Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof

The technology of sarpogrelate hydrochloride and single-layer osmotic pump, which is applied in the field of medicine, can solve the problems of reduced medication frequency, large fluctuation of blood drug concentration, easy accumulation of drugs, etc., and achieves the effects of less toxic and side effects, lasting effect and stable curative effect.

Inactive Publication Date: 2008-09-10
THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patients take frequent doses every day, easily forgetting or omissions, resulting in missing the time of taking the medicine or reducing the frequency of t

Method used

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  • Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof
  • Sarpogrelate hydrochloride single layer osmotic pump regulated-release preparations and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Chip composition:

[0025] Sagrelate Hydrochloride 25%

[0026] Polyoxyethylene (molecular weight: 300,000) 42.5%

[0027] Citric acid 32.0%

[0028] Magnesium Stearate 0.5%

[0029] Composition of semi-permeable membrane coating solution:

[0030] Cellulose acetate 2.0%

[0031] Macrogol 400 0.16%

[0032] Acetone solvent

[0033] Preparation method: crush the prescription amount of medicine, citric acid and polyoxyethylene respectively, pass through a 100-mesh sieve, mix well, soften with starch slurry, pass through 18-mesh granulation, oven-dried at 60°C, pass through a 20-mesh sieve Granules, add lubricant, mix evenly, and directly compress into tablets to obtain tablet cores. Dissolve cellulose acetate and plasticizer PEG400 in acetone solution as a coating solution, put the tablet core in a coating pan, and coat at a coating temperature of 40-60°C. After coating, coat the tablet at 40 Dry in a drying oven at ℃ to solidify the coating film, and then prepare...

Embodiment 2

[0035] Chip composition:

[0036] Sagrelate Hydrochloride 20%

[0037] Polyoxyethylene (molecular weight: 300,000) 15%

[0038] Citric acid 64.5%

[0039] Magnesium Stearate 0.5%

[0040] Composition of semi-permeable membrane coating solution:

[0041] Cellulose acetate 2.5%

[0042] Macrogol 400 0.25%

[0043] Acetone solvent

[0044]Preparation method: crush the prescription amount of medicine, citric acid and polyoxyethylene respectively, pass through a 100-mesh sieve, mix well, soften with starch slurry, pass through 18-mesh granulation, oven-dried at 60°C, pass through a 20-mesh sieve Granules, add lubricant, mix evenly, and directly compress into tablets to obtain tablet cores. Dissolve cellulose acetate and plasticizer PEG400 in acetone solution as a coating solution, put the tablet core in a coating pan, and coat at a coating temperature of 40-60°C. After coating, coat the tablet at 40 Dry in a drying oven at ℃ to solidify the coating film, and then prepare a ...

Embodiment 3

[0046] Chip composition:

[0047] Sagrelate Hydrochloride 30%

[0048] Polyoxyethylene (molecular weight: 300,000) 50%

[0049] Lactose 19.5%

[0050] Magnesium Stearate 0.5%

[0051] Composition of semi-permeable membrane coating solution:

[0052] Cellulose acetate 3.0%

[0053] Macrogol 400 0.3%

[0054] Acetone: isopropanol (4:1) solvent

[0055] Preparation method: respectively pulverize the prescribed amount of medicine, lactose and polyoxyethylene through a 100-mesh sieve, mix uniformly, then add lubricant, mix uniformly, and directly compress into tablets to obtain tablet cores. Dissolve cellulose acetate and plasticizer PEG 400 in acetone solution as a coating solution, put the tablet core in a coating pan, and coat at a coating temperature of 40-60°C. After coating, coat the tablet in the Dry in a drying oven at 40°C to solidify the coating film, and then prepare a 0.5mm drug release hole on one side of the coating tablet by laser or mechanical means to obtain...

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Abstract

The invention relates to the medicine technical filed, in particular to a monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride and a preparation method thereof, which is characterized by lasting drug effect, constant curative effect, slight toxic and side effect. The monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride comprises by weight percentage of 1 to 40 percent of sarpogrelate hydrochloride, 30 to 90 percent of auxiliary material that can promote osmosis, 1 to 40 percent of membrane material that performs controlled release and the rest is other auxiliary material; the diameter of a small drug release hole is 0.1 to 2.0 mm. The preparation method comprises: a certain amount of drug according to the prescription is mixed with an adhesive, a bulking agent and a co-penetrant which are respectively ground and screened, prepared into soft material and palletized, dried and particle finished and then added with a lube and pressed to obtain tablet core. Coating liquid is prepared and the tablet core coated, after coating, drying is done to solidify the coating membrane, and then one side of coated tablet is provided with the small drug release hole, thus obtaining an osmotic pump controlled release tablet. The monolayer osmotic pump controlled release preparation of sarpogrelate hydrochloride of the invention has the advantages of reducing times of dosage, promoting the compliance of sufferers and satisfying the requirements of clinical medication.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically a drug for improving ischemic symptoms such as ulcers, pain and coldness caused by chronic arterial occlusive disease-sargrelate hydrochloride monolayer osmotic pump controlled release preparation and its preparation method . Background technique [0002] Sarpogrelate hydrochloride (English name: sarpogrelate hydrochloride) is a 5-HT receptor blocker originally developed by Mitsubishi Corporation, a cardiovascular drug. Launched in 1993, it is clinically used to improve ischemic symptoms such as ulcers, pain and cold sensation caused by chronic arterial occlusive disease. [0003] Its pharmacological characteristics are as follows: ①Inhibition of platelet aggregation: This product selectively antagonizes the 5-hydroxytryptamine (5-HT) receptors of platelets and blood vessels, and inhibits platelet aggregation. This product inhibits platelet aggregation caused by collagen alone, an...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/225A61P9/10
Inventor 曹高忠傅红兴张福志朱新波汤从容张秀华赵艳花
Owner THE FIRST AFFILIATED HOSPITAL OF WENZHOU MEDICAL COLLEGE
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