發(fā)布時間：2018-08-06 11:27

【摘要】：微囊化技術是指利用天然或者合成的高分子包囊材料,將固體、液體或氣體物質包在微小、半透性或密封的囊內,使內容物在特定條件下以可控的速率進行釋放的技術。 本文利用三種理化性質截然不同的模型藥物,篩選出各自有針對性的處方和工藝條件,對制備微囊和微球有理論指導意義;實驗通過對噴霧干燥制備微囊的介紹和影響因素的探究,找出了影響藥物微囊化的因素及解決辦法,并將影響因素分為工藝因素和處方因素兩方面。處方影響因素包括藥物及囊材的選擇及濃度、藥物與囊材的比例、各種輔料的用量及選擇;工藝影響因素包括進料速率、霧化壓力、進風溫度等。同時本文制定了微囊評價的的質量標準,通過對其評價指標如微囊載藥量、包封率、粒徑大小、粒徑分布、微囊外觀、釋放度等方面的測定,找出了噴霧干燥制備微囊的最佳工藝條件和最佳處方。并對樣品分別進行了穩(wěn)定性考察,結果表明被檢測樣品符合質量標準。 在乙醇不溶性藥物的噴霧干燥實驗中,我們選取二甲雙胍作為模型藥物,并以此制備二甲雙胍緩釋微囊。我們經過對單因素考察確定了噴霧干燥法制備二甲雙胍微囊的工藝及處方的大致范圍,并利用正交試驗法確定了最優(yōu)工藝及處方條件,得到最優(yōu)參數為:噴霧干燥法制備微囊的最佳處方為囊材用量為5%,芯材比1:3,增塑劑用量為5%,抗粘劑的用量為20%;進風溫度145℃,出風溫度80℃,噴霧壓力0.30Mpa,進料速度10ml/min。經考察,二甲雙胍微囊具有良好的緩釋效果,且粒徑分布均勻,穩(wěn)定性良好。 在乙醇可溶性藥物的噴霧干燥實驗中,我們選取具有苦味的羅紅霉素作為模型藥物制備微囊,并以掩味效果作為新的評價指標之一。我們經過對單因素考察確定了噴霧干燥法制備羅紅霉素微囊的工藝及處方的大致范圍,并利用正交試驗法確定了最優(yōu)工藝及處方條件:進風溫度170℃,出風溫度80℃,噴霧壓力0.40Mpa,進料速度15ml/min;處方因素:囊材Eudragit L100用量為6%,芯材比1:4,增塑劑用量為5%,抗粘劑的用量為20%。同時,所制得微囊包封率在95%上,同時微囊具有良好的掩味效果。 在液體藥物固體化實驗中,我們選取的模型藥物為維生素A,以提高維生素A的穩(wěn)定性,使其更便于貯藏和應用。本文主要研究了噴霧干燥法制備維生素A微囊的制備工藝、理化性質和穩(wěn)定性。我們探究了影響維生素A微囊化的多種因素,如壁材的濃度,芯材的質量,高速剪切轉度,并對工藝因素等進行了研究并利用正交試驗進行優(yōu)化,確定最優(yōu)實驗條件如下:進風溫度175℃,攪拌時間35min,攪拌速度4800 r/min,霧化壓力0.26MPa。囊材用量6%、乳化劑用量2.5%、芯材比0.55:1、油水相比例20%。所得微囊固體化效果良好,穩(wěn)定性良好。 實驗結果表明,對三種不同類型藥物利用噴霧干燥法制備微囊,均取得了良好的效果,達到了預期期望。
[Abstract]:Microencapsulation technology refers to the technology of using natural or synthetic polymer encapsulation materials to encapsulate solid, liquid or gaseous substances in tiny, semi-permeable or sealed capsules, so that the contents can be released at a controllable rate under certain conditions. In this paper, three different physicochemical properties of model drugs were used to screen out their respective prescriptions and technological conditions, which have theoretical significance for the preparation of microcapsules and microspheres. Through the introduction of the preparation of microcapsules by spray drying and the study of the influencing factors, the factors affecting the drug microencapsulation and their solutions were found out, and the influencing factors were divided into two aspects: technological factors and prescription factors. The factors influencing prescription include the choice and concentration of medicine and capsule material, the ratio of drug to capsule material, the dosage and selection of various excipients, and the technological factors include feed rate, atomization pressure, inlet air temperature and so on. At the same time, the quality standard of microencapsulation evaluation was established, and the evaluation indexes such as drug loading, encapsulation efficiency, particle size, particle size distribution, appearance and release of microcapsules were determined. The optimum conditions and prescription of spray drying for preparation of microcapsules were found out. The stability of the samples was investigated, and the results showed that the samples met the quality standard. In the spray drying experiment of ethanol insoluble drugs we selected metformin as model drug and prepared metformin sustained-release microcapsules. The preparation process of metformin microcapsules by spray drying method and the general range of its formulation were determined by single factor investigation, and the optimum process and prescription conditions were determined by orthogonal test. The optimum parameters are as follows: the best formulation for the preparation of microcapsules by spray drying method is as follows: the amount of capsule material is 5, the ratio of core to material is 1: 3, the amount of plasticizer is 5 and the amount of anti-viscosity is 20. The inlet temperature is 145 鈩，

本文編號：2167594