Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach
To develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethyle...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2018-09-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1999-4923/10/3/161 |
| _version_ | 1828112698848575488 |
|---|---|
| author | Prakash Thapa Seong Hoon Jeong |
| author_facet | Prakash Thapa Seong Hoon Jeong |
| author_sort | Prakash Thapa |
| collection | DOAJ |
| description | To develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethylene oxide WSR 303 (PEO), sodium bicarbonate, and tablet compression force were used as independent variables. Various times required to release the drug, tablet tensile strength, floating lag time, tablet ejection force, and tablet porosity, were selected as the responses. Polymer screening showed that PEO had the highest gel strength among the various tested polymers. Sodium bicarbonate had the most significant effect on the release rate and floating lag time by retarding the rate from the hydrophilic matrices, whilst tablet compression force and PEO exerted the greatest influence on tablet properties (p < 0.0001). The design space was built in accordance with the drug release profiles, tensile strength, and floating lag time, following failure probability analysis using Monte Carlo simulations. The kinetic modeling revealed that the release mechanism was best described by the Korsmeyer-Peppas model. Overall, the current study provided a perspective on the systematic approach of gastro-retentive EFT, loaded with highly water-soluble drugs by applying quality by design concepts. |
| first_indexed | 2024-04-11T11:53:28Z |
| format | Article |
| id | doaj.art-ca1a6b084ccc4ee4ad2460d0d8c4fddd |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-11T11:53:28Z |
| publishDate | 2018-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-ca1a6b084ccc4ee4ad2460d0d8c4fddd2022-12-22T04:25:14ZengMDPI AGPharmaceutics1999-49232018-09-0110316110.3390/pharmaceutics10030161pharmaceutics10030161Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design ApproachPrakash Thapa0Seong Hoon Jeong1College of Pharmacy, Dongguk University-Seoul, Gyeonggi 10326, KoreaCollege of Pharmacy, Dongguk University-Seoul, Gyeonggi 10326, KoreaTo develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethylene oxide WSR 303 (PEO), sodium bicarbonate, and tablet compression force were used as independent variables. Various times required to release the drug, tablet tensile strength, floating lag time, tablet ejection force, and tablet porosity, were selected as the responses. Polymer screening showed that PEO had the highest gel strength among the various tested polymers. Sodium bicarbonate had the most significant effect on the release rate and floating lag time by retarding the rate from the hydrophilic matrices, whilst tablet compression force and PEO exerted the greatest influence on tablet properties (p < 0.0001). The design space was built in accordance with the drug release profiles, tensile strength, and floating lag time, following failure probability analysis using Monte Carlo simulations. The kinetic modeling revealed that the release mechanism was best described by the Korsmeyer-Peppas model. Overall, the current study provided a perspective on the systematic approach of gastro-retentive EFT, loaded with highly water-soluble drugs by applying quality by design concepts.http://www.mdpi.com/1999-4923/10/3/161polyethylene oxidesodium bicarbonategel strengthfloating lag timedrug release kineticsexperimental design |
| spellingShingle | Prakash Thapa Seong Hoon Jeong Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach Pharmaceutics polyethylene oxide sodium bicarbonate gel strength floating lag time drug release kinetics experimental design |
| title | Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach |
| title_full | Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach |
| title_fullStr | Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach |
| title_full_unstemmed | Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach |
| title_short | Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach |
| title_sort | effects of formulation and process variables on gastroretentive floating tablets with a high dose soluble drug and experimental design approach |
| topic | polyethylene oxide sodium bicarbonate gel strength floating lag time drug release kinetics experimental design |
| url | http://www.mdpi.com/1999-4923/10/3/161 |
| work_keys_str_mv | AT prakashthapa effectsofformulationandprocessvariablesongastroretentivefloatingtabletswithahighdosesolubledrugandexperimentaldesignapproach AT seonghoonjeong effectsofformulationandprocessvariablesongastroretentivefloatingtabletswithahighdosesolubledrugandexperimentaldesignapproach |