本文選題：肛裂　切入點(diǎn)：地爾硫革　出處：《湖北中醫(yī)藥大學(xué)》2014年碩士論文　論文類型：學(xué)位論文

【摘要】：背景： 肛裂是一種在臨床上十分常見(jiàn)的肛腸疾病,其臨床癥狀主要表現(xiàn)為便痛、便血。目前認(rèn)為主要發(fā)病機(jī)制是由于肛門處括約肌高度緊張而導(dǎo)致肛管靜息壓力增加,繼而進(jìn)一步誘發(fā)肛管后中線供血不良而導(dǎo)致缺血性的潰瘍。 鹽酸地爾硫(?)是一種苯并硫氮雜(?)類化合物,為鈣離子通道阻滯劑,口服時(shí)藥物通過(guò)血液轉(zhuǎn)運(yùn)、分布,抑制心臟與血管平滑肌去極化時(shí)的鈣離子內(nèi)流從而發(fā)揮其藥理作用,臨床上常用于心動(dòng)過(guò)速、心絞痛和高血壓的治療。最近國(guó)外研究顯示局部應(yīng)用鹽酸地爾硫革,能夠使肛管平滑肌松弛,降低肛管內(nèi)靜息壓力,減輕便血、便痛等臨床癥狀；擴(kuò)張血管,改善缺血區(qū)供血,從而達(dá)到治療肛裂的效果。 方法： 本課題以羥丙基甲基纖維素作為凝膠基質(zhì),采用溶脹法制備凝膠。通過(guò)單因素實(shí)驗(yàn)考查羥丙基甲基纖維素的濃度對(duì)凝膠黏度的影響,篩選出適宜凝膠羥丙基甲基纖維素的濃度范圍。通過(guò)正交實(shí)驗(yàn)設(shè)計(jì),以粘度、離心穩(wěn)定性、體外釋放度作為指標(biāo),篩選出鹽酸地爾硫(?)凝膠的最佳的處方。采用高效液相色譜法,對(duì)所制備鹽酸地爾硫(?)凝膠進(jìn)行含量測(cè)定,并且通過(guò)專屬性試驗(yàn)驗(yàn)證含量測(cè)定方法的可靠性。對(duì)所制備的鹽酸地爾硫(?)凝膠進(jìn)行初步穩(wěn)定性試驗(yàn),考察在室溫條件下放置3個(gè)月所制備凝膠的性狀、pH、含量以及有關(guān)物質(zhì)的變化情況。 結(jié)果： 處方篩選結(jié)果表明,最佳處方中鹽酸地爾硫(?)、羥丙基甲基纖維素、甘油和丙二醇的用量分別為2%、2%、15%、10%,并加入0.3%對(duì)羥基苯甲酸乙酯作為防腐劑。含量測(cè)定結(jié)果表明鹽酸地爾硫(?)在10μg/mL90μg/mL濃度范圍內(nèi),峰面積與濃度呈良好的線性關(guān)系,平均回收率為101.0%,RSD=1.08%。通過(guò)專屬性試驗(yàn)證明,高溫、光照、強(qiáng)酸、強(qiáng)堿、氧化等不同條件下強(qiáng)制降解的雜質(zhì)以及空白凝膠對(duì)主藥鹽酸地爾硫(?)的含量測(cè)定均無(wú)影響。初步穩(wěn)定性試驗(yàn)結(jié)果表明鹽酸地爾硫(?)凝膠在室溫下放置3個(gè)月,凝膠的性狀為無(wú)色透明的半固體制劑,pH值變化不大,在5.6～6.1之間。含量在97.9%-100.2%之間,有關(guān)物質(zhì)在0.51%-2.85%之間。
[Abstract]:Background:. Anal fissure is a very common anorectal disease in clinic, and its clinical symptoms are mainly stool pain and bloody stool. At present, it is believed that the main mechanism of anal fissure is the increase of resting anal pressure due to high tension of anal sphincter. In turn, anus posterior midline blood supply is induced to lead to ischemic ulcers. Dilthion Hydrochloride? Is a benzothiazepine? ) compounds, calcium channel blockers, which are transported and distributed through the blood during oral administration, inhibit the influx of calcium ions during depolarization of the heart and vascular smooth muscle and thus play a pharmacological role, and are commonly used in tachycardia clinically. Treatment of angina pectoris and hypertension. Recent foreign studies have shown that local application of diltiazem hydrochloride can relax the smooth muscle of the anal canal, reduce the resting pressure in the anal canal, relieve the clinical symptoms such as bloody stool and stool pain, dilate blood vessels, and improve the blood supply in the ischemic area. So as to achieve the effect of anal fissure treatment. Methods:. In this paper, hydroxy propyl methyl cellulose was used as gel matrix to prepare gel by swelling method, and the effect of concentration of hydroxypropyl methyl cellulose on gel viscosity was investigated by single factor experiment. The optimum concentration range of hydroxy propyl methylcellulose was screened out by orthogonal design, and the viscosity, centrifugation stability and release rate in vitro were used as indexes to screen diltiazone hydrochloride? ) the best formulation of gel. Determination of diltiazone hydrochloride by HPLC. The content of the gel was determined and the reliability of the method was verified by specific test. A preliminary stability test was carried out to investigate the changes of pH, content and related substances of gel prepared at room temperature for 3 months. Results:. The results showed that the best prescription was diltidine hydrochloride? The dosage of HPMC, Glycerol and Propylene Glycol were 2 and 10, respectively, and 0.3% ethyl p hydroxybenzoate was added as preservative. ) within the range of 10 渭 g / mL 90 渭 g / mL, the peak area and concentration showed a good linear relationship, and the average recovery was 101.0% RSD 1.08.The specificity test proved that high temperature, light, strong acid, strong alkali, Under different conditions, such as oxidation, impurity degradation and blank gel to the main drug diltiazem hydrochloride? The results of preliminary stability test showed that diltithione hydrochloride had no effect on the determination of Diltidine hydrochloride. When the gel was stored at room temperature for 3 months, the pH value of semisolid preparation with colorless and transparent properties changed little, ranging from 5.6 to 6.1, the content of gel was between 97.9- 100.2%, and the related substance was between 0.51-2.85%.
【學(xué)位授予單位】：湖北中醫(yī)藥大學(xué)
【學(xué)位級(jí)別】：碩士
【學(xué)位授予年份】：2014
【分類號(hào)】：R943

【參考文獻(xiàn)】

相關(guān)期刊論文 前2條

1 馬小琴,賀同慶,鄭濤,徐冰心,肖成榮,鄭思新,林曉榮,高沛永,申戈,鮑云華,高紅軍,楊武威;地爾硫怡防治腫瘤病人放療不良反應(yīng)的臨床研究[J];中國(guó)藥學(xué)雜志;2004年03期

2 薛武軍,丁小明,田普訓(xùn),潘曉鳴,燕航,侯軍,馮新順,項(xiàng)和立;應(yīng)用環(huán)孢素A的腎移植患者合用地爾硫芯卓的臨床效果觀察[J];中華器官移植雜志;2005年01期

，

本文編號(hào)：1592452