Anhydroicaritin pharmaceutical composition and preparation method thereof

The technology of icariin and composition is applied in the directions of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. Low bioavailability and other problems, to achieve the effect of increasing dissolution and stability, continuous operation reproducibility, and simple preparation process

Active Publication Date: 2020-12-04
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, icariin has poor solubility, the solubility in water is less than 1 μg / ml, and it is insoluble or almost insoluble in different pH buffers, resulting in poor oral absorption and low bioavailability, which limits its efficacy. No related preparations listed
[0005] CN101485630B discloses a kind of icariin liposome, which contains soybean lecithin and cholesterol. Although the low bioavailability of icariin is improved, the yield is low and it is not easy to scale up production
Although the problem of low bioavailability of icarigenin has been improved, a large amount of surfactants added will cause greater toxic and side effects to the human body
[0007] CN101637467A discloses an icariin or cyclic icariin phospholipid complex, which greatly improves the solubility of icariin, but there are safety hazards such as lysophospholipid and phospholipid oxidation
[0008] A kind of icariin capsule is reported in the literature of "Pharmaceutical Research of Icarigenin Capsule", which lists icariin and carrier polymer (P188, PEG4000, HP-p-CD, PEG6000, PVP K30, PVP K90, Co-PVP and SOLUPLUS)) prepared solid dispersions by melting method and solvent method respectively, and determined that the solid dispersion of icariin and P188 prepared by melting-solvent method was the best by single factor investigation. Prescription technology significantly improves the dissolution rate of icariin in vitro, but organic solvents are used in the preparation process, and the rotary evaporation process is not easy for industrial scale-up production
[0009] To sum up, the preparation of icariin preparations in the prior art has defects such as low bioavailability, use of a large amount of surfactants and organic solvents in the preparation process, causing relatively large toxic and side effects on the human body, and difficult to scale up production. Therefore, it is necessary to A pharmaceutical composition of icarigenin is provided to improve the above deficiencies

Method used

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  • Anhydroicaritin pharmaceutical composition and preparation method thereof
  • Anhydroicaritin pharmaceutical composition and preparation method thereof
  • Anhydroicaritin pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] (1) Preparation of solid dispersion

[0032] Party:

[0033]

[0034] Preparation Process:

[0035] (1) Mix the icariin, PEG6000 and triethyl citrate in the prescription amount to make a physical mixture A;

[0036] (2) mix the copovidone of formula quantity and physical mixture A uniformly, make physical mixture B;

[0037] (3) Set the extrusion temperature of the twin-screw hot-melt extruder to 120°C. When the preset temperature is reached, add the physical mixture B in step (2) into the extruder for melting-dissolving- Mix, start the screw after the melting is complete, and extrude strips through the screw.

[0038] (2) Preparation of icarigenin tablet

[0039] Party:

[0040]

[0041] Preparation Process:

[0042] Weigh the icariin solid dispersion prepared in the above (1) and mix with lactose monohydrate, microcrystalline cellulose, sodium carboxymethyl starch and magnesium stearate, and directly compress the powder to obtain Icarigenin Tablets.

Embodiment 2

[0044] (1) Preparation of solid dispersion

[0045] Party:

[0046]

[0047] Preparation Process:

[0048] (1) Mix the icariin, PEG4000 and triethyl citrate in the prescription amount to make a physical mixture A;

[0049] (2) mix the copovidone of formula quantity and physical mixture A uniformly, make physical mixture B;

[0050] (3) Set the extrusion temperature of the twin-screw hot-melt extruder to 100°C. When the preset temperature is reached, add the physical mixture B in step (2) into the extruder for melting-dissolving- Mix, start the screw after the melting is complete, and extrude strips through the screw.

[0051] (2) Preparation of Icarigenin Capsules

[0052] Party:

[0053]

[0054] Preparation Process:

[0055] Weigh the icariin solid dispersion prepared in the above (1) of the recipe, mix with lactose monohydrate, sodium carboxymethyl starch and talcum powder, and mix the powder into capsules to obtain icarigenin capsules .

Embodiment 3

[0057] (1) Preparation of solid dispersion

[0058] Party:

[0059]

[0060] Preparation Process:

[0061](1) Mix the icariin, PEG5000 and triethyl citrate in the prescription amount to make a physical mixture A;

[0062] (2) mix the copovidone of formula quantity and physical mixture A uniformly, make physical mixture B;

[0063] (3) Set the extrusion temperature of the twin-screw hot-melt extruder to 110°C. When the preset temperature is reached, add the physical mixture B in step (2) into the extruder for melting-dissolving- Mix, start the screw after the melting is complete, and extrude strips through the screw.

[0064] (2) Preparation of icarigenin tablet

[0065] Party:

[0066]

[0067] Preparation Process:

[0068] Weigh the icariin solid dispersion prepared in the above (1) of the recipe, mix with microcrystalline cellulose, croscarmellose sodium and micropowder silica gel, and directly compress the powder to obtain Epimedium Aglycone Tablets.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to an anhydroicaritin pharmaceutical composition and a preparation method thereof. The preparationmethod of the anhydroicaritin pharmaceutical composition comprises the following steps of: firstly, preparing an anhydroicaritin solid dispersion from anhydroicaritin, copovidone (PVP/VA), polyethylene glycol and triethyl citrate by adopting a hot-melt extrusion technology, and then uniformly mixing the anhydroicaritin solid dispersion with pharmaceutically acceptable auxiliary materials to prepare a preparation. According to the anhydroicaritin pharmaceutical composition prepared by the method, the solubility and the in-vitro dissolution rate of the anhydroicaritin are improved; and in addition, the anhydroicaritin pharmaceutical composition prepared by the method is stable in process, controllable in quality and convenient for industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an icarigenin pharmaceutical composition and a preparation method thereof. Background technique [0002] Icari agenin is a polyhydroxy flavonoid monomer component in Epimedium genus Epimedium of Berberidaceae. Its chemical structural formula is as follows: [0003] [0004] Pharmacological studies have shown that the anti-osteoporosis effect of icariin is stronger than that of other flavonoid glycosides in Epimedium. It can promote the activity of osteoblasts and inhibit the activity of osteoclasts in vitro, and has a good application prospect. However, icariin has poor solubility, the solubility in water is less than 1 μg / ml, and it is insoluble or almost insoluble in different pH buffers, resulting in poor oral absorption and low bioavailability, which limits its efficacy. There are no related preparations listed. [0005] CN101485630B disc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/10A61K47/32A61K47/14A61K31/352
CPCA61K9/146A61K9/145A61K31/352
Inventor 李倩刘德鹏
Owner LUNAN PHARMA GROUP CORPORATION
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