Diacerein capsule with high bioavailability and preparation method thereof
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
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
View PDF9 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
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.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
PUM
Login to view more
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more