發(fā)布時(shí)間：2018-01-03 15:31

  本文關(guān)鍵詞：兩種AngⅡ拮抗劑片劑和ST1213滲透泵控釋片的制備　出處：《廣東藥學(xué)院》2015年碩士論文　論文類型：學(xué)位論文

  更多相關(guān)文章： ST0723 ST0903 固體分散體 滲透泵控釋片 星點(diǎn)設(shè)計(jì)-效應(yīng)面法

【摘要】：本課題主要研究兩種AngⅡ拮抗片劑即ST0723、ST0903片劑的處方工藝以及ST1213滲透泵控釋片的制備。ST0723采用濕法制粒工藝,通過選擇粘合劑1,ST0903則采用干法制粒工藝。ST1213滲透泵控釋片的制備選用輔料V、輔料VII,ST1213固體分散體作為片芯材料,采用輔料VIII,輔料IX、輔料X作為包衣材料來制備ST1213滲透泵片。本實(shí)驗(yàn)主要分以下三個(gè)部分。1、ST0723片劑的制備ST0723為血管緊張素Ⅱ(AngiotensinⅡ,AngⅡ)受體抑制劑,為AngⅡ型拮抗片劑,屬于難溶性藥物。為了提高其溶出度,選擇輔料I,輔料V作為填充劑,輔料VI作為崩解劑,輔料IV作為助流劑,輔料III作為潤滑劑。實(shí)驗(yàn)分別考察了粘合劑的選擇,崩解劑的用量,不同壓力等對溶出度的影響。通過微調(diào)處方,以溶出度為考察指標(biāo),以達(dá)到與原研藥的溶出度相似性。2、ST0903片劑的制備ST0903同樣屬于血管緊張素Ⅱ(AngiotensinⅡ,AngⅡ)受體抑制劑,為AngⅡ型拮抗片劑,不僅為難溶性藥物,而且不穩(wěn)定,具有一定的引濕性,存在多種晶型�？紤]濕法制粒中產(chǎn)生晶型轉(zhuǎn)變和性質(zhì)變化,采用干法制粒,選擇輔料I作為填充劑,輔料II作為崩解劑,輔料IV作為助流劑,輔料III作為潤滑劑。實(shí)驗(yàn)分別考察了輥輪轉(zhuǎn)速、輥輪壓力、崩解劑用量等對溶出度的影響,通過微調(diào)處方改變相關(guān)參數(shù)工藝,來提高溶出度,與原研藥進(jìn)行曲線對比,達(dá)到原研藥的溶出效果。3、ST1213滲透泵控釋片的制備本實(shí)驗(yàn)利用紫外分光度法對ST1213滲透泵片的體外釋放度進(jìn)行測定。通過制備ST1213固體分散體達(dá)到增溶效果,以星點(diǎn)設(shè)計(jì)-效應(yīng)面法優(yōu)化包衣液處方。片芯材料選用輔料V、輔料VII作為填充劑。包衣液處方選用輔料VIII,輔料IX、輔料X、丙酮:異丙醇為4:1的溶媒作為包衣材料,以12h累計(jì)釋放度為指標(biāo),以不同包衣增重,釋藥孔徑大小,輔料IX用量、增塑劑用量四個(gè)因素考察對釋放的影響,利用星點(diǎn)設(shè)計(jì)對ST1213滲透泵控釋片處方進(jìn)行處方優(yōu)化,根據(jù)效應(yīng)面得到最優(yōu)處方:包衣增重3.00%,致孔劑用量0.71%,釋藥孔徑大小為0.40mm。制備三批最優(yōu)處方樣品與預(yù)測的值進(jìn)行模型驗(yàn)證,自制滲透泵與預(yù)測值相一致,12 h內(nèi)藥物呈零級釋放特征,重現(xiàn)性良好。
[Abstract]:This paper mainly studies two kinds of Ang II antagonist tablets ST0723, ST0903 tablet prescription and ST1213 osmotic pump tablets.ST0723 was prepared by the wet granulation method, by choosing 1 ST0903 with.ST1213 adhesive, dry granulation process of osmotic pump tablets were prepared using V materials, VII materials, ST1213 solid dispersion as core materials, the materials VIII, IX accessories, X accessories as coating materials to prepare ST1213 osmotic pump tablets. This experiment is mainly divided into the following three parts.1, ST0723 tablet preparation for ST0723 angiotensin II (Angiotensin II, Ang II) receptor inhibitor, Ang type II antagonist tablets. Belong to the insoluble drug. In order to improve the dissolution rate of I, the choice of materials, accessories and accessories as VI V as a filler, disintegrating agent, IV as glidants accessories, accessories III as lubricant. Experimental investigation of the binder selection, disintegrating agent used Different amount of pressure on the degree of dissolution. By means of adjusting the prescription to dissolution rate as indices to achieve with the original drug dissolution of similar.2, ST0903 in the preparation of tablets ST0903 also belong to angiotensin II (Angiotensin II, Ang II) for type II receptor inhibitor, Ang antagonistic tablets, not only for insoluble drugs, and unstable, with wet properties, there are a variety of crystal type. Considering the changes of crystal transformation and properties of wet granulation, by dry granulation, the choice of materials I as filler materials II as disintegrating agent, IV as glidants accessories, accessories as III lubricant. Experimental investigation of the roller speed, roller pressure, disintegrating agent dosage on the dissolution effect, by means of adjusting the parameters related to prescription change process, to improve the dissolution curve compared with the original drug, reach the dissolution effect of.3 of the original drug, ST1213 osmotic pump controlled release The preparation of this experiment using the ultraviolet spectrophotometry of ST1213 osmotic pump tablets in vitro release were determined. Through the preparation of ST1213 solid dispersion to solubilization effect, with ccd-rsm optimized coating formulation. The core material selection of materials V, VII materials as filler. The coating formulation of selected materials VIII X, IX accessories, accessories, acetone and isopropanol as solvent: 4:1 as coating material, 12h cumulative release rate as the index in different coating weight, release pore size, the amount of IX accessories, plasticizer four factors on the release effect of ST1213 osmotic pump controlled release tablets optimized by central composite design, according to the effect of the optimal prescription: surface coating weight of 3%, the amount of the porogen 0.71% release pore size samples and prepare for the three batch of the optimal prescription of 0.40mm. was predicted value of model validation, osmotic pump and forecast The values were the same. The drug in 12 h was characterized by zero level release, and the reproducibility was good.

【學(xué)位授予單位】：廣東藥學(xué)院
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2015
【分類號】：R943

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本文編號：1374500