Levomilnacipran hydrochloride sustained release capsule and preparation method thereof

A technology of milnacipran hydrochloride and sustained-release capsules is applied in pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc. Well-tolerated, easy-to-use results

Inactive Publication Date: 2016-07-20
SHANGHAI SUNTECH PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is necessary to solve the problem that milnacipran is affected by the release rate of environmental conditions

Method used

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  • Levomilnacipran hydrochloride sustained release capsule and preparation method thereof
  • Levomilnacipran hydrochloride sustained release capsule and preparation method thereof
  • Levomilnacipran hydrochloride sustained release capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025]

[0026] 459 grams of L-milnacipran hydrochloride are uniformly dispersed in 1836 grams of isopropanol, and the resulting drug-on-dose suspension is sprayed on 247 grams of 30-35 mesh sucrose cores using a fluidized bed GPCG2, and dried to obtain drug-containing Small Maru.

[0027] 141 grams of hypromellose phthalate and 565 grams of ethyl cellulose are dissolved in a mixed solvent of acetone and isopropanol to make a coating solution; use the fluidized bed GPCG2 at a temperature of 26°C The coating liquid is spray-coated on the drug-containing pellets of L-milnacipran hydrochloride, and the weight of the coating is increased by 50%, so as to obtain the coated pellets.

Embodiment 2

[0029]

[0030] 459 grams of L-milnacipran hydrochloride are uniformly dispersed in 1836 grams of isopropanol, and the resulting drug-on-dose suspension is sprayed on 247 grams of 30-35 mesh sucrose cores using a fluidized bed GPCG2, and dried to obtain drug-containing Small Maru.

[0031] Dissolve 578 grams of ethyl cellulose and 386 grams of cellulose acetate in a mixed solvent of acetone and isopropanol to make a coating solution; use the fluidized bed GPCG2 at a temperature of 26 ° C to spray the coating solution Coating on the drug-containing pellets of L-milnacipran hydrochloride, the coating weight increased by 57.7%, to obtain the coated pellets. The coated pellets were filled into capsules, and the release of the preparation at each set time point at 100 rpm in the USP device 1 (small basket) at 37° C. in pH6.8 buffer was as follows: 17% in 2 hours, released in 4 hours 41%, 62% released in 8 hours, 87% released in 12 hours.

Embodiment 3

[0033]

[0034] 459 grams of L-milnacipran hydrochloride are uniformly dispersed in 1836 grams of isopropanol, and the resulting drug-on-dose suspension is sprayed on 247 grams of 30-35 mesh sucrose cores using a fluidized bed GPCG2, and dried to obtain drug-containing Small Maru.

[0035] Dissolve 262 grams of ethyl cellulose and 262 grams of hypromellose phthalate in a mixed solvent of acetone and ethanol to make a coating solution; use the fluidized bed GPCG2 at a temperature of 26 ° C to use the coating solution Spray coating on the drug-containing pellets of L-milnacipran hydrochloride, the coating weight increased by 31.4%, to obtain the coated pellets.

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PUM

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Abstract

The invention provides a levomilnacipran hydrochloride sustained release capsule. The sustained release capsule is prepared from a levomilnacipran hydrochloride drug application pill core and a sustained release coating, wherein the weight ratio of the sustained release coating to the levomilnacipran hydrochloride drug application pill core is at (15-35) to (65-85). According to the method disclosed by the invention, a mixed coating liquid of a pH non-dependent material and a pH dependent material is coated on the core material of levomilnacipran hydrochloride. A pH value in a human body from stomach to small intestine is gradually increased to about 7 from 1.2, and the pH dependent material in a coating membrane provided by the invention is gradually dissolved in the intestine which is higher than 5 in pH value, so that small pores are formed in the membrane; therefore, the permeability of the coating membrane in the intestines is enhanced, and subsequently, the purpose of improving release of drugs in the intestine is achieved. The preparation method disclosed by the invention is simple and convenient, applicable to industrial production and is relatively high in practical value.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a L-milnacipran hydrochloride sustained-release capsule and a preparation method thereof. Background technique [0002] Milnacipran was first developed by the PierreFabre laboratory in France, and it was launched in the United States in 2009 for the treatment of fibromyalgia. In 2013, the U.S. Food and Drug Administration approved levomilnacipran for the treatment of major depressive disorder in adults. This is the fourth serotonin and norepinephrine reuptake inhibitor approved by the FDA for marketing in the United States. Manufactured by Forest Laboratories, the product is in an extended-release dosage form and is taken once a day. According to the guidance of the manufacturer's forest laboratory, the reuptake inhibitory effect of levomilnacipran on norepinephrine in vitro is stronger than the similar effect on serotonin, and the drug does not directly affect the process of pharm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/165A61P21/00A61P29/00A61P25/24
Inventor 钱晓明刘学军陈历胜
Owner SHANGHAI SUNTECH PHARMA
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