Tropisetron hydrochloride liposome injection

A technology for tropisetron hydrochloride and tropane hydrochloride, applied in the field of medicine, can solve the problems of easy separation by hydrolysis, low bioavailability, influence on drug quality, etc., and achieves improved bioavailability, simple preparation method, and increased retention time Effect

Inactive Publication Date: 2012-01-25
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Patent document CN1682721A discloses a kind of tropisetron hydrochloride orally disintegrating tablet and its preparation method, with lactose, mannitol, crospovidone, magnesium stearate, microcrystalline cellulose, distilled water, stevioside as auxiliary materials, Prepared by wet granulation tableting method, but the traditional tablet has poor stability and low bioavailability
[0006] Patent document CN1666747A discloses a fructose injection of an antineoplastic drug, which is composed of an antineoplastic drug, fructose, and water as an appropriate additive. However, tropisetron hydrochloride is unstable in an aqueous solution and is easily separated by hydrolysis, resulting in insoluble visible foreign matter , affecting the quality of medicines and reducing the curative effect
[0007] Patent literature CN101278921A discloses a tropisetron hydrochloride microcapsule and its freeze-dried preparation, which contains tropisetron hydrochloride, gelatin, dextran, lipophilic emulsifier, hydrophilic emulsifier and freeze-dried support agent. The microcapsule shell is easy to oxidize and the stability is not high
[0008] Patent document CN101732252A discloses a suspension injection of tropisetron hydrochloride, which is characterized in that it is made of the following components by weight: 1 part of tropisetron hydrochloride, 2.5-15 parts of surfactant, 0.1-15 parts of antioxidant 5 parts, 5-40 parts of additives, wherein the surfactant is composed of sodium deoxycholate and povidone, but the drug will cause agglomeration during long-term storage, and it is not easy to redisperse

Method used

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  • Tropisetron hydrochloride liposome injection
  • Tropisetron hydrochloride liposome injection
  • Tropisetron hydrochloride liposome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Cefadroxil liposome injection

[0033] Prescription (1000 bottles):

[0034]

[0035] Preparation Process:

[0036] (1) Accurately weigh 2g Tropisetron Hydrochloride, 140g Sodium Taurocholate, 70g Cholesterol and 40g Gelatin and be dissolved in 500ml volume ratio is 3: 1 in the mixed solvent of n-butanol and chloroform, stirring and dissolving;

[0037] (2) 600ml of a phosphate buffer solution with a pH of 6.0 dissolved in 2g of ascorbic acid and 100g of trehalose was dissolved in the above solution, and short-term ultrasonic was performed until a stable W / O emulsifier was formed;

[0038] (3) The above-mentioned emulsifier is evaporated under reduced pressure to remove the organic solvent. After reaching the colloidal state, add 700ml PH of 6.0 phosphate buffer solution, rotate and vibrate until the gel on the wall of the device comes off, and continue to evaporate under pressurized conditions. Prepare an aqueous suspension, and then sonicate for a short...

Embodiment 2

[0040] Embodiment 2 cefadroxil liposome injection

[0041] Prescription (1000 bottles):

[0042]

[0043] Preparation Process:

[0044] (1) Accurately weigh 2g tropisetron hydrochloride, 120g sodium taurocholate, 40g cholesterol and 20g gelatin and dissolve in 500ml volume ratio of n-butanol and chloroform mixed solvent of 3: 1, stirring and dissolving;

[0045] (2) Dissolve 1220ml of phosphate buffer solution with 2g ascorbic acid and 120g trehalose at a pH of 6.0 into the above solution, and perform short-time ultrasonication until a stable W / O emulsifier is formed;

[0046] (3) The above-mentioned emulsifier is evaporated under reduced pressure to remove the organic solvent. After reaching the colloidal state, add 1000ml PH of 6.0 phosphate buffer solution, rotate and vibrate until the gel on the wall of the device comes off, and continue to evaporate under pressurized conditions. Prepare an aqueous suspension, and then sonicate for a short time;

[0047] (4) Centrifu...

Embodiment 3

[0048] Example 3 Preparation of Comparative Examples 1-5

[0049] The components other than the preferred components of the present invention and the combinations other than the preferred content ratio of the components of the present invention were respectively selected to carry out comparative experiments, and the preparation process was the same as that of Example 1, so as to obtain Comparative Examples 1-3. Each comparative example component is shown in the table below:

[0050]

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PUM

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Abstract

The invention provides a tropisetron hydrochloride liposome injection. The tropisetron hydrochloride liposome injection is mainly prepared from tropisetron hydrochloride, glycocholatesodium, cholesterol, gelatin, antioxygen and additive. The liposome injection improves the quality of preparation products, reduces toxic and side effects, improves bioavailability, and is high in preparation stability; and liposome is not broken due to dehydration, fusion, crystallization and the like during freeze-drying, and the liposome still keeps a good entrapment rate after the liposome is subjected to hydration and dissolution.

Description

technical field [0001] The invention relates to a new preparation of tropisetron hydrochloride, in particular to a tropisetron hydrochloride liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Tropisetron hydrochloride, the chemical name is 3-indolecarboxylic acid (8-methyl-8-azabicyclo[3.2.1]-3α-octyl) ester hydrochloride, molecular formula C 17 h 20 N 2 o 2 .HCl, molecular weight 320.82, structural formula: [0003] [0004] Tropisetron hydrochloride is a highly efficient and highly selective competitive antagonist of peripheral neurons and central nervous system 5-hydroxytryptamine 3 (5-HT3) receptors. Certain substances, including some chemotherapeutic drugs, can stimulate the chromaffin-like cells of the visceral mucosa to release 5-hydroxytryptamine (5-HT), thereby inducing the vomiting reflex with nausea, and tropisetron hydrochloride can selectively block the reflex in the peripheral ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/46A61P1/08
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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