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Method for preparing cyclodextrin inclusion compound of silybum mariamum extract and medicinal formulation thereof

A cyclodextrin inclusion complex and cyclodextrin technology are applied in the directions of drug combination, drug delivery, inactive components of polymer compounds, etc., and can solve the problems of high cost, affecting human absorption, and low oral bioavailability, etc. The effect of low cost and simple preparation process

Inactive Publication Date: 2005-03-16
邢为藩
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Since silibinin is insoluble in water, the oral bioavailability is low, and it is difficult to prepare injections, so try to increase its solubility to improve its oral bioavailability or prepare injections
The current commercially available preparation of silibinin is silybin meglumine tablet, which is prepared by salting silibinin and meglumine into water-soluble derivatives to increase its water solubility, in order to increase the body's absorption; but water When silybin meglumine encounters gastric juice, it will be quickly decomposed into silybin and precipitated, which will affect the absorption of the human body, so the human bioavailability of silybin meglumine is still very low
[0004] CN1391894 discloses that milk thistle extract is prepared into β-cyclodextrin or its derivative clathrate to increase drug solubility and prepare injection preparations, which enriches the preparation varieties of this type of drug; however, due to its preparation cycle Due to the limitation of dextrin inclusion compound technology, it can only be prepared into liquid preparations, and then freeze-drying technology is used, which is costly and not conducive to industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Inclusion complex of silybin and cyclodextrin and preparation method thereof

[0016] Precisely weigh silibinin and hydroxypropyl-β-cyclodextrin according to the prescription listed in Table 1, dissolve with an appropriate amount of absolute ethanol, and remove the organic solvent under reduced pressure to obtain a silibinin cyclodextrin inclusion complex.

[0017] Table 1 The formulation composition of silybin-cyclodextrin inclusion complex

[0018] Ingredient Weight (g)

[0019] Silybin 350

[0020] Hydroxypropyl-β-cyclodextrin 1400

Embodiment 2

[0022] Silibinin inclusion compound hard capsule and preparation method thereof

[0023] Weigh the recipe quantities of silibinin and hydroxypropyl-β-cyclodextrin according to the mass percentages listed in Table 2, and obtain the hydroxypropyl-β-cyclodextrin inclusion complex of silibinin as in Example 1, and then Add appropriate amount of starch to make soft material, pass through a 14-mesh sieve to granulate, dry at 80°C, pass through a 16-mesh sieve to granulate, canned in hard capsules, wiped, fully inspected, packaged, and packaged.

[0024] Table 2 The formulation composition of silibinin inclusion complex hard capsules

[0025] Ingredient Weight (g)

[0026] Silybin 350

[0027] Hydroxypropyl-β-cyclodextrin 1400

[0028] Starch 350

[0029] Pregelatinized starch slurry Q.S.

[0030] Magnesium Stearate Q.S.

Embodiment 3

[0032] Silibinin inclusion compound tablet and preparation method thereof

[0033] According to the mass percentage listed in Table 3, take by weighing the recipe amounts of silibinin and hydroxypropyl-β-cyclodextrin, and obtain silibinin hydroxypropyl-β-cyclodextrin inclusion complex as in Example 1 , add an appropriate amount of microcrystalline cellulose and lactose, mix to make a soft material, pass through a 14-mesh sieve for granulation, dry at 80°C, pass through a 16-mesh sieve to granulate, add an appropriate amount of magnesium stearate and press into tablets.

[0034] Table 3 The formula composition of silibinin inclusion tablets

[0035] Ingredient Weight (g)

[0036] Silybin 350

[0037] Hydroxypropyl-β-cyclodextrin 1400

[0038] Microcrystalline Cellulose 600

[0039] Lactose 600

[0040] Magnesium Stearate Q.S.

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Abstract

The invention belongs to the field of pharmaceutical preparation, in particular a method for preparing cyclodextrin inclusion compound of silybum mariamum extract and medicinal formulation thereof, wherein a dissolvent method is employed to prepare beta-cyclodextrin or its derivative inclusion compound from the Silybum marianum extract, the organic solvent is removed through depression. The advantages of the method include simple process for manufacturing, low cost of manufacture, and fitting for mass production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a new preparation method of a cyclodextrin inclusion complex of milk thistle extract and a pharmaceutical preparation thereof. Background technique [0002] Silibinin is a lignin flavonoid extracted and isolated from the fruit of the genus Silybum marianum (Silybum marianum Gaertin.) of the Compositae family. Pharmacological and toxicological studies have shown that silibinin has obvious protective and stabilizing effects on liver cell membranes, and can promote liver cell regeneration. Clinically, silibinin is mainly used for the treatment of various acute and chronic hepatitis, initial liver cirrhosis and liver poisoning. It is one of the main therapeutic drugs for chronic persistent hepatitis and liver cirrhosis currently on the market. [0003] Since silibinin is insoluble in water, its oral bioavailability is low, and it is difficult to prepare an injection, so tr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/22A61K9/48A61K9/52A61K31/357A61K47/40
Inventor 邢为藩龚明涛
Owner 邢为藩
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