SeDeM expert system a new innovator tool to develop pharmaceutical forms

Context: The SeDeM expert system is based on the experimental study and quantitative determination of the characterization parameters of powdered substances, the aim being to determine whether a substance is suitable for producing tablets by means of direct compression (DC) technology, thereby reducing the lead time for pre-formulation studies. Additionally, this expert system also provides formulations with a minimum number of excipients.

Objective: We used this system to analyze suitable formulas for the production of orodispersible ibuprofen tablets.

Method: Twenty-one disintegrants and ibuprophen were characterized using SeDeM methodology.

Results: The results indicated that production of ibuprofen tablets by DC would require improvements in the dimension and compressibility factors of the active pharmaceutical ingredient. The expert system analysis provided the specific percentage of disintegrant needed to blend with ibuprofen and a standardized formula of lubricants in order to obtain a powder mix that would successfully produce tablets by DC. The eight formulas proposed by SeDeM were produced and tested in the laboratory.

Conclusion: All eight formulas successfully produced tablets by DC, but only four of them could be considered suitable for use as an orodispersible tablet and accomplishes all the pharmaceutical quality parameters. So, in fact, the use of the SeDeM system reduced the time of medicine’s development and therefore the cost of the activity.     

Preparation of medicinal carbon tablets by modified wet compression method

Background: Although medicinal carbon (MC) is useful to treat intoxications caused by orally taken toxic chemicals or toxins, high dose of MC is a burden on patients and sticks to oral mucosa or throat. A tablet dosage form of MC is useful to solve such problems. Fast-disintegration, adequate hardness, and quick and high-adsorption potential are required for MC tablets. Method: A modified wet compression method using carboxymethylcellulose sodium (CMC-Na) solution as binder solution was newly developed. Croscarmellose sodium (CC-Na) was used as a disintegration agent. MC granules, binder solution, and MC granules were placed in the cylinder in that order, and the resultant mass was compressed. The obtained tablets were examined for hardness, disintegration rate, and acetaminophen adsorption profiles. Results: The tablets, produced with MC granules containing CMC-Na and CC-Na at 10% each and using 280?μL of 2.5% (w/w) CMC-Na binder solution in compression, showed adequate hardness (more than 4?kg), short disintegration time (less than 6 min), and almost the same acetaminophen adsorption profile as intact MC powder. Conclusion: The modified wet compression with CMC-Na and CC-Na is suggested to be useful to obtain MC tablets with good quality.     

Fast relief from migraine attacks using fast-disintegrating sublingual zolmitriptan tablets

Zolmitriptan is a potent molecule for treatment of migraine. Its current oral therapies present drawbacks such as slow onset of action, low bioavailability and large inter-subject variability. Fast disintegrating sublingual zolmitriptan tablet (FDST) using freeze-drying technique has been developed to enhance tablet disintegration and dissolution with the intention of speeding drug absorption and onset of effect, hence mitigating the effects on the gastrointestinal dysmotility that typically accompanies the migraine attack. The FDSTs were prepared using different concentrations of gelatin as binder and mannitol or L-alanine as matrix supporting/disintegration enhancing agents. The effect of formulation variables on the physicochemical and solid-state properties, as well as the dissolution behaviour of the tablets, was studied. The formulated FDSTs disintegrated within 30 s and showed significantly faster dissolution rate of zolmitriptan compared to the zolmitriptan oral tablet. Tablet containing 2% gelatin and mannitol showed acceptable weight variation, drug content and friability values. Furthermore, it had a low in-vitro and in-vivo disintegration time (11 s) and it reached 100% of drug release within 30 s. This sublingual formulation gave faster and higher zolmitriptan plasma concentration in rabbits compared to the oral zolmetriptan market product. Zolmitriptan FDST may therefore constitute an advance in the management of acute migraine attacks.     

Formulation and In Vitro Studies of a Fixed-Dose Combination of a Bilayer Matrix Tablet Containing Metformin HCl as Sustained Release and Glipizide as Immediate Release

The emerging new fixed dose combination of metformin hydrocholride (HCl) as sustained release and glipizide as immediate release were formulated as a bilayer matrix tablet using hydroxy propyl methyl cellulose (HPMC) as the matrix-forming polymer, and the tablets were evaluated via in vitro studies. Three different grades of HPMC (HPMC K 4M, HPMC K 15M, and HPMC K 100M) were used. All tablet formulations yielded quality matrix preparations with satisfactory tableting properties. In vitro release studies were carried out at a phosphate buffer of pH 6.8 with 0.75% sodium lauryl sulphate w/v using the apparatus I (basket) as described in the . The release kinetics of metformin were evaluated using the regression coefficient analysis. There was no significant difference in drug release for different viscosity grade of HPMC with the same concentration. Tablet thus formulated provided sustained release of metformin HCl over a period of 8 hours and glipizide as immediate release.     

Evaluation and comparison of five matrix excipients for the controlled release of acrivastine and pseudoephedrine

For treatment of allergic rhinitis, acrivastine with pseudoephedrine in Semprex®-D conventional capsules requires dosing every 6-8 hours. This study was designed to develop a controlled release matrix tablet of acrivastine and pseudoephedrine and evaluate 5 different matrix excipients for their in vitro controlled-release profiles. Compritol® 888ATO, Eudragit® RS, Methocel® K100M, Polyox® WSR301 and Precirol® ATO5 were used alone or in varying combinations for the formulation of controlled release matrix tablets. In vitro drug dissolution and mathematical modeling were used to characterize drug release rate and extent. All tablet formulations yielded quality matrix preparations with satisfactory tableting properties. Due to the aqueous solubility of pseudoephedrine and the size of the dose, none of the matrix excipients used alone prolonged drug release significantly to meet the desired twice-daily administration frequency. The use of two excipients in combination, however, significantly decreased the dissolution rate of both active ingredients. A combined lipid-based Compritol® and hydrophilic Methocel® produced optimal controlled drug release for longer than 8 hours for both acrivastine and pseudoephedrine.     

基于手写笔的多功能电子白板系统的实现

该文针对当前电子白板系统对个性化支持的不足,引入手写笔作为输入设备,充分利用其功能参数,设计开发了具有模拟毛笔、钢笔、铅笔等真实笔特征的多笔型功能的电子白板系统。     

电子病历在移动医疗中的研究与发展

随着移动医疗在医院的广泛应用,医生迫切需要能够在病人床边通过iPad等智能平板设备查看、检索病人的电子病历信息,以提高诊疗效率并使查房过程更为准确、安全。但是由于现有的电子病历系统客户端多是基于Windows平台,如何支持在智能平板设备上访问电子病历系统成为移动医疗领域亟待解决的问题。本文系统地介绍这一崭新领域的基本概念,详细阐述需要解决的几个关键问题,比较几种主流解决方案的异同,最后对未来研究方向和工作进行展望。     

近红外反射光谱分析在抗生素片剂质量控制中的应用

本文讨论了近红外反射光谱分析在头孢片剂固体样品物理化学性质测定方面的应用,分析结果显示该方法可以很好的确认生产过程中的原料及其制品的质量,同时还可以得到满意的水分含量测定结果。     

Effect of Kollidon VA®64 particle size and morphology as directly compressible excipient on tablet compression properties

The study evaluates use of Kollidon VA^®64 and a combination of Kollidon VA^®64 with Kollidon VA^®64 Fine as excipient in direct compression process of tablets. The combination of the two grades of material is evaluated for capping, lamination and excessive friability. Inter particulate void space is higher for such excipient due to the hollow structure of the Kollidon VA^®64 particles. During tablet compression air remains trapped in the blend exhibiting poor compression with compromised physical properties of the tablets. Composition of Kollidon VA^®64 and Kollidon VA^®64 Fine is evaluated by design of experiment (DoE). A scanning electron microscopy (SEM) of two grades of Kollidon VA^®64 exhibits morphological differences between coarse and fine grade. The tablet compression process is evaluated with a mix consisting of entirely Kollidon VA^®64 and two mixes containing Kollidon VA^®64 and Kollidon VA^®64 Fine in ratio of 77:23 and 65:35. A statistical modeling on the results from the DoE trials resulted in the optimum composition for direct tablet compression as combination of Kollidon VA^®64 and Kollidon VA^®64 Fine in ratio of 77:23. This combination compressed with the predicted parameters based on the statistical modeling and applying main compression force between 5 and 15?kN, pre-compression force between 2 and 3?kN, feeder speed fixed at 25?rpm and compression range of 45–49?rpm produced tablets with hardness ranging between 19 and 21?kp, with no friability, capping, or lamination issue.