Calciparine/sodium salt nano oral preparation and preparation technique thereof

Abstract

The invention relates to a calcium heparin / sodium salt nano-sized oral preparation and a preparation method thereof, and a calcium heparin / sodium salt nano-sized liposome with high encapsulation rate for preparing the calcium heparin / sodium salt nano-sized oral preparation. The calcium heparin / sodium salt nano-sized liposome is obtained by the following steps: dissolving chitosan in 1-10% dilutedsolution of acetic acid (the usage amount of chitosan is 0.5-5g per 100ml acetic acid solution) to obtain an acidified chitosan solution, filtering, collecting filtrate, adding dropwise 1-99% aqueoussolution of calcium heparin / sodium salt into the filtrate under magnetic stirring until milk white precipitate occurs, centrifugating the resulating suspension, collecting precipitates, and freezes-drying to obtain calcium heparin / sodium salt nano-sized liposome. The calcium heparin / sodium salt nano-sized oral preparation is characterized in that the preparation has good stability, high encapsulation rate (up to 98%), and high in vitro release rate (up to 25% at hour 4); the preparation is absorbed in the intestinal tract with high absorption rate and high concentration; the half life is prolonged upon the increase of oral dosage, showing zero-order kinetics; the tissue concentration is larger than blood concentration; the preparation is released sustainedly; and study in rabbits (20mg oral intake) shows that the blood concentration in vivo is kept high for over 50 hours, thereby proving sustained release.

Description

(1) Technical field [0001] The invention relates to a heparin calcium / sodium nanometer oral preparation, a preparation process and a method thereof, and a heparin calcium / sodium nanometer liposome used for preparing the heparin calcium / sodium nanometer oral preparation. (2) Background technology [0002] Heparin is a commonly used natural anticoagulant. It has been used clinically for more than 70 years. It is mainly used to treat hypertension, cardiovascular disease, stroke, thrombosis, nephrotic syndrome and other diseases. It is widely used and has more than 20 functions. mechanism. Recent studies have found that heparin can inhibit the proliferation and metastasis of malignant tumors, and increase the 5-year survival rate of patients with malignant tumors by more than 90%. However, heparin is only available as an injection, which is inconvenient to use. [0003] In the long-term clinical work, it was found that the patient's compliance with injection heparin was poor, ...

AI Technical Summary

Problems solved by technology

Due to the low encapsulation efficiency of the low molecular weight heparin nano-liposomes prepared by the above method, it cannot reach the 80% standard stipulated in the "Chinese Pharmacopoeia", so there is no literature about the low molecular weight heparin calcium / sodium nanometer oral dosage form at present. According to reports, more oral preparations are put on the market

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