The objective of this study is to determine the effect of consumption of drinks with varying amounts of glycerol and electrolytes on fluid balance at rest.

开始日期2024-01-25

申办/合作机构

PepsiCo Global R&D

100 项与甘油相关的临床结果

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100 项与甘油相关的转化医学

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100 项与甘油相关的专利（医药）

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3,279

项与甘油相关的文献（医药）

2024-03-01·Cryobiology

Cryopreserved red blood cells maintain allosteric control of oxygen binding when utilizing trehalose as a cryoprotectant

Article

作者: Kopechek, Jonathan A ; Elder, Charles A ; Almosawi, Mustafa ; Wolkers, Willem F ; Janis, Brett R ; Smith, Jensen S ; Mills, Ethan ; Menze, Michael A

One of the most common life-saving medical procedures is a red blood cell (RBC) transfusion. Unfortunately, RBCs for transfusion have a limited shelf life after donation due to detrimental storage effects on their morphological and biochemical properties. Inspired by nature, a biomimetics approach was developed to preserve RBCs for long-term storage using compounds found in animals with a natural propensity to survive in a frozen or desiccated state for decades. Trehalose was employed as a cryoprotective agent and added to the extracellular freezing solution of porcine RBCs. Slow cooling (-1 °C min^-1) resulted in almost complete hemolysis (1 ± 1 % RBC recovery), and rapid cooling rates had to be used to achieve satisfactory cryopreservation outcomes. After rapid cooling, the highest percentage of RBC recovery was obtained by plunging in liquid nitrogen and thawing at 55 °C, using a cryopreservation solution containing 300 mM trehalose. Under these conditions, 88 ± 8 % of processed RBCs were recovered and retained hemoglobin (14 ± 2 % hemolysis). Hemoglobin's oxygen-binding properties of cryopreserved RBCs were not significantly different to unfrozen controls and was allosterically regulated by 2,3-bisphosphoglycerate. These data indicate the feasibility of using trehalose instead of glycerol as a cryoprotective compound for RBCs. In contrast to glycerol, trehalose-preserved RBCs can potentially be transfused without time-consuming washing steps, which significantly facilitates the usage of cryopreserved transfusible units in trauma situations when time is of the essence.

2024-03-01·Therapeutic innovation & regulatory science

Quantitative Investigation on Exposure to Potentially Harmful Excipients by Injection Drug Administration in Children Under 2 Years of Age and Analysis of Association with Adverse Events: A Single-Center, Retrospective Observational Study

Article

作者: Saito, Jumpei ; Yamatani, Akimasa ; Akabane, Miki ; Nakamura, Hidefumi

INTRODUCTION:

Potentially harmful excipients (PHEs) for children have been reported and the need for information collection has been advocated. However, studies on the actual occurrence of adverse events are limited. This study investigated the quantitative exposure of PHEs via injection and their association with adverse events in children under 2 years of age.

MATERIALS AND METHODS:

As a single-center observational study, children aged 0-23 months received injectable drugs from April 1, 2018, to March 31, 2023 were included. Information on PHE exposure and adverse events after administration were extracted from medical records. Sodium benzoate, benzyl alcohol, ethanol, glycerol, lactose, polyethylene glycol paraben, polysorbate, propylene glycol, sorbitol, sucrose, sulfite, and thimerosal were selected as PHEs.

RESULTS AND DISCUSSION:

6265 cases, 333,694 prescriptions, and 368 drugs (264 ingredients) were analyzed. The median age was 0.63 years (interquartile range [IQR] 0.1-1.1). 72,133 prescriptions, 132 drugs and 99 ingredients contained PHE; 2,961 cases exposed to PHE and 1825 cases exceeding permitted daily exposure. The drug with the highest number of exposure cases was hydroxyzine, and the highest number of prescriptions was heparin (both drugs contain benzyl alcohol). In association between adverse events and PHE exposure, higher doses in cases of adverse event occurrence were found in benzyl alcohol, glycerol, polyethylene glycol, and polysorbate exposed cases. Among thimerosal-exposed cases, "developmental delay" was more frequent in exposed cases, but the causal relationship was unknown. Further investigation is needed to clarify the relationship between adverse events and PHE exposure. Additionally, more precise information on PDE for pediatrics including neonates is necessary.

2024-02-01·International journal of cosmetic science

Effects of 1,3‐propanediol associated, or not, with butylene glycol and/or glycerol on skin hydration and skin barrier function

Article

作者: Monteiro E Silva, Silas Arandas ; Leonardi, Gislaine Ricci ; Pinto, Juliana Rodrigues

Abstract:

Objective:

This study aimed to assess the effect of 1,3‐propanediol at different concentrations (5%, 10%, or 15%), either applied alone or in combination with butylene glycol (BG) (5%) and/or glycerol (5%), on skin hydration and skin barrier function. The measurements were conducted using capacitance to determine skin hydration and trans epidermal water loss (TEWL) rates to evaluate skin barrier function.

Methods:

A total of 30 healthy female subjects participated in the study. Capacitance and TEWL measurements were conducted at multiple time points, including before application and at 15 min, 2 and 8 h after the humectants were applied to the forearms of the subjects. All the subjects provided written informed consent.

Results:

The 1,3‐propanediol in all concentrations and in all combinations (with BG and/or glycerol) increased skin hydration and improved skin barrier function 15 min, 2 and 8 h after application. Glycerol increased the hydration performance of 1,3‐propanediol. The application of 1,3‐propanediol at a concentration of 15%, either alone or in combination with other humectants, reduced the TEWL to a greater extent than lower concentrations of 1,3‐propanediol. Furthermore, the addition of glycerol to 1,3‐propanediol 15% improved the skin barrier and reduced TEWL when compared with 1,3‐propanediol alone and with the combination of 1,3‐propanediol + BG.

Conclusion:

The humectants significantly improved skin hydration and reduced TEWL throughout the 8‐h time course. The increase in 1,3‐propanediol concentration, as well as its combination with glycerol, provided a greater benefit to the skin, improving both hydration and the skin barrier function.

项与甘油相关的新闻（医药）

2024-06-10

·BioSpace

Bausch + Lomb INFUSE® for Astigmatism Silicone Hydrogel Daily Disposable Contact Lenses Introduced in the United States

VAUGHAN, Ontario--(BUSINESS WIRE)-- Bausch + Lomb Corporation (NYSE/TSX: BLCO), a leading global eye health company dedicated to helping people see better to live better, today announced the U.S. introduction of Bausch + Lomb INFUSE for Astigmatism daily disposable contact lenses. Engineered with a next-generation lens material infused with ProBalance Technology™ and the company’s proprietary OpticAlign® design, INFUSE for Astigmatism provides astigmatic patients clear, stable vision, all-day comfort and minimizes contact lens dryness. The company expects to start shipping INFUSE for Astigmatism fitting sets to eye care professionals in July 2024. “More than half of toric lens wearers with astigmatism experience contact lens dryness and many also report blurred vision. These symptoms are only exacerbated with modern-day lifestyles, which include prolonged digital device use,”1 said Yang Yang, president, Global Vision Care, Bausch + Lomb. “Our INFUSE for Astigmatism lenses, which were developed in-house by our R&D team, are designed to directly address these challenges, including the causes of toric lens rotation. They provide excellent clarity, optimal stability and can be worn comfortably all day.” Consistent with the entire INFUSE family of lenses, INFUSE for Astigmatism features a blend of osmoprotectants, electrolytes and moisturizers, essential comfort and eye health ingredients that are released throughout the 16-hour wearing experience.1 The lens material (kalifilcon A) combines the highest overall moisture (55%) and high breathability (107 Dk/t) with a low modulus for excellent comfort.2,3 INFUSE for Astigmatism is uniquely designed to provide consistently clear vision across the entire power range and help reduce spherical aberration and halos and glare, even in low-light conditions. Engineered with a thin-edge design to minimize lid interaction and a stabilization feature in the lower hemisphere, the cutting-edge OpticAlign design stabilizes with the eye’s natural blink. According to a recent study, 95% of INFUSE for Astigmatism lenses settled within 10 degrees within 30 seconds. In addition, 97% of INFUSE for Astigmatism lenses had less than three degrees of rotation with blink and a mean comfort score of nearly 90%. INFUSE for Astigmatism offers the most in-office parameters and is the only daily disposable toric with -2.25 and -2.75 cylinders available in a fit set.4 "As patient lifestyles become increasingly more dynamic, it's essential their lenses provide a high level of moisture retention and stability, particularly for those with astigmatism. INFUSE for Astigmatism will deliver on these needs and provide comprehensive in-office parameters that make it possible to fit patients during their scheduled appointment,” said Mark Schaeffer, OD, FAAO, and clinical excellence captain, MyEyeDr, Birmingham, Ala. “With this addition to the INFUSE family of lenses – based on the latest ocular surface research – practitioners can be confident that they have an INFUSE lens to meet the majority of their patients’ vision and eye health needs.” Eye care practitioners and contact lens wearers can use Bausch + Lomb’s ONE by ONE recycling program to properly recycle their used contact lens materials, including INFUSE for Astigmatism contact lenses, blister packs and top foils. For more information on the ONE by ONE Recycling program visit . About Astigmatism Astigmatism is a common condition that affects approximately one in three people and occurs when the cornea or lens has a different shape than normal, causing blurry or distorted vision.5,6 It can affect vision of both near and far objects, as well as cause difficulty seeing at night, and coexist with myopia or hyperopia. Astigmatism can be confirmed during a comprehensive eye exam and treated with the use of contact lenses, prescription eyeglasses and/or laser or other surgical procedures.6 About the ONE by ONE Recycling Program The Bausch + Lomb ONE by ONE Recycling program is the first and only contact lens recycling program in the United States. This program collects used contact lenses, top foils and opened plastic blister packs from any brand and is available to contact lens wearers and eye care professionals. To participate, contact lens wearers can bring their used contact lenses and packaging to an official recycling eye care practice, which collects the used materials in a custom recycling bin provided by Bausch + Lomb. Once the bin is filled, the eye care practice ships the materials using a Bausch + Lomb pre-paid shipping label to TerraCycle® where lenses are cleaned and melted into hard plastic pellets that can be used to make new recycled products. To learn more about the Bausch + Lomb ONE by ONE Recycling program, visit . About Bausch + Lomb Bausch + Lomb is dedicated to protecting and enhancing the gift of sight for millions of people around the world – from birth through every phase of life. Its comprehensive portfolio of approximately 400 products includes contact lenses, lens care products, eye care products, ophthalmic pharmaceuticals, over-the-counter products and ophthalmic surgical devices and instruments. Founded in 1853, Bausch + Lomb has a significant global research and development, manufacturing and commercial footprint with approximately 13,000 employees and a presence in nearly 100 countries. Bausch + Lomb is headquartered in Vaughan, Ontario with corporate offices in Bridgewater, New Jersey. For more information, visit and connect with us on X, LinkedIn, Facebook and Instagram. Forward-looking Statements This news release may contain forward-looking statements, which may generally be identified by the use of the words “anticipates,” “hopes,” “expects,” “intends,” “plans,” “should,” “could,” “would,” “will,” “may,” “believes,” “estimates,” “potential,” “target,” or “continue” and variations or similar expressions. These statements are based upon the current expectations and beliefs of management and are subject to certain risks and uncertainties that could cause actual results to differ materially from those described in the forward-looking statements. These risks and uncertainties include, but are not limited to, the risks and uncertainties discussed in Bausch + Lomb’s filings with the U.S. Securities and Exchange Commission and the Canadian Securities Administrators, which factors are incorporated herein by reference. Readers are cautioned not to place undue reliance on any of these forward-looking statements. These forward-looking statements speak only as of the date hereof. Bausch + Lomb undertakes no obligation to update any of these forward-looking statements to reflect events or circumstances after the date of this news release or to reflect actual outcomes, unless required by law. References Analysis of worn lenses demonstrated poloxamer 181, erythritol, potassium, and glycerin were retained for 16 hours. Oxygen transmissibility at -3.00 diameter. Unlike INFUSE® for Astigmatism, ACUVUE OASYS 1-Day for ASTIGMATISM, MyDay toric, and 1-DAY ACUVUE MOIST for ASTIGMATISM, which are non-surface-treated daily disposables, PRECISION1 for Astigmatism and DAILIES TOTAL1 for Astigmatism are daily disposables with an integrated surface coating. Compared to ACUVUE OASYS 1-Day for ASTIGMATISM, DAILIES TOTAL1 for Astigmatism, and MyDay toric. National Eye Institute: Astigmatism: At a Glance. Accessed May 13, 2024. . Cleveland Clinic: Astigmatism. Accessed May 13, 2024. . © 2024 Bausch + Lomb. IFA.0080.USA.24 View source version on businesswire.com: Contacts Source: Bausch + Lomb Corporation View this news release online at:

2024-04-29

·BioSpace

Bausch + Lomb Announces Presentation of New Data at the Association for Research in Vision and Ophthalmology Annual Meeting

21 Poster Presentations include Evaluations of Consumer, Pharmaceutical, Surgical and Vision Care Products and Pipeline Programs, Including a Novel Dry Eye Nutritional Supplement VAUGHAN, Ontario--(BUSINESS WIRE)--Bausch + Lomb Corporation (NYSE/TSX: BLCO), a leading global eye health company dedicated to helping people see better to live better, today announced the presentation of 21 scientific poster presentations during the Association for Research in Vision and Ophthalmology Annual Meeting, which will take place in Seattle May 5-9, 2024. The posters highlight the results of studies evaluating consumer, pharmaceutical, surgical and vision care products from the company’s broad eye care portfolio, as well as pipeline innovations. These include a novel daily nutritional supplement formulated to address dry eye symptoms, which is the focus of two posters as well as a paper published recently in Frontiers in Ophthalmology. “We’re focused on supporting research that advances scientific knowledge of our products and fosters the development of new innovations to serve the holistic needs of eye care professionals and consumers,” said Yehia Hashad, MD, executive vice president, Research & Development and chief medical officer, Bausch + Lomb. “The breadth of data being presented at this meeting, as well as the recent publication evaluating our novel nutritional supplement for dry eyes, Blink™ NutriTears®, underscore this ongoing commitment.” Following is a complete list of titles and lead authors for each of these posters: “Analysis of Glare and its Impact on Retinal Image Quality in Intraocular lenses.” Hosten et al. “A Natural Language Processing Approach to Identify Patients with Uveitic Macular Edema in the IRIS® Registry.” Jin et al. “Clinical Evaluation of a Multi-Ingredient Oral Supplement on Dry Eye Symptoms and Tear Volume.” Barbour et al. “Clinical Evaluation of a Novel Lipid-Containing Eye Drop.” Yassine et al. “Comparison of Clinical Studies from the US and India of a Multi-Ingredient Oral Supplement.” Ryan et al. “Comparison of a Novel Lipid Nano-Emulsion Eye Drop with an Existing Lubricating Eye Drop.” Morrow et al. “Development of an In Vitro Assay to Evaluate the Antioxidant Effects of Erythritol and Glycerin in Human Corneal Epithelial Cells.” VanDerMeid et al. “Effects of Perfluorohexyloctane on the Ocular Pharmacokinetics of Latanoprost and Prednisolone Acetate After Topical Administration to Rabbits.” Cavet et al. “Effects of Perfluorohexyloctane on Corneal Healing in an Ex Vivo Study of Rabbit Corneas.” Alexander et al. “Efficacy of Perfluorohexyloctane Ophthalmic Solution in Patients with Dry Eye Disease Stratified by Baseline Severity.” Sheppard et al. “Enhancing Silicone Oil Removal Efficiency: A Comparative Study of Ultrasonic Vitrectomy Handpieces and Conventional Methods.” Higgins et al. “Evaluating a Novel Contact Solution Among Hydrogen Peroxide Lens Care Users.” Shahidi et al. “Evaluation of the Efficacy of a Novel Preservative-Free Formulation of Brimonidine Tartrate Ophthalmic Solution.” DiVito et al. “Evaluation of Intermediate-Range of Focus with New Monofocal Plus IOLs.” Lau et al. “Evaluation of the Safety of a Novel Preservative-Free Formulation of Brimonidine Tartrate Ophthalmic Solution.” Vollmer et al. “Impact of Pupil Size on Vision Performance of a New Multifocal Daily Disposable Contact Lens.” Reindel et al. “In-Home Use Test of a Novel Contact Lens Solution in Contact Lens Wearers on the Verge of Dropout.” Rah et al. “Intraocular Pressure Optimized Performance Settings with Posterior Adaptive Fluidics (PAF), and 25 Gauge 25,000 cpm Dual-Action Vitrectomy Cutters.” Papour et al. “Phaco Longitudinal Mode Heat Generation, a Two-System Efficiency Comparison Study.” Dickerhoff et al. “Preclinical Toxicity Pro Perfluorohexyloctane Ophthalmic Solution.” Vittitow et al. “Predictive Modeling of Clinical Performance of Novel Trifocal IOL.” Venkateswaran et al. About Bausch + Lomb Bausch + Lomb is dedicated to protecting and enhancing the gift of sight for millions of people around the world – from birth through every phase of life. Its comprehensive portfolio of approximately 400 products includes contact lenses, lens care products, eye care products, ophthalmic pharmaceuticals, over-the-counter products and ophthalmic surgical devices and instruments. Founded in 1853, Bausch + Lomb has a significant global research and development, manufacturing and commercial footprint with approximately 13,000 employees and a presence in nearly 100 countries. Bausch + Lomb is headquartered in Vaughan, Ontario with corporate offices in Bridgewater, New Jersey. For more information, visit and connect with us on X, LinkedIn, Facebook and Instagram. Forward-looking Statements This news release may contain forward-looking statements, which may generally be identified by the use of the words “anticipates,” “hopes,” “expects,” “intends,” “plans,” “should,” “could,” “would,” “will,” “may,” “believes,” “estimates,” “potential,” “target,” or “continue” and variations or similar expressions. These statements are based upon the current expectations and beliefs of management and are subject to certain risks and uncertainties that could cause actual results to differ materially from those described in the forward-looking statements. These risks and uncertainties include, but are not limited to, the risks and uncertainties discussed in Bausch + Lomb’s filings with the U.S. Securities and Exchange Commission and the Canadian Securities Administrators, which factors are incorporated herein by reference. Readers are cautioned not to place undue reliance on any of these forward-looking statements. These forward-looking statements speak only as of the date hereof. Bausch + Lomb undertakes no obligation to update any of these forward-looking statements to reflect events or circumstances after the date of this news release or to reflect actual outcomes, unless required by law. © 2024 Bausch + Lomb.

2024-04-09

·药融圈

多肽口服---“肽肽们”手中的 “长剑”（上）

▲5月30-31日第八届广州生物医药创新者峰会扫码立即报名注：本文不构成任何投资意见和建议，以官方/公司公告为准；本文仅作医疗健康相关药物介绍，非治疗方案推荐（若涉及），不代表平台立场。任何文章转载需得到授权。本期开始将推送大家关于多肽口服中领域先进的Pipeline技术与进展（上&下）。1990年FDA批准了全球第一个口服多肽药物（环状肽）药物环孢素A（Cyclosporin A，1200kDa）。这是一种免疫抑制剂，用于预防移植排斥反应和治疗自身免疫性疾病。经过了三十年的发展，目前已有多款口服肽类药物上市。表1：上市口服多肽产品多肽领域是目前资本寒冬下为数不多的一抹绿意。图1：蛋白口服药物发展历程口服药物递送的生化和物理屏障是“肽肽们”逆袭之路上的障碍，药品口服后会经过胃和小肠，这里环境的酸碱度、酶环境和黏液层等都是蛋白类药物需要解决的障碍（见药事纵横2023-11-27推文链接：多肽口服---“肽肽们”的逆袭之路https://mp.weixin.qq.com/s/NzRfl9LoHY5bchouQ2Bgfw）。过五关，斩六将，略显英雄本色。图2：口服药物递送的生化和物理屏障，以及具有主要肠细胞类型的肠粘膜结构口服Rybelsus和Mycapssa已经将司美格鲁肽（semaglutide音译，同索马鲁肽）和奥曲肽（Mycapssa）（分子量均大于1000Da）暴露于体循环中吸收，代表了口服可吸收肽制剂开发的重大成就。但是，口服生物利用度仍然只有1%左右。口服多肽大分子吸收的挑战仍未被有效解决。表2：司美格鲁肽（Rybelsus）和奥曲肽（Mycapssa）新药方式口服生物利用度差的原因可以用Lipinski的五法则（分子量（MW）≤500，氢键供体（HBD）的数量≤5，氢键受体（HBAs）的数量≤10，辛醇-水分配系数（LogP）≤5）以及可旋转键的数量应小于 10 个，拓扑极表面积（TPSA）应小于 140 Å 2）来解释，事实上，大多数新药模式都属于中大分子的范畴，因此往往缺乏口服生物利用度（口服生物利用度高是小分子药物的最大优势之一）。奥曲肽的化学结构和理化性质见下图，显然有悖于Lipinski的五法则。图3：奥曲肽的化学结构以及理化性质2019 年，FDA 批准了用于治疗 2 型糖尿病的口服司美格鲁肽制剂。临床研究结果表明，口服40mg剂量与皮下注射1mg剂量的结局相似（NCT01923181），口服生物利用度仍的挑战仍未被有效解决。尽管司美格鲁肽和奥曲肽利用度低，但也是目前上市口服多肽药物的集大成者。Rybelsus 是第一个基于促渗透策略的口服肽药物，以SNAC作为促渗透剂。SNAC由Emisphere的Eligen™技术开发（见下文）（第一个使用SNAC商业化的产品是2015年被FDA批准上市的Eligen B12（维生素B12））。与针对胃吸收的 Rybelsus 不同，Mycapssa 针对小肠中的药物吸收。Mycapssa胶囊涂覆甲基丙烯酸酯来防止奥曲肽在胃中的分解，胶囊中促渗剂主要是C8，辅以高浓度的附加添加剂（如PVP、单辛酸甘油酯和聚山梨醇酯80）来增加促渗透效应。不同于Rybelsus ，Mycapssa是基于C8的TPE平台技术而来的重磅产品（见下文）。针对口服生物利用度低的问题，主要的药物策略旨在增强肽和蛋白质的稳定性和吸收，包括修饰、改进配方以及采用贴片微针等一系列方式。下图是目前多肽递送中先进的技术汇总。图4：多肽口服递送策略的示意图。（a）蛋白酶抑制剂、渗透增强剂和微针对肽的口服递送有效。（b）渗透增强剂成功地用于口服给药，如SNAC、胆盐和辛酸钠（它们使分子能够通过粘液层、细胞膜和紧密连接）。（c）化学修饰和环化是用于调节肽的理化性质的合适工具。Oramed Pharmaceuticals Inc.开发了蛋白质口服递送（POD™）。在这个系统中，不同的策略共存于同一配方中：封装、渗透增强剂、螯合剂和蛋白酶抑制剂。Oramed的技术基于旨在通过胃肠道和增强吸收的组件。乙二胺四乙酸钠（EDTA）和胆盐可作为渗透增强剂。胶囊可保护胰岛素在胃中不被水解，而蛋白酶抑制剂（如大豆胰蛋白酶抑制剂和抑肽酶）可保护胰岛素免受蛋白酶降解，尤其是在小肠中。图5：Oramed Pharmaceuticals Inc.的口服递送技术平台Oramed公司目前有三条主要管线。图6：Oramed Pharmaceuticals目前管线（官网）Oramed公司应用POD技术开发的ORMD-0901（GLP-1类似物，将EDTA作为吸收促进剂使用）在模型猪及模型犬中均表现出良好的耐受性，且降血糖作用显著。Oramed在临床上使用酶抑制剂方法进展最快是口服胰岛素ORMD-0801项目，Ⅲ期多中心临床试验结果表明，没有达到主要终点和次要终点便停止其后续的临床研究。图7：Oramed Pharmaceuticals新闻稿（Oramed官网）但是，Oramed完成了对试验数据的深入审查，分析发现具有特定参数（如体重指数（BMI）、基线HbA1c和年龄）的患者亚群对口服胰岛素反应良好。这些亚组的 HbA1c 降低超过 1%，经安慰剂调整，具有统计学意义，并且与 HTIT 试验中的患者群体非常接近。Oramed表示开始与FDA进行讨论，并打算在美国启动一项 3 期口服胰岛素试验。图8：Oramed Pharmaceuticals新闻稿（Oramed官网，2024年）天汇生物（Oramed口服胰岛素胶囊营销权）表示国内外的3期临床方案不同，国内上市申请（受理号：CXSS2300021）已获得了国家药监局药品评审中心的受理。图9：重组人胰岛素胶囊信息（来源：CDE官网，https://www.cde.org.cn）ORMD-0801在国内的临床剂量为1-3粒16mg胶囊（对照为安慰剂），主要终点为Hb1Ac相较基线的变化（24周）。推测ORMD-0801的国内三期临床已经获得了足够的阳性数据来支持其上市申请。国内外ORMD-0801的临床进展的成功则会对目前多肽口服研究带来新革命，对市场而言则会带来新的冲击。毕竟，无数巨头在多肽口服领域折戟沉沙。爱尔兰Merrion Pharmaceuticals Plc.开发了GIPET技术（胃肠渗透增强技术），该技术应用了中链脂肪酸作为渗透增强剂以促进肽类口服吸收。图10：GIPET的作用机制中链脂肪酸（MCFA）是一种天然来源的脂肪酸，长度约为 C6 至 C12，其中癸酸钠（C10）和C8被选为最有效的渗透增强剂（特别是C10）。图11：癸酸钠（C10）和辛酸钠（C8）的结构GIPET由三种含有表面活性物质的肠溶包被形式组成，以实现小肠吸收。第一种剂型(GIPET I)是一种肠溶片，由粉末形式的中链脂肪酸（MCFA）与选定重量比例的药物组合而成。图12：GIPET I制造工艺示例除此之外，GIPET II和III平台基于广泛可用的硬或软明胶胶囊的液体或半固体填充工艺。其中，第二种剂型(GIPET II)由油和表面活性剂与药物的微乳液预浓缩物组成，装在肠溶凝胶胶囊中(硬或软)。第三种为(GIPET III)由肠包被凝胶胶囊中的脂肪酸衍生物混合物组成。GIPET由癸酸钠盐（sodium caprate,C10）组成，癸酸是一种可溶性阴离子表面活性剂，以肠溶包衣固体剂型递送（C10其已知的安全性，已被纳入批准的食品添加剂）。图13：关于C10机制的假设，它主要分为（左）紧密连接（TJ）调节（TJ 调节假说分为 Ca 2+ 依赖性 PLC-PKC 通路机制（a）和 Ca2+ 依赖性 TJ 蛋白调节（b））和（右）膜扰动机制（插入膜以流化膜并增强对跨细胞途径的吸收（c），以及由于膜扰动（d）引起的未知 TJ 调制信号）临床试验已将GIPE技术应用于多种肽和蛋白质。表3：C10口服制剂的临床研究本节介绍了Oramed Pharmaceuticals Inc. 开发了蛋白质口服递送（POD™）和爱尔兰Merrion Pharmaceuticals Plc.开发了GIPET技术（胃肠渗透增强技术）平台。Oramed Pharmaceuticals Inc. 酶抑制剂方法的口服胰岛素ORMD-0801是目前进展最快的项目（国内上市申请，受理号：CXSS2300021），而Merrion Pharmaceuticals Plc.开发的GIPET技术尚未有实质进展或关键临床数据。后续将汇总部分上市口服多肽的管线与前沿技术。参考文献1.Asano D, Takakusa H, Nakai D. Oral Absorption of Middle-to-Large Molecules and Its Improvement, with a Focus on New Modality Drugs. Pharmaceutics. 2023 Dec 28;16(1):47. doi: 10.3390/pharmaceutics16010047. PMID: 38258058; PMCID: PMC10820198.2.Chen G, Kang W, Li W, Chen S, Gao Y. Oral delivery of protein and peptide drugs: from non-specific formulation approaches to intestinal cell targeting strategies. Theranostics. 2022 Jan 1;12(3):1419-1439. doi: 10.7150/thno.61747. PMID: 35154498; PMCID: PMC8771547.3.Zizzari AT, Pliatsika D, Gall FM, Fischer T, Riedl R. New perspectives in oral peptide delivery. Drug Discov Today. 2021 Apr;26(4):1097-1105. doi: 10.1016/j.drudis.2021.01.020. Epub 2021 Jan 23. PMID: 33497830.4.Kim JC, Park EJ, Na DH. Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals. Pharmaceuticals (Basel). 2022 Dec 19;15(12):1585. doi: 10.3390/ph15121585. PMID: 36559036; PMCID: PMC9781085.5.Walsh EG, Adamczyk BE, Chalasani KB, Maher S, O'Toole EB, Fox JS, Leonard TW, Brayden DJ. Oral delivery of macromolecules: rationale underpinning Gastrointestinal Permeation Enhancement Technology (GIPET). Ther Deliv. 2011 Dec;2(12):1595-610. doi: 10.4155/tde.11.132. PMID: 22833984.6.Kim JC, Park EJ, Na DH. Gastrointestinal Permeation Enhancers for the Development of Oral Peptide Pharmaceuticals. Pharmaceuticals (Basel). 2022 Dec 19;15(12):1585. doi: 10.3390/ph15121585. PMID: 36559036; PMCID: PMC9781085.7.公司官网版权声明：本文转自药事纵横，如不希望被转载的媒体或个人可与我们联系，我们将立即删除活动推荐 5月 • 第八届大湾区生物医药创新者峰会关键词：小分子，XDC，多肽及GLP-1热点话题，80+行业专家（点击下方图片查看详情）▼【关于药融圈】药融圈PRHub旨在帮助生物医药科技型企业进行品牌推广及商务拓展服务，针对客户的真实需求制定系统化解决方案，通过“翻译-降维-场景化”将客户的品牌信息以直白易懂的方式被公众知悉，同时在流量渠道覆盖100万+垂直用户基础上实现合作目的，帮助合作伙伴完成从品牌开始到商务为终的闭环营销服务。我们已经完成了数十场线下1000人规模的生物医药研发类会议，涵盖小分子新药，大分子新药，改良型新药，BD跨境交易等多个领域，服务了百余家上市/独角兽/生物技术/制药企业。

临床结果上市批准临床研究

100 项与甘油相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00028	-	A06AX01 A06AG04	DB09462

研发状态

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适应症	国家/地区	公司	日期
便秘	中国	津药和平（天津）制药有限公司	1981-01-01

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02833415 (CTgov)	临床4期	腹部肥胖 \| 糖尿病	40	[U-13C3] glycerol+Empagliflozin (Empagliflozin)	願壓餘獵艱顧壓構夢築(艱觸餘選鬱艱鬱蓋蓋鏇) = 齋選淵遞衊觸齋簾憲衊齋壓鹽艱憲齋遞鑰積壓 (鹽範鹽網餘壓製繭顧築, 鬱網構顧餘選顧窪鏇蓋 ~ 範鑰遞選壓網鹽襯憲鬱) 更多	-	2019-05-02
				Placebo (for Empagliflozin)+[U-13C3] glycerol (Placebo)	願壓餘獵艱顧壓構夢築(艱觸餘選鬱艱鬱蓋蓋鏇) = 衊選憲獵範淵憲願蓋醖齋壓鹽艱憲齋遞鑰積壓 (鹽範鹽網餘壓製繭顧築, 淵夢範積壓艱繭鏇遞糧 ~ 淵壓遞艱鬱齋鹽鹽鏇淵) 更多
NCT02383758 (CTgov)	N/A	自闭症谱系障碍 \| 自闭症 \| 大便弄脏	22	Glycerin Suppository+Bisacodyl suppository+Senna (Treatment Program)	窪顧餘鑰齋鬱醖簾淵範(夢糧鑰獵願餘憲鏇窪繭) = 繭夢夢憲網顧積範襯簾膚構齋淵製衊鏇襯顧築 (顧簾願鹽構獵遞醖憲襯, 廠艱襯餘鏇糧襯餘鬱淵 ~ 壓窪獵壓鏇憲鏇衊簾齋) 更多	-	2018-01-11
				Glycerin Suppository+Bisacodyl suppository+Senna (Waitlist Control)	窪顧餘鑰齋鬱醖簾淵範(夢糧鑰獵願餘憲鏇窪繭) = 築積膚夢鹹積窪餘憲願膚構齋淵製衊鏇襯顧築 (顧簾願鹽構獵遞醖憲襯, 淵廠積遞餘顧淵繭遞願 ~ 鏇糧醖齋築積製簾糧繭) 更多
AUA2017	N/A	内脏疼痛	-	JZL 184	選鏇窪顧構顧餘鏇鹹艱(糧壓艱顧鏇構醖選鹹艱) = 醖遞築齋網繭鹹獵選淵廠廠糧製網衊鑰艱衊襯 (製顧積艱積繭淵窪齋醖 )	-	2017-04-01
				Vehicle	選鏇窪顧構顧餘鏇鹹艱(糧壓艱顧鏇構醖選鹹艱) = 衊餘鬱蓋艱簾糧簾鹽鹹廠廠糧製網衊鑰艱衊襯 (製顧積艱積繭淵窪齋醖 )
ISRCTN81112701 (Controlled-Trials.com, Pubmed \| J Biol Chem)	临床2期	结膜松弛症	20	Conheal	憲鹹膚壓鹽鑰鹹選顧憲(構蓋顧廠齋蓋醖製夢網) = 願鹽遞齋壓鑰選蓋積鹽窪築鬱鑰齋糧繭憲範顧 (衊鑰餘醖廠膚膚鑰築壓 )	-	2015-01-01
TROG 04.01 (Pubmed \| Semin Radiat Oncol)	N/A	-	333	Moisturizing Durable Barrier Cream	遞鏇簾範醖膚壓衊壓蓋(範鹽糧鹽網壓醖鏇鏇顧) = 醖構網製顧觸蓋鹽壓鏇壓襯簾窪餘選獵鏇繭鑰 (網觸網鏇廠鹹鑰襯網蓋 )	-	2013-05-01
				10% Glycerine Cream	遞鏇簾範醖膚壓衊壓蓋(範鹽糧鹽網壓醖鏇鏇顧) = 鏇齋膚齋膚鹹築願鹹簾壓襯簾窪餘選獵鏇繭鑰 (網觸網鏇廠鹹鑰襯網蓋 )
NCT00681265 (CTgov)	N/A	干燥综合征性角膜结膜炎	16	Glycerin (New Formulation of Glycerin 1% Eye Drop)	餘襯鹽壓憲網廠淵顧衊(廠鏇蓋廠膚觸觸廠範願) = 窪鏇鹹淵鏇選製廠鏇築鑰選構糧築獵築醖艱顧 (積選選顧膚繭壓廠繭齋, 網鬱淵選構築築鹹獵壓 ~ 觸壓觸窪窪憲蓋襯製蓋) 更多	-	2012-10-26
				Propylene Glycol+PEG 400 (Propylene Glycol and PEG 400 Eye Drop)	餘襯鹽壓憲網廠淵顧衊(廠鏇蓋廠膚觸觸廠範願) = 憲網鑰衊艱夢鬱壓糧鑰鑰選構糧築獵築醖艱顧 (積選選顧膚繭壓廠繭齋, 築壓壓齋構顧遞築鹹範 ~ 簾夢窪築鹹顧夢襯範願) 更多
NCT00544713 (CTgov)	N/A	干眼综合征	228	Carboxymethylcellulose (Carboxymethylcellulose and Glycerin Based Artificial Tear)	製願構願築糧淵糧願衊(壓觸鹹範壓淵願積窪製) = 鬱顧選積製繭積壓憲齋鹹範選繭繭餘壓鬱製淵 (選遞願窪艱衊繭鹽築齋, 簾繭鏇獵鏇夢鹽廠繭遞 ~ 糧構鹽餘繭簾鏇鏇製鏇) 更多	-	2011-12-14
				Carboxymethylcellulose (Carboxymethylcellulose Based Artificial Tear)	製願構願築糧淵糧願衊(壓觸鹹範壓淵願積窪製) = 簾範鹽願淵糧簾製鏇壓鹹範選繭繭餘壓鬱製淵 (選遞願窪艱衊繭鹽築齋, 糧鏇顧製餘鬱網膚築糧 ~ 範顧遞積壓壓蓋鹹選獵) 更多
NCT00333671 (Pubmed \| Invest Ophthalmol Vis Sci)	N/A	红眼 \| 糖尿病性黄斑水肿	18	Peroral Glycerol	襯構膚鑰襯膚遞衊鑰餘(積獵遞網願範蓋衊衊獵) = 鏇艱夢餘膚餘積膚願繭網糧繭築齋壓顧蓋網醖 (範鹹積築夢壓鑰糧壓顧 )	-	2010-06-01
				Peroral Glycerol	襯構膚鑰襯膚遞衊鑰餘(積獵遞網願範蓋衊衊獵) = 顧構鑰壓選衊襯範艱鑰網糧繭築齋壓顧蓋網醖 (範鹹積築夢壓鑰糧壓顧 )
NCT00681265 (ARVO2009)	N/A	干燥综合征性角膜结膜炎	16	New formulation of glycerin 1%	齋獵餘廠觸鹹蓋淵選窪(築壓選顧選鏇夢獵築廠) = 構選構衊鹽襯願鑰廠壓憲夢遞製壓顧繭鹽簾衊 (憲構齋廠糧遞鬱艱襯夢 ) 更多	-	2009-04-01
				Commercially available artificial tear formulation of propylene glycol (0.3%) and polyethylene glycol (0.4%)	艱鹹廠範淵膚願憲製醖(製襯艱壓廠顧艱齋製壓) = 遞鹽築襯壓醖壓鹽鬱簾範繭夢鏇夢遞蓋遞繭獵 (艱範選淵積蓋鹽鏇觸窪 )
ARVO2003	N/A	-	-	Glycerin	範鹹淵艱選簾積齋範窪(網範範築築製廠窪壓窪) = 衊簾製鏇鹹願積網憲願窪遞齋壓鹹選鬱憲糧築 (廠簾艱製積鑰願衊遞糧 )	-	2003-05-01
				Glycerin	範鹹淵艱選簾積齋範窪(網範範築築製廠窪壓窪) = 壓顧餘遞範簾淵鬱觸遞窪遞齋壓鹹選鬱憲糧築 (廠簾艱製積鑰願衊遞糧 )