دورية أكاديمية
Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclodextrin) and computational calculation of their inclusion complexes.
| العنوان: | Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclodextrin) and computational calculation of their inclusion complexes. |
|---|---|
| المؤلفون: | Salman ZN; Pharmacological and Diagnostic Research Center (PDRC), Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan., Al-Ani I; Pharmacological and Diagnostic Research Center (PDRC), Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan., Al Azzam KM; Pharmacological and Diagnostic Research Center (PDRC), Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan., Majeed BJM; Pharmacological and Diagnostic Research Center (PDRC), Faculty of Pharmacy, Al-Ahliyya Amman University, Amman 19328, Jordan., Abdallah HH; Chemistry Department, College of Education, Salahaddin University-Erbil, Iraq., Negim ES; School of Materials Science and Green Technologies, Kazakh-British Technical University, St. Tole bi, 59, Almaty 050000, Kazakhstan.; School of Petroleum Engineering, Satbayev University, 22 Satpayev Street, Almaty 050013, Kazakhstan. |
| المصدر: | ADMET & DMPK [ADMET DMPK] 2023 Aug 10; Vol. 11 (4), pp. 533-550. Date of Electronic Publication: 2023 Aug 10 (Print Publication: 2023). |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: IAPC Publishing Country of Publication: Croatia NLM ID: 101660124 Publication Model: eCollection Cited Medium: Internet ISSN: 1848-7718 (Electronic) Linking ISSN: 18487718 NLM ISO Abbreviation: ADMET DMPK Subsets: PubMed not MEDLINE |
| أسماء مطبوعة: | Original Publication: [Zagreb] : IAPC Publishing, [2013]- |
| مستخلص: | Background and Purpose: Apixaban (AP) is a factor X inhibitor, an orally active drug that inhibits blood coagulation for better prevention of venous thromboembolism. It has poor solubility, dissolution rate and low bioavailability. The aim of this study was to improve the aqueous solubility and dissolution rate of oral AP as a step to enhance its bioavailability by preparing it as an inclusion complex with beta- and hydroxy propyl beta-cyclodextrin. Experimental Approach: A simple, rapid method of analysis of AP was developed using ultraviolet spectrophotometry (UV) and partially validated in terms of linearity, precision and accuracy, recovery, and robustness. AP was prepared as a complex with beta cyclodextrin (βCD) and hydroxy propyl beta cyclodextrin (HPβCD) in weight ratios 1:1, 1:2, and 1:3 by kneading, solvent evaporation and spray drying methods and characterized by Fourier transfer infra-red (FTIR), differential scanning calorimetry (DSC), and percent drug content in each of the prepared complex. Using the computer simulation, the interactions of AP with βCD and HPβCD were investigated. Key Results: The phase solubility study showed that the solubility of AP was greatly enhanced from 54×10 -3 mmol /L to 66 mmol/L using HPβCD with acceptable stability constant. Computer docking supports the formation of a stable 1:1 complex between AP and CD's. The dissolution test results showed that the complex gave a significantly higher percentage of drug release (95%) over one hour compared to the free AP (60%) (p<0.05). Conclusion: AP- HPβCD complex in the ratio of 1:2 (w/w) can significantly improve the solubility and in vitro dissolution rate of AP. Competing Interests: Conflict of interest: The authors declare no conflict of interest, financial or otherwise. (Copyright © 2023 by the authors.) |
| References: | Drugs. 2012 Jun 18;72(9):1271-91. (PMID: 22686618) Nat Rev Drug Discov. 2004 Dec;3(12):1023-35. (PMID: 15573101) Chest. 2012 Feb;141(2 Suppl):e278S-e325S. (PMID: 22315265) Drug Metab Dispos. 2009 Apr;37(4):802-8. (PMID: 19131519) AAPS PharmSciTech. 2008;9(1):314-21. (PMID: 18446497) J Thromb Thrombolysis. 2011 May;31(4):478-92. (PMID: 21318583) Heliyon. 2022 Oct 12;8(10):e11015. (PMID: 36281394) Int J Pharm. 2021 Jan 5;592:120026. (PMID: 33137448) J Med Chem. 2007 Nov 1;50(22):5339-56. (PMID: 17914785) Nat Biotechnol. 2001 Aug;19(8):722-6. (PMID: 11479558) Pharmaceutics. 2022 Nov 16;14(11):. (PMID: 36432664) ISRN Pharm. 2012;2012:195727. (PMID: 22830056) Thromb J. 2013 Dec 31;11(1):27. (PMID: 24380488) Drug Metab Dispos. 2013 Apr;41(4):827-35. (PMID: 23382458) Clin Pharmacokinet. 2019 Oct;58(10):1265-1279. (PMID: 31089975) |
| فهرسة مساهمة: | Keywords: HPβCD; apixaban; bioavailability; capsule; solubility; βCD |
| تواريخ الأحداث: | Date Created: 20231108 Latest Revision: 20231109 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC10626519 |
| DOI: | 10.5599/admet.1885 |
| PMID: | 37937243 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1848-7718 |
|---|---|
| DOI: | 10.5599/admet.1885 |