洛汀烟酸缓释片中洛伐他汀溶出度的测定

目的建立了洛汀烟酸缓释片中洛伐他汀溶出度测定方法。方法采用转蓝法,以2%十二烷基硫酸钠溶液1 000 m l(内含1.38 g磷酸二氢钠,并用1 mol.L-1氢氧化钠溶液调pH至7.0)为溶出介质,转速为75 r.m in-1,采用HPLC法检测。结果洛伐他汀在2.5~25 mg.L-1范围内峰面积与浓度呈良好的线性关系,r=0.9998,平均回收率为97.39%,RSD=1.68%(n=9),与国外同品种AdvicorTM中洛伐他汀溶出度一致。结论方法准确可靠,可用于洛汀烟酸缓释片的质量控制。     

液固压缩技术在药剂学中的应用

液固压缩技术是利用液体赋形剂溶解难溶性药物,然后用涂层材料吸收后得到固体粉末的一种技术。该技术可有效增加生物药剂学分类系统(BCS)Ⅱ类水难溶性药物溶出速率,通过液固压缩技术制得的粉末具有良好的流动性和可压性,工艺简单、成熟。重点介绍液固压缩技术的理论基础、作用机制和制备方法,并对液固压缩技术在难溶药物固体制剂和缓控释制剂中的应用进行归纳总结。     

Mesoporous silica formulation strategies for drug dissolution enhancement: a review

Introduction: Silica materials, in particular mesoporous silicas, have demonstrated excellent properties to enhance the oral bioavailability of poorly water-soluble drugs. Current research in this area is focused on investigating the kinetic profile of drug release from these carriers and manufacturing approaches to scale-up production for commercial manufacture.

Areas covered: This review provides an overview of different methods utilized to load drugs onto mesoporous silica carriers. The influence of silica properties and silica pore architecture on drug loading and release are discussed. The kinetics of drug release from mesoporous silica systems is examined and the manufacturability and stability of these formulations are reviewed. Finally, the future prospects of mesoporous silica drug delivery systems are considered.

Expert opinion: Substantial progress has been made in the characterization and development of mesoporous drug delivery systems for drug dissolution enhancement. However, more research is required to fully understand the drug release kinetic profile from mesoporous silica materials. Incomplete drug release from the carrier and the possibility of drug re-adsorption onto the silica surface need to be investigated. Issues to be addressed include the manufacturability and regulation status of formulation approaches employing mesoporous silica to enhance drug dissolution. While more research is needed to support the move of this technology from the bench to a commercial medicinal product, it is a realistic prospect for the near future.     

4种市售5-单硝酸异山梨酯缓释片的体外释放度比较

目的：考察4种市售5－单硝酸异山梨酯缓释片的体外释放度，评价其内在质量。方法：采用溶出度测定法转篮法的装置进行体外溶出实验，用高效液相色谱法进行含量测定，计算累积释放百分率。以威布尔方程拟合溶出参数，并用q检验对组间溶出参数进行统计学分析。结果：在A、B、C、D4种市售5－单硝酸异山梨酯缓释片中，B、C、D3药的体外释药过程符合药典规定，D药的T50、Td最长，并与A、B、C3药的T50、Td存在显著性差异。结论：不同厂家产品的内在质量存在差异，提示在临床用药时应加以注意。     

阿西美辛缓释片的制备及其稳定性考察

目的:制备阿西美辛缓释片并考察其释药影响因素及稳定性.方法:采用湿法制粒工艺,以羟丙基甲基纤维素(HPMC)为骨架材料,制备了阿西美辛缓释片.对影响释药的因素,如HPMC规格、用量、润湿剂的用量、制片压力等因素进行了考察,并参照中国药典2000年版附录考察了制剂的稳定性.结果:除了HPMC规格对药物的释放产生一定的影响,而HPMC用量、润湿剂的用量、制片压力对阿西美辛缓释片的释药影响不大.在光、湿、热等因素影响下及长期试验时,本制剂稳定性良好.结论:采用HPMC作为基本骨架材料制备阿西美辛缓释片,具有较强的光稳定性、热稳定性、湿稳定性,长期放置稳定性良好.     

双氯芬酸钠缓释制剂含量及体外溶出度的测定

目的：考察不同厂家双氯芬酸钠（DS）缓释制剂的含量及溶出度,评价 其内在质量。方法：紫外分光光度法测定含量及溶出度,检测波长：276nm。结果：不同厂家的DS缓释制剂的体外溶出度有显著性差异。结论：为了确保DS缓释制剂的临床疗效,应对其进行体外溶出度的测定。     

缓释控释制剂的释放度测定方法的研究进展

目的　介绍缓、控释制剂的体外释放度测定方法 ,使其能更好地模拟体内状态。方法　综述最近的中外文献中有关缓释、控释制剂的体外释放度测定实验方法 ,实验条件的选择及影响因素。结果　体外释放度实验条件如释放介质的 pH值、离子强度、增溶剂、表面活性剂和释放仪器等可影响缓、控释制剂的体外释放度。结论　根据不同药物选择尽可能接近体内状态的方法     

尼索地平缓释片处方工艺的研究

目的:研制尼索地平缓释片.方法:通过试验筛选合适的阻滞剂等辅料,确定处方及制备工艺,并进行质量考察.结果:确定了以羟丙基甲基纤维素为阻滞剂、羟丙基纤维素为黏合剂的处方.尼索地平缓释片在4～5h释放50%,可缓慢释放12h以上.结论:制备缓释片的工艺简便,易于控制和操作,缓释片释放度指标均符合规定.     

美沙拉嗪缓释片的处方筛选及体外释放度研究

目的:制备美沙拉嗪缓释片剂,并评价其体外释放特性。方法:用正交试验设计对片剂的处方进行筛选,制备美沙拉嗪缓释片剂,测定其释放特性。结果:以优选的处方所制备的片剂,体外释药性能符合Higuchi模型,持续释药达8h。结论:该片剂工艺简单,可适合工业化生产     

阿莫西林缓释片的研制

目的：探讨阿莫西林缓释片的研制。方法：以HPMC为骨架制成阿莫西林缓解片,分别测定当HPMC用量为5％、8％、10％和15％时,以前当释放介质pH值为1．2、5．6和6．8时阿莫西林的释放度,并测定压片机压力为5～7kg和7～9kg时药物的释放度。结果：当HPMC的用量为10％时阿莫西林较为理想;缓释片介质pH值升高,释放度明显降低;片剂硬度对释放度几乎无影响。结论：阿莫西林缓释片体外释放度符合要求。     

Solid dispersions,Part II: new strategies in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs

Introduction: The absorption of poorly water-soluble drugs, when presented in the crystalline state to the gastrointestinal tract, is typically dissolution rate-limited, and according to BCS these drugs belong mainly to class II. Both dissolution kinetics and solubility are particle size dependent. Nowadays, various techniques are available to the pharmaceutical industry for dissolution rate enhancement of such drugs. Among such techniques, nanosuspensions and drug formulation in solid dispersions are those with the highest interest.

Areas covered: This review discusses strategies undertaken over the last 10 years, which have been applied for the dissolution enhancement of poorly water-soluble drugs; such processes include melt mixing, electrospinning, microwave irradiation and the use of inorganic nanoparticles.

Expert opinion: Many problems in this field still need to be solved, mainly the use of toxic solvents, and for this reason the use of innovative new procedures and materials will increase over the coming years. Melt mixing remains extremely promising for the preparation of SDs and will probably become the most used method in the future for the preparation of solid drug dispersions.     

盐酸万乃洛韦缓释片的释放度

目的:建立盐酸万乃洛韦缓释片体外释放度测定的质量标准.方法:以水为释放介质,检测波长为251 nm,对其进行常规的方法学进行研究.结果:本法的平均回收率分别为99.8%,99.9%,100.0%,RSD分别为0.96%,0.41%,0.59%,在2.7～19.5 mg*L-1浓度范围内,浓度与吸收度有良好的线性关系,r=0.9999(n=7).本品释放度受转速影响较小,而不同方法及介质pH值影响较大,同批产品的释放度均一性较好.结论:本法适用于该制剂的质量控制.     

Drug release from liquisolid systems: speed it up,slow it down

Introduction: Today, the properties of many new chemical entities have shifted towards higher molecular weights and this in turn increases the lipophilicity hence decreasing aqueous solubility. The low solubility of drugs usually has in vivo consequences such as low bioavailability, increased chance of food effect and incomplete release from the dosage form.

Areas covered: The present review discusses the advantages of the liquisolid technology in formulation design of poorly water soluble drugs for dissolution enhancement and highly water soluble drugs for slow release pattern.

Expert opinion: With the advent of high throughput screening and combinatorial chemistry, it has been shown that most of the new chemical entities have a high lipophilicity and poor aqueous solubility, hence poor bioavailability. In order to improve the bioavailability, the release rate of these drugs should be enhanced. Although there are multiple technologies to tackle this issue, they are not cost effective due to the involvement of sophisticated machinery, advanced preparation techniques and complicated technology. As the liquisolid technology uses a similar production process as the conventional tablets, this technology to improve the release rate of poorly water soluble drugs will be cost effective. This technology also has the capability to slow down drug release and allows preparing sustained release tablets with zero order drug release pattern. The excipients required for this technology are conventional and commonly available in the market. The technology is in the early stages of its development with extensive research currently focused on. It is envisaged that the liquisolid compacts could play a major role in the next generation of tablets.     

罗格列酮缓释片释放度测定方法的研究

目的建立罗格列酮缓释片的释放度的测定方法。方法《中国药典》附录ⅩC第三法,pH=1.2的盐酸缓冲液和pH=6.8磷酸盐缓冲液(含0.25%十二烷基硫酸钠)为释放介质,转速100r·min-1,在318nm处测定紫外吸收并计算累计释药量。结果平均回收率100.3%,RSD%=1.55%,三批产品平均累积释药量为2h(30.7%),6h(78.3%),12h(98.0%),药物释放符合Higuchi方程模型。结论方法可靠准确,可用于罗格列酮缓释片释放度的测定。     

Compression of coated drug beads for sustained release tablet of glipizide: formulation,and dissolution

Abstract

A promising glipizide formulation comprising compression of four-layer coated beads into tablets was prepared. The tablet offered the advantages of: a two-hour lag time before drug release, retaining sustained release characteristics and providing approximately zero-order drug release. Drug release was nearly independent of paddle speeds of 50 and 100?rpm releasing 80% over 14?h similar to the commercial glipizide osmotic pump tablet during dissolution testing while keeping the benefits of multiparticular dosage forms. The tablets contain beads with four layers: (1) the innermost layer consists of 2.5?g glipizide and 3.75?g solid ethylcellulose (Surelease®) coated onto 71.25?g of sugar beads; (2) next a hardening layer of 5?g of hypromellose; (3) the controlled release layer of 7.5?g of Surelease®:lactose at a solids ratio of 100:7 and (4) an outermost layer of 20?g of lactose:sodium starch glycolate (Explotab®) at a 2:1 ratio. Then, beads were compressed into tablets containing 11?mg of glipizide using 1500?lbs of compression pressure. The dissolution test similarity factor (f₂) was above 50 for all test conditions for formulation F13 and Glucotrol® with a high of 69.9. The two Surelease® layers both aid controlling drug release, with the Surelease®-drug layer affecting drug release to a greater extent.     

高效液相色谱法测定24h型硝苯地平缓释片释放度

目的　建立高效液相色谱法测定 2 4h型硝苯地平缓释片的释放度。方法　采用Shim PackC 18柱 (15 0× 4.6mm ,5 μ) ,甲醇 水 (70∶3 0 )为流动相 ,流速 0 .8mL/min ,检测波长为 2 3 7nm ,外标法测定硝苯地平缓释片溶出液中的硝苯地平浓度 ,计算相应时间内的累积释放百分率。结果　在 1.0 48～ 2 0 .960 μg/mL范围内 ,浓度与峰面积呈良好线性系 (r =0 .9992 ) ,平均加样回收率为 99.6% ,RSD为 1.6%。三批样品 2、4、8及 12h平均累积释放度分别为 (8.0± 1.1) % ,(17.7± 2 .1) % ,(3 3 .7±1.6) %和 (3 9.1± 1.0 ) % ,n =18。结论　本法灵敏、准确 ,适用于该缓释片的释放度测定     

双氯芬酸钠缓释制剂的释放度考察

目的:考察双氯芬酸钠缓释制剂的体外释放度.方法:采用转篮法和pH6.8的人工肠液对市售4个厂家的双氯芬酸钠缓释片和缓释胶囊的释放度进行了测定,并对释放度数据进行方程拟合及t检验.结果:A、C厂家产品的释放规律较符合Weibull方程,而B、D厂家产品的释放规律较符合Higuchi方程.各厂家产品的释放度在1 h,6 h时差异有显著性,在12 h时差异无显著性.结论:不同厂家双氯芬酸钠缓释制剂的释放度差异存在显著性.     

氢氯噻嗪缓释片的制备及体外释放考察

目的:制备氢氯噻嗪亲水凝胶缓释片,并评价其体外释放特性. 方法:以羟丙基甲基纤维素和卡波姆为骨架材料,运用正交设计法,粉末直接压片制备氢氯噻嗪缓释片, 并测定其释放度.结果:正交设计获最优处方为A1B3(R3),药物体外释放行为符合Higuchi方程.结论:该方法制得的缓释片具有明显的缓释效果,影响药物释放的主要因素是卡波姆的用量.     

非洛地平缓释制剂体外释放度比较

目的:对不同厂家非洛地平缓释制剂的体外释放度进行比较。方法:按照非洛地平的部颁标准,采用桨法测定非洛地平缓释制剂的释放度,通过选用数学模型线性拟合,求出参数,进行方差分析。结果:B样品释放度的均一性和重现性均好于A样品,A样品同一样品不同批号间释放度差异极具显著性(P<0.01),B样品有2个批号间差异具显著性(P<0.05)。结论:两个厂家的产品的释放度均符合部颁标准规定,B样品释放度好于A样品。