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Sustained release liquid preparation using sodium alginate for eradication of Helicobacter pyroli
H Katayama1, T Nishimura, S Ochi
1Fukuyama University, Faculty of Pharmacy and Pharmaceutical Sciences, Hiroshima, Japan.
Abstract:
We prepared a new liquid preparation for eradication of Helicobacter pylori (HP), and examined drug release in vitro and in vivo. The liquid preparation mainly consisted of a sodium alginate (AG) aqueous solution containing ampicillin (ABPC), an antibiotic drug, or methylene blue, a dye. Drug release was retarded by Ca pre-treatment (0.10 M, 20 s) of the AG preparation in in vitro drug release studies due to gel-formation at the liquid surface. In in vivo experiments, the AG preparations were administered orally to rats. The rats were divided into two groups, with or without pre-administration of ranitidine hydrochloride (RH, an H2-blocker). The total remaining % of ABPC in the stomach was high in the rats administered the AG preparation compared to the ABPC solution. The AG preparation might float in the stomach without adhering to the gastric wall in the rats without pre-administration of RH. The total remaining % of ABPC at 30 min was almost 100% in the RH pre-administration rats administered the AG preparation, and about 80% of the drug existed in fraction 2 (implying adhesion of the preparation on the gastric mucus). At 60 min, the total remaining % in the AG preparation plus Ca (mean 87%) increased about 2-fold compared to that in the AG preparation alone (mean 44%). In this case, a large portion of the remaining ABPC also existed in fraction 2. This preparation may be useful for eradication of HP.
Insights
A novel liquid preparation using sodium alginate enhanced antibiotic retention in the stomach for potential Helicobacter pylori eradication. Calcium pre-treatment improved drug adhesion and prolonged drug presence.
Area of Science:
- Pharmaceutical Sciences
- Gastroenterology
- Drug Delivery Systems
Background:
- Helicobacter pylori (HP) infection is a major cause of gastrointestinal diseases.
- Effective eradication requires sustained drug levels at the infection site.
- Current treatments face challenges with drug release and gastric retention.
Purpose of the Study:
- To develop and evaluate a novel liquid preparation for improved Helicobacter pylori eradication.
- To assess the in vitro and in vivo drug release characteristics of the preparation.
- To investigate the effect of calcium pre-treatment and ranitidine hydrochloride on drug retention.
Main Methods:
- A liquid preparation of sodium alginate (AG) containing ampicillin (ABPC) was formulated.
- In vitro drug release was studied with and without calcium (Ca) pre-treatment.
- In vivo studies involved oral administration to rats, with and without ranitidine hydrochloride (RH) pre-administration.
- Gastric retention and drug adhesion were assessed over time.
Main Results:
- Calcium pre-treatment of the AG preparation retarded in vitro drug release due to gel-formation.
- In vivo, the AG preparation showed higher ampicillin retention in the stomach compared to a simple solution.
- Ranitidine hydrochloride pre-administration resulted in nearly 100% ABPC retention at 30 minutes, with significant adhesion.
- Calcium addition further increased ABPC retention and adhesion at 60 minutes.
Conclusions:
- The novel sodium alginate liquid preparation demonstrates enhanced gastric retention of ampicillin.
- Calcium pre-treatment and ranitidine hydrochloride significantly improve drug adhesion and prolong its presence in the stomach.
- This formulation holds promise as a potential therapeutic strategy for Helicobacter pylori eradication.