A fluvastatin sodium microporous osmotic pump controlled-release tablet and preparation method thereof

Abstract

The invention relates to a fluvastatin sodium microporous osmotic pump controlled-release tablet and a preparation method thereof. The preparation comprises a drug-containing tablet core, a semipermeable controlled-release coating film and a common film coating film wrapped outside the tablet core. The core contains fluvastatin sodium, fillers, blockers, osmotic pressure active substances, alkali stabilizers and lubricants; semipermeable coatings include cellulose acetate, porogens and plasticizers; ordinary film coatings Gastric Opadry for film coating premix. The present invention slows down the release rate of the drug by adding a polymer blocker to the tablet core, and then wraps the tablet core with a semipermeable controlled-release coating and a common coating with a light-shielding effect in order to prepare fluvastatin sodium The microporous osmotic pump controlled-release preparation can maintain constant drug release within 24 hours, the blood drug concentration is more stable, the curative effect is long-lasting, the toxicity and side effects are small, and the patient's compliance is good. The preparation process of the preparation is simple and easy for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a fluvastatin sodium microporous osmotic pump controlled-release tablet and a preparation method thereof. Background technique [0002] With the development of social economy, the improvement of people's living standards and the change of lifestyle, the average serum TC (total cholesterol) level of the population is gradually increasing. At the same time, diabetes and metabolic syndrome, which are closely related to dyslipidemia, are developing in my country It is also very common. According to a study published by Professor Yang Wenying of the China-Japan Friendship Hospital of the Ministry of Health, the prevalence of hypercholesterolemia among people over the age of 20 in my country is 9.0%, and the prevalence of borderline hypercholesterolemia is 9.0%. 22.5%, and showing an upward trend. [0003] At present, the commonly used drugs for the clinical treatment of hyper...

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Problems solved by technology

[0004] Fluvastatin (Fluvastatin) is the first fully synthetic HMG-CoA reductase inhibitor developed by "SANDOS" company. It is usually used as sodium salt clinically. Currently, there is only Ordinary capsules (specification: 20mg or 40mg, calculated as fluvastatin) and sustained-release tablets (specification: 80mg, calculated as fluvastatin), of which ordinary capsules need to be administered multiple times a day, and the blood concentration fluctuates greatly. Serious adverse reactions; while fluvastatin sodium sustained-release tablets need to be administered once a day, which improves the patient’s medication compliance to a certain extent, but there are problems of uneven sustained-release effects and non-constant-rate drug release

[0005] Disclosed the pharmaceutical composition of commercially available fluvastatin sodium sustained-release tablet as U.S. Patent US6242003B1, this pharmaceutical composition comprises fluvastatin sodium, hypromellose and other pharmaceutical excipients, but with hypromellose The fluvastatin sodium slow-release preparation, which is a slow-release matrix material, has a slow-release effect after long-term placement (for example, more than 18 months of storage); patent CN101385729A is a combination of osmotic pump controlled-release preparations for the treatment of hyperlipidemia A tablet core composed of acipimox, fluvastatin, a penetration enhancer, a filler, a lubricant, and a layer containing a polymer film-forming material, a plasticizing An osmotic pump controlled-release preparation composed of a semi-permeable film coating of an agent and a pore-forming agent. In this preparation, fluvastatin sodium is released completely within 12 hours, but fluvastatin is absorbed rapidly, and the peak concentration can be reached within 1 hour after taking it on an empty stomach. , and its half-life is short, only 0.5-0.8h. Therefore, the once-a-day acipimox and fluvastatin microporous osmotic pump preparations prepared by this technical scheme are difficult to maintain 24h drug release, and the effective action time of the drug is short

[0006] Patent CN102755284A discloses a sustained release pharmaceutical composition of fluvastatin sodium, the pharmaceutical composition of fluvastatin sustained release uses polyethylene oxide as a controlled release matrix material and a coating containing a light-shielding material, which can effectively solve the following problems: Hypromellose, as a controlled-release matrix material, has the problem that the sustained-release effect of long-term placement is significantly reduced; although the above-mentioned sustained-release tablets solve the trouble of frequent administration of common preparations, due to its non-constant release rate, the release of the drug And the absorption rate will be affected by factors such as the pH of the gastrointestinal fluid in the patient's body; in addition, due to the high solubility of fluvastatin sodium, sustained-release preparations are prone to drug burst release, and the fluctuation of blood drug concentration is still large. The time and the size of side effects vary from person to person and are uncontrollable; therefore, it is necessary to develop fluvastatin sodium controlled-release formulations with a constant release rate

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