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Slow release preparation of cilostazol

A sustained-release preparation, the technology of cilostazol, which is applied to the sustained-release preparation of cilostazol and the field of preparation thereof, can solve the problems of affecting drug efficacy, inconvenient use of patients, affecting the steady-state blood concentration of the drug, and the like, and achieving effective The effect of improving sex or adaptability, reducing the frequency of medication

Inactive Publication Date: 2007-08-01
刘凤鸣
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The serum half-life of cilostazol is diphasic, the α-phase is 2.2 hours, and the β-phase is 18.0 hours. A dose of 100mg is usually administered 2-3 times a day, which brings inconvenience to patients. The influence of other factors affects the steady-state blood drug concentration of the drug, thereby affecting the efficacy of the drug

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] The preparation of embodiment 1-cilostazol sustained-release tablet (1)

[0051] Method: Take 50 grams of cilostazol, 50 grams of hydroxypropyl cellulose, 15 grams of hypromellose, 10 grams of lactose, 10 grams of microcrystalline cellulose, 1 gram of carbomer, and 30 grams of polyethylene glycol. gram, mixed evenly, granulated by dry method, mixed with magnesium stearate, and tableted to obtain the finished product, and the drug content is 50 mg / tablet. Then, the dissolution rate of cilostazol sustained-release tablet (1) in 900 ml of water at 37°C was determined. After the release degree measurement, the results are shown in Table 1, which meets the requirements.

[0052] Table 1 Dissolution of Cilostazol Sustained-Release Tablets (1)

[0053] Sampling time (hours)

Embodiment 2

[0054] The preparation of embodiment 2-cilostazol sustained-release tablet (2)

[0055] Method: Take 50 grams of cilostazol, 10 grams of hydroxypropyl cellulose, 20 grams of stearyl alcohol, 15 grams of hypromellose, 1 gram of carbomer, and 10 grams of lactose, respectively, pass through an 80-mesh sieve, and grind them. Mix well, add a 95% ethanol solution of polyvinylpyrrolidone with a concentration of 10% as a binder and stir to make a soft material, pass through a 16-mesh sieve for granulation, dry the granules at room temperature for 2 hours, 16-mesh sieve for granulation, and then add hard material. 4.5 grams of magnesium fatty acid, 2 grams of micropowder silica gel, mix well, and press into tablets to obtain the finished product, and the drug content is 50 mg / tablet. Then, the dissolution rate of cilostazol sustained-release tablet (2) in 900 ml of water at 37°C was determined. After the release degree measurement, the results are shown in Table 2, which meet the requ...

Embodiment 3

[0058] The preparation of embodiment 3-cilostazol sustained-release tablet (3)

[0059] Method: Take 50 g of cilostazol, 35 g of hypromellose, 5 g of microcrystalline cellulose, and 1 g of carbomer, respectively, pass through an 80-mesh sieve, mix well, and add 95% ethanol with a concentration of 10% polyvinylpyrrolidone. The solution was used as a binder and stirred to make a soft material, passed through a 16-mesh sieve for granulation, dried at 60°C for 1 hour, 16-mesh sieve and granulated, and then added 2.5 grams of magnesium stearate, mixed evenly, and pressed into a tablet to obtain a finished product, containing The dosage of the drug is 50 mg / tablet. Then, the dissolution rate of cilostazol sustained-release tablet (3) in 900 ml of water at 37°C was determined. After the release degree measurement, the results are shown in Table 3, which meets the requirements.

[0060] The dissolution rate of table 3 cilostazol sustained-release tablets (3)

[0061] Sampl...

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PUM

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Abstract

The invention discloses a slow release preparation of cilostazol and its preparing process, wherein the raw materials of the preparation include cilostazol of a predetermined proportion, slow release matrix material and medicinal material, the preparation can be prepared into solid dispersing agent, wherein the medicament can be released slowly and continuously after being administrated, the effective concentration in blood can be maintained, and long action can be achieved. The advantages of the invention include decreased frequency of medicinal administration, improved patient's adaptability, lowered blood concentration peak-valley, increased medicinal effect and safety, and reduced total medicinal dose, thereby optimum curative effect can be achieved through minimum dose, thus the preparation is more suitable for patients.

Description

[0001] [Technical Field] The present invention relates to a sustained-release preparation of cilostazol and a preparation method thereof. [Background technique] [0002] The research and development of sustained-release preparations has a history of more than 40 years. It is released slowly and non-constantly according to requirements in a specified environment, and the number of daily doses is reduced by at least one time compared with the corresponding ordinary preparations or the interval between doses is longer. Prolonged formulation. This preparation can maintain the blood concentration of the drug for a long time in the human body, instead of falling as quickly as ordinary preparations, so as to avoid the "peak and valley" phenomenon caused by frequent administration of ordinary preparations, and make the drug safer The performance, effectiveness or adaptability are improved, thus reducing the frequency of medication, which greatly facilitates patients, especially those ...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/48A61K47/02A61K47/12A61K47/34A61K47/38A61K47/42A61K47/44A61K31/4709A61P7/02A61K47/10A61K47/32
Inventor 刘凤鸣
Owner 刘凤鸣
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