Solid dispersion adsorbate technique for improved dissolution and flow properties of lurasidone hydrochloride: characterization using 32 factorial design

The aim of the present study was to improve the dissolution and flow properties of lurasidone hydrochloride (LH) by solid dispersion adsorbate (SDA) technique. Solid dispersions (SDs) of LH were prepared by fusion method using Poloxamer P188. The melt dispersion was adsorbed onto the porous carrier Florite (calcium silicate). A 3² factorial design was employed to quantify the effect of two independent variables, namely ratio of carrier (Poloxamer 188) and LH in SD and ratio of adsorbent (Florite) to SD. SDA granules of LH were studied for flow properties and characterized using differential scanning calorimetry, scanning electron microscopy, and X-ray diffraction. Tablets of optimized composition of SDA granules (equivalent to 20?mg of drug) and plain tablets were prepared by direct compression method. The dissolution studies were carried out in Mcllvaine buffer (pH 3.8) as per USFDA guidelines and characterized for parameters such as percent dissolution efficiency, t₅₀, and Q₃₀. Tablets prepared from SDA granules showed almost four-fold increase in cumulative percentage drug release as compared to tablets prepared from plain LH. The value of dissolution efficiency was enhanced from 49.60% for plain tablets to 94.15% for SDA tablets. SDA granules did not show any change in drug release and X-ray diffraction pattern after storage at 40?°C/75% of RH for 3?months, which confirms that Florite prevented conversion of drug from amorphous form to crystalline form improving physical stability of the amorphous state of LH.     

乙苯甲喹唑啉酮盐酸盐合成方法的改进

以邻乙酰氨基苯甲酸为原料，在POCl3作用下与2－乙基苯胺缩合得3－（2－乙基苯基）－2－甲基－4－（3H）－喹唑啉酮盐酸盐，其条件为：以甲苯为溶剂，邻乙酰氨基苯甲酸与2－乙基苯胺摩尔比为1：1，反应时间3h，产物收率为80％。     

柳杉KP浆高白度漂白方法的研究

本文对柳杉ＫＰ浆的高白度漂白方法进行了研究。研究表明，采用硫酸盐法能够煮出卡伯值在２８～３２范围内的可漂浆，而且细浆得率高。采用Ｃ－Ｅｏｐ－ＨＡ－Ｐ四段漂（Ｃ－氯化，Ｅｏｐ－添加Ｈ２Ｏ２的氧碱抽提，ＨＡ－高温次氯酸盐漂后直接酸处理，Ｐ－过氧化氢漂白），能够将柳杉ＫＰ浆漂到白度８８％以上，而且漂白得率达９４％，返黄值仅０．３左右，漂后浆的强度比原浆强度约下降１０％（打浆度４２°ＳＲ）。     

Development of local injectable dental gel: the influence of certain additives on physicochemical properties of glycerylmonooleate-based formulations

The current research study is based on the design and development of a sol-gel biodegradable controlled-release formulation for use in the treatment of periodontal diseases. Glycerylmonooleate (GMO) was used as a main composition in the gel base. The influence of various additives, e.g., glycerylmonostearate (GMS), methylcellulose (MC), surfactants, and triglycerides, in GMO formulations on rheologic and swelling properties and release characteristics was described. It was demonstrated that the surfactants and triglycerides affected rheologic behavior, whereas GMS and MC influenced both rheologic and swelling properties of the bases. The release study revealed that drug released from the gel bases depended on the square root of time. The kinetics can be explained by the Higuchi's diffusion theory. Some polyols could enhance drug release from the gel. The stability results suggested that the dental gels obtained should be kept in the low temperature range.     

Development and in vitro evaluation of diltiazem hydrochloride transdermal patches based on povidone-ethylcellulose matrices

To select a suitable formulation for the development of transdermal drug-delivery system of diltiazem hydrochloride. Transdermal patches of the drug, employing different ratios of polymers, ethylcellulose (EC), and povidone (PVP) were developed and evaluated for the potential drug delivery using depilated freshly excised abdominal mouse skin. The influence of different film compositions on in vitro drug permeation into receptor fluid were studied using a modified Franz diffusion cell. The cumulative amount of drug was found to be proportional to the square root of time, i.e., Higuchi kinetics. From this study, it was concluded that the films composed of povidone:ethylcellulose (1:2) should be selected for the development of transdermal drug-delivery system of diltiazem hydrochloride, using a suitable adhesive layer and backing membrane, for potential therapeutic use.     

环（D-天冬氨-D-脯）二肽的合成

以D-天冬氨酸和D-脯氨酸为原料,先合成N-叔丁氧羰基-D-天冬氨酸-β-苄酯和D-脯氨酸甲酯盐酸盐,然后经DCC缩合得直链二肽,再经Pd/C催化氢解,HCl/Et2O脱Boc保护,最后弱碱性条件下成环得环（D-天冬氨-D-脯）二肽,结构经ESI-MS、IR、^1HNMR、^13CNMR等表征。     

膜控释盐酸二甲双胍缓释片的研制

制备膜控释盐酸二甲双胍缓释片并对其体外释放度的相关影响因素进行研究。以释放度作为判断原则,采用薄膜包衣法,通过正交试验确定最佳处方和工艺,制得盐酸二甲双胍缓释片,并对溶出方法、转速和溶出介质等因素进行考察,确定了制备盐酸二甲双胍包衣片的最佳处方和工艺。本制剂工艺简单,所用各种辅料成本低,制得盐酸二甲双胍包衣片释放度符合规定。     

环保增塑剂柠檬酸三丁酯的催化合成工艺研究

采用活性炭固载对甲苯磺酸催化合成了环保增塑剂柠檬酸三丁酯（TBC）。考察了酸醇比、催化剂用量、反应时间、反应温度等工艺条件的变化对柠檬酸三丁酯合成的影响。实验得到制备柠檬酸三丁酯最佳工艺条件：酸醇比为1∶4.0,催化剂质量浓度为2.2%,催化剂负载量为21.0%,反应温度为120℃,反应时间3.0h。在以上条件下,酯化率可达到98.3%。     

PEI-CDs复合物的制备及其在药物传输中的应用研究

癌症是21世纪威胁人类健康的三大杀手之一。目前,治疗癌症的药物由于缺乏靶向性和选择性对正常细胞和组织也会造成严重损害。靶向性载药体系的构建是解决这一难题的关键。碳点(Cardon dots,CDs)是近年来发展起来的一种新型荧光纳米材料,因其具有无毒性、优良的生物兼容性、良好的发光性能等优点,在肿瘤标记及药物的靶向输送中具有重大的应用潜力。本实验以枸杞为碳源,采用水热法制备碳量子点,通过静电作用将聚乙烯亚胺(PEI)修饰在碳量子点表面,形成PEI-CDs复合物,在室温下通过物理吸附的手段使盐酸阿霉素(Dox)组装到PEI-CDs复合物表面,形成PEI-CDs-Dox型荧光载药系统,并对该载药体系进行体外释放模拟实验。实验结果表明,阿霉素的负载显著增强了碳点复合物的荧光性能,24 h释放率可达90%,随着药物的释放,体系的荧光强度逐渐下降,据此可以将其进一步应用于细胞靶向成像及药物靶向监测。     

单烷基取代苯基哌嗪衍生物的合成

单烷基取代苯基哌嗪衍生物是合成苯基哌嗪类化合物的重要中间体。以二乙醇胺为起始原料,在10℃滴加氯化亚砜,室温反应1 h,再于60℃反应5 h,经氯代反应制得β,β′-二氯代二乙胺盐酸盐,然后分别与2-甲基苯胺、4-叔丁基苯胺、4-甲基苯胺在130℃反应50 h,得2-甲基苯基哌嗪盐酸盐、4-叔丁基苯基哌嗪盐酸盐、4-甲基苯基哌嗪盐酸盐3个目标化合物,收率分别为78%、61%、67%。其结构经1HNMR、13CNMR、MS证实与目标化合物的结构一致。