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Fighting type 2 diabetes: Formulation strategies for peptide-based therapeutics

Acta Pharmaceutica Sinica B 2022年第2期12卷 621-636页

作者： Carlos Bendicho-Lavilla Iria Seoane-Viano Francisco J.OteroEspinar asteria luzardo-alvarez Department of Pharmacology Pharmacy and Pharmaceutical TechnologyFaculty of PharmacyUniversity of Santiago de Compostela(USC)Santiago de Compostela 15782Spain Paraquasil Group Health Research Institute of Santiago de Compostela(IDIS)Santiago de Compostela 15706Spain Department of Pharmacology Pharmacy and Pharmaceutical TechnologySchool of SciencesCampus de LugoUniversity of Santiago de CompostelaLugo 27002Spain

Diabetes mellitus is a major health problem with increasing prevalence at a global *** discovery of insulin in the early 1900 s represented a major breakthrough in diabetes management,with further milestones being subsequently achieved with the identification of glucagon-like peptide-1(GLP-1)and the introduction of GLP-1 receptor agonists(GLP-1 RAs)in clinical ***,the subcutaneous delivery of biotherapeutics is a well-established route of administration generally preferred over the intravenous route due to better patient compliance and prolonged drug ***,current subcutaneous formulations of GLP-1 RAs present pharmacokinetic problems that lead to adverse reactions and treatment *** this review,we discuss the current challenges of subcutaneous administration of peptide-based therapeutics and provide an overview of the formulations available for the different routes of administration with improved bioavailability and reduced frequency of administration.

关键词： Type 2 diabetes mellitus Glucagon-like peptide-1 receptor agonists Exenatide Subcutaneous administration Amylin mimetics Drug delivery systems Biotherapeutics Peptide delivery Controlled-release formulations Microparticles Nanoparticles

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3D printed tacrolimus suppositories for the treatment of ulcerative colitis

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Asian Journal of Pharmaceutical Sciences 2021年第1期16卷 110-119页

作者： Iria Seoane-Viano Jun Jie Ong asteria luzardo-alvarez Miguel Gonzalez-Barcia Abdul W.Basit Francisco J.Otero-Espinar Alvaro Goyanes Department of Pharmacology Pharmacy and Pharmaceutical TechnologyFaculty of PharmacyUniversity of Santiago de CompostelaSantiago de Compostela 15782Spain Department of Pharmaceutics UCL School of PharmacyUniversity College LondonLondon WC1N 1AXUK Pharmacy Department University Clinical Hospital Santiago de Compostela(SERGAS)(CHUS)Santiago de Compostela 15706Spain FabRx Ltd. AshfordKent TN240RWUK Departamento de Farmacologia Farmacia y Tecnologia FarmaceuticaI+D Farma Group(GI-1645)Universidade de Santiago de CompostelaSantiago de Compostela 15782Spain

Ulcerative colitis is a global health problem,affecting millions of individuals *** an inflammatory condition localised in the large intestine,rectal delivery of immunosuppressive therapies such as tacrolimus is a promising strategy to maximise drug concentration at the site of action whilst minimising systemic side ***,for the first time,self-supporting 3D-printed tacrolimus suppositories were prepared without the aid of moulds using a pharmaceutical semi-solid extrusion(SSE)3D *** suppositories were printed vertically in three different sizes using combinations of two lipid pharmaceutical excipients(Gelucire 44/14 or Gelucire 48/16)and coconut *** both suppository formulations had the appropriate viscosity characteristics for printing,the Gel 44 formulation required less energy and force for extrusion compared to the Gel 48 *** Gel 44 disintegrated more rapidly but released tacrolimus more slowly than the Gel 48 *** the tacrolimus release profiles were significantly different,both suppository systems released more than 80% drug within 120 *** and XRD analysis was inconclusive in determining the solid-state properties of the drug in the *** summary,this article reports on the fabrication of 3D printed selfsupporting suppositories to deliver personalised doses of a narrow therapeutic index drug,with potential benefits for patients with ulcerative colitis.

关键词： 3D printed drug products Semi-solid extrusion 3D printing Inflammatory bowel disease Suppository drug delivery Pressure assisted syringe M3dimaker

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Neuromodulation for fecal incontinence: An effective surgical intervention

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World Journal of Gastroenterology 2013年第41期19卷 7048-7054页

作者： Giuseppe Chiarioni Olafur S Palsson Corrado R asteria William E Whitehead Division of Gastroenterology of the University of Verona Valeggio s/M HospitalAzienda Ospedaliera Universitaria Integrata di Verona37067 Valeggio sul MincioVeronaItaly Division of Gastroenterology and Hepatology and Center for Functional Gastrointestinal and Motility Disorders University of North Carolina at Chapel HillChapel HillNC 27516United States Department of Surgery and Orthopedics General Surgery UnitAzienda Ospedaliera Carlo Poma di MantovaAsola General Hospital46041 AsolaMantovaItaly

Fecal incontinence is a disabling symptom with medical and social implications,including fear,embarrassment,isolation and even *** patients live in seclusion and have to plan their life around the symptom,with secondary impairment of their quality of *** management and biofeedback therapy are reported to benefit a good percentage of those ***,surgery must be considered in the nonresponder ***,sacral nerve electrostimulation,lately named neuromodulation,has been reported to benefit patients with fecal incontinence in randomized controlled trials more than placebo stimulation and conservative management,by some unknown *** is a minimally invasive procedure with a low rate of adverse events and apparently favorable cost-efficacy *** review is intended to expand knowledge about this effective intervention among the non-surgically skilled community who deals with this disabled group of patients.

关键词： Fecal incontinence Neuromodulation Sacral nerve stimulation Biofeedback Anal sphincter

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Chronic proctalgia and chronic pelvic pain syndromes:New etiologic insights and treatment options

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World Journal of Gastroenterology 2011年第40期17卷 4447-4455页

作者： Giuseppe Chiarioni Corrado asteria William E Whitehead Division of Gastroenterology of the University of Verona Azienda Ospedaliera Universitaria Integrata di Verona Valeggio sul Mincio Hospital 37067 Valeggio sul Mincio Verona Italy Department of Surgery and Orthopedics General Surgery Unit Azienda Ospedaliera Carlo Poma di Mantova Asola General Hospital 46041 Asola Mantova Italy Division of Gastroenterology and Hepatology Division of Urogynecology and Center for Functional Gastrointestinal and Motility Disorders University of North Carolina at Chapel Hill Chapel Hill NC 27599-7080 United States

This systematic review addresses the pathophysiology, diagnostic evaluation, and treatment of several chronic pain syndromes affecting the pelvic organs:chronic proctalgia, coccygodynia, pudendal neuralgia, and chronic pelvic pain. Chronic or recurrent pain in the anal canal, rectum, or other pelvic organs occurs in 7% to 24% of the population and is associated with impaired quality of life and high health care costs. However, these pain syndromes are poorly understood, with little research evidence available to guide their diagnosis and treatment. This situation appears to be changing:A recently published large randomized,controlled trial by our group comparing biofeedback, electrogalvanic stimulation, and massage for the treatment of chronic proctalgia has shown success rates of 85% for biofeedback when patients are selected based on physical examination evidence of tenderness in response to traction on the levator ani muscle-a physical sign suggestive of striated muscle tension. Excessive tension (spasm) in the striated muscles of the pelvic floor appears to be common to most of the pelvic pain syndromes. This suggests the possibility that similar approaches to diagnostic assessment and treatment may improve outcomes in other pelvic pain disorders.

关键词： Biofeedback Chronic pelvic pain Chronicproctalgia Coccygodynia Levator ani syndrome Pudendal neuralgia

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可逆乳状液乳液的制备及其转化机理

可逆乳状液乳液的制备及其转化机理

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作者： asteria M. Kimambo 中国石油大学(华东)

学位级别：硕士

在钻井和完井过程中通过使用环境友好的钻井液来降低储层损害并保持储层的渗透性,可以提高天然气和石油产能。可逆乳化钻井液兼具水基钻井液和油基钻井液的优点,被认为是钻井液技术的突破。本研究使用胺表面活性剂、油田乳化剂、SKALN 5... 详细信息

在钻井和完井过程中通过使用环境友好的钻井液来降低储层损害并保持储层的渗透性,可以提高天然气和石油产能。可逆乳化钻井液兼具水基钻井液和油基钻井液的优点,被认为是钻井液技术的突破。本研究使用胺表面活性剂、油田乳化剂、SKALN 5#白油和蒸馏水制备了可逆乳状液,研究了乳化剂浓度,搅拌时间,强度,温度,酸碱比等体积因素的影响,分析了所制备的可逆乳状液的性质,如电稳定性、电导率、粘度和微观形貌,探讨了可逆转相机理。结果表明,制备的乳状液的稳定性很大程度上取决于各种制备工艺,如乳化剂浓度、搅拌时间、强度和温度。在使用胺表面活性剂和油田乳化剂制备w/o乳状液的最佳乳化剂浓度分别为0.33%和0.44%,搅拌时间分别为20分钟和40分钟。讨论了酸的类型对相转化的影响(包括盐酸、甲酸、乙酸、丙烯酸和硫酸),除了用胺表面活性剂稳定的乳状液不能用硫酸转相之外,都可以转化为o/w乳状液。在转相后的乳状液中加入碱溶液(如NaOH、Ca(OH)或NaCO),乳状液又可以反转为w/o乳状液。乳状液的可逆转相机理被认为是通过改变乳液的pH值,使得乳化剂的质子化和去质子化。

关键词：可逆乳状液乳化剂相转化可逆转相机理

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