Preparation containing bendopa methyl ester and preparation method thereof

A technology of levodopa methyl ester and preparation, which is applied in the field of prescription and preparation of levodopa methyl ester solid dispersion, and can solve problems such as high drug concentration, fluctuation of blood drug concentration, and gastrointestinal irritation

Active Publication Date: 2008-10-15
NANJING CHANGAO PHARMA SCI & TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the release of common preparations in the gastrointestinal tract will lead to excessive local drug concentration, the irritation to the gastrointestinal tract is particularly obvious
At the same time, due to the irregular drug release of common preparations, the blood drug concentration in the body fluctuates rapidly after drug absorption, which is one of the reasons for the fluctuation of these clinical symptoms. directly related to concentration

Method used

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  • Preparation containing bendopa methyl ester and preparation method thereof
  • Preparation containing bendopa methyl ester and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Levodopa methyl ester 1

[0029] PEG6000 10

[0030] Lactose 0.2

[0031] Magnesium stearate 0.2

[0032]

[0033] Take 1 part by weight of levodopa methyl ester, 10 parts by weight of PEG6000, and 0.2 part by weight of lactose, first pass PEG6000 through a 65-mesh sieve, heat to melt, and then gradually add levodopa methyl ester (passed 100-mesh sieve) and lactose (passed through a 100-mesh sieve), stir vigorously until completely melted, and set to cool to solidify. After curing, put it in a vacuum drying oven, take it out after embrittlement, pulverize it, and pass through an 80-mesh sieve to obtain a solid dispersion of levodopa methyl ester. Get this solid dispersion and magnesium stearate, mix uniformly, pack into capsules, and make capsules.

Embodiment 2

[0035] Levodopa methyl ester 1

[0036] PEG4000 2

[0037] Lactose 0.1

[0038] Microcrystalline Cellulose 2

[0039] starch 3

[0040] Sodium carboxymethyl starch 1

[0041] Magnesium stearate 0.06

[0042]

[0043] Take 1 part by weight of levodopa methyl ester, 2 parts by weight of PEG4000, and 0.1 part by weight of lactose, first pass PEG4000 through a 65 sieve, heat to melt, and then gradually add levodopa methyl ester in small amounts (over 100 mesh sieve) and lactose (passed through a 100 mesh sieve), stir vigorously until completely melted, and set to cool to solidify. After curing, put it in a vacuum drying oven, take it out after embrittlement, pulverize it, and pass through an 80-mesh sieve to obtain a solid dispersion of levodopa methyl ester. Get this solid dispersion and mix homogeneously with microcrystalline cellulose, starch, carboxymethyl starch sodium, with 5% povidone K 30 Granulated, dried, mixed evenly with magnesium ste...

Embodiment 3

[0045] Levodopa methyl ester 1

[0046] Poloxamer 188 6

[0047] Lactose 0.3

[0048] Sucrose 1

[0049] Magnesium stearate 0.15

[0050]

[0051] Get 1 part by weight of levodopa methyl ester, 6 parts by weight of Poloxamer (Poloxamer) 188, and 0.3 part by weight of lactose, first pass Poloxamer (Poloxamer) 188 through a 65-mesh sieve, heat to melt, and then Gradually add levodopa methyl ester (passed through a 100-mesh sieve) and lactose (passed through a 100-mesh sieve) in small amounts and several times, stir vigorously until completely melted, and set to cool to solidify. After curing, put it in a vacuum drying oven, take it out after embrittlement, pulverize it, and pass through an 80-mesh sieve to obtain a solid dispersion of levodopa methyl ester. Get this solid dispersion and mix evenly with 1 part by weight of sucrose, add 5% povidone K 30 Granulate, dry, and mix evenly with magnesium stearate to prepare granules.

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Abstract

The invention discloses a preparation containing L-dopa methyl ester and a preparation method thereof. The preparation method comprises the following steps of: adding L-dopa methyl ester into a melted carrier material such as polyethylene glycol (PEG), poloxamer 188 or hydroxypropyl cellulose (HPC), stirring at high speed to uniformly disperse drug particulates into the carrier material, making into solid dispersion, and further making into capsule, tablet or granule containing 50-500mg L-dopa methyl ester, as required. The preparation increases the dispersion degree of L-dopa methyl ester and reduces the local gastrointestinal concentration thereof, so as to reduce the side effects thereof; and at the same time, the absorption of L-dopa methyl ester is improved, so that the in vivo pharmacokinetic curve is more stable. The L-dopa methyl ester solid dispersion is a new preparation for treating Parkinson's disease.

Description

technical field [0001] The invention relates to a solid dispersion preparation containing levodopa methyl ester. Compared with common preparations, it can quickly disperse in the gastrointestinal tract, reduce the stimulation to the gastrointestinal tract, and increase the absorption of the drug in the gastrointestinal tract. The invention also relates to the prescription and preparation method of the levodopa methyl ester solid dispersion. Background technique [0002] Levodopa methyl ester hydrochloride is a dopamine-like drug, which is clinically used to treat Parkinson's disease (Parkinson's Disease, PD). It has the same pharmacological effect as levodopa, and it is used to control the involuntary muscle movement of patients by cooperating with peripheral dopa decarboxylase inhibitors (IPDD). After the product is hydrolyzed into levodopa in the body, it enters the central system through the blood-brain barrier, and is transformed into dopamine by dopa decarboxylase to e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/325A61P25/16
Inventor 张自强许枚李战
Owner NANJING CHANGAO PHARMA SCI & TECH CO LTD
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