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Raloxifene hydrochloride tablet and preparation method thereof

A technology of raloxifene hydrochloride and tablets, which is applied in the field of raloxifene hydrochloride tablets and its preparation, can solve the problems of easy oxidation stability and photodegradation, and achieve good fluidity, good bulkiness, and application promising effect

Active Publication Date: 2021-12-28
澳美制药(苏州)有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of this application is to provide a raloxifene hydrochloride tablet and its preparation method, aiming to solve the problems of poor stability such as photodegradation in the existing raloxifene hydrochloride tablet preparation process, easy oxidation during storage, etc.

Method used

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  • Raloxifene hydrochloride tablet and preparation method thereof
  • Raloxifene hydrochloride tablet and preparation method thereof
  • Raloxifene hydrochloride tablet and preparation method thereof

Examples

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preparation example Construction

[0042] The second aspect of the embodiment of the present application provides a preparation method of raloxifene hydrochloride tablet, comprising the following steps:

[0043] S1: Mix and granulate an effective dose of raloxifene hydrochloride with the first filler, binder, and part of the disintegrant, and then dry to obtain granules;

[0044] S2: The granules, the remaining disintegrant, the second filler, and the lubricant are mixed and tabletted to obtain raloxifene hydrochloride tablets.

[0045] The preparation method of the raloxifene hydrochloride tablet provided in the embodiment of the present application uses anhydrous lactose as the first filler to carry out wet granulation, which can reduce the moisture of the granules, avoid the tablet being in a watery microenvironment, and improve the raloxifene hydrochloride. The stability of loxifene hydrochloride tablet; With titanium dioxide as coating layer raw material and by coating layer weight gain, can isolate tablet...

Embodiment 1

[0053] The present embodiment provides a kind of preparation method of raloxifene hydrochloride tablet, comprising:

[0054] S10: Add 2.4g Tween 80 and 14.4g povidone into 43.2g water to make a suspension as a binder; add 60g non-solvated I crystalline raloxifene hydrochloride, 120g anhydrous lactose, 9g cross-linked polyvinyl chloride Vitone is added to the wet granulator for pre-mixing; then the binder is sprayed into the wet granulator through a peristaltic pump, atomized to make wet granules, and then sprayed and dried through a fluidized bed to control the dried granules Moisture content ≤ 1.5%, to obtain granulated dry granules; finally use a 0.8mm aperture sieve to sieve the granules to obtain granules;

[0055] S20: Add 30 g of spray-dried lactose monohydrate and 3 g of crospovidone to the granules prepared in step S10, and mix them in a mixer, then add 1.2 g of magnesium stearate for mixing, mix well and then press into tablets to obtain sulphate hydrochloride Loxife...

Embodiment 2

[0062] The present embodiment provides a kind of preparation method of raloxifene hydrochloride tablet, comprising:

[0063] S10: 2.4g Tween 80 and 18.0g povidone were added to 39.6g water to make a suspension as a binder; 60g non-solvated I crystalline raloxifene hydrochloride, 133.8g anhydrous lactose, 14g Add povidone into the wet granulator for pre-mixing; then directly add the binder into the wet granulator through the feeding port for granulation, and then pass through the drying oven for drying treatment, and control the moisture content of the dried granules to ≤1.5%, to obtain the Dry granules of granules; Finally, use a 0.8mm aperture sieve to sieve to obtain granules;

[0064] S20: Add 10 g of spray-dried lactose monohydrate to the granules prepared in step S10 and mix in a mixer, then add 1.8 g of magnesium stearate for mixing, mix evenly, and perform tablet compression to obtain raloxifene hydrochloride tablets;

[0065] S30: 14.4 g of the film coating premix is ...

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and provides a raloxifene hydrochloride tablet. The raloxifene hydrochloride tablet provided by the invention comprises an effective dose of raloxifene hydrochloride as an active component and a tablet excipient mixed with raloxifene hydrochloride, and the tablet excipient comprises a disintegrating agent, an adhesive, a lubricant and a filler. According to the tablet excipient, lactose anhydrous is adopted as a first filling agent, and lactose monohydrate is adopted as a second filling agent, so that the moisture of particles can be reduced, the pore-forming property of the tablet can be improved, the bulkiness and the flowability of the particles are good, the dissolution release rate of a main drug can be promoted, and the stability of the tablet can be improved; according to the raloxifene hydrochloride tablet, polyvinylpolypyrrolidone is adopted as a disintegrating agent, so that the raloxifene hydrochloride tablet has the advantages of being high in hydration capacity, large in specific surface area, capable of rapidly absorbing a large amount of water and large in water swelling volume, and the raloxifene hydrochloride tablet has the advantages of being high in main drug dissolution speed, high in bioavailability and the like and is good in application prospect.

Description

technical field [0001] The application belongs to the technical field of pharmaceutical preparations, in particular to a raloxifene hydrochloride tablet and a preparation method thereof. Background technique [0002] The chemical name of raloxifene hydrochloride (Raloxifene Hydrochloride, RH) is [6-hydroxyl-2-(4-hydroxyphenyl)benzo[b]thiophen-3-yl]-[4-[2-(1- Piperidinyl) ethoxyl]-phenyl]-methanone hydrochloride, the structural formula is: [0003] [0004] Raloxifene hydrochloride is a non-steroidal benzothiophene derivative, a second-generation selective estrogen receptor modulator, and a drug widely used in the prevention and treatment of postmenopausal osteoporosis in women. However, the alkyl tertiary amine of raloxifene is easy to generate N-oxide under aerobic conditions; the benzothiophene ring of raloxifene is easy to generate free radical intermediates under the excitation of visible light or ultraviolet light, Raloxifene dimers are further formed in the absenc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/36A61K9/28A61K31/4535A61K47/26A61K47/32A61P19/10A61P15/12
CPCA61K9/2027A61K9/2018A61K9/2866A61K9/2813A61K31/4535A61P19/10A61P15/12
Inventor 魏建华刘路路陈明文孟中斌王瑞
Owner 澳美制药(苏州)有限公司
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