| Background:As we know, constipation is one of the common gastrointestinal diseases in the worldwide. In recent years, the prevalence of constipation is rapidly increasing worldwide. Epidemiological investigation demonstrated that the prevalence of constipation varies 0.7%from 79%in the world and 1.4% from 32.9% in Asia according to the report of Centers for Disease Control and Prevention in 2011. The crowd of constipation is extensive and widespread in women, which is higher than men. It aroused more attentions from people since it seriously affects the health of people. In addition, it also may cause the rupture of blood vessels in patient with cardiovascular disease.Currently, the major treatment of constipation is drug including western and traditional Chinese medicine. The western medicine has the advantage of fast effect although it may cause some side effects and does not complete treat constipation. However, Traditional Chinese medicine treat constipation for long time, it has many advantages such as low side and lasting effects. Decoction is the major form of traditional Chinese medicine. Besides, the formulations of Chinese medicine are including enemas, pills, tablets, capsules, patches and poultices. However, these formulations have some disadvantage such as short storage time, first pass effect, intestinal metabolism and so on. Thus, further exploration of these low side effect of formulation in traditional Chinese medicine is urgently needed. Interestingly, recent studies have provided compelling clues that suppository have such merits, such as long-term storage, watch lesion site and voiding hepatic first-pass effect. The suppository may be taken as novel formulation for treatment of constipation, although 6 reports of suppositories were observed in patients with constipation in previous study.To investigate the effect of the suppository of traditional Chinese medicine on loperamide induced rats of constipation. To develop a pharmaceutical dosage form has the advantage including resident long time in the intestine, easy of administration from the end of the colon to the rectum.Method:In compound comfrey suppository, Lithospermum and Houttuynia cordata as king medicine with the efficacy of detoxification and blood cooling. Litchi nuclear as minister because of the effect Qi Sanjie. Humifusae and Fern as adjuvant result from it has the effect of heat dampness. Gall as courier medicine because it meridian enter in lungs, stomach, large intestine and can grabbing the lung, intestinal astringent.Then, the methods of alkali extraction and acid precipitation were employ to obtain comfrey. Besides, the extractions of 5 herbs are water. Then prepare suppositories with emulsion matrix. The methods of TLC and UV-visible spectrophotometry were employ to measure active ingredients of the extractions respectively and suppositories. At the same time, According to the requirement of the suppository of Chinese Pharmacopoeia (2010 version) check the quality of compound comfrey suppository. The model of loperamide-induced constipation, which was judged by measuring the change of total weight, oral-anal transit time, stool water content in 5h, food intake in 24h, water intake in 24h, neurotransmitters content(NO,Ach) and gastrointestinal hormone content (MTL) in plasma observed distal colon histological. The experimental animals were divided into control group, model group, compound comfrey suppository with once a time group, compound comfrey suppository with twice a time group, enema group, TCM group, comparison group. All animal were administered by 14 days. The effects of drug on model of rats were examined by the indicators.Results:In the section of suppositories, the same spots may appear on the corresponding position of the standard product in the TLC test. Besides, the test sample has the corresponding peaks in the similar position of standard in the UV experiment and the wavelength from 200nm to 600nm. The drug and matrix of suppository mixed uniformly. Suppositories have smooth surface, good uniformity and melting fast at 37 ℃. It can melt fully in 19 minutes. Weight is (0.3618±0.02)g and the variation of it is ±0.08%. The stripping of the index components and content, Quercetin and Shikonin, are 75% and 82.4% and 0.02% and 0.01% respectively.In the part of model of the constipation, compared with the control group, the weight change, stool water content, food intake,water intake, stool water content, Ach content and MTL content of model group are reduced significantly(P<0.01). However, the content of NO and oral-anal transit time are increased significantly(P<0.01). In addition, the distal colonic mucosa layer thickness and crypt cells of the model group are reduced compared with the control group.In the part of efficacy study, compared with the model group, the weight change, stool water content, food intake, water intake, stool water content, MTL content, the length of the small intestine and gastric emptying capacity are increased significantly (P<0.01). Furthermore, the increasing of Ach content of administration group has significant differences compared with the control group (P<0.05). Also, the distal colonic mucosa layer thickness and crypt cells of the administration group are increased. The NO content and oral-anal transit time of the administration group are reduced significantly (P<0.01).Conclusion:The quality of compound comfrey suppository has meeted withthe requirement of the suppository of the Chinese Pharmacopoeia (2010 version). The result of efficacy in model rats of constipation showed that the differences between administration group and model group are significant, although they are not significant between different dose groups. According to these results, we have suggested that the suppository has a therapeutic effect on the Loperamide-induced model of constipation. The suppository was applied to treat constipation resulting from promote gastrointestinal peristalsis, increase intestinal moisture content, decrease the water reabsorption of the intestinal. |
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