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Eltrombopag inclusion compound and preparations and preparation method thereof

A technology for eltrombopag and inclusion complex, which is applied in the field of eltrombopag inclusion complex and its preparation and preparation, can solve problems such as the need for further research, and achieves improving water solubility, avoiding curative effect reduction, and reducing chelation effect Effect

Pending Publication Date: 2018-04-17
SUNSHINE LAKE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, at this stage, the research on Eltrombopag drug needs to be deepened.

Method used

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  • Eltrombopag inclusion compound and preparations and preparation method thereof
  • Eltrombopag inclusion compound and preparations and preparation method thereof
  • Eltrombopag inclusion compound and preparations and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0050] Preparation of clathrates: including but not limited to freeze-drying method: Weigh each component separately, dissolve the clathrate material completely in water, add the drug, stir, centrifuge, take the supernatant, and then freeze the supernatant Dry to obtain clathrate.

[0051] Preparation of capsules: including but not limited to powder method: specifically, weigh each composition separately, make inclusion compound of Eltrombopag according to the above-mentioned inclusion compound preparation method, sieve the inclusion compound, add disintegrant, Part of the filler, mixed, then add the rest of the filler, mix, finally add lubricant, mix evenly and fill in capsules (enteric-coated capsules or gastric-coated capsules), to obtain capsules for in vitro dissolution test.

[0052] Preparation of tablets: including but not limited to powder direct compression method: specifically, each component is weighed separately, and Eltrombopag is prepared into an inclusion compo...

Embodiment 1

[0060] In this embodiment, according to the above-mentioned preparation process and test conditions, the Eltrombopag inclusion compound was dissolved in pH6.8 phosphate buffer solution containing 0.5% by weight SDS, containing 2.78mmol / L calcium chloride and containing 0.5% by weight After the pH 6.8 phosphate buffer solution medium solution of %SDS is filtered, the two filtrates are subjected to HPLC test respectively. Wherein, the concrete composition of clathrate is as follows:

[0061] prescription composition

Prescription ratio (weight%)

Eltrombopag olamine

1.43

α-cyclodextrin

8.96

purified water

89.61

total

100.00

[0062] And in this example, the clathrate was prepared by freeze-drying method, weighed separately, the weight ratio of Eltrombopag to α-cyclodextrin was 1:6.3, dissolved α-cyclodextrin in purified water, and waited After the solution is clarified, dissolve Eltrombopag in α-cyclodextrin aqueous soluti...

Embodiment 2

[0065] In this example, according to the preparation process and test conditions substantially the same as in Example 1, the Eltrombopag inclusion complex was dissolved in a pH6.8 phosphate buffer solution containing 0.5% by weight of SDS, containing 2.78mmol / L chlorine After the solution of calcium chloride in a pH 6.8 phosphate buffer solution medium containing 0.5% by weight SDS was filtered, HPLC tests were performed on the two filtrates respectively. The difference is that, in this embodiment, the specific composition of Eltrombopag inclusion compound is as follows:

[0066] prescription composition

Prescription ratio (weight%)

Eltrombopag olamine

1.48

β-cyclodextrin

16.42

purified water

82.10

total

100.00

[0067] Moreover, the weight ratio of Eltrombopag to β-cyclodextrin is 1:11.1, after Eltrombopag is dissolved in β-cyclodextrin aqueous solution, stir in a water bath at 70°C. The inclusion rate of the Eltrombo...

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Abstract

The invention provides an Eltrombopag inclusion compound and preparations and a preparation method thereof. The Eltrombopag inclusion compound contains: Eltrombopag or a pharmaceutically acceptable salt thereof and an inclusion material, and the inclusion material is cyclodextrin or a derivative thereof. The inclusion compound provided by the invention can reduce the contact between polyvalent metal ions and Eltrombopag, thus reduce the formation of chelate, and increase medicine solubility. The preparations prepared from the inclusion compound and other pharmaceutically acceptable excipientswhich are provided by the invention can all increase the speed of drug dissolution, are favorable for the absorption of Eltrombopag drugs, increase the flexibility and compliance of medication by patients, and can also prevent a decrease in therapeutic effect or even ineffectiveness as the result of improper medication, thus ensuring the normal exertion of efficacy. In addition, the preparation method of the Eltrombopag inclusion compound provided by the invention has the advantages of high inclusion rate, low production cost, simple process and suitability for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular, the invention relates to an inclusion compound of Eltrombopag and its preparation and preparation method. Background technique [0002] Eltrombopag is used for the treatment of thrombocytopenia in patients with chronic idiopathic thrombocytopenic purpura (ITP) after glucocorticoids, immunoglobulin therapy or splenectomy, and in patients with chronic hepatitis C Symptoms such as hypopenias and severe aplastic anemia that do not respond adequately to immunosuppressive therapy. [0003] Eltrombopag is taken once a day, and it must be taken orally on an empty stomach, that is, it must be taken 1 hour before or 2 hours after meals, and it must not be taken before or after 4 hours of taking the medicine containing polyvalent metal ions (such as: Iron ions, calcium ions, zinc ions, magnesium ions), such as antacids, calcium ion-rich products, and mineral supplements. Therefore...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/4152A61P7/06A61P7/00A61P7/04
CPCA61K31/4152Y02A50/30
Inventor 石添香黄心游劲松黄芳芳邢斌涛
Owner SUNSHINE LAKE PHARM CO LTD
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