Preparation of hydroxypropyl betadeclodextrin inclusion compound with neperol hydrochloride

Neprorol hydrochloride is mainly used to treat high blood pressure and has fewer adverse reactions than similar drugs that have been marketed.The pharmacological action is unique.Oral administration is one of the most commonly used and convenient dosage forms for drug administration. However, the bioavailability of currently marketed nevilol hydrochloride tablets varies greatly among individuals, and for patients with strong metabolic type, the bioavailability is only 12%, the reason may be related to the first-pass effect of liver, low solubility of drugs, and different degrees of degradation in gastrointestinal tract.Therefore, improving the solubility and stability of drugs and changing the absorption pathway of drugs are important means to improve the bioavailability of oral drugs.Hydroxypropyl-beta-cyclodextrin (hp-beta-cd) is an ideal inclusion material due to its high water-solubility, weak renal toxicity, almost no stimulation to the mucosa and good safety.In the phase solubility study, the solubility of nebiolol hydrochloride in hp-bet-cd solution with different concentrations was determined. The drug solubility increased linearly with the increase of hp-bet-cd concentration. The phase solubility diagram showed the typical AL type, which verified the formation of inclusion complex and the inclusion ratio was 1:1.Shandong binzhou zhiyuan biotechnology co., ltd. has a professional production, research cyclodextrin derivatives team, and provide customized services.Welcome to the large and medium-sized enterprises to inquire, 0543-2616568.