Method for preparing indapamide sustained-release preparation

Abstract

The invention discloses a method for preparing an indapamide sustained-release preparation. The preparation method includes the following steps: premixing microcrystalline cellulose, lactose, indapamide and starch, making acrylic resin, triethyl citrate and talcum powder into a suspension using water, spraying most suspension into the premixed material in an atomizing manner at a high mixing speed and a high cut-off velocity, reducing the mixing speed and adding the remaining suspension, and stirring continuously at a low speed to prepare sustained-release pellets; in combination with pharmaceutically acceptable excipients, carrying out tablet coating or filling hollow capsules to prepare the sustained-release preparation. The method provided by the invention not only solves the defects that the drug applying rate is low, active substances are liable to crystal transformation, and the stability is low, but also solves the problems that the production safety is low and environment pollution is caused due to the use of a large amount of organic solvents when high-viscosity sustained-release framework materials are prepared into granules. The production process of the invention is simple, safe and environment-friendly, and avoids loss of active ingredient substances; the prepared drug can keep a constant release speed after being taken, and can continuously and stably lower the blood pressure.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a preparation method of an indapamide sustained-release agent, belonging to the field of pharmaceutical processing. Background technique [0002] Indapamide, a non-thiazide sulfonamide derivative, is a drug with dual effects of reducing blood pressure and diuresis. By regulating the transmembrane transport of calcium ions, it weakens the contraction of smooth muscle and stimulates the synthesis of prostaglandin vasodilators; at the same time, it has the effect of reversing the left ventricular hypertrophy of the heart to achieve the antihypertensive effect of regulating blood vessels. In short, medium and long-term antihypertensive treatment, indapamide does not affect the metabolism of cholesterol and triglycerides, and is a basic antihypertensive drug. [0003] Indapamide was first launched in Switzerland in 1975 and domestically in 1988. The cur...

AI Technical Summary

Problems solved by technology

For example, in the patent "Indapamide Sustained-release Capsules and Preparation Method" (Patent No. 03104699.1), it adopts the technology of wrapping the sustained-release material layer after applying medicine to the blank core, and dissolves indapamide in absolute ethanol. Finally, it is wrapped on the blank pellet core by a fluidized bed spray system. Although this method can better solve the problem of content uniformity, in actual industrial production, the drug is dissolved in ethanol and dried, and the behavior of drug recrystallization is prone to occur. Affect the stability and bioavailability of medicine, adopt dehydrated alcohol to carry out production simultaneously, the risk factor of production process is higher, is unfavorable for safe production and environmental protection; Patent " a kind of indapamide controlled-release tablet and its preparation method " Patent No. CN101756930B), it adopts the controlled-release tablet prepared by osmotic pump technology. In theory, this technology can better control the release rate of the drug in the body, but the industrial production of this technology is difficult and the production cost is high; the patent "A Indapamide Sustained-release Pharmaceutical Composition and Preparation Method thereof" (Patent No. CN103142529B), which uses HPMC as a sustained-release matrix material, and after mixing the medicine with the matrix material and other adjuvants, water or ethanol is added for granulation to make a sustained-release preparation Product, in this method, due to the high viscosity of the skeleton material HPMC, when water is added as a binder for granulation, because water meets high-viscosity HPMC to form agglomerates, the difficulty of granulation increases, and the drug is in the granulation after the formation of agglomerates. The uniformity of distribution in the block is affected, and the drug that is locally too high will also affect the safety of clinical medication; and in the patent "Preparation Method for Sustained-release Tablets Containing Indapamide Drugs" (Patent No. 102579382), the HPMC is granulated separately and then mixed with other raw materials and excipients to form tablets. In this method, the active ingredient does not enter the sustained-release matrix material, and the sustained-release effect cannot be achieved uniformly and stably.

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