Study On Preparation Process And Quality Standard Of Berberine Hydrochloride Sustained-release Tablets

Berberine hydrochloride is the main active ingredient of Coptidis Rhizoma.Traditional Chinese Medicine mainly uses Coptidis Rhizoma to treat gastrointestinal infections such as diarrhea,dysentery and malaria,and is also used in the treatment of"emaciation-thirst disease".In recent years,pharmacological studies have shown that berberine has the functions of lowering blood sugar,lowering blood lipid,anti-inflammation and anti-oxidation,and has a better mitigation and prevention effect on the complications of type 2 diabetes mellitus and diabetes mellitus,such as cardiovascular disease,hypertension and hyperlipidemia.Diabetes is a chronic disease requiring long-term medication,the current Western medicine with short-term treatment has significant hypoglycemic effect but it will have a lot of adverse reactions to the human body.The natural active ingredient berberine,which has a wide range of sources,small toxic and side effects,safe and effective,and low in price,is expected to be a long-term medication option for the treatment of type 2 disabetes and its complications.The available berberine hydrochloride dosage forms on the market are ordinary tablets and capsules.In order to reduce the number of patients to take medication,maintain stable blood concentration in the body,improve patient compliance,according to the physical and chemical properties of berberine hydrochloride and requirements of sustained-release preparation.This project innovatively uses the new technology of pharmaceutical preparation to develop berberine hydrochloride sustained-release tablets,which will provide a certain experimental basis for the future registration of drugs for the treatment of type 2 diabetes.In this paper,the formulation and preparation process of berberine hydrochloride sustained release tablets were optimized.Taking the extracorporal release rate as the investigation index,the skeletal material,release rate regulator,filler,adhesive and lubricant of berberine hydrochloride sustained release tablets were screened.The L9(3~4)orthogonal test method was used to optimize the prescription of berberine hydrochloride sustained-release tablets,and three batches of process were verified to determine the optimal prescription and preparation process of berberine hydrochloride sustained-release tablets.The results showed that the prescription process was feasible and reproducible.The quality standard of the sustained release tablets of berberine hydrochloride was also studied in this paper.The characters of berberine hydrochloride sustained-release tablets,the difference of tablet weight,hardness and brittleness were examined.The methods of dissolution in vitro and the determination of drug release and content were established,and the corresponding methodological studies were carried out.The results showed that the characters,weight difference,hardness and brittleness of berberine hydrochloride sustained-release tablets were all in accordance with the relevant provitions of Chinese Pharmacopoeia,and the release degree and content determination method were sensitive,precise and accurate.The preliminary stability of berberine hydrochloride sustained-release tablets was studied.The influencing factors(high temperature,light and high humidity)were tested on a batch of berberine hydrochloride sustained release tablets,and the acceleration test and long-term test were carried out on three batches of berberine sustained release tablets.The results showed that berberine hydrochloride sustained-release tablets had no significant change in the characteristics,release degree,content and other indicators when placed under high temperature,light and high humidity,accelerated and long-term test conditions for 3 months.The experimental results show that the optimized formulation of berberine hydrochloride sustained-release tablets is reasonable,the process is stable and feasible.And the establishment of quality standards lays a foundation for the quality control of the preparation,and the stability study provides corresponding reference materials for the packaging selection,storage conditions and expiration date of the drug.