本文選題：肉桂油微乳 + 穩(wěn)定性考察�。� 參考：《南昌大學(xué)》2014年碩士論文

【摘要】：本文構(gòu)建了一種安全性高、載油量適中的肉桂油微乳體系，測定其理化參數(shù)，考察其穩(wěn)定性，并研究其體外釋放和腸吸收情況，主要研究內(nèi)容及結(jié)果如下： 1.肉桂油微乳體系的構(gòu)建 以轉(zhuǎn)相乳化法制備微乳。通過電導(dǎo)率法精確控制水相的加入，并以離心法作為微乳的初步判斷方法，以離心結(jié)果和偽三元相圖中微乳區(qū)域面積大小，作為微乳穩(wěn)定性的初步判斷依據(jù)，對肉桂油微乳體系構(gòu)建的原料和工藝參數(shù)進(jìn)行初步篩選，最終優(yōu)化微乳體系組成為：Tween80/EL-40/丙三醇/無水乙醇/IPM/肉桂油/水，其中Tween80：EL-40=3：1，丙三醇：無水乙醇=1：1，肉桂油：IPM=1：1，Km=4，制備溫度為40℃，水相為64.29%。所制備微乳為O/W型微乳，淡黃色，澄清透明；平均粒徑為14.6nm，pH、電導(dǎo)率、折光率、粘度分別為5.03、228μs/cm、1.3829、46.5mpa·s，肉桂醛含量為21.27mg/mL。 2.肉桂油微乳體系穩(wěn)定性考察 參考本實(shí)驗(yàn)室建立的高效液相色譜法檢測肉桂醛，以加熱-冷卻循環(huán)試驗(yàn)、高速離心試驗(yàn)和恒溫加速試驗(yàn)考察肉桂油微乳穩(wěn)定性。結(jié)果顯示：在20μg/mL～160μg/mL范圍內(nèi)，峰面積與肉桂醛濃度有良好的線性關(guān)系，標(biāo)準(zhǔn)曲線方程為：y=162.7x+169，決定系數(shù)R2=0.998。加熱冷卻循環(huán)試驗(yàn)和高速離心試驗(yàn)中，肉桂油微乳體系均未出現(xiàn)相分離；恒溫加速試驗(yàn)中除pH值變化較大外，其他參數(shù)變化較小，恒溫加速六個(gè)月后，肉桂醛含量保留率依然維持在90%以上，而相同條件下的肉桂油中肉桂醛含量保留率僅為46.52%，表明本實(shí)驗(yàn)構(gòu)建的微乳體系穩(wěn)定性良好，，且能有效減少肉桂醛的損失。 3.肉桂油微乳體系的體外釋放 以正向透析擴(kuò)散法分別考察肉桂油微乳體系在人工胃液、pH6.8和pH7.4人工腸液中的釋放情況，并對釋放情況進(jìn)行擬合。結(jié)果顯示：人工胃液中，肉桂醛遭到破壞，所選五種方程均無法較好的描述其釋放情況，但從實(shí)驗(yàn)結(jié)果看，由于實(shí)際應(yīng)用中肉桂油微乳體系在胃中停留時(shí)間一般不超過1.5h，因此并不影響肉桂醛等物質(zhì)的釋放或者影響很小；人工腸液中pH值不同，釋放情況有所不同，但肉桂油微乳的釋放情況均符合Retger-peppas方程。其中pH6.8人工腸液中釋放方程為：Q=8.6642t0.6118，R2=0.9980；pH7.4人工腸液中釋放方程為：Q=3.9064t0.7904，R2=0.9719。 4.肉桂油微乳體系腸吸收 以外翻腸囊法考察肉桂油微乳體系離體腸吸收情況，并比較肉桂油微乳體系與普通乳液小腸吸收情況，結(jié)果表明：①肉桂醛在小腸的吸收速度為空腸十二指腸回腸，且空腸腸段的吸收明顯大于十二指腸和回腸；②離體實(shí)驗(yàn)中肉桂醛累積吸收量并不隨時(shí)間延長而呈現(xiàn)一直增長的趨勢，但本實(shí)驗(yàn)條件下，相同時(shí)間內(nèi)，肉桂油微乳體系累積吸收百分?jǐn)?shù)均高于肉桂油普通乳液。 以單向腸灌流實(shí)驗(yàn)考察肉桂油微乳體系在體腸吸收情況，考察恒流泵流速和劑型對小腸吸收的影響，結(jié)果表明：①在設(shè)定的恒流泵流速（204μL/min、301μL/min）下，恒流泵流速越大，小腸肉桂醛階段吸收量和累積吸收量越大；②本實(shí)驗(yàn)條件下，小腸對肉桂醛的累積吸收量與吸收時(shí)間呈良好的線性關(guān)系，R20.99；③相同條件下，肉桂油微乳體系中肉桂醛階段吸收量普遍高于肉桂油普通乳液；肉桂油微乳體系中肉桂醛累積吸收量和累積吸收百分?jǐn)?shù)均高于肉桂油普通乳液。表明肉桂油微乳體系小腸吸收要優(yōu)于肉桂油普通乳液，生物利用度可能更高。
[Abstract]:In this paper, a high safety, oil loaded cinnamon oil microemulsion system was constructed, its physical and chemical parameters were measured, its stability was investigated, and its in vitro release and intestinal absorption were studied. The main contents and results were as follows:
Construction of 1. cinnamon oil microemulsion system
The microemulsion was prepared by the method of phase transfer emulsification. The water phase was accurately controlled by the conductivity method, and the centrifugal method was used as the preliminary judgment method of microemulsion. The size of the microemulsion area in the centrifuge result and the pseudo three element phase diagram was used as the preliminary judgement basis for the stability of microemulsion. The raw materials and technological parameters of the microemulsion system of cinnamon oil were preliminarily screened. The final optimization microemulsion system consists of Tween80/EL-40/ glycerol / anhydrous ethanol /IPM/ cinnamon oil / water, of which Tween80:EL-40=3:1, glycerol: anhydrous ethanol =1:1, cinnamon oil: IPM=1:1, Km=4, the preparation temperature is 40 C, the microemulsion prepared by the water phase is O/W microemulsion, yellowish yellow, clear and transparent; the average particle size is 14.6nm, pH, The conductivity, refractive index and viscosity were 5.03228 s/cm, 1.3829,46.5mpa? S and cinnamaldehyde 21.27mg/mL. respectively.
Study on the stability of 2. cinnamon oil microemulsion system
The performance of cinnamaldehyde was examined by high performance liquid chromatography (HPLC) established in our laboratory. The stability of cinnamon oil microemulsion was investigated by heating cooling cycle test, high speed centrifugation test and constant temperature accelerated test. The results showed that there was a good linear relationship between the peak area and the concentration of cinnamaldehyde in the range of 20 to 160 g/mL, and the standard curve equation was y=162.7x+169 The determination coefficient R2=0.998. heating cooling cycle test and high speed centrifugation test, cinnamon oil microemulsion system has no phase separation; in the constant temperature acceleration test, the change of pH value is relatively large, the other parameters are small, and after six months of constant temperature acceleration, the retention rate of cinnamaldehyde is still more than 90%, and cinnamon oil in cinnamon oil under the same condition The retention rate of aldehyde content is only 46.52%, indicating that the microemulsion system constructed in this experiment has good stability and can effectively reduce the loss of cinnamaldehyde.
In vitro release of 3. cinnamon oil microemulsion system
The release of cinnamon oil microemulsion system in artificial gastric juice, pH6.8 and pH7.4 artificial intestinal fluid was investigated by positive dialysis diffusion method, and the release conditions were fitted. The results showed that cinnamaldehyde was destroyed in the artificial gastric juice, and the five equations were not good to describe the release situation, but from the experimental results, the actual application was used. The retention time of cinnamon oil microemulsion system generally does not exceed 1.5h in the stomach, so it does not affect the release or effect of Cinnamaldehyde and other substances. The release of pH in the artificial intestinal fluid is different, but the release of cinnamon oil microemulsion is in accordance with the Retger-peppas equation. The release equation in the pH6.8 artificial intestinal fluid is: Q=8.6642t0 The release equation of.6118, R2=0.9980 and pH7.4 artificial intestinal juice is: Q=3.9064t0.7904, R2=0.9719.
Intestinal absorption of 4. cinnamon oil microemulsion system
The absorption of cinnamon oil microemulsion system in vitro, and the absorption of cinnamon oil microemulsion system and common emulsion small intestine were compared. The results showed that: (1) the absorption rate of cinnamaldehyde in the small intestine was the jejunum duodenum, and the absorption of the jejunum intestine was greater than that of the twelve finger intestine and ileum; The cumulative absorption did not increase with time, but in the same time, the cumulative absorption percentage of cinnamon oil microemulsion system was higher than that of cinnamon oil in the same time.
The absorption of cinnamon oil microemulsion system in the intestines was investigated by one way intestinal perfusion test. The effect of the flow rate and dosage form on the absorption of small intestine was investigated. The results showed that the greater the flow velocity of constant current pump (204 L/min, 301 L/min), the greater the absorption and cumulative absorption of cinnamaldehyde in the small intestine; Under the same condition, the absorption of cinnamaldehyde in cinnamaldehyde oil microemulsion system is generally higher than that of cinnamaldehyde oil in the same condition. The cumulative absorption and cumulative absorption percentage of cinnamaldehyde in cinnamon oil microemulsion system are higher than that of cinnamon oil in the same condition. The absorption of cinnamon oil microemulsion in the small intestine is better than that in cinnamon oil emulsion, and the bioavailability may be higher.
【學(xué)位授予單位】：南昌大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2014
【分類號】：R96


本文編號：2049937