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Transdermal metformin

Hudson Polonini, Paulo José Lopes Cândido, Junquiera Laura Andrade, Sharlene Loures, Nádia Rb Raposo, Marcos Antônio Fernandes Brandão, Anderson de Oliveira Ferreira
Metformin hydrochloride is a traditional, FDA-approved drug used as a first-line drug of choice to treat type 2 diabetes. Research has shown metformin hydrochloride effective in injuries, including age-related maladies. The purpose of this ex vivo study was to evaluate the use of a commercial transdermal vehicle as a semisolid, liposomal vanishing cream (Pentravan) to deliver metformin hydrochloride through the human skin. The experiments were conducted as percutaneous absorption assay in Franz Diffusion Cells, coupled with freshly excised human skin and analyzed by high-performance liquid chromatography...
January 2019: International Journal of Pharmaceutical Compounding
Mohamed S El-Ridy, Soad A Yehia, Ibrahim El-Sayed, Mostafa M Younis, Rehab Fawzy Abdel Rahman, Menna Ahmed El-Gamil
Niosomes as drug delivery systems have the ability to decrease drugs' side effects and increase their therapeutic effectiveness. Metformin HCl is an oral anti-hyperglycemic agent belonging to biguanides. It is the most commonly chosen drug as a start-up therapy for patients newly diagnosed with type 2 diabetes. This study aims to encapsulate metformin HCl inside niosomes to be used as a transdermal formulation helping to prolong its anti-diabetic effect and investigate its ability to enhance wound healing in diabetic patients...
December 10, 2018: Journal of Liposome Research
Eman M Migdadi, Aaron J Courtenay, Ismaiel A Tekko, Maelíosa T C McCrudden, Mary-Carmel Kearney, Emma McAlister, Helen O McCarthy, Ryan F Donnelly
We investigated, for the first time, the potential for a hydrogel-forming microneedle (MN) patch to deliver the high-dose drug metformin HCl transdermally in a sustained manner. This may minimize some gastrointestinal side effects and small intestine absorption variations associated with oral delivery. Patches (two layers) were assembled from a lyophilised drug reservoir layer, with the MN layer made from aqueous blend of 20% w/w poly (methylvinylether-co-maleic acid) crosslinked by esterification with 7.5% w/w poly (ethylene glycol) 10,000 Da...
September 10, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Xiang Yu, Yiguang Jin, Lina Du, Mengchi Sun, Jian Wang, Qiu Li, Xiangyu Zhang, Zisen Gao, Pingtian Ding
Transdermal delivery is one of important controlled drug release strategies for drug development. Cubic phases are the assemblies of amphiphilic molecules in water with the hydrophilic-hydrophobic interpenetrating network for transdermal delivery of both hydrophilic and hydrophobic drugs. However, many details about the transdermal delivery of drugs from cubic phases remain unclear. Here, metformin hydrochloride (Met) cubic phases were prepared with glyceryl monooleate (GMO), ethanol, and water. The cubic structure was identified with the polarizing light microscopy and small-angle X-ray scattering method...
August 6, 2018: Molecular Pharmaceutics
Anushree Herwadkar, Neha Singh, Carter Anderson, Andrew Korey, William Fowler, Ajay K Banga
PURPOSE: The objective of this work was to identify deactivation agents and develop a disposal system for unused/ residual/ expired medications. METHODS: Deactivation agents screened included oxidizing agent-sodium percarbonate, hydrolysis agent- sodium carbonate and adsorbants- zeolite and activated carbon. Deactivation studies using these agents were performed on four active pharmaceutical agents (APIs) including ketoprofen, dexamethasone sodium phosphate, metformin hydrochloride and amoxicillin trihydrate...
January 2016: Pharmaceutical Research
Hélène M Faessel, R Scott Obach, Hans Rollema, Patanjali Ravva, Kathryn E Williams, Aaron H Burstein
Varenicline tartrate (Chantix®/Champix®) is a selective partial agonist of the α(4)β(2) nicotinic acetylcholine receptor and is approved as an aid to smoking cessation. The usual oral dosage in adults is 1 mg twice daily for 12 weeks, with an initial titration week. Several clinical pharmacology studies have characterized the pharmacokinetics of varenicline in adult smokers aged 18-55 years, elderly smokers and nonsmokers aged ≥ 65 years, adolescent smokers aged 12-17 years and subjects with impaired renal function...
December 2010: Clinical Pharmacokinetics
Lourdes Ibáñez, Abel López-Bermejo, Marta Díaz, Goya Enríquez, Carme Valls, Francis de Zegher
BACKGROUND AND AIM: Low-dose pioglitazone (Pio), flutamide (Flu), metformin (Met) plus an oestro-progestagen is a novel polytherapy lowering total and visceral adiposity, and reducing carotid intima media thickness (IMT) in hyperinsulinaemic women with androgen excess, without changing their body mass index (BMI). In a search for mediators of PioFluMet's actions, we measured serum levels of visfatin and high molecular weight (HMW) adiponectin. DESIGN AND PATIENTS: In a double-blind study, we enrolled 38 young women with hyperinsulinaemic androgen excess [mean BMI: 23...
February 2008: Clinical Endocrinology
Lisa A Potts, Candice L Garwood
PURPOSE: The pharmacology, pharmacokinetics, clinical efficacy, safety, dosage and administration, and place in therapy of varenicline are reviewed. SUMMARY: Varenicline is the newest therapy approved by the Food and Drug Administration for smoking cessation and the first in its class targeting the neurobiology of nicotine addiction. Varenicline is selective for the alpha4beta2 acetylcholine-receptor subtype as a partial agonist, thus conferring its effect in limiting the reinforcing aspect of the addictive nicotine molecule...
July 1, 2007: American Journal of Health-system Pharmacy: AJHP
Lourdes Ibáñez, Abel López-Bermejo, Luis del Rio, Goya Enríquez, Carme Valls, Francis de Zegher
CONTEXT AND OBJECTIVE: One of the treatments for hyperinsulinemic hyperandrogenism in nonobese women is combined androgen receptor blockade (with flutamide; Flu), insulin sensitization (with metformin; Met) plus an estroprogestagen contraceptive. We tested whether adding low-dose pioglitazone (Pio; 7.5 mg/d) confers more benefit. SETTING: The study was conducted at a university hospital. STUDY POPULATION AND DESIGN: This double-blind study enrolled 38 young women with hyperinsulinemic hyperandrogenism [mean body mass index (BMI) 24 kg/m(2)], all of whom started on Flu (62...
May 2007: Journal of Clinical Endocrinology and Metabolism
Seena L Zierler-Brown, Jeffrey A Kyle
OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, and safety of varenicline and provide a review of relevant clinical data. DATA SOURCES: A MEDLINE search (2001-December 2006) was conducted using the key words varenicline and nicotine replacement therapy for clinical trials limited to human subjects and published in English. STUDY SELECTION AND DATA EXTRACTION: All available human trials of varenicline were selected for review...
January 2007: Annals of Pharmacotherapy
Lourdes Ibáñez, Francis de Zegher
Hyperinsulinemic hyperandrogenism is the core of polycystic ovary syndrome (PCOS), and, accordingly, low-dose flutamide-metformin proved so far to be a most effective approach to normalize the broad spectrum of PCOS anomalies in nonobese adolescents and young women. For safety reasons, it is wise to combine flutamide-metformin with a contraceptive, for example, an oral or transdermal estroprogestagen.
July 2006: Fertility and Sterility
Lourdes Ibáñez, Francis de Zegher
Polycystic ovary syndrome (PCOS) is a variable disorder that is characterized in adolescents and young women by a broad spectrum of anomalies, including hyperandrogenemia, insulin resistance, dyslipidemia, body adiposity and low-grade inflammation. At present, there is no approved therapy for PCOS. Recent studies indicate that a low-dose combination of flutamide (Flu; a generic androgen-receptor blocker) and metformin (Met; a generic insulin-sensitizer) normalizes the adolescent PCOS spectrum more than an oral contraceptive (OC); in young women, the PCOS spectrum was found to be more normalized by OC plus Flu-Met than by OC alone...
May 2006: Human Reproduction Update
Lourdes Ibáñez, Carme Valls, Francis de Zegher
BACKGROUND: Low-dose flutamide-metformin (Flu-Met) with an oral contraceptive is a therapeutic option for women with hyperinsulinaemic hyperandrogenism. We questioned (i) whether Flu-Met maintains efficacy if given discontinuously; (ii) how the efficacy of discontinuous Flu-Met plus a transdermal contraceptive compares with Flu-Met plus oral contraceptive; and (iii) whether these treatments also lower circulating C-reactive protein (CRP) and tumour necrosis factor alpha (TNF-alpha) and the high neutrophil/lymphocyte ratio...
February 2006: Human Reproduction
M Bayés, X Rabasseda, J R Prous
Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables has been retrieved from the Clinical Studies Knowledge Area of Prous Science Integrity, the drug discovery and development portal, This issue focuses on the following selection of drugs: Abetimus sodium, ademetionine, agalsidase alfa, agalsidase beta, alemtuzumab, alfimeprase, AMG-162, androgel, anidulafungin, antigastrin therapeutic vaccine, aripiprazole, atomoxetine hydrochloride; Bazedoxifene acetate, bevacizumab, bosentan; Caldaret hydrate, canfosfamide hydrochloride, choriogonadotropin alfa, ciclesonide, combretastatin A-4 phosphate, CY-2301; Darbepoetin alfa, darifenacin hydrobromide, decitabine, degarelix acetate, duloxetine hydrochloride; ED-71, enclomiphene citrate, eplerenone, epratuzumab, escitalopram oxalate, eszopiclone, ezetimibe; Fingolimod hydrochloride, FP-1096; HMR-3339A, HSV-TK/GCV gene therapy, human insulin, HuOKT3gamma1(Ala234-Ala235); Idursulfase, imatinib mesylate, indiplon, InnoVax C insulin glargine, insulin glulisine, irofulven; Labetuzumab, lacosamide, lanthanum carbonate, LyphoDerm, Lyprinol; Magnesium sulfate, metelimumab, methylphenidate hydrochloride; Natalizumab, NO-aspirin; OROS(R); PC-515, pegaptanib sodium, peginterferon alfa-2a, peginterferon alfa-2b, peginterferon alfa-2b/ribavirin, pemetrexed disodium, peptide YY3-36, posaconazole, pregabalin, PT-141, pyridoxamine; R-744, ramelteon, ranelic acid distrontium salt, rebimastat, repinotan hydrochloride, rhC1, rhGAD65, rosiglitazone maleate/metformin hydrochloride; Sardomozide, solifenacin succinate; Tadalafil, taxus, telavancin, telithromycin, tenofovir disoproxil fumarate, teriparatide, testosterone transdermal patch, tetomilast, tirapazamine, torcetrapib; Valspodar, vardenafil hydrochloride hydrate, vildagliptin; Yttrium Y90 epratuzumab; Ziprasidone hydrochloride...
December 2004: Methods and Findings in Experimental and Clinical Pharmacology
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