner layer is a taxol anticancerogen soft capsule, and an outer layer is a ciclosporin A solid or semisolid capsule; and the taxol double-layer soft capsule oral preparation medicine comprises taxol anticancerogen, the inner layer soft capsule, the ciclosporin A solid or semisolid and an outer layer capsule from the inside to the outside, wherein the taxol anticancerogen comprises taxol active substances and medicinal carriers; the ciclosporin A solid or semisolid comprises ciclosporin A and matched carriers; and the weight ratio of the taxol active substances to the ciclosporin A is 1:2-1:20 in unit dose. The medicament preparation method of the invention comprises the following steps: preparing the taxol anticancerogen; wrapping the taxol anticancerogen in the inner layer soft capsule; preparing the ciclosporin A solid or semisolid; coating the ciclosporin A solid or semisolid outside the inner layer soft capsule; and then wrapping the outer layer capsule outside the ciclosporin A solid or semisolid. The taxol double-layer soft capsule oral preparation medicament has the advantages of small toxicity, convenient taking and good anticancer treatment effect.

Description

Technical field: [0001] The invention relates to the field of medicaments, in particular to an anticancer paclitaxel double-layer soft capsule oral preparation drug with a double-layer structure. Background technique: [0002] Paclitaxel and docetaxel injections are currently the first choice for anticancer chemotherapy. Although paclitaxel and docetaxel have been proven to be the best drugs for current chemotherapy, there are still some insurmountable shortcomings in the current injection formulations. One is that it has a lot of toxic and side effects. Paclitaxel itself has certain toxic and side effects, and the solvent castor oil used in the injection also has strong toxic and side effects, which must be neutralized by another drug. Second, the dosage form is single. The only dosage form of paclitaxel is injection, which is relatively complicated to produce and use, and has more prominent toxic and side effects. The third is to affect the curative effect. With injecti...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K31/337A61K38/13A61P35/00
Inventor 蔺新力单宝华
Owner 辽宁奥佳生物制药有限公司
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