دورية أكاديمية
Pharmacokinetics and pharmacodynamics of glimepiride polymorphs.
| العنوان: | Pharmacokinetics and pharmacodynamics of glimepiride polymorphs. |
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| المؤلفون: | Viana ALM; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil., Doriguetto AC; Chemistry Institute, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil. Electronic address: doriguetto@unifal-mg.edu.br., Viana OMMS; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil; Chemistry Institute, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil., Ruela ALM; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil; Multidisciplinary Health Institute, Federal University of Bahia, Vitória da Conquista, Bahia, Brazil., Freitas JTJ; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil., Souto BEM; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil., de Araújo MB; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil., de Araújo Paula FB; Pharmaceutical Sciences Faculty, Federal University of Alfenas, Alfenas, Minas Gerais, Brazil. |
| المصدر: | International journal of pharmaceutics [Int J Pharm] 2018 Dec 20; Vol. 553 (1-2), pp. 272-280. Date of Electronic Publication: 2018 Oct 23. |
| نوع المنشور: | Comparative Study; Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier/North-Holland Biomedical Press Country of Publication: Netherlands NLM ID: 7804127 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3476 (Electronic) Linking ISSN: 03785173 NLM ISO Abbreviation: Int J Pharm Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Amsterdam, Elsevier/North-Holland Biomedical Press. |
| مواضيع طبية MeSH: | Blood Glucose/*drug effects , Hypoglycemic Agents/*chemistry , Insulin/*blood , Sulfonylurea Compounds/*chemistry, Administration, Oral ; Animals ; Capsules ; Crystallization ; Gelatin ; Hypoglycemic Agents/pharmacokinetics ; Hypoglycemic Agents/pharmacology ; Male ; Rats ; Rats, Wistar ; Solubility ; Sulfonylurea Compounds/pharmacokinetics ; Sulfonylurea Compounds/pharmacology |
| مستخلص: | Glimepiride (GLIM) is used as an oral antihyperglycemic agent for treatment of type 2 diabetes. The drug presents two polymorphic forms (GLIM form I and GLIM form II) described in the literature, and according to in vitro data, GLIM form II is about 3.5 times more soluble and releases 2 times the drug amount than GLIM form I in the physiological pH range. Considering the literature in vitro data and that the diabetes treatment demands glycemic control, avoiding abrupt fluctuations in the blood glucose levels, this work aimed to study the impact of GLIM polymorphism in the in vivo performance of GLIM solid oral dosages. For this, hard gelatin capsules with GLIM form I or II were prepared and orally administered in rats. After that, pharmacokinetic studies were performed by sampling animal blood at different times, and biochemical parameters (pharmacodynamic), such as glucose and insulin, were also evaluated. Our results showed that the in vitro data corroborate with our in vivo assays. GLIM form II provided higher plasma concentration of drug than form I (at baseline up to approximately 200 min after oral administration) and, consequently, increased insulin release and reduced levels of glucose, showing good correlation between pharmacokinetic and pharmacodynamics assays. Thus, this study demonstrated that GLIM polymorphs in oral dosages might alter the drug efficacy, which may expose the patients to risks, such as hypoglycemia. (Copyright © 2018 Elsevier B.V. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Glimepiride; In vivo studies; Pharmacodynamics; Pharmacokinetics; Polymorphism; Solid-state; Type 2 diabetes |
| المشرفين على المادة: | 0 (Blood Glucose) 0 (Capsules) 0 (Hypoglycemic Agents) 0 (Insulin) 0 (Sulfonylurea Compounds) 6KY687524K (glimepiride) 9000-70-8 (Gelatin) |
| تواريخ الأحداث: | Date Created: 20181026 Date Completed: 20190308 Latest Revision: 20190308 |
| رمز التحديث: | 20221213 |
| DOI: | 10.1016/j.ijpharm.2018.10.050 |
| PMID: | 30359686 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1873-3476 |
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| DOI: | 10.1016/j.ijpharm.2018.10.050 |