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Diacerein capsule with high bioavailability and preparation method thereof

A technology for diacerein and capsules, applied in the field of pharmaceutical preparations, can solve problems such as reduced bioavailability, achieve the effects of improving bioavailability, inhibiting recrystallization, and shortening production time

Pending Publication Date: 2022-07-29
SUZHOU CHUNGHWA CHEM & PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In order to achieve the above-mentioned technical objectives, the inventors conducted a large number of experimental studies and unremitting explorations, and finally adopted the technical means of melt granulation to effectively solve the problem of the decrease in bioavailability of diacerein caused by recrystallization in the gastrointestinal tract

Method used

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  • Diacerein capsule with high bioavailability and preparation method thereof
  • Diacerein capsule with high bioavailability and preparation method thereof
  • Diacerein capsule with high bioavailability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] (1) Prescription

[0030]

[0031] (2) Preparation process

[0032] The prescription amount of diacerein, hypromellose phthalate and poloxamer F188 are mixed and then melt granulated.

[0033] Hot melt extrusion parameters: temperature setting: 80℃ / 120℃ / 160℃ / 160℃ / 160℃ / 160℃ / 160℃ / 160℃; screw speed: 150rpm; feeding speed: 2kg / h.

[0034] After crushing, pass through an 80-mesh sieve, mix with mannitol, croscarmellose sodium, and magnesium stearate evenly, then fill in capsules, package, and inspect to obtain a finished product.

Embodiment 2

[0036] (1) Prescription

[0037]

[0038] (2) Preparation process

[0039] The prescription amount of diacerein, hypromellose acetate succinate LF type and sodium cholate are mixed and then melt granulated.

[0040] Hot melt extrusion parameters: temperature setting: 120℃ / 150℃ / 170℃ / 170℃ / 170℃ / 170℃ / 170℃ / 170℃; screw speed: 100rpm; feeding speed: 2kg / h.

[0041] After crushing, pass through an 80-mesh sieve, mix with mannitol, croscarmellose sodium, and magnesium stearate evenly, then fill in capsules, package, and inspect to obtain a finished product.

Embodiment 3

[0043] (1) Prescription

[0044]

[0045] (2) Preparation process

[0046] The diacerein in the prescribed amount, acrylic resin L100-55 type and Tween 80 are mixed and then melted and granulated.

[0047] Hot melt extrusion parameters: temperature setting: 120℃ / 150℃ / 175℃ / 175℃ / 175℃ / 175℃ / 175℃ / 175℃; screw speed: 120rpm; feeding speed: 2kg / h.

[0048] After crushing, pass through an 80-mesh sieve, mix with microcrystalline cellulose, low-substituted hydroxypropyl cellulose, and magnesium stearate, and then fill in capsules, package, and inspect to obtain the finished product.

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PUM

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Abstract

The invention discloses a diacerein capsule and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. The capsule is composed of a content and a capsule shell, the content comprises enteric drug particles, a filler, a disintegrating agent and a lubricant, and the enteric drug particles are prepared by uniformly mixing, hot-melting, extruding and crushing the following components in percentage by mass: 10-40% of diacerein, 50-80% of an enteric polymer carrier material and 5-20% of a surfactant. The enteric polymer carrier contained in the capsule can inhibit recrystallization of diacerein in gastrointestinal tracts, so that the bioavailability is improved, and adverse reactions are reduced. Dissolution tests and beagle in-vivo pharmacokinetic tests show that the diacerein capsule prepared by the invention is good in dissolution effect and high in bioavailability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a capsule, in particular to a high bioavailability diacerein capsule and a preparation method thereof. Background technique [0002] Diacerein, whose chemical name is diacetylrhein, an anthraquinone derivative, belongs to a new generation of disease-modifying antirheumatic drugs (DMARDs) or slow-acting antirheumatic drugs (SAARDs). Its active metabolite rhein can inhibit the production of interleukin IL-1. At the same time, this product does not inhibit the synthesis of prostaglandins, so compared with non-steroidal anti-inflammatory drugs (NSAIDs), it has relatively less damage to the mucosa. Cell experiments and animal experiments have confirmed that diacerein can induce cartilage formation, has analgesic, anti-inflammatory and antipyretic effects, significantly improves joint function in patients with osteoarthritis (OA), delays the course of the disease, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K31/222A61K47/36A61K47/38A61K47/32A61P13/12A61P19/02A61P29/00
CPCA61K9/1652A61K9/1635A61K9/4808A61K9/4866A61K31/222A61P19/02A61P29/00A61P13/12
Inventor 马晓华
Owner SUZHOU CHUNGHWA CHEM & PHARMA IND
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