Preparation of inclusion complex of nepirolol hydrochloride hydroxypropyl beta-cyclodextrin

Nebirolol hydrochloride is mainly used in the treatment of hypertension. Compared with similar drugs on the market, it has fewer adverse reactions.
Pharmacological action is unique. Oral administration is one of the most commonly used and convenient dosage forms. However, the bioavailability of Nebirolol Hydrochloride Tablets on the market varies greatly among individuals. The bioavailability of Nebirolol Hydrochloride Tablets for patients with strong metabolic type is only 12%.
The reason may be related to the first-pass effect of liver, low drug solubility and degradation in different degrees in gastrointestinal tract. Therefore, improving the solubility and stability of drugs and changing the way of drug absorption are important means to improve the bioavailability of oral drugs.
Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) is considered as an ideal inclusion material because of its high water solubility, weak nephrotoxicity, little irritation to mucosa and good safety. In the phase solubility study, the solubility of nepimolol hydrochloride in HP-beta-CD solution with different concentration was determined. The solubility of nepimolol hydrochloride increased linearly with the increase of HP-beta-CD concentration. The phase solubility diagram of nepimolol hydrochloride was typical AL type, which verified the formation of inclusion complex and the inclusion ratio was 1:1.
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