Lesinurad controlled-release pharmaceutical composition

A technology for controlled release of drugs and compositions, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of harsh drug taking conditions, toxic and side effects of Resinad, and reduce the risk of drug use, The effect of enhancing drug efficacy, improving release and dissolution rate

Active Publication Date: 2020-12-11
SHANGHAI JINGXIN BIOLOGICAL MEDICAL +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is to overcome the defects that the existing Resinard has severe toxic and side effects when used in high doses, and the conditions for taking the drug are relatively strict, and provides a kind of Resinard control release pharmaceutical composition

Method used

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  • Lesinurad controlled-release pharmaceutical composition
  • Lesinurad controlled-release pharmaceutical composition
  • Lesinurad controlled-release pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Table 1 Sustained-release component formula (100 tablets)

[0050]

[0051]

[0052] Table 2 Immediate Release Component Formulation (100 Tablets)

[0053] Raw materials Content per tablet (mg) Proportion(%) Prescription dosage (g) Recinard 150.00 66.67 15.000 HPMC E5 4.50 2.00 0.450 lactose 33.25 14.78 3.325 MCC102 23.75 10.56 2.375 Crospovidone 11.25 5.00 1.125 Magnesium Stearate (additional) 2.25 1.00 0.225 total 225.00 100.00 22.500

[0054] (1) prepare sustained-release component according to the formula of table 1:

[0055] 1) Mixing: Mix the weighed Recinard, HPMC E50LV, lactose, and MCC102 for 3 minutes, pass through a 24-mesh sieve, and mix for another 3 minutes;

[0056] 2) Granulation: adding a wetting agent (50% ethanol), wet granulation, and passing through a 24-mesh sieve;

[0057] 3) Drying: drying in an oven at 60°C, moisture <3%;

[0058] 4) Grain sizing: dry granules p...

Embodiment 2

[0068] Table 3 Sustained Release Component Formula (100 Tablets)

[0069] Raw materials Content per tablet (mg) Proportion(%) Prescription dosage (g) Recinard 100.00 36.36 10.000 HPMC E50LV 55.00 20.00 5.500 lactose 78.18 28.43 7.818 MCC102 39.07 14.21 3.907 Magnesium Stearate (additional) 2.75 1.00 0.275 total 275.00 100.00 27.500

[0070] Table 4 Immediate Release Component Formulation (100 Tablets)

[0071] Raw materials Content per tablet (mg) Proportion(%) Prescription dosage (g) Recinard 150.00 66.67 15.000 HPMC E5 4.50 2.00 0.450 lactose 33.25 14.78 3.325 MCC102 23.75 10.56 2.375 Crospovidone 11.25 5.00 1.125 Magnesium Stearate (additional) 2.25 1.00 0.225 total 225.00 100.00 22.500

[0072] According to the method in Example 1, the sustained-release component and the immediate-release component were prepared, and then double-la...

Embodiment 3

[0074] Table 5 Immediate Release Component Formulation (1000 capsules)

[0075] Raw materials Content per tablet (mg) Proportion(%) Prescription dosage (g) Recinard 150.00 66.67 150.00 Ball core 56.66 28.33 56.66 Hypromellose 10.00 5.00 10.00 total 200.00 100.00 200.00

[0076] Table 6 Sustained-release component formula (1000 grains)

[0077] Raw materials Content per tablet (mg) Proportion(%) Prescription dosage (g) Recinard 100.00 36.36 100.000 Ball core 110.00 33.64 110.00 Hypromellose 15.00 5.00 15.00 Surelease 75.00 25.00 75.00 total 300.00 100 300.00

[0078] (1) According to the formula preparation of table 5 release component immediately:

[0079] 1) Preparation of the medicinal solution: add the adhesive to an appropriate amount of water, stir until it is completely dissolved, add Recinard, continue to stir, and suspend evenly.

[0080] 2) Preparation of ...

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Abstract

The invention discloses a lesinurad controlled-release pharmaceutical composition. The lesinurad controlled-release pharmaceutical composition has the following characteristics: (i), within 12 hours after oral administration of the pharmaceutical composition, the plasma concentration of lesinurad is kept above 6 mu g/mL; and (ii), after oral administration of the pharmaceutical composition, the maximum plasma concentration of lesinurad is 45%-60% of the equal dose of lesinurad administered orally alone. The lesinurad controlled-release pharmaceutical composition in the invention has improved release and dissolution rates; and, compared with common quick-release tablets, the lesinurad controlled-release pharmaceutical composition has lower toxic and side effects, enhances the drug effect, can obviously reduce the medication risk of lesinurad, and meanwhile, enhances the drug administration compliance.

Description

technical field [0001] The invention relates to a drug composition for controlled release of lesinard. Background technique [0002] Lesinurad (Lesinurad) is a urate transporter 1 (URAT1) inhibitor, its structure is shown in formula I, chemical name: 2-(5-bromo-4-(4-cyclopropylnaphthalene- 1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid, or 2-[[5-bromo-4-(4-cyclopropyl-1-naphthalene)-4H-1 , 2,4-triazol-3-yl]thio]acetic acid, CAS: 878672-00-5. [0003] [0004] The patent CN102643241B of the original research company discloses the use of Resinard in the treatment or prevention of abnormal tissue uric acid levels, such as gout, hyperuricemia, etc., and also mentions various forms of Resinard German pharmaceutical composition. In the phase 3 clinical trial, although the 400mg group of Recinard showed additional efficacy, it had more serious adverse reactions and nephrotoxicity. Therefore, the specification of Zurampic, which was approved by the FDA in 2015, was only 200mg. Z...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/48A61K47/38A61K47/26A61K47/32A61K47/12A61K31/4196A61P19/06
CPCA61K9/209A61K9/2018A61K9/2054A61K9/2027A61K9/2013A61K9/1652A61K31/4196A61P19/06Y02A50/30
Inventor 徐文婷唐春兰黄悦
Owner SHANGHAI JINGXIN BIOLOGICAL MEDICAL
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