Isosorbide mononitrate osmotic pump type controlled-release preparation and preparation method thereof

Abstract

The invention relates to an isosorbide mononitrate osmotic pump type controlled-release preparation and a preparation method thereof. The preparation can release the isosorbide mononitrate at a constant medicament release rate. The preparation mainly comprises a tablet core, a semipermeable coating film and medicament release pores, wherein the tablet core is prepared from the isosorbide mononitrate, a penetrating agent, a filling agent and other pharmaceutic adjuvants; and the semipermeable coating film is prepared from cellulose acetate or ethylcellulose, a plasticizer and a pore former. Theosmotic pressure on the inner side and the outer side of a semipermeable film is taken as a driving force, and a medicament is released at a zero level release rate to maintain stable internal bloodconcentration. The preparation has the characteristics of moderate internal medicament action time, small side effect, and less drug resistance for repeated dose.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, specifically it is a long-term treatment of coronary heart disease, prevention of vasospasm type and mixed angina pectoris, also suitable for the treatment after myocardial infarction and long-term treatment of chronic heart failure - iso-mononitrate Sorbitate monolayer osmotic pump controlled release preparation and preparation method thereof. Background technique: [0002] Isosorbide mononitrate, molecular formula: C 6 h 9 NO 6 Molecular weight: 191.14 [0003] Molecular formula: [0004] [0005] Isosorbide mononitrate can promote the relaxation of vascular smooth muscle and dilate blood vessels. Its main function is to dilate veins to reduce blood return in veins, thereby reducing the load on the heart. Isosorbide mononitrate also makes systemic arteries and main coronary arteries The arteries dilate. Therefore, taking isosorbide mononitrate will reduce the cardiac load and...

AI Technical Summary

Problems solved by technology

Since its sustained-release mechanism is a gel matrix sustained-release tablet, the drug is released through erosion and diffusion mechanisms, and its drug release rate is greatly affected by environmental factors such as eating, gastrointestinal motility, etc. After individual differences are large, it is difficult to ensure the safety of patients

[0008] Qian Yu (China Pharmaceutical Industry, Volume 16, No. 5, 2007) reported his research on Isosorbide Mononitrate Osmotic Pump Controlled Release Tablets. The dose is 50 mg, and cellulose acetate is used as a semipermeable membrane material. , 4, 6, 8, 10, and 12h in vitro release test results were 16.2%, 40.6%, 57.0%, 70.5%, 79.2%, and 91.5%, but no detailed prescription was given, and its formulation combination was unknown The type and amount of excipients

The disadvantage of this design is that the release is slow with a large dose, which increases the burden on the body's metabolism, resulting in some drug residues in the body when the drug is administered again, which is prone to drug resistance. The biggest problem with the application of isosorbide mononitrate is drug residues. The resulting drug resistance forces patients to interrupt their medication to eliminate the residual drug in the body, and their risk of disease increases greatly during the interruption of medication

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