Novel penetration and controlled-release medicament delivery system and preparation method thereof

Abstract

The invention provides a penetration and controlled-release medicament delivery system for low-solubility active medicaments. The system is characterized in that: the system comprises a sheet core consisting of a medicament containing layer and a boosting layer, an isolation coat layer, and a controlled-release coat layer with medicament releasing holes and an unnecessary aesthetic coat, wherein the medicament containing layer comprises the low-solubility active medicaments and hydrophilic polymer support; and the boosting layer comprises penetration-promoting polymer, unsoluble polymer and an osmotic pressure promoting agent. The invention also provides a method for preparing the penetration and controlled-release medicament delivery system, which comprises the following steps of: (1) preparing the medicament containing layer; (2) preparing the boosting layer; (3) preparing the sheet core; (4) coating an isolation coat; (5) coating a controlled-release coat; (6) perforating coating tablets; and (7) coating the aesthetic coat.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, including providing an osmotic controlled-release drug delivery system and a preparation method thereof, which are especially suitable for controlled-release administration of drugs with low solubility. Background technique [0002] Oral osmotic pump preparations are made by using the principle of osmotic pressure to release drugs uniformly and at a constant rate, and are the most ideal oral controlled-release preparations so far. ALZA Corporation of the United States first developed osmotic pump controlled-release tablets in 1970. Since 1983, more than ten products have been on the market, all of which are administered once a day. The drug release rate of the osmotic controlled release drug delivery system can be several orders of magnitude higher than that through the diffusion controlled release barrier (such as the matrix drug release system), and the constant release characteristic...

AI Technical Summary

Problems solved by technology

[0008] (1) The water absorption rate and hydration rate of polyoxyethylene are slow, and the drug release time lag is long

[0009] (2) Polyoxyethylene has a low glass transition temperature (65°C to 67°C), poor thermal stability, and instability in the preparation and storage of osmotic pump tablets

For example, during the granulation process, the drying temperature of polyoxyethylene should usually not exceed 40°C, which will easily cause a high residual amount of organic solvents. If the drying is to be relatively complete, a relatively long drying time will be required, which will cause adverse effects on the quality and release of the preparation. Influence; in the high-speed tableting process, the die will generate heat after repeated use, which may easily lead to adverse phenomena such as sticking and punching during the tableting process; therefore, special cooling facilities are required to control the temperature of the die or reduce the tableting speed

[0010] (3) Polyoxyethylene is prone to degradation under high temperature and oxidation conditions, and the molecular weight decreases, resulting in a decrease in solution viscosity, which will affect the release of controlled-release tablets to a certain extent, making the release faster

[0011] (4) The cost of auxiliary materials is high

However, this osmotic pump controlled-release tablet also has some disadvantages: povidone and copovidone materials have strong water absorption and are easy to absorb moisture and get damp, which will have a certain impact on the long-term stability of some moisture-sensitive compounds

[0013] In addition, during the preparation of osmotic pump controlled-release tablets, we also found that there are some inherent disadvantages in directly coating the controlled-release film on the outside of the double-layer tablet core. Most of the solvents used for the controlled-release coating are organic solvents. It is acetone, and acetone has very strong dissolving power, and can dissolve some components of the drug-containing layer and the booster layer in the tablet core composition, so that a large number of tablet core components including active pharmaceutical ingredients adhere to the controlled-release coating film, During the swelling and release process of the osmotic pump formulation in the water environment, the shear force between the tablet core and the controlled-release coating increases, making it difficult for the drug in the drug-containing layer to be fully released.

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