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Cilostazol sustained-release capsule compound and preparation method thereof

A technology of cilostazol and sustained-release capsules, which is applied in the field of cilostazol sustained-release capsule compositions and its preparation, can solve problems such as difficulty in large-scale production, side effects of patients, and inconvenient dosage, and achieve product controllability Strong, easy to industrialize, and simple preparation process

Active Publication Date: 2017-03-22
浙江为康制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing cilostazol preparations are mostly in the form of immediate-release tablets and capsules. When patients are administered orally, this immediate-release formulation of cilostazol can cause a sudden increase in drug concentration in the blood and headache side effects, and due to In order to maintain its pharmacological activity at a constant level, the immediate release dosage form should be administered in an amount of 50 to 100 mg twice a day, so its dosage is inconvenient
[0004] In order to overcome these defects, CN1168102A discloses a kind of cilostazol resin particles that can continuously release the required amount in the body for a long time. It is mainly prepared by melting method, but organic solvents such as chloroform are needed when the melting method is prepared. Residues of these solvents will cause side effects to patients; patent CN101340882B manufacture method of wax matrix particles containing medicine, extruder used for the method and sustained-release preparation containing cilostazol, the patent process is complex and difficult to achieve large-scale Production; cilostazol sustained-release tablets disclosed in patent CN102548543A, the specification is 200mg / tablet, using hypromellose and carbomer as a mixed controlled-release product, carbomer has a characteristic odor and strong hygroscopicity; Patent CN100551369C in vitro dissolution test The dissolution medium is an aqueous solution of 0.45% sodium lauryl sulfate, blue-turning method, 100 rpm, according to the prescription analysis and multiple tests, the cilostazol sustained-release capsule enters the dissolution medium for about half an hour. Dispersed into small particles and deposited at the bottom of the dissolution vessel, the value measured by the blue-turning method is lower than that of the paddle method at 75 rpm

Method used

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  • Cilostazol sustained-release capsule compound and preparation method thereof
  • Cilostazol sustained-release capsule compound and preparation method thereof
  • Cilostazol sustained-release capsule compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6

[0027] The cilostazol sustained-release capsules (specification: 100 mg / capsule) of Examples 1-6 are composed of the raw and auxiliary materials in the following weight ratios as shown in Table 1.

[0028] Table 1

[0029]

Embodiment 7-11、 comparative example 1

[0031] The cilostazol sustained-release capsules (specification: 200 mg / capsule) of Examples 7-11 and Comparative Example 1 are composed of the following raw and auxiliary materials in the weight ratio as shown in Table 2.

[0032] Table 2

[0033]

[0034]

Embodiment 12

[0036] The preparation method of the cilostazol sustained-release capsules of the present embodiment is as follows:

[0037] The cilostazol is micronized and passed through a 200-mesh sieve before mixing; the anti-sticking agent is passed through a 200-mesh sieve before mixing; the hypromellose phthalate sustained-release skeleton material and blocker Pass through a 80-mesh sieve before mixing; the filler pass through a 100-mesh sieve before mixing; and the lubricant pass through a 100-mesh sieve before mixing.

[0038] Mix the prescribed amount of cilostazol, hypromellose phthalate sustained-release matrix material, blocker, filler, and anti-sticking agent evenly; dissolve the adhesive with ethanol; put the evenly mixed Cilostazol, hypromellose phthalate sustained-release framework material, blocker, filler, anti-adhesive agent made of soft material, granulated twice with 16-24 mesh sieve; After drying at 55°C, sieve with 16-24 mesh, add lubricant and mix well for 15 minutes...

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Abstract

The invention relates to the pharmaceutical field and discloses a cilostazol sustained-release capsule compound and a preparation method thereof. The sustained-release capsule compound comprises a medicinal hollow capsule body and contents arranged in the medicinal hollow capsule body. The contents comprise cilostazol, a hydroxypropyl methylcellulose phthalate sustained-release framework material, a retardant, an adhesive, a filler, an antisticking agent and a lubricating agent. Hydroxypropyl methylcellulose phthalate is used as the framework sustained-release material and is a product obtained by performing an esterification reaction between hydroxypropyl methylcellulose and phthalic anhydride in acetic acid with sodium acetate serving as a catalyst. Molecules have carboxyl negative charge intermolecular repulsion under a carboxyl alkaline environment, so that twinned macromolecules are stretched to be dissolved, and enteric solubility is achieved. The absorption of the cilostazol by the upper gastrointestinal tract can be reduced while the absorption of the cilostazol by the lower gastrointestinal tract is improved. Adverse drug reactions such as headaches, head heaviness and tachycardia caused by sudden increase of the drug concentration are overcome. In addition, the cilostazol sustained-release capsule compound is taken only one time per day, so that the adaptability of patients is improved.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a cilostazol sustained-release capsule composition and a preparation method thereof. Background technique [0002] Cilostazol is a typical intracellular cAMPPDE (cyclic AMP phosphodiesterase) inhibitor, and it has been known that it inhibits platelet aggregation and dilates arteries by inhibiting PDE activity, and is effective in inhibition of blood coagulation, promotion of central blood circulation, anti-inflammatory It plays an important role in anti-ulcer effect, prevention and treatment of cerebral infarction, and improvement of cerebral circulation. [0003] Cilostazol has poor water solubility, and orally administered cilostazol has been shown to be absorbed primarily in the upper gastrointestinal tract and its absorption decreases as it moves to the lower gastrointestinal tract. Existing cilostazol preparations are mostly in the form of immediate-release tablets and capsules. Whe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K47/38A61K47/32A61K31/4709A61P7/02A61P9/10A61P29/00A61P17/02A61P9/06
CPCA61K9/0002A61K9/1635A61K9/1652A61K31/4709
Inventor 刘利清罗益彪
Owner 浙江为康制药有限公司
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