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Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique
[Image: see text] The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble drug amoxicillin (AM) by the solid dispersion (SD) technique. Six different SDs of AM, F1–F6, wer...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9798760/ https://www.ncbi.nlm.nih.gov/pubmed/36591136 http://dx.doi.org/10.1021/acsomega.2c06662 |
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author | Hassan, Faiza Sher, Muhammad Hussain, Muhammad Ajaz Saadia, Mubshara Naeem-Ul-Hassan, Muhammad Rehman, Muhammad Fayyaz ur Haseeb, Muhammad Tahir Bukhari, Syed Nasir Abbas Abbas, Azhar Peng, Bo Kanwal, Fariha Deng, Huibiao |
author_facet | Hassan, Faiza Sher, Muhammad Hussain, Muhammad Ajaz Saadia, Mubshara Naeem-Ul-Hassan, Muhammad Rehman, Muhammad Fayyaz ur Haseeb, Muhammad Tahir Bukhari, Syed Nasir Abbas Abbas, Azhar Peng, Bo Kanwal, Fariha Deng, Huibiao |
author_sort | Hassan, Faiza |
collection | PubMed |
description | [Image: see text] The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble drug amoxicillin (AM) by the solid dispersion (SD) technique. Six different SDs of AM, F1–F6, were prepared by the spray drying technique using two other carriers, HP-β-CD (F1–F3) and HPMC (F4–F6), in 1:1, 1:2, and 1:3 drug-to-polymer ratios. These SDs were analyzed to determine their practical yield, drug content, and aqueous solubility using analytical techniques such as Fourier transform infrared spectroscopy, scanning electron microscopy, thermogravimetric analysis, and powder X-ray diffraction. The effect of polymer concentration on SDs was determined using aqueous solubility, in vitro dissolution, and in vivo studies. The results showed no drug–polymer interactions in SDs. Solubility studies showed that SDs based on the drug-to-polymer ratio of 1:2 (F2 and F5) were highly soluble in water compared to those with ratios of 1:1 and 1:3. In vitro dissolution studies also showed that SDs with a ratio of 1:2 released the highest drug concentration from both polymeric systems. The SDs based on HPMC confirmed the more sustained release of the drug as compared to that of HP-β-CD. All the SDs were observed as stable and amorphous, with a smooth spherical surface. In vivo studies reveal the enhancement of pharmacokinetics parameters as compared to standard AM. Hence, it is confirmed that spray drying is an excellent technique to enhance the solubility of AM in an aqueous medium. This may contribute to the enhancement of the pharmacokinetic behaviors of SDs. |
format | Online Article Text |
id | pubmed-9798760 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-97987602022-12-30 Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique Hassan, Faiza Sher, Muhammad Hussain, Muhammad Ajaz Saadia, Mubshara Naeem-Ul-Hassan, Muhammad Rehman, Muhammad Fayyaz ur Haseeb, Muhammad Tahir Bukhari, Syed Nasir Abbas Abbas, Azhar Peng, Bo Kanwal, Fariha Deng, Huibiao ACS Omega [Image: see text] The dose frequency of drugs belonging to class II is usually high and associated with harmful effects on the body. The study aimed to enhance the solubility of the poorly water-soluble drug amoxicillin (AM) by the solid dispersion (SD) technique. Six different SDs of AM, F1–F6, were prepared by the spray drying technique using two other carriers, HP-β-CD (F1–F3) and HPMC (F4–F6), in 1:1, 1:2, and 1:3 drug-to-polymer ratios. These SDs were analyzed to determine their practical yield, drug content, and aqueous solubility using analytical techniques such as Fourier transform infrared spectroscopy, scanning electron microscopy, thermogravimetric analysis, and powder X-ray diffraction. The effect of polymer concentration on SDs was determined using aqueous solubility, in vitro dissolution, and in vivo studies. The results showed no drug–polymer interactions in SDs. Solubility studies showed that SDs based on the drug-to-polymer ratio of 1:2 (F2 and F5) were highly soluble in water compared to those with ratios of 1:1 and 1:3. In vitro dissolution studies also showed that SDs with a ratio of 1:2 released the highest drug concentration from both polymeric systems. The SDs based on HPMC confirmed the more sustained release of the drug as compared to that of HP-β-CD. All the SDs were observed as stable and amorphous, with a smooth spherical surface. In vivo studies reveal the enhancement of pharmacokinetics parameters as compared to standard AM. Hence, it is confirmed that spray drying is an excellent technique to enhance the solubility of AM in an aqueous medium. This may contribute to the enhancement of the pharmacokinetic behaviors of SDs. American Chemical Society 2022-12-15 /pmc/articles/PMC9798760/ /pubmed/36591136 http://dx.doi.org/10.1021/acsomega.2c06662 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/). |
spellingShingle | Hassan, Faiza Sher, Muhammad Hussain, Muhammad Ajaz Saadia, Mubshara Naeem-Ul-Hassan, Muhammad Rehman, Muhammad Fayyaz ur Haseeb, Muhammad Tahir Bukhari, Syed Nasir Abbas Abbas, Azhar Peng, Bo Kanwal, Fariha Deng, Huibiao Pharmaceutical and Pharmacological Evaluation of Amoxicillin after Solubility Enhancement Using the Spray Drying Technique |
title | Pharmaceutical
and Pharmacological Evaluation of Amoxicillin
after Solubility Enhancement Using the Spray Drying Technique |
title_full | Pharmaceutical
and Pharmacological Evaluation of Amoxicillin
after Solubility Enhancement Using the Spray Drying Technique |
title_fullStr | Pharmaceutical
and Pharmacological Evaluation of Amoxicillin
after Solubility Enhancement Using the Spray Drying Technique |
title_full_unstemmed | Pharmaceutical
and Pharmacological Evaluation of Amoxicillin
after Solubility Enhancement Using the Spray Drying Technique |
title_short | Pharmaceutical
and Pharmacological Evaluation of Amoxicillin
after Solubility Enhancement Using the Spray Drying Technique |
title_sort | pharmaceutical
and pharmacological evaluation of amoxicillin
after solubility enhancement using the spray drying technique |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9798760/ https://www.ncbi.nlm.nih.gov/pubmed/36591136 http://dx.doi.org/10.1021/acsomega.2c06662 |
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