A kind of lorcaserin hydrochloride pellets, its preparation method and its preparation

A technology of lorcaserin hydrochloride and lorcaserin hydrochloride, which is applied in the directions of pill delivery, pharmaceutical formulations, and medical preparations with non-active ingredients, etc., can solve problems such as unfavorable health of patients and large fluctuation of drug concentration peaks and valleys.

Active Publication Date: 2020-05-05
珠海万钜生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] From the physical and chemical properties of lorcaserin hydrochloride raw materials, its half-lives in plasma and brain are 4.9 and 4.7 hours respectively. (trade name Belviq, specification is 10mg) needs to be taken twice a day, one tablet each time, which makes the peak and valley fluctuations of the drug concentration in the patient's blood larger, which is not conducive to the patient's health

Method used

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  • A kind of lorcaserin hydrochloride pellets, its preparation method and its preparation
  • A kind of lorcaserin hydrochloride pellets, its preparation method and its preparation
  • A kind of lorcaserin hydrochloride pellets, its preparation method and its preparation

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preparation example Construction

[0060] The present invention also provides a preparation method of lorcaserin hydrochloride pellets, comprising the following steps:

[0061] mixing lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropyl cellulose, and talcum powder with a first solvent to obtain a drug-loaded layer solution, and the first solvent includes water and ethanol;

[0062] Mixing ethyl cellulose, highly substituted hydroxypropyl cellulose, talcum powder, and triethyl citrate with a second solvent to obtain a sustained-release layer solution, the second solvent including ethanol;

[0063] mixing lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropyl cellulose, and talc with a third solvent to obtain an immediate-release layer solution, the third solvent including water and ethanol;

[0064] The drug-loading layer solution, the slow-release layer solution and the quick-release layer solution are coated on the blank pill cores in sequence by a drug-on-s...

Embodiment 1

[0084] The preparation of embodiment 1 lorcaserin hydrochloride

[0085] Add 1.5L of methanol and 150g of isopropanolamine into a 5L reaction vessel, stir evenly, add 307.7g of p-chlorophenylacetic acid, heat to 50°C, keep warm for 6 hours, recover the solvent under reduced pressure, add purified water, and control the temperature at 20°C Crystallize, filter, and dry the filter cake to obtain 368.5 g of 2-(4-chlorophenyl)-N-(2-hydroxypropyl)acetamide with a purity of 96.8%.

[0086]After obtaining 2-(4-chlorophenyl)-N-(2-hydroxypropyl)acetamide, 1.5L toluene and 342g2-(4-chlorophenyl)-N-(2-hydroxypropyl)acetamide Mix, stir to dissolve, cool down to 0°C in an ice-water bath, slowly add 150 g of thionyl chloride (halogenation reagent) dropwise, after the dropwise addition, add 15 mL of triethylamine, control the temperature at 15°C, react for 2 hours, recover the solvent, and then add 1.5L 2-Methyltetrahydrofuran, 600mL 1mol / L sodium hydroxide solution, separate the liquid, dry...

Embodiment 2

[0090] The preparation of embodiment 2 lorcaserin hydrochloride pellets

[0091] Take 15.8g of high-substituted hydroxypropyl cellulose and add it to 750g of purified water at 50°C, stir and swell until it becomes clear, and cool to the greenhouse for use; add 63g of lorcaserin hydrochloride and 63g of lactose monohydrate, stir well, and obtain a suspension liquid. Pass the above suspension through an 80-mesh sieve, rinse it with 375g of 95% ethanol, add 375g of 95% ethanol, and stir evenly to obtain a drug-loaded layer solution. Fill 750g of sucrose-starch microspheres into the fluidized bed granulator coating machine, the fan frequency is 30Hz, the air inlet temperature is 60°C, the material temperature is 35°C, the atomizing pressure is 0.18MPa, and the spray pump speed is 6 rpm. Drug operation (coating) until the drug-loaded layer solution is sprayed out. Set the material temperature at 40°C, fluidize and dry the pellets coated with the drug-loaded layer solution for 10 ...

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Abstract

A lorcaserin hydrochloride mini-pill is provided. The mini-pill comprises a blank pill core, a medicine loading layer, a slow-release layer and a quick-release layer in order from inside to outside. The medicine loading layer comprises lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropylcellulose and talcum powder. The slow-release layer comprises ethyl cellulose, highly substituted hydroxypropylcellulose, talcum powder and triethyl citrate. The quick-release layer comprises lorcaserin hydrochloride, lactose monohydrate, highly substituted hydroxypropylcellulose and talcum powder. The mass ratio of the sum of the weight of the blank pill core and the weight of the medicine loading layer to the mass of the slow-release layer is 1:(0.25-0.35). The mini-pill comprises the slow-release layer and the quick-release layer, and therefore a medicine can rapidly work and functions of the medicine in a body are prolonged. A preparing method of the lorcaserin hydrochloride mini-pill and a preparation of the lorcaserin hydrochloride mini-pill are also provided.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a lorcaserin hydrochloride pellet, a preparation method and a preparation thereof. Background technique [0002] On June 27, 2012, the U.S. Food and Drug Administration (FDA) officially approved the listing of Arena Pharmaceuticals' new weight-loss drug lorcaserin hydrochloride (trade name Belvip), becoming the first new weight-loss drug approved for marketing in the United States in 13 years. prescription. The drug is approved for obese or overweight adults with a body mass index (BMI) ≥ 27 and who have at least one weight-related disorder (such as hypertension, type 2 diabetes, or hyperlipidemia). [0003] Lorcaserin hydrochloride is a highly selective 5-HT2C receptor agonist (Smith et al., 2008) synthesized by U.S. Arena Pharmaceuticals (Arena Pharmaceuticals, Inc., San Diego, California, USA). The research data of serin affinity inhibition constant (Ki), potency and eff...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/55A61P3/04A61K47/38A61K47/26A61K47/04A61K47/14A61K9/20A61K9/48
Inventor 谢斌
Owner 珠海万钜生物医药有限公司
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