Journal of Medicinal Materials, 2021, Vol. 26, No. 5 (pp. 300 - 307)

PREPARATION AND CHARACTERIZATION OF STEPHANIA

DERIVED - L - TETRAHYDROPALMATINE DRIPPING PILLS

Tran Trong Bien^1,*, Hoang Thi Ngoc Anh², Nguyen Thi Thanh Duyen¹, Dao Anh Hoang³

¹Hanoi University of Pharmacy, Hanoi, Vietnam; ²Dai Nam University, Hanoi, Vietnam;

 ³National Institute of Medicinal Materials, Hanoi, Vietnam

*Corresponding author: trantrongbien@gmail.com

(Received August 30^th, 2021)

Summary

Preparation and Characterization of Stephania Derived - L-Tetrahydropalmatine Dripping Pills

The objective of this work was to enhance the aqueous dissolution behaviour of a poorly water-soluble alkaloid drug namely l-tetrahydropalmatine (THP), a widely used sedative drug extracted from herbs belonging to Stephania sp., by developing a new THP dripping pills (THP-DPs) formulation using melt mixing-dropping technique with Polyethylene glycol 4000 (PEG 4000) as a main carrier and Glycyrrhizic Acid (GA) as a dissolution stabilizer. After screening experiments, the optimum formulation was THP : PEG 4000 : GA = 1 : 5.64 : 0.36 (w/w) with the technical conditions of melting liquid temperature 65^oC; the condensate temperature 0-2^oC; dropping distance 15 cm; dropping speed 20 ± 2 drops/min and condensate height 40 cm. The formation of THP-DPs was confirmed by using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD), and Fourier-Transform Infrared Spectroscopy (FT-IR). All the physical characterization information proved the formation of THP-DPs, and the results illustrated the superiority of the DPs in dissolution. And the stability of prepared THP-DP was also in a good state after one month in accelerated conditions. These results showed the DPs was an effective new approach for pharmaceutical application.

Keywords: l-tetrahydropalmatine, Dripping pills, Polyethylene glycol, Glycyrrhizic acid, Pharmaceutical.