發(fā)布時間：2018-05-10 16:09

  本文選題：鴉膽子油 + 乳劑　； 參考：《廣東藥學院》2014年碩士論文

【摘要】：當今，惡性腫瘤依然是人類的頭號殺手，化療則是目前主要的治療手段之一，但化療的嚴重副作用卻給患者帶來了很大的痛苦。近年來，由于中藥在腫瘤治療方面具有副作用少、療效較好的優(yōu)勢，已經得到了大家的肯定。鴉膽子油乳劑是臨床上治療腫瘤的常用的中藥制劑之一，主要包括口服乳劑和注射劑兩種劑型。由于乳劑為動力學和熱力學不穩(wěn)定體系，若處方欠佳或保存不當，往往會出現(xiàn)乳滴變大，進而破乳分層等現(xiàn)象，極大影響了產品的質量。本文主要從鴉膽子油乳劑的處方優(yōu)化、制劑的生物等效性進行研究，主要包括以下四部分： 1.鴉膽子油乳劑處方優(yōu)化研究 本文對鴉膽子油乳劑的制備工藝進行了優(yōu)化，并以外觀、離心穩(wěn)定性參數(shù)Ke、平均粒徑和d90為穩(wěn)定性指標，對單獨使用大豆卵磷脂為乳化劑制備鴉膽子油乳劑進行乳化劑用量考察，最終確定單一乳化劑的合適用量為1.4%。通過處方優(yōu)選得到最佳的復合乳化劑配比為大豆卵磷脂-泊洛沙姆188（2.75:1），在乳化劑用量相同的條件下，于一定條件下（30℃和4℃下各12小時交替）放置4周后對比發(fā)現(xiàn)，用該復合乳化劑所制備的鴉膽子油乳劑穩(wěn)定性優(yōu)于單獨使用卵磷脂所制備的乳劑；另外對復合乳化劑的用量進行優(yōu)選發(fā)現(xiàn)，與單獨使用大豆卵磷脂作為乳化劑相比，使用該配比的乳化劑，還可以減少乳化劑的總用量且獲得更好的乳劑穩(wěn)定性。 2.氣相色譜法測定血樣中油酸和亞油酸濃度方法學的建立 本文建立了用氣相色譜法測定全血中油酸和亞油酸含量的分析方法，其色譜條件為色譜柱：Aglient DB-FFAP（30m×0.25mm×0.25μm）；檢測器：300℃；進樣口：250℃；柱溫：205℃；進樣量：2μl；分流比：10:1；載氣流速：1mL·min-1。本方法具有專屬性強、穩(wěn)定性好、準確度高等特點，可滿足樣品測定的需要。 3.處方優(yōu)化后的鴉膽子油乳劑與市售鴉膽子油乳劑的生物等效性研究 把SD大鼠隨機分成兩組，并分別灌胃給予油酸等量的市售鴉膽子油乳劑和處方優(yōu)化后的鴉膽子油乳劑，以AUC0-t、Cmax、Tmax為指標，評價處方優(yōu)化后的鴉膽子油乳劑的生物等效性。實驗結果顯示，處方優(yōu)化后的鴉膽子油乳劑具有生物等效性。 4.平均粒徑大小不同的兩種鴉膽子油乳劑的藥代動力學研究 本文采用相同的鴉膽子油乳劑處方，通過不同的制備工藝得到兩種平均粒徑大小不同的鴉膽子油乳劑，并分別給予兩組大鼠相同劑量的兩種乳劑，實驗結果顯示，大粒徑的鴉膽子油乳劑吸收慢且差，，Cmax和AUC0-t明顯低于小粒徑的乳劑。
[Abstract]:Nowadays, malignant tumor is still the leading killer of human beings, chemotherapy is one of the main treatment methods, but the serious side effects of chemotherapy bring great pain to patients. In recent years, traditional Chinese medicine has been affirmed because of its advantages of less side effects and better curative effect. Brucea javanica oil emulsion is one of the commonly used traditional Chinese medicine preparations in the treatment of tumor, mainly including oral emulsion and injection. Because the emulsion is an unstable system of dynamics and thermodynamics, if the prescription is not good or the storage is not proper, the emulsion droplets will become larger and demulsifying and delamination will occur, which will greatly affect the quality of the product. In this paper, the optimization of the formulation of Brucea javanica oil emulsion and the bioequivalence of the preparation were studied, including the following four parts: 1. Optimization study on the formulation of Brucea javanica Oil Emulsion In this paper, the preparation process of Brucea javanica oil emulsion was optimized. The appearance, centrifugal stability parameter Ke, average particle size and d90 were taken as the stability index. The amount of emulsifier used in the preparation of Brucea javanica oil emulsion by soybean lecithin alone was investigated, and the suitable amount of single emulsifier was determined to be 1.4%. The optimum compound emulsifier ratio of soybean lecithin to Poloxamer 2.75: 1 was obtained by optimum selection of the formula. Under the same emulsifier dosage, the emulsifier was alternately stored at 30 鈩

本文編號：1869976