Phenobarbital sustained-release preparation and preparation method thereof

Abstract

The invention belongs to the field of medicinal materials and carriers, and particularly discloses a phenobarbital sustained-release preparation which comprises a phenobarbital pharmaceutical active component, an excipient and a lubricant. The phenobarbital pharmaceutical active component accounts for 25-60% of the weight of the sustained-release preparation. The excipient is prepared from a gel skeleton material, a swelling material and a diluent, the gel skeleton material accounts for 10-50% of the weight of the sustained-release preparation, the swelling material accounts for 10-30% of theweight of the sustained-release preparation, and the diluent accounts for 0-15% of the weight of the sustained-release preparation. The gel skeleton material is composed of alginate and calcium salt,and the weight ratio of alginate to calcium salt is 2: 1 to 8: 1. The lubricant accounts for 0.7-2.5% of the weight of the sustained-release preparation. After the sustained release preparation disclosed by the invention is used, acid-insoluble gel with good strength is rapidly formed, so that the phenobarbital drug release speed is reduced, the drug can be released and absorbed for a longer time,and the bioavailability of the drug is improved.

Description

technical field [0001] The invention relates to the field of medicinal materials and carriers, in particular to a phenobarbital sustained-release preparation and a preparation method. Background technique [0002] Phenobarbital is a white shiny crystalline powder, and its saturated solution is acidic. It is a long-acting barbiturate. It is mainly used clinically to treat antiepileptic and anticonvulsant and achieve sedative and hypnotic effects. Clinical studies have shown that phenobarbital is well absorbed in the small intestine and ascending colon, but after exceeding the hepatic flexure of the colon, its absorption is very poor, which means that the average absorption window of phenobarbital is 5h or less. In terms of medication for patients, If the drug can be developed into a once-daily sustained-release formulation, it can improve patients' medication compliance, reduce or prevent dose-related adverse reactions, and improve efficacy. However, there are some problems ...

AI Technical Summary

Problems solved by technology

Clinical studies have shown that phenobarbital is well absorbed in the small intestine and ascending colon, but after exceeding the hepatic flexure of the colon, its absorption is very poor, which means that the average absorption window of phenobarbital is 5h or less. In terms of medication for patients, If the drug can be developed into a once-daily sustained-release formulation, it can improve patient compliance, reduce or prevent dose-related adverse reactions, and improve efficacy

However, there are some problems in the common sustained-release preparations of phenobarbital developed at present. When the sustained-release preparations of phenobarbital are transferred to the colon flexure after about 5 hours of administration, the medicine will be wasted and cannot play any role. Barbiturate is mainly composed of phenobarbital, matrix forming agent and swelling agent. This dosage form stays in the stomach through the size change after swelling, thereby prolonging the drug absorption time in the stomach and improving the efficacy of the drug; but this type of preparation has certain limitations. The sudden release effect of the drug is not conducive to controlling the slow and stable release of the drug, and the size of the preparation after rapid swelling is not significantly larger than the diameter of the human pylorus. sustained release mode