دورية أكاديمية
Composites of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide with Polymers: Effect of Crystallinity on Solubility and Stability.
| العنوان: | Composites of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide with Polymers: Effect of Crystallinity on Solubility and Stability. |
|---|---|
| المؤلفون: | Markeev VB; V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia., Blynskaya EV; V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia.; Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia., Tishkov SV; V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia., Alekseev KV; V.V. Zakusov Research Institute of Pharmacology, 8 Baltiyskaya St., 125315 Moscow, Russia., Marakhova AI; Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia., Vetcher AA; Institute of Biochemical Technology and Nanotechnology, Peoples' Friendship University of Russia n.a. P. Lumumba (RUDN), 6 Miklukho-Maklaya St., 117198 Moscow, Russia.; Complementary and Integrative Health Clinic of Dr. Shishonin, 5, Yasnogorskaya St., 117588 Moscow, Russia., Shishonin AY; Complementary and Integrative Health Clinic of Dr. Shishonin, 5, Yasnogorskaya St., 117588 Moscow, Russia. |
| المصدر: | International journal of molecular sciences [Int J Mol Sci] 2023 Jul 30; Vol. 24 (15). Date of Electronic Publication: 2023 Jul 30. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: MDPI Country of Publication: Switzerland NLM ID: 101092791 Publication Model: Electronic Cited Medium: Internet ISSN: 1422-0067 (Electronic) Linking ISSN: 14220067 NLM ISO Abbreviation: Int J Mol Sci Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Basel, Switzerland : MDPI, [2000- |
| مواضيع طبية MeSH: | Polymers*/chemistry , Povidone*/chemistry, Solubility ; Water ; Pyrazines ; Calorimetry, Differential Scanning ; X-Ray Diffraction |
| مستخلص: | This work aimed to develop and characterize a water-soluble, high-release active pharmaceutical ingredient (API) composite based on the practically water-insoluble API N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide (GML-3), a substance with antidepressant and anxiolytic action. This allows to ensure the bioavailability of the medicinal product of combined action. Composites obtained by the method of creating amorphous solid dispersions, where polyvinylpyrrolidone (PVP) or Soluplus ® was used as a polymer, were studied for crystallinity, stability and the release of API from the composite into purified water. The resulting differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), and dissolution test data indicate that the resulting composites are amorphous at 1:15 API: polymer ratios for PVP and 1:5 for Soluplus ® , which ensures the solubility of GML-3 in purified water and maintaining the supercritical state in solution. |
| References: | Int J Pharm. 2020 Apr 30;580:119240. (PMID: 32197983) Eur J Pharm Sci. 2021 Feb 1;157:105642. (PMID: 33189903) Eur J Pharm Biopharm. 2018 Mar;124:147-157. (PMID: 29269154) Pharm Res. 2017 Sep;34(9):1754-1772. (PMID: 28523384) Eur J Pharm Biopharm. 2019 Dec;145:98-112. (PMID: 31698042) J Pharm Sci. 2021 Apr;110(4):1470-1479. (PMID: 33333143) Int J Pharm. 2019 May 1;562:113-123. (PMID: 30902705) J Pharm Sci. 2021 Jul;110(7):2703-2717. (PMID: 33609521) Carbohydr Polym. 2014 Apr 15;104:166-74. (PMID: 24607174) J Pharm Sci. 2018 Sep;107(9):2385-2398. (PMID: 29752945) J Pharm Sci. 2022 Nov;111(11):3114-3129. (PMID: 35921915) Mol Pharm. 2016 Apr 4;13(4):1339-46. (PMID: 26954586) Int J Pharm. 2020 Nov 30;590:119925. (PMID: 33011255) Bioorg Med Chem. 2015 Jul 1;23(13):3368-78. (PMID: 25937237) Eur J Pharm Sci. 2022 Feb 1;169:106086. (PMID: 34861411) Eur J Pharm Biopharm. 2021 Jan;158:323-335. (PMID: 33296719) Mol Pharm. 2014 Nov 3;11(11):4228-37. (PMID: 25325389) Int J Pharm. 2020 Oct 15;588:119741. (PMID: 32783978) J Pharm Anal. 2019 Feb;9(1):34-39. (PMID: 30740255) Int J Pharm. 2021 Sep 5;606:120902. (PMID: 34293468) Int J Pharm. 2022 Apr 5;617:121625. (PMID: 35259442) J Pharm Sci. 2021 Apr;110(4):1495-1512. (PMID: 32818440) Saudi Pharm J. 2017 Mar;25(3):419-439. (PMID: 28344498) Life Sci. 2022 Feb 15;291:120301. (PMID: 34999114) Eksp Klin Farmakol. 2016;79(1):7-11. (PMID: 27159950) Int J Pharm. 2020 Nov 15;589:119845. (PMID: 32931845) Int J Pharm. 2023 Feb 5;632:122564. (PMID: 36586638) Eur J Pharm Sci. 2020 Apr 15;146:105276. (PMID: 32092362) J Control Release. 2018 Jan 10;269:110-127. (PMID: 29117503) Int J Pharm. 2023 Apr 5;636:122745. (PMID: 36822340) J Pharm Sci. 2023 Jan;112(1):8-18. (PMID: 35948156) Saudi Pharm J. 2022 Jun;30(6):711-725. (PMID: 35812143) J Pharm Sci. 2022 Sep;111(9):2496-2504. (PMID: 35405124) |
| فهرسة مساهمة: | Keywords: amorphous solid dispersions; antidepressants; anxiolytics; bioavailability; composite; solubility |
| المشرفين على المادة: | 0 (Polymers) 0 (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer) FZ989GH94E (Povidone) 059QF0KO0R (Water) 0 (Pyrazines) |
| تواريخ الأحداث: | Date Created: 20230812 Date Completed: 20230814 Latest Revision: 20230814 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC10418436 |
| DOI: | 10.3390/ijms241512215 |
| PMID: | 37569589 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1422-0067 |
|---|---|
| DOI: | 10.3390/ijms241512215 |