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Emodin solid dispersion, drug-containing pellet core, colonic targeted micropill, and applications of three

A technology of solid dispersion and emodin, which is applied in the field of pharmacy, can solve the problems of affecting oral drug efficacy and poor solubility of emodin, and achieve the effect of improving bioavailability and significant protective effect

Inactive Publication Date: 2014-02-05
ZHONGSHAN HOSPITAL FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of emodin is poor, the solubility in water is only 1.98μg / mL, and the solubility in artificial colonic fluid is 4.68μg / mL, which greatly affects the oral efficacy.

Method used

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  • Emodin solid dispersion, drug-containing pellet core, colonic targeted micropill, and applications of three
  • Emodin solid dispersion, drug-containing pellet core, colonic targeted micropill, and applications of three
  • Emodin solid dispersion, drug-containing pellet core, colonic targeted micropill, and applications of three

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Preparation of emodin-containing pill core (1)

[0039] Emodin 10g

[0040] Carrier material: Copovidone (Kollidon VA64) 20g

[0041] Diluent: Microcrystalline Cellulose pH101 70g

[0042] Binder: 5% hydroxypropyl cellulose (HPC) 20mL

[0043] According to the above weight, weigh emodin and copovidone (Kollidon VA64), mix them evenly, place them in a hot-melt extrusion equipment, set the temperature at about 160 ℃, screw speed at 30 rpm, melt and extrude, after cooling, pulverize , through a 60-mesh sieve to obtain a solid dispersion of emodin. Mix emodin solid dispersion and microcrystalline cellulose pH101 evenly, then add binder 5% HPC, knead evenly, make soft material, extrude through extruder, sieve into thin strips, cut and spheronize in spheronizer, 50 Dry at ℃ for 3 h to obtain emodin-containing pellets.

Embodiment 2

[0044] Example 2 Preparation of Emodin-containing Pill Core (2)

[0045] Emodin 10g

[0046] Carrier material: Soluplus 30g

[0047] Diluent: microcrystalline cellulose pH101 30g, lactose 30g

[0048] Wetting agent: water 15mL

[0049] According to the above weight, weigh emodin and Soluplus, mix them evenly, place them in a hot-melt extrusion equipment, set the temperature at about 130 ℃, screw speed at 40 rpm, melt and extrude, after cooling, pulverize, pass through a 60-mesh sieve, That is, the emodin solid dispersion is obtained. Mix emodin solid dispersion with microcrystalline cellulose pH 101 and lactose evenly, add appropriate amount of water, knead evenly, make soft material, extrude through extruder and sieve into thin strips, cut and spheronize in spheronizer, dry at 50 ℃ 3 h, the emodin-containing pellets were obtained.

Embodiment 3

[0050] Example 3 Preparation of Emodin-containing Pill Core (3)

[0051] Emodin 10g

[0052] Carrier material: polyethylene glycol / polyvinyl alcohol graft copolymer (Kollicoat IR) 40g

[0053] Diluent: Chitosan 30g

[0054] Wetting agent: 30% ethanol 15mL

[0055] According to the above weight, weigh emodin and polyethylene glycol / polyvinyl alcohol graft copolymer (Kollicoat IR), mix evenly, and place it in a hot-melt extrusion equipment, set the temperature at about 170 °C, and the screw speed at 50 rpm , melted and extruded, cooled, crushed, and passed through a 60-mesh sieve to obtain a solid dispersion of emodin. Mix the emodin solid dispersion and chitosan evenly, add 30% ethanol, knead evenly, make a soft material, extrude through an extruder and sieve into thin strips, cut and spheronize in a spheronizer, dry at 50 °C for 3 h, That is, the drug-containing pellets are obtained.

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Abstract

The invention relates to emodin solid dispersion, a drug-containing pellet core, a colonic targeted micropill, and applications of the three. The emodin solid dispersion is prepared from emodin and a carrier material, wherein the carrier material is one or several selected from poloxamer 188, poloxamer 407, Kollidon 12 PF, Kollidon VA 64, Kollicoat IR or Soluplus, and the weight ratio of emodin to the carrier material is 1:2-1:15. The drug-containing pellet core and the colonic targeted micropill both contain the emodin solid dispersion. The emodin solid dispersion is substantially improved in solubility of indissolvable drug emodin; and the targeted micropill helps to realize colonic positioning release in vivo / vitro of emodin, and has substantial protective effect on intestinal barrier of a rat severe acute pancreatitis pancreatitis model.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to an emodin solid dispersion, colon targeting pellets and a preparation method thereof. Background technique [0002] Acute pancreatitis is a serious disease with serious condition, many complications, high treatment cost and dangerous prognosis. So far, there is no ideal treatment. Severe acute pancreatitis (SAP) is often accompanied by multiple organ failure (MSOF), with a fatality rate of 10% to 30%, while the fatality rate of fulminant pancreatitis can reach 80%. How to prevent and treat MSOF is an important issue that must be solved in the treatment of SAP. Intestinal barrier dysfunction, secondary intestinal flora and endotoxin translocation are important links in triggering systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS) and MSOF. [0003] Traditional Chinese medicine believes that the pathogenesis of pancreatitis is dampness acc...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/28A61K31/122A61K47/34A61K47/32A61P1/18
Inventor 杜施霖童朝阳韩丽妹
Owner ZHONGSHAN HOSPITAL FUDAN UNIV
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