[Studies on the bioavailability of nitrendipine tablet]

Area of Science:

• Pharmaceutical Sciences
• Pharmacokinetics
• Drug Formulation

Background:

• Nitrendipine tablets manufactured in China exhibit low oral bioavailability.
• Improving nitrendipine bioavailability is crucial for therapeutic efficacy.

Purpose of the Study:

• To develop a novel nitrendipine tablet formulation with enhanced bioavailability.
• To compare the in vitro and in vivo performance of the new formulation against conventional and reference products.

Main Methods:

• A new tablet formulation was developed using a milling method.
• Comparative in vitro and in vivo studies were conducted using conventional tablets (A, C) and a reference tablet (B).
• Pharmacokinetic parameters were determined using GC-MS and nonlinear least square analysis.

Main Results:

• The relative bioavailability of the new formulation (D) was 138.9% compared to the reference tablet (B).
• Conventional Chinese tablets (A, C) showed significantly lower relative bioavailability (31.8% and 72.2%, respectively).
• The new formulation D demonstrated superior extent and rate of absorption compared to the reference tablet B.

Conclusions:

• The milling method successfully improved nitrendipine bioavailability.
• The new tablet formulation D offers a superior alternative to existing products, including imported ones.
• This enhanced formulation holds promise for improved therapeutic outcomes in patients requiring nitrendipine.