Huperzine-A solid dispersion and method for preparing tablet thereof

A technology of solid dispersion and huperzine A, which is applied in the field of medicine, can solve the problems of difficult industrial production, complicated preparation by melting method, and low bioavailability, so as to improve the dissolution rate and bioavailability, and the preparation process is simple and easy , play a therapeutic effect

Inactive Publication Date: 2010-04-28
HENAN TALOPH PHARMACEUTICAL STOCK CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, huperzine A is mainly administered in the form of oral tablets and capsules, but because huperzine A is insoluble in water, its bioavailability is low
[0008] Generally, the preparation methods of solid dispersions are divided into melting method, solvent method, melting-solvent method, etc., but the preparation of the melting method is more complicated and industrial production is more difficult, and the usual solvent method contains organic solvents, which are not easy to remove completely.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] First take by weight ratio:

[0025] Huperzine A 100mg

[0026] Lactose 40g

[0027] Polyvinylpyrrolidone 50mg

[0028] Dextrin 30g

[0029] Starch 65g

[0030] Magnesium Stearate 140mg

[0031] Sodium carboxymethyl starch 680mg

[0032] 40ml solution containing ethanol 50% (ml / ml)

[0033]

[0034] Makes 1000 pieces

[0035] The specific preparation method is as follows:

[0036] a. After uniformly mixing huperzine A, polyvinylpyrrolidone and 50 mg of lactose, place it in a grinder and grind for about 45 minutes to obtain huperzine A solid dispersion powder with a particle size of 40 μm or less.

[0037] b. Add the remaining lactose, dextrin and starch and mix evenly, make a soft material with 50% ethanol aqueous solution, pass through a 20-mesh sieve to granulate, and dry at 50-60°C.

[0038] c. Add sodium carboxymethyl starch and magnesium stearate to the dried granules, sieve the granules with 18 mesh, and press into tablets ...

Embodiment 2

[0040] First take by weight ratio:

[0041] Huperzine A 100mg

[0042] Macrogol 4000 1g

[0043] Mannitol 20g

[0044] Dextrin 40g

[0045] Starch 65.5g

[0046] Calcium Stearate 280mg

[0047] Sodium carboxymethyl starch 5g (ratio of internal and external: 2:1)

[0048] 10% starch slurry 40ml

[0049]

[0050] Makes 1000 pieces

[0051] The specific preparation method is as follows:

[0052] a. After mixing huperzine A with polyethylene glycol 4000 and 500 mg mannitol evenly, place it in a grinder and grind for about 30 minutes to obtain huperzine A solid dispersion powder with a particle size below 40 μm;

[0053] b. Add remaining mannitol, dextrin, starch, sodium carboxymethyl starch and mix evenly, make soft material with starch slurry, granulate through 20-mesh sieve, and dry at 50-60°C;

[0054] c. Add sodium carboxymethyl starch and calcium stearate to the dried granules, sieve the granules with 18 meshes, and press into tablets (pressu...

Embodiment 3

[0056] First take by weight ratio:

[0057] Huperzine A 100mg

[0058] Polyethylene glycol 6000 1g

[0059] Microcrystalline Cellulose 7g

[0060] Sorbitol 20g

[0061] Starch 66g

[0062] Lactose 30g

[0063] Talc powder 300mg

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Abstract

The invention discloses a huperzine-A solid dispersion and a method for preparing a tablet thereof. The huperzine-A solid dispersion comprises huperzine-A and a carrier used as a dispersant; the weight ratio range of the carrier to the huperzine-A is 1-25:1; the carrier material may be one or more of polyvinylpyrrolidone, polyethylene glycol 4000, polyethylene glycol 6000, Poloxamer 188, mannitol, lactose or microcrystalline cellulose; and the huperzine-A solid dispersion is prepared by adopting a grinding method, and the obtained solid dispersion can be prepared into huperzine-A tablets by adopting a wet granulating and tabletting method. The huperzine-A solid dispersion can remarkably increase the solubility of a medicament and promote the absorption so as to greatly improve the dissolution and bioavailability of the medicament.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a huperzine A solid dispersion capable of improving the dissolution rate and bioavailability of medicines and a method for preparing tablets thereof. Background technique [0002] Huperzine A chemical name: (5R,9R,11E)-5-amino-11-ethylene-5,8,9,10-tetrahydro-7-methyl-5,9-methylenecyclooctyl Tetraeno[b]pyridin-2(1H)-ones. [0003] Molecular formula: C 15 h 18 N 2 O molecular weight: 242.32 [0004] Huperzine A Tablet is suitable for benign memory disorders, improving the ability of patients to point to memory, associative learning, image recall, meaningless graphic recognition and portrait recall. It can also improve memory impairment caused by dementia patients and brain organic diseases. [0005] Pharmacology and Toxicology: Huperzine A Tablet is a cholinesterase inhibitor, which has a selective inhibitory effect on true ChE and can easily pass through the blood-brain ba...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K31/4748A61P25/28
Inventor 郭中华邢文清张志平
Owner HENAN TALOPH PHARMACEUTICAL STOCK CO LTD
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