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Rosuvastatin calcium oral solid preparation and applications thereof

A technology of rosuvastatin calcium and solid preparations, which is applied in the fields of pill delivery, medical preparations of non-active ingredients, metabolic diseases, etc., which can solve the problems of high cost of preparations, few adverse reactions, low bioavailability, etc. The effects of complete release, avoidance of adverse reactions, and simple preparation process

Active Publication Date: 2012-07-04
SUZHOU HOMESUN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the rosuvastatin calcium solid preparation prepared by making liposomes has increased stability, the liposome preparation process is complicated, the quality is difficult to control, and the price of phospholipids as auxiliary materials is very high, resulting in high preparation costs, which is not conducive to Production and sales
[0012] In addition, since rosuvastatin calcium is almost insoluble in water or in 0.1mol / L hydrochloric acid or 0.1mol / L sodium hydroxide solution, the oral solid preparations of rosuvastatin calcium prepared according to conventional methods all have different cumulative dissolution rates. High, low bioavailability in vivo
At the same time, although rosuvastatin calcium has a significant lipid-lowering effect, it is easy to produce "peak-to-valley" fluctuations in blood concentration when taken in larger doses (10-40mg), resulting in occurrences such as rhabdomyolysis, proteinuria, kidney disease, kidney disease, etc. Adverse reactions such as failure, hepatotoxicity, pharyngitis, headache and flu-like symptoms
[0013] At present, there is no document in the prior art to report a kind of rosuvastatin calcium oral solid preparation with good stability, high cumulative dissolution rate and few adverse reactions.

Method used

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  • Rosuvastatin calcium oral solid preparation and applications thereof
  • Rosuvastatin calcium oral solid preparation and applications thereof
  • Rosuvastatin calcium oral solid preparation and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Preparation of Rosuvastatin Calcium Solid Dispersion

[0035] Combine 42g polyethylene glycol 6000 and 59g Add S100 (commercialized polyacrylic acid resin) into 350ml chloroform successively, stir until dissolved, add 20g of rosuvastatin calcium dissolved in a small amount of chloroform while stirring, rotary evaporate below 45°C, evaporate the chloroform and quickly pour into the culture medium Spread it flat in a dish, place it in the freezer layer of the refrigerator for 6 hours, then freeze-dry it for 24 hours, wait for embrittlement, take it out and pulverize it and pass it through an 80-mesh sieve to obtain the solid dispersion of rosuvastatin calcium.

Embodiment 2

[0036] Example 2 Preparation of Rosuvastatin Calcium Solid Dispersion

[0037] 58g polyethylene glycol 6000, 76g S100 and 65g Add L100 (commercialized polyacrylic acid resin) into 700ml chloroform successively, stir until dissolved, then add 10g rosuvastatin calcium dissolved in a small amount of chloroform while stirring, rotary evaporate below 45°C, evaporate the chloroform and quickly pour into the culture medium Spread it flat in a dish, place it in the freezer layer of the refrigerator for 6 hours, then freeze-dry it for 24 hours, wait for embrittlement, take it out and pulverize it and pass it through an 80-mesh sieve to obtain the solid dispersion of rosuvastatin calcium.

Embodiment 3

[0038] Example 3 Preparation of Rosuvastatin Calcium Solid Dispersion

[0039] Combine 35g polyethylene glycol 4000 and 28g Add S100 to 300ml chloroform one after another, stir until dissolved, add 20g rosuvastatin calcium dissolved in a small amount of chloroform while stirring, rotary evaporate below 45°C, evaporate the chloroform, quickly pour it into a petri dish, and freeze in the refrigerator The layer is placed for 6 hours, and then freeze-dried for 24 hours. After being embrittled, it is taken out and pulverized and passed through an 80-mesh sieve to obtain a solid dispersion of rosuvastatin calcium.

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Abstract

The invention relates to a rosuvastatin calcium oral solid preparation and applications thereof. The rosuvastatin calcium oral solid preparation is prepared in tablets and capsules by a solid dispersion technology so as to increase the stability of the preparation, simultaneously enable the medicine to be released slowly and continuously and further effectively avoid the adverse effect caused by peak-valley fluctuation of the blood concentration.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, and relates to an oral solid preparation of rosuvastatin calcium and its application, in particular to a tablet of rosuvastatin calcium and its application. Background technique [0002] Vascular disease is a kind of disease that seriously endangers human health. In recent years, the morbidity and mortality of this type of disease have shown an obvious upward trend in both western and eastern countries. According to the statistics of the World Health Organization, about 15 million people die of cardiovascular and cerebrovascular diseases in the world every year. In my country, the incidence of cardiovascular and cerebrovascular diseases is as high as 8%, and the mortality rate is close to 50% of the total mortality rate; One person died from cardiovascular and cerebrovascular diseases. Cardiovascular and cerebrovascular diseases are mainly rooted in atherosclerosis, and more...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/20A61K31/505A61K47/32A61K47/34A61P3/06
Inventor 不公告发明人
Owner SUZHOU HOMESUN PHARMA
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