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. |
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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. |
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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 |
تدمد: | 1422-0067 |
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DOI: | 10.3390/ijms241512215 |