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Novel formulation of cilostazol, a quinolinone-derivative used for alleviating the symptom of intermittent claudication in patients with peripheral, vascular disease

A technology of cilostazol and composition, applied in the field of pharmaceutical preparations, capable of solving problems such as adverse reactions of cilostazol

Active Publication Date: 2016-05-25
GENELABS TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

They are immediate-release lozenges that disintegrate rapidly in the body and can cause serious adverse reactions when blood levels of cilostazol suddenly rise

Method used

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  • Novel formulation of cilostazol, a quinolinone-derivative used for alleviating the symptom of intermittent claudication in patients with peripheral, vascular disease
  • Novel formulation of cilostazol, a quinolinone-derivative used for alleviating the symptom of intermittent claudication in patients with peripheral, vascular disease
  • Novel formulation of cilostazol, a quinolinone-derivative used for alleviating the symptom of intermittent claudication in patients with peripheral, vascular disease

Examples

Experimental program
Comparison scheme
Effect test

example 1-4

[0045] Examples 1-4: Cilostazol Extended Release Lozenges and Their In Vitro Dissolution Profiles

[0046] PMR Examples 1-4, each containing 100 mg of non-particulate cilostazol, were prepared following Workflow Mode 1 described in Table 1 from the ingredients shown in Table 2 below.

[0047] Table 2. Compositions for PMR Examples 1-4

[0048]

[0049] A study was performed to evaluate the in vitro dissolution profiles of Examples 1-4. The study was performed according to the procedures described in the United States Pharmacopeia (USP36, 2031). More specifically, Examples 1-4 were each placed in a dissolution medium at a temperature of about 37°C, and the dissolution medium was stirred at a speed of about 50 or 100 rpm. The concentration of cilostazol in the dissolution medium was measured at different time periods. The results are shown in Table 3 below and figure 1 middle.

[0050] Table 3. In Vitro Dissolution Profiles of PMR Examples 1-4

[0051]

[0052] The r...

example 5-7

[0053] Examples 5-7: Cilostazol Extended Release Lozenges and Their In Vitro Dissolution Profiles

[0054] PMR Examples 5-7, each containing 100 mg of particulate cilostazol, were prepared following Workflow Mode 1 described in Table 1 from the ingredients shown in Table 4 below. It is noted that the particulate cilostazol used in Examples 5-7 had a D(0.9) of 5.1-75.2 μm compared to Examples 1-4.

[0055] Table 4. Compositions for PMR Examples 5-7

[0056]

[0057] Studies were performed to evaluate the in vitro dissolution profiles of Examples 5-7. The study was performed according to the procedure described above. The results are shown in Table 5 below and figure 2 middle.

[0058] Table 5. In Vitro Dissolution Profiles of PMR Examples 5-7

[0059]

[0060]

[0061] These results show that, compared to Examples 1-4, Examples 5-7 prepared with particulate cilostazol exhibited a more consistent zero-degree release profile in the dissolution medium. See figure ...

example 8-10

[0062] Examples 8-10: Cilostazol Extended Release Lozenges and Their In Vitro Dissolution Profiles

[0063] PMR Examples 8-10, each containing 100 mg of microparticulate cilostazol, were prepared following Workflow Mode 2 described in Table 1 from the ingredients shown in Table 6 below.

[0064] Table 6. Compositions for PMR Examples 8-10

[0065]

[0066] A study was performed to evaluate the in vitro dissolution profiles of Examples 8-10. The study was performed according to the procedure described above. The results are shown in Table 7 below and image 3 middle.

[0067] Table 7. In Vitro Dissolution Profiles of PMR Examples 8-10

[0068]

[0069] These results show that varying amounts of povidone product used in preparation did not affect the in vitro dissolution profile of PMR lozenges.

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Abstract

A pharmaceutical composition in solid form containing particulate cilostazol or a salt thereof, a cellulose, a diluent, and a lubricant. The pharmaceutical composition features an in vivo plasma profile for cilostazol of C24h / Cmax vo plasma profile for cilostazol of C24h / Cmax> 0.25. Also disclosed is a method of preparing the above-described pharmaceutical composition.

Description

technical field field of invention [0001] The present invention relates to pharmaceutical formulations of cilostazol, a phosphodiesterase inhibitor, and more particularly to extended-release dosage forms suitable for once-daily administration. Background technique Background of the invention [0002] Cilostazol, a selective inhibitor of phosphodiesterase-3, inhibits platelet aggregation and acts as a direct arterial vasodilator. It is commercially available as manufactured by Otsuka Pharmaceutical (Otsuka Pharmaceutical) Lozenge, whose listed indications include relief of symptoms of intermittent claudication. [0003] Patients with intermittent claudication tend to develop leg pain and limp and are unable to walk long distances without rest. The intensity of the disease can be measured clinically, either by initial limping distance (i.e., the distance the patient can walk before pain develops), or by the absolute limping distance (i.e., the distance the patient can w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/38A61K31/4709A61P9/10
CPCA61K9/2018A61K9/2054A61K9/2077A61K31/4709A61P43/00A61P7/02A61P9/00A61P9/08A61P9/10A61K47/38A61K9/14A61K47/26A61K9/00
Inventor 陈凤珠王尹珊杨宜伦林玉瑛
Owner GENELABS TECH INC
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