Preparation and in Vitro Evaluation of a Self-Microemulsifying Drug Delivery System for Insoluble Drug Nebivolol Hydrochloride

Mingzhi XU; Yucheng CHEN; Tingyu XIAO; Lili HUANG; Huaqing LIN

Return

Preparation and in Vitro Evaluation of a Self-Microemulsifying Drug Delivery System for Insoluble Drug Nebivolol Hydrochloride

VernacularTitle:难溶性药物盐酸奈必洛尔口服自微乳化给药系统的制备以及体外评价
Author: Mingzhi XU ¹ ; Yucheng CHEN ¹ ; Tingyu XIAO ¹ ; Lili HUANG ¹ ; Huaqing LIN ¹
Author Information

1. Guangdong Provincial Key Laboratory of Advanced Drug Delivery, Guangdong Pharmaceutical University, Guangzhou 510006, China
Publication Type:Journal Article
Keywords: nebivolol hydrochloride ； self-microemulsifying drug delivery system ； pseudo-ternary phase diagrams；central composite design-response surface method；dissolution rate
From: Chinese Journal of Modern Applied Pharmacy 2024;41(9):1214-1221
CountryChina
Language:Chinese
Abstract: OBJECTIVE :To prepare a self-microemulsifying drug delivery system(SMEDDS) for the oral administration of nebivolol hydrochloride(NBH) and to conduct in vitro evaluation. METHODS The solubility of NBH was determined using various oil phases, surfactants, and co-surfactants. The composition of the blank self-microemulsifying formulation was determined using pseudo-ternary phase diagrams. A centralcomposite design-response surface method was employed to screen and optimize the formulation variables, and an excess amount of NBH raw material was incorporated to determine the drug loading capacity. RESULTS The optimized composition of the NBH-SMEDDS formulation consisted of medium-chain glycerides, capryl caproyl macrogol glycerides, and 2-(2-ethoxyethoxy) ethyl acetate at a ratio of 20∶48∶32, with a drug loading capacity of 20.05 mg. The particle size, self-emulsification time, and particle size distribution range of the formulation were in agreement with the predicted values. Dissolution testing demonstrated that the overall dissolution trend of NBH-SMEDDS in the medium was higher than that of NBH powder and NBH ordinary tablet. The stability of NBH-SMEDDS was found to be satisfactory under accelerated conditions for 1, 2, and 3 months. CONCLUSION The SMEDDS shows potential for enhancing the in vitro dissolution of NBH and demonstrates good stability.