Intragastric floating slowly releasing micropill and preparation method thereof

Abstract

The invention discloses an intragastric floating slowly releasing micropill preparation and a preparation method thereof. The micropill preparation mainly comprises three parts, namely a light medicament-carrying pill core, a gas-producing layer coating and a blocking layer coating, wherein the light pill core comprises 1 to 40 percent of medicament, 40 to 70 percent of wax material, and 20 to 30 percent of filling agent; the gas-producing layer coating comprises 3 to 7 percent of coating material, 5 to 20 percent of plasticizer, 2 to 8 percent of gas-producing component, and 5 to 20 percent of antiplastering aid; and the blocking layer coating comprises 20 to 50 percent of coating material, 0 to 30 percent of plasticizer, and 10 to 30 percent of antiplastering aid. A spheronization methodand a fluidized bed coating method are adopted to prepare the micropills, the prepared micropills float after entering water and persistently float for 24 hours, and medicaments of the micropills rea lize the slowly releasing effect. The prepared micropills have the characteristics of large distribution area, small local irritation and the like; and the micropill has floating characteristics, greatly prolongs the retention time in stomachs, and ensures that the bioavailability of the medicaments which have best absorption in the stomachs and at special positions of upper parts of small intestines is greatly improved. The micropill is prepared by adopting the prior method, and is easy to realize industrialized production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a stomach-floating sustained-release pellet and a preparation method thereof Background technique [0002] Gastric floating preparations mainly refer to preparations that are designed according to the principle of hydrodynamic balance and can maintain a floating state in gastric juice. It is generally believed that the density of such preparations is generally less than that of gastric juice (1.004-1.01g / cm 3 ), floating in the stomach for a long time and releasing the drug continuously. The advantage of the gastric floating preparation is that the preparation can prolong the residence time of the drug in the stomach, and is suitable for the drug whose absorption site is in the stomach and duodenum, so as to improve the absorption of such drugs, reduce toxic side effects, and stabilize blood. Increase the drug concentration and improve the bioavailability of the drug. [0003...

AI Technical Summary

Problems solved by technology

[0004] Among the existing patents, more than 90% of the patents on gastric floating preparations are related to tablets and capsules, but as a single unit system, its disadvantage is that it may produce sudden release or the floating performance of individual preparations is not good, so it is regarded as Gastric emptying rapidly does not achieve the expected sustained and controlled release effect, and due to individual differences in gastric emptying rates of patients, it often leads to uncertainty and lack of reproducibility of prolonged gastric residence time, so individual differences in drug release are relatively large. Big

Images