Novel dosage form of sinomenine medicament or hydrochlorate thereof and preparation technique thereof

Abstract

The invention discloses a sinomenine or an enteric-coated controlled-release tablet of hydrochloride thereof. The prepared enteric-coated controlled-release tablet hardly releases the drug in artificial simulated gastric juice, but can slowly and smoothly release the drug in artificial simulated intestinal juice; the sustained release time of the drug can achieve more than 12 hours or even 24 hours; the enteric-coated controlled-release tablet is taken once or twice daily, the plasma drug concentration in vivo is smooth, and the peak-valley phenomenon of the plasma drug concentration is reduced; as the prepared enteric-coated controlled-release tablet hardly releases the drug in stomach, the contacted concentration of the drug with the gastric mucosa is small, the stimulation of the stomach caused by the drug is alleviated. As the prepared enteric-coated controlled-release tablet sustainedly slowly releases the drug in intestinal tract, the times of the drug administration are reduced, and the patient compliance is improved, thereby being applicable to the needs of the clinical development.

Description

technical field [0001] The invention relates to a new drug dosage form of sinomenine or its hydrochloride, in particular to a sinomenine or its hydrochloride enteric-coated controlled-release tablet and a preparation process thereof. Background technique [0002] Sinomenine (sinomenine) is the main active ingredient in the rhizomes of Chinese medicine Fangjiaceae plants such as Qingfengteng and Xunfengteng. At present, its hydrochloride is mainly used clinically. Sinomenine hydrochloride is a long needle-like crystal with a melting point of 233°C , easily soluble in water and dilute sodium hydroxide, soluble in ethanol, insoluble in chloroform and ether, and the equilibrium solubility in water, 0.1mol / L hydrochloric acid, pH6.8 phosphate buffer solution is 42.57, 23.73, 58.84 mg / ml. Sinomenine has pharmacological effects such as anti-inflammation, immunosuppression, analgesia, lowering blood pressure, anti-arrhythmia, anti-allergy, releasing histamine, and affecting gastroi...

AI Technical Summary

Problems solved by technology

At present, the existing sinomenine preparations mainly include enteric-coated film-coated tablets, sinomenine gel matrix sustained-release tablets twice a day, and injections, etc. Due to the constraints of various factors, the existing dosage forms are far from being suitable for clinical needs.

Due to the low bioavailability and short half-life of sinomenine when administered orally, clinical treatment of rheumatism and rheumatoid diseases requires long-term medication. Due to its strong histamine release effect, a large dose can cause some patients to develop Scalp and face itching, flushing, pain, aggravated swelling, accompanied by rash, sweating, occasional abdominal pain, gastric discomfort, etc.; the blood concentration of sinomenine ordinary enteric-coated tablets is very low for a period of time at the beginning, and then rapidly release, the blood concentration suddenly rises, and there is an obvious peak; compared with other common preparations, sinomenine hydrochloride gel matrix sustained-release tablets have the characteristics of stable blood concentration in the body, fewer administration times, and longer duration of drug effects. , but the clinical application found that its toxic and side effects are also obvious, mainly manifested as severe gastrointestinal allergic reactions, especially the stimulation of gastric mucosa; general topical preparations are difficult to penetrate the skin into the lesion, and it is difficult to obtain a satisfactory therapeutic effect

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