我院2005～2007年钙制剂及钙吸收促进剂利用分析

目的:评价我院钙制剂及钙吸收促进剂的应用情况及趋势。方法:对我院2005～2007年钙制剂及钙吸收促进剂的应用品种、数量、销售金额、用药频度(DDDs)等进行统计、分析。结果:氨基酸鳌合钙(乐力胶囊)、碳酸钙咀嚼片等在临床应用中占主导地位。DDDs排序列前3位的分别是氨基酸鳌合钙(乐力胶囊)、碳酸钙咀嚼片、牡蛎碳酸钙片(盖天力),老一代钙制剂渐趋淘汰。结论:我院钙制剂及钙吸收促进剂应用基本合理,但也存在一些问题需引起重视。     

我院口服钙制剂的应用分析

目的通过了解我院口服钙制剂的应用情况,分析其应用的合理性及必要性并预测发展趋势。方法通过调查我院2003年~2005年的口服钙制剂的应用情况,并统计分析该类药品的品种、用药金额、DDDs。结果含碳酸钙尔奇D和凯思立D不论是用药金额还是DDDs均排在前列。结论我院口服钙制剂主要以碳酸钙为主要药物,同时应合理补钙。     

我院门诊口服钙制剂临床应用分析

目的评估口服钙制剂的临床应用情况。方法对医院2007年11月至2008年1月口服钙制剂的门诊处方进行统计分析。结果口服钙制剂的临床应用广泛,女性与中老年人使用尤多,补钙现象普遍。结论钙制剂有过度使用的趋势,补钙需谨慎。     

利用DDDs数据排序分析我院补钙剂的应用

目的:了解钙制剂的应用情况及趋势。方法:回顾性分析某院2005年1~6月及2006年1~6月的口服补钙剂的品种、数量、金额,DDDs等并进行统计分析。结果:迪巧、凯思立D等碳酸钙在临床应用中占主导地位,老一代钙制剂已趋于淘汰。结论:该院钙制剂应用合理,但补钙人群主要集中在婴幼儿,其他人群补钙问题尚未得到足够重视。     

骨质疏松症的发生与钙治疗

目的倡导合理应用钙制剂防治骨质疏松症。方法探讨钙与骨质疏松症的关系,并对当前国内钙制剂进行再评价。结果与结论钙代谢障碍是引致骨质疏松症的重要原因,补钙被认为是防治骨质疏松症的重要手段。但目前流行的补钙“多多益善”的观点欠妥,应根据各种钙制剂自身的不同特点及具体情况合理选用补钙药物     

钙制剂的临床应用

随着人民生活水平的不断提高，人们自我保健意识的不断增强，补钙已成为广大群众生活中的一大热门话题。但是许多人却对钙的认识不足。补钙者面对市场上品种繁杂的钙剂无从下手，盲目补钙的情况屡见不鲜。现对钙制剂对人体的作用、人体利用钙的影响因素、目前钙制剂的特点、目前市场上常见的钙制剂选用等问题作一分析。     

钙也是双刃剑?

我国居民需安全有效的补钙和阻钙,为了科学应用钙制剂和钙阻断剂,作者提出钙有双向作用,犹如双刃剑,作者从介绍钙代谢基础知识入手,阐述过度补钙和细胞内钙超载的不良作用和可能的危害,以趋利避弊,更好地应用和发挥钙制剂和钙阻断剂的效用。     

钙制剂的应用及探讨

随着人民生活水平的不断提高，人们自我保健意识的不断增强，补钙已成为广大群众生活中的一大热门话题。但是许多人却对钙的认识不足。补钙者面对市场上品种繁杂的钙剂无从下手，盲目补钙的情况也就屡见不鲜。现对钙制剂对人体的作用、人体利用钙的影响因素、目前钙制剂的特点、目前市场上常见的钙制剂选用等问题作一分析。     

口服钙制剂的评价与合理补钙

近年来,随着人们对补钙问题的重视,钙制剂应用越来越多,新的品种也层出不穷。据初步统计[1],仅国内钙制剂生产厂就有70多家,上市品种达200余个,令医生和使用者无所适从,以下就口服钙制剂的特点和使用问题做以概述。1钙制剂种类与评价根据钙制剂的发展情况,一般将钙制剂分成三类     

钙制剂进入品牌消费

随着众多医药、保健食品企业簇拥下兴起的“补钙热”，人们对“补钙”这一概念的认知程度越来越高，使得中国补钙产品市场备受关注，也成为竞争异常激烈的市场，那么目前中国钙制剂零售市场是何种情况呢？《中国药店》杂志在2007年第3期刊登了有关钙制剂零售渠道的调查，     

Effects of various absorption enhancers on transport of clodronate through Caco-2 cells

The major disadvantage concerning clinical use of bishosphonate drugs, like clodronate, is their poor and variable absorption after oral administration. The objective of this study was to assess the effects of four different absorption enhancers-palmitoyl carnitine chloride (PCC), N-trimethyl chitosan chloride (TMC), sodium caprate (C10), and ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA)-on the transport of clodronate using Caco-2 cell culture model. The transport experiments were performed in a normal (1.3mM) and in a minimum-calcium concentration (apically calcium-free medium and basolaterally 100 microM calcium concentration). In the normal calcium concentration, a strong enhancement in clodronate permeation was observed with the enhancers: EGTA (2.5mM), TMC (1.5% w/v), and PCC (0.2mM) increased the transport of 1mM clodronate 190-, 20-, and 10-fold, respectively, and the transport of 10mM clodronate 130-, 70-, and 35-fold. In the minimum-calcium concentration, the effects of the absorption enhancers on the transport of clodronate were not so potent: TMC, PCC, and EGTA caused 2- to 20-fold enhancement in clodronate permeation whereas C10 (10mM) was without any effect. According to the results, the permeation of clodronate through Caco-2 cells could be significantly promoted by the absorption enhancers, which cause widening of the tight junctions and, thus, increase the permeability of the paracellular route.     

络合钙在小鼠体内的药代动力学研究

目的：测定络含钙在小鼠体内的血药浓度,对其进行药代动力学研究。方法：口服给予高、低两个剂量的络合钙,于给药后不同时间采用原子吸收法测定血钙浓度,并与维丁钙片进行比较,对所得参数用计算机进行房室模型模拟。结果：高、低络含钙组以及维丁钙组小鼠的血钙浓度明显升高,高剂量组的血钙浓度明显高于维丁钙组（P≤0．01）。所得的动力学参数经计算机模拟表明络合钙在体内的药代动力学符合一室模型。结论：络合钙口服可明显提高小鼠的血钙水平。     

Absorption Enhancers: Applications and Advances

Absorption enhancers are functional excipients included in formulations to improve the absorption of a pharmacologically active drug. The term absorption enhancer usually refers to an agent whose function is to increase absorption by enhancing membrane permeation, rather than increasing solubility, so such agents are sometimes more specifically termed permeation enhancers. Absorption enhancers have been investigated for at least two decades, particularly in efforts to develop non-injection formulations for peptides, proteins, and other pharmacologically active compounds that have poor membrane permeability. While at least one product utilizing an absorption enhancer for transdermal use has reached the market, quite a few more appear to be at the threshold of becoming products, and these include oral and transmucosal applications. This paper will review some of the most advanced absorption enhancers currently in development and the formulation technologies employed that have led to their success. In addition, a more basic review of the barriers to absorption and the mechanisms by which those barriers can be surmounted is presented. Factors influencing the success of absorption-enhancing formulations are discussed. If ultimately successful, the products now in development should offer non-injection alternatives for several peptide or protein drugs currently only administered by injection. The introduction of new absorption enhancers as accepted pharmaceutical excipients, and the development of formulation technologies that afford the greatest benefit/risk ratio for their use, may create opportunities to apply these enabling technologies more broadly to existing drugs with non-optimal delivery properties.     

Calcium absorption in man: some dosing recommendations

The absorption of calcium involves a saturable (active) and a nonsaturable (passive) component. The work of several investigators indicates that an inverse relationship exists between calcium intake and absorption efficiency. Human calcium absorption data from the literature were analyzed using a model which included both an active and a passive absorption component. Simulations were provided to illustrate the suitability of this model, and another previously reported model, to fit the data and to estimate the absorption efficiency of calcium when using different dosing regimens. Comparisons of the values predicted in this study with some literature values are provided and some assumptions and potential limitations associated with the use of this method are discussed. The division of the daily dose into equal increments taken at equally spaced intervals over the course of the day is recommended as a useful procedure for increasing the absorption efficiency and efficacy of calcium.     

吸收促进剂对蚓激酶肠道吸收的影响

目的研究蚓激酶(YJM-I)和吸收促进剂合用时在大鼠肠道各段的吸收特点，寻找YJM-I经肠道吸收的最佳位置和考察吸收促进剂对YJM-I在肠道吸收过程中的影响。方法采用体外扩散池法、十二指肠部位直接给药、在体循环灌流及肠段原位结扎等方法对荧光标记的FITC-YJM-I在大鼠肠道的吸收情况进行了研究。结果十二指肠部位给药后的药代动力学和药效学评价结果显示YJM-I药物分子可被大鼠肠道吸收进入血液循环并保持生物学活性，但其绝对生物利用度较低。体外肠黏膜通透性试验及体内肠段吸收试验结果显示部分吸收促进剂表现出良好的促进YJM-I肠道吸收的作用。十二指肠、空肠和回肠段体外肠黏膜通透性均显示了相似的吸收促进剂作用强弱趋势： 1%壳聚糖>1%去氧胆酸钠>1% Na₂EDTA>1%十二烷基硫酸钠>1%辛酸钠>1%泊洛沙姆>1%羟丙基-β-环糊精。而在体内十二指肠部位给药则显示的强弱顺序为： 2.5%去氧胆酸钠>2.5% Na₂EDTA>2.0%壳聚糖>2.5%十二烷基硫酸钠>2.5%辛酸钠>2.5%泊洛沙姆>2.5%羟丙基-β-环糊精。结论吸收促进剂能有效地增加YJM-I肠道吸收程度，其中具有生物黏附作用的壳聚糖有望成为YJM-I肠道吸收的良好促进剂。     

吸收促进剂对人参皂苷Rg1鼻腔吸收的促进作用及鼻腔毒性

目的考察吸收促进剂对人参皂苷Rg1鼻腔黏膜的吸收促进作用以及对鼻腔黏膜毒性。方法采用大鼠在体鼻腔循环考察人参皂苷Rg1鼻腔吸收及吸收促进剂的促吸收作用，在体蟾蜍上腭纤毛法评价药物对纤毛运动的影响；考察吸收促进剂对家兔血红细胞的溶血作用、对鼻腔循环液中总蛋白和乳酸脱氢酶的影响及对鼻腔黏膜形态学的影响。结果人参皂苷Rg1鼻腔吸收必须加入吸收促进剂。各种吸收促进剂的促进作用为：1%去氧胆酸钠作用显著；1%甘草酸二钾和1%氮酮作用中等；1% Tween-80，2% β-环糊精、0.5%冰片、0.5%壳聚糖、5%羟丙-β-环糊精和0.1% EDTA等作用微弱。吸收促进剂对鼻腔黏膜毒性影响：1%去氧胆酸钠、1%氮酮和1%甘草酸二钾毒性大；1% Tween-80，2% β-环糊精及5%羟丙-β-环糊精等毒性中等；0.5%冰片、0.5%壳聚糖和0.1% EDTA毒性小。结论0.5%冰片与0.5%壳聚糖可安全有效地促进人参皂苷Rg1的鼻腔吸收。     

不同吸收促进剂对大鼠口腔胰岛素吸收作用的影响

目的 :研究胰岛素的口腔吸收及吸收促进剂、酶抑制剂对药物吸收的影响。方法 :以血糖水平为指标 ,考察各种吸收促进剂和酶抑制剂经糖尿病模型的大鼠口腔给药后对胰岛素溶液 (insulinsolution ,INS SOL)和胰岛素贴片 (insulinpatch ,INS PAT)降血糖作用的影响 ,以皮下注射为对照 ,计算不同条件下INS SOL和INS PAT的药理生物利用度。结果 :不加吸收促进剂的条件下 ,32U·kg-1的INS SOL和10U·kg-1的INS PAT经口腔给药后的生物利用度较低 (0 .77%和 1.82 % )。 3%去氧胆酸钠和 5 %壬苯醇醚均能显著增加INS SOL和INS PAT的降血糖作用 (P <0 .0 5 )。其中 3%去氧胆酸钠作用最明显 ,INS SOL和INS PAT的生物利用度增加了近 3倍(2 .83%和 7.2 6 % )。结论 :胰岛素可通过口腔吸收 ,适当的吸收促进剂对其吸收具有显著的促进作用。     

Pulmonary Delivery of Salmon Calcitonin Dry Powders Containing Absorption Enhancers in Rats

Purpose. To evaluate the effects of absorption enhancers in dry powders and in liquids, pulmonary absorption of salmon calcitonin (sCT) in various formulations was measured. Methods. The dry powder of sCT was prepared by a freeze-drying method with a jet mill. After intratracheal administration of sCT dry powder and liquid (solution) preparations to rats, plasma sCT levels and calcium levels were measured. Results. After intratracheal administration without absorption enhancers, sCT in the dry powder and in the liquid were absorbed nearly to the same degree. Absorption enhancers (oleic acid, lecithin, citric acid, taurocholic acid, dimethyl-β-cyclodextrin, octyl-β-D-glucoside) were much more effective in the dry powder than in the solution. The reason may be that the enhancers added to the dry powder dissolved at high concentrations in a trace volume of the fluid lining the alveolar epithelium. Conclusions. The present results suggest that the pulmonary absorption of peptides and proteins can be greatly improved by formulating them into dry powders with smaller amounts of enhancers than in liquid dosage forms.     

Calcium absorption in man: Some dosing recommendations

The absorption of calcium involves a saturable (active) and a nonsaturable (passive) component. The work of several investigators indicates that an inverse relationship exists between calcium intake and absorption efficiency. Human calcium absorption data from the literature were analyzed using a model which included both an active and a passive absorption component. Simulations were provided to illustrate the suitability of this model, and another previously reported model, to fit the data and to estimate the absorption efficiency of calcium when using different dosing regimens. Comparisons of the values predicted in this study with some literature values are provided and some assumptions and potential limitations associated with the use of this method are discussed. The division of the daily dose into equal increments taken at equally spaced intervals over the course of the day is recommended as a useful procedure for increasing the absorption efficiency and efficacy of calcium.The receipt of a Gustavus A. Pfeiffer Memorial Fellowship is gratefully acknowledged.