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Compound controlled-release preparation containing topiroxostat

A controlled-release preparation, the technology of topiramast, is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, pharmaceutical formulas, etc., and can solve the problems of obvious side effects and the like

Inactive Publication Date: 2020-04-10
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the number of gout patients in my country is still increasing, and there is a trend of spreading to a younger age. Therefore, anti-gout drugs have great potential in the Chinese market. However, most of the anti-gout drugs on the market are old drugs. Although they are cheap, they have obvious side effects. , if there are new drugs launched in time, the market prospect will be very impressive

Method used

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  • Compound controlled-release preparation containing topiroxostat
  • Compound controlled-release preparation containing topiroxostat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Prescription 1 (according to 1000 capsules)

[0012] A. Topirast immediate-release granules

[0013] Topirast 5g

[0014] Microcrystalline Cellulose 2.85g

[0015] Low-substituted hydroxypropyl cellulose 6.0g

[0016] Crospovidone 0.9g

[0017] Lactose 3.0g

[0018] Magnesium stearate 0.15g

[0019] B. Topirast controlled-release granules

[0020] Topirast 15g

[0021] Microcrystalline Cellulose 8.5g

[0022] Low-substituted hydroxypropyl cellulose 7.8g

[0023] Croscarmellose 10g

[0024] Lactose 9.0g

[0025] Magnesium Stearate 4.0g

[0026] C. Febuxostat controlled-release granules

[0027] Febuxostat 40g

[0028] Hydroxypropyl Methyl Cellulose 38g

[0029] Ethylcellulose 6.0g

[0030] Lactose 6.0g

[0031] Magnesium Stearate 0.3g.

[0032] Preparation method:

[0033] (1) Topiralast and febuxostat are pulverized through an 80 mesh sieve;

[0034] (2) Mix the controlled-release material evenly, and pulverize through a 120-mesh sieve;

[0035] (3) ...

Embodiment 2

[0039] Prescription 2 (according to 1000 capsules)

[0040] A. Topirast immediate-release granules

[0041] Topirast 5g

[0042] Microcrystalline Cellulose 2.85g

[0043] Low-substituted hydroxypropyl cellulose 6.0g

[0044] Crospovidone 0.9g

[0045] Lactose 3.0g

[0046] Magnesium stearate 0.15g

[0047] B. Topirast controlled-release granules

[0048] Topirast 15g

[0049] Microcrystalline Cellulose 10.5g

[0050] Low-substituted hydroxypropyl cellulose 8.5g

[0051] Croscarmellose 12g

[0052] Lactose 8.0g

[0053] Magnesium Stearate 4.0g

[0054] C. Febuxostat controlled-release granules

[0055] Febuxostat 40g

[0056] Hydroxypropyl Methyl Cellulose 45g

[0057] Ethylcellulose 8.0g

[0058] Lactose 4.0g

[0059] Magnesium Stearate 0.3g.

[0060] Preparation method is the same as embodiment 1.

Embodiment 3

[0062] Prescription 3 (according to 1000 capsules)

[0063] A. Topirast immediate-release granules

[0064] Topirast 5g

[0065] Microcrystalline Cellulose 2.85g

[0066] Low-substituted hydroxypropyl cellulose 6.0g

[0067] Crospovidone 0.9g

[0068] Lactose 3.0g

[0069] Magnesium stearate 0.15g

[0070] B. Topirast controlled-release granules

[0071] Topirast 15g

[0072] Microcrystalline Cellulose 8.5g

[0073] Low-substituted hydroxypropyl cellulose 9.5g

[0074] Croscarmellose 10g

[0075] Lactose 9.0g

[0076] Magnesium Stearate 4.5g

[0077] C. Febuxostat controlled-release granules

[0078] Febuxostat 40g

[0079] Hydroxypropyl Methyl Cellulose 35g

[0080]Ethylcellulose 6.0g

[0081] Lactose 8.0g

[0082] Magnesium Stearate 0.25g.

[0083] Preparation method is the same as embodiment 1.

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Abstract

The invention relates to the field of pharmaceutical preparations, and in particular relates to a compound drug controlled-release preparation containing topiroxostat and febuxostat. The invention also discloses a preparation method of the compound drug controlled-release preparation containing topiramate and febuxostat. Compared with the prior art, the compound drug controlled-release preparationprovided by the invention can release a drug slowly at a constant speed in a prescribed release medium, so that the release rate and bioavailability of the compound drug controlled-release preparation are effectively improved, the preparation can be rapidly released in the early stage of medication to produce drug effects and can be slowly released at a constant speed in the later stage to maintain a normal blood drug concentration, and the preparation maintains the drug effects for a long time without producing toxic and side effects or causing drug accumulation and poisoning, improves the efficacy, and is safe and quick; and at the same time, the preparation method provided by the invention is suitable for scale-up production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a compound controlled-release preparation containing topiramate, which belongs to the technical field of medicine. Background technique [0002] Uric acid is a normal product of purine nucleotide metabolism. When uric acid is produced excessively and uric acid excretion decreases, hyperuricemia is formed when the uric acid in the blood rises beyond the normal range; excessive uric acid in the blood is mainly deposited in the joints, cartilage, Subcutaneous soft tissue and kidneys cause comprehensive clinical manifestations such as arthritis and kidney disease, which is called gout. Therefore, hyperuricemia and uric acid deposition in organ tissues are the basic pathogenesis of gout. The etiology leading to elevated uric acid is more complex and can be divided into two categories: primary and secondary. [0003] With the improvement of people's living standards, improve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/426A61K31/444A61K9/52A61K47/38A61P19/06
CPCA61K9/5042A61K9/5047A61K31/426A61K31/444A61P19/06A61K2300/00
Inventor 陈阳生王明刚刘晓霞吕义强游福山张春利王贤贤朱兆刚
Owner CP PHARMA QINGDAO CO LTD
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