Preparation and preliminary quality evaluation of aspirin/L-glutamate compound pellets

Mengchang Xu,Songwen Tan,Fenglin Liu,Wenhu Zhou,Binsheng He

doi:10.1007/s10856-021-06594-8

Abstract

L-glutamate is an important component of protein. It can prevent gastrointestinal damage caused by NSAIDs. We constructed two-phase enteric-coated granules of aspirin and L-glutamate compound by extrusion spheronization method and fluidized bed coating. The subliminal effective dose of L-glutamate is 100 mg/kg tested by model of gastric ulcer of rats induced by aspirin and drug administration. HPLC-UV and UV–Vis methods were adopted to determine content and cumulative release of aspirin and L-glutamate as quality analysis method indexes. The prescription and process optimization were carried out with yield, sphericity and dissolution. The two-phase compound granules have good sphericity of 0.93 ± 0.05 (aspirin pellets) and 0.94 ± 0.02 (L-glutamate pellets), content of salicylic acid (0.24 ± 0.03)%, dissolution of aspirin (2.36 ± 0.11)%. Quality evaluation and preliminary stability meet the commercial requirements. The stored environment of compound preparation should be sealed in a cool and dark place.

Highlights

It can be seen that the gastric injury effect of Non-steroidal anti-inflammatory drugs (NSAIDs) has become a huge obstacle to the clinical use of such drugs, and it is of great clinical significance to find a safe and effective way to prevent gastric injury caused by NSAIDs
The common methods to prevent gastric injury caused by NSAIDs include the combination use of antiulcer drugs or mucosal protection drugs, or use of selection COX-2 inhibitors, dual pathway inhibitors of COX and 5-LOX [6]
The most common anti-ulcer drug to protect gastric injury caused by NSAIDs is proton pump inhibitor (PPI)

Summary

Introduction

The most common anti-ulcer drug to protect gastric injury caused by NSAIDs is proton pump inhibitor (PPI). PPI can effectively inhibit incidence of gastric ulcers caused by NSAIDs, while long-term use of PPI can cause fractures (hip, wrist, and spinal) and gastrointestinal microbial homeostasis [7,8,9]. Gastric mucosal protective drugs such as misoprostol can effectively reduce the gastric ulcer caused by NSAIDs, but the effect on dyspepsia is poor which limits its application [10]. COX-2 selection inhibitors can significantly reduce gastrointestinal adverse reactions [11]. COX and 5-COX dual pathway inhibitors have anti-inflammatory and analgesic effects almost no gastrointestinal side effects, but benzoxprofen was withdrawn from global market due to severe hepatotoxicity [12]. There is still no ideal approach to gastric injury resistance caused by NSAIDs

Methods

Results

Conclusion