Selecting Developing Agent In Synthesis Process Of Roxatidine Acetate By TLC

Peptic ulcer (PU) has an experience of a gastrointestinal mucosa and submucosa muscle necrosis in the pathological injury. It has to build a healing epithelial tissue and connective tissue. H2- receptor antagonists set up the H2- receptor selectively on the membrane so that the cell wall of cyclic amp (cAMP) is generated and reduced gastric acid secretion. H2 receptor antagonist not only is inhibited to histamine-stimulated acid secretion, but also the gastrin is partially inhibited and the acid secretion which stimulated by acetylcholine is inhibited.The pathogenesis of digestible ulcer and the cure function for H2-Receptor antagonists were reviewed in this paper. The pharmacological peculiarity of the fourth histamine H2-Receptor antagonists(Roxatidine) is described in much detail.Roxatidine acetate is usually obtained from 3-hydroxybenzaldehyde by chemosynthesis. Researches on detecting of source material, intermediates and the end products are seldom reported as well as quality control of the production process.This project, which as a part of"industrial production of roxatidine acetate", studies on the determination methods on objects that involve in the chemosynthesis process and the stability of the main product. It helps give the necessary scientific basis for setting down the determination and control standards of synthesizing, separation and conservation of roxatidine acetate as GMP requires.Based on the demanding of high efficiency and convenient of the determination method for industrial producing. This paper discusses the combined determination method of TLC in tracing the chemosynthesis process.TLC experiments showed that when choose petroleum ether: chloro form:acetone: ethanol (23:12:2:3;V/V/V/V) as developer, Rf of intermediates and the end products can be controlled between 0.3～0.5, objects can be well separated on silicagel plate. The Rf of roxatidine acetate, N-{3-[3-(1- piperidinylmethyl) phenoxy]propyl}amine and N-{3-[3-(1-piperidinylmethyl) phenoxy]propyl} amine was 0.42 respectively. It can be regarded as a main detecting method for quickly tracing the chemosynthesis process.The applying of determination method of TLC can analyze all objects that involved in the chemosynthesis process. Meanwhile, technical parameter of quality control for synthesizing, separation and preservation of roxatidine acetate were found out by studying the stability of it. It gives credible references to industrial producing of roxatidine acetate and technical references of quality control to other natural products.