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Novel high-purity silybin meglumine medicine preparation as well as preparation method and application thereof

A technology of silibinin and pharmaceutical preparations, which is applied in the field of pharmaceutical preparation technology and pharmacology, can solve the problems of low bioavailability, low absolute value, low stability, etc., and achieve high bioavailability, short half-life, and fast absorption Effect

Pending Publication Date: 2022-06-03
NANJING CHENXIANG MEDICAL RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of its low water solubility, low stability and high heat sensitivity, the bioavailability is extremely low, the bioavailability of silibinin is only 0.73%, and the bioavailability of silibinin meglumine is about 2.5% %, although the latter is 3.4 times that of the former, its absolute value is still very low and needs to be improved

Method used

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  • Novel high-purity silybin meglumine medicine preparation as well as preparation method and application thereof
  • Novel high-purity silybin meglumine medicine preparation as well as preparation method and application thereof
  • Novel high-purity silybin meglumine medicine preparation as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1 Preparation of silybin meglumine sustained-release pellet capsules

[0115] Prescription specification: silybin meglumine 150.0mg / capsule, composed of:

[0116] (1) Prescription of sustained-release pellet core:

[0117]

[0118]

[0119] (2) Prescription of sustained-release coating liquid

[0120]

[0121] (3) Process

[0122] ①, raw materials pretreatment

[0123] The raw and auxiliary materials were respectively passed through 80 mesh sieves, and the prescription amount was weighed for use;

[0124] Dissolve PVPk30 with 60% ethanol to prepare a 5wt.% PVPK30 ethanol solution;

[0125] Take the slow-release 12h coating material (ethyl cellulose, dibutyl sebacate, PVPk30 and 60% ethanol) and add an appropriate amount of purified water to make a 12 wt.% suspension to fully swell;

[0126] ②, mixing and making soft materials

[0127] Weigh silibinin meglumine, microcrystalline cellulose, sucrose, and sodium chloride according to the prescripti...

Embodiment 2

[0143] Preparation of silibinin meglumine for injection

[0144] prescription:

[0145]

[0146]

[0147] Preparation:

[0148] 1. Preparation Take PVPc12, add 900ml of freshly prepared water for injection at 10-15°C and stir to dissolve, add high-purity silibinin meglumine and stir to dissolve, add freshly prepared water for injection at 10-15°C to 1000ml, and use 0.2μm cross-flow fine filtration, first circularly filtered for 3min and then filtered to collect the filtrate.

[0149] 2. Dispense it into 7ml borosilicate bottles, 1.0ml (25mg) per bottle, and suspend the stopper.

[0150] 3. Freeze-drying Immediately place the vials in a freeze dryer that has been pre-cooled to -50°C, freeze for 2 hours, start drying for 20 hours, then rise to 25°C for 2 hours, heat up to 35°C for 2 hours, and press the stopper.

[0151] 4. Packing with lids Take out the freeze-dried products with pressed plugs, tie aluminum-plastic composite lids, label, pack, and store them.

[0152]...

Embodiment 3

[0155] Pharmacodynamic study on the prevention and treatment of acute liver failure with silybin meglumine (SM) for injection (iv)

[0156] experimental method:

[0157] (1) Experimental animals

[0158] The experimental animals were C57BL / 6J male mice, weighing 22-25 g, 8 weeks old, SPF grade, purchased from the Comparative Medical Center of Yangzhou University, which met the quality standards of ordinary experimental animals. License number SYXK (Su) 2018-0019. Mice were reared in separate cages, with free access to water and food, at room temperature of 23 to 25°C and relative humidity of 40 to 80%.

[0159] (2) Animal grouping and drug intervention

[0160] The C57BL / 6J mice were randomly divided into 6 groups, namely blank group, model group, SM 1.25 mg / kg, SM 2.5 mg / kg, SM 5 mg / kg, acetylcysteine ​​injection group (NAC group 1.04 mg / kg). g / kg). The acute liver failure model was induced in mice by intraperitoneal injection of D-GalN (500mg / kg) combined with 10LPS (μg...

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Abstract

The invention provides a silybin meglumine pharmaceutical preparation and a preparation method and application thereof, and belongs to the field of pharmaceutical preparation technologies and pharmacology, the silybin meglumine pharmaceutical preparation comprises silybin, meglumine and auxiliary materials, the purity of the silybin is 99%-100%, and the silybin meglumine pharmaceutical preparation is a silybin meglumine pharmaceutical preparation. The auxiliary material is prepared from polyvinylpyrrolidone. According to the silybin meglumine pharmaceutical preparation provided by the invention, the silybin raw material with high purity (the purity is greater than or equal to 99%) is adopted, the pharmaceutical preparation is prepared from the silybin, the meglumine and the auxiliary material polyvinylpyrrolidone, the polyvinylpyrrolidone has dual effects of helping dissolution and promoting absorption, and the prepared pharmaceutical preparation is high in bioavailability and good in curative effect; in particular to a silybin meglumine injection preparation, which is applied to prevention and treatment of acute, dangerous and severe hepatic failure and hepatic encephalopathy (hepatic coma), fills the blank of medicines for clinical prevention and treatment of hepatic failure and hepatic encephalopathy, and brings good news to patients with acute, dangerous and severe hepatic diseases.

Description

[0001] The present invention is an application document for which the application date is March 31, 2021, the application number is 202110369625.5, and the invention name is "a pharmaceutical preparation of silibinin meglumine and its preparation method and application". technical field [0002] The invention belongs to the field of pharmaceutical preparation technology and pharmacology, and in particular relates to a silibinin meglumine pharmaceutical preparation and a preparation method and application thereof. Background technique [0003] With the vigorous and rapid development of the social economy, people's living standards have been greatly improved, and people's lifestyles have undergone great changes. The incidence of liver disease is increasing year by year, ranking first among the three major fatal diseases. Liver disease has the characteristics of high morbidity, high prevalence, high mortality, high disability rate, high recurrence rate, and many complications. ...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K47/32A61K9/20A61K9/52A61K31/357A61P1/16
CPCA61K9/0019A61K9/08A61K47/32A61K9/5026A61K9/28A61K9/2027A61K31/357A61P1/16Y02A50/30
Inventor 邢为藩
Owner NANJING CHENXIANG MEDICAL RES
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