Muzammil Husain , Vinit V. Agnihotri , Sameer N. Goyal , Yogeeta O. Agrawal
{"title":"替米沙坦治疗高血压用水胶体口腔溶膜的研制、优化及表征","authors":"Muzammil Husain , Vinit V. Agnihotri , Sameer N. Goyal , Yogeeta O. Agrawal","doi":"10.1016/j.fhfh.2022.100064","DOIUrl":null,"url":null,"abstract":"<div><p>Telmisartan, a BCS class II antihypertensive, has low oral bioavailability due to first-pass metabolism and a poor solubility profile, causing dissolving problems. Telmisartan is a suitable choice for the Rapid Release Drug Delivery System since it needs rapid absorption for a quick beginning of the activity. The goal of this research was to create and describe a solid dispersion employing hydrocolloid incorporated mouth dissolving film of Telmisartan. To make a Mouth Dissolving Film, first, prepare a solid dispersion using the Kneading Method, then use the Solvent Casting Metrpose of screening Carrier for the further formulation, solid dispersion is assessed for solubility, drug content, and drug release rate. The in-vitro drug release investigation revealed that solid dispersion had better solubility and rapid drug release than pure drug. Physical appearance, surface PH, thickness uniformity, disintegration duration, drug content uniformity, folding durability, and in-vitro drug release were among the physicochemical and mechanical parameters assessed on the produced films. A 3<sup>2</sup>-level factorial design was used to improve the approach. The effects of film appearance, disintegrating time, and in-vitro drug release behavior on the composition of Film-forming polymer(hydrocolloids) and Super disintegration were investigated. The in-vitro drug release and disintegration time of the optimized batch were found to be 91.83 percent and 29 sec, respectively. These positive conclusions demonstrated that mouth dissolving film of Telmisartan can be formulated using HPMC E15 as a film-forming polymer and Sodium Starch Glycolate as a super disintegrant for improving bioavailability and therapeutic outcome.</p></div>","PeriodicalId":12385,"journal":{"name":"Food Hydrocolloids for Health","volume":null,"pages":null},"PeriodicalIF":4.6000,"publicationDate":"2022-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2667025922000115/pdfft?md5=2e529dbd69625ceef89b1d4dd7d1b275&pid=1-s2.0-S2667025922000115-main.pdf","citationCount":"3","resultStr":"{\"title\":\"Development, optimization and characterization of hydrocolloid based mouth dissolving film of Telmisartan for the treatment of hypertension\",\"authors\":\"Muzammil Husain , Vinit V. Agnihotri , Sameer N. Goyal , Yogeeta O. Agrawal\",\"doi\":\"10.1016/j.fhfh.2022.100064\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Telmisartan, a BCS class II antihypertensive, has low oral bioavailability due to first-pass metabolism and a poor solubility profile, causing dissolving problems. Telmisartan is a suitable choice for the Rapid Release Drug Delivery System since it needs rapid absorption for a quick beginning of the activity. The goal of this research was to create and describe a solid dispersion employing hydrocolloid incorporated mouth dissolving film of Telmisartan. To make a Mouth Dissolving Film, first, prepare a solid dispersion using the Kneading Method, then use the Solvent Casting Metrpose of screening Carrier for the further formulation, solid dispersion is assessed for solubility, drug content, and drug release rate. The in-vitro drug release investigation revealed that solid dispersion had better solubility and rapid drug release than pure drug. Physical appearance, surface PH, thickness uniformity, disintegration duration, drug content uniformity, folding durability, and in-vitro drug release were among the physicochemical and mechanical parameters assessed on the produced films. A 3<sup>2</sup>-level factorial design was used to improve the approach. The effects of film appearance, disintegrating time, and in-vitro drug release behavior on the composition of Film-forming polymer(hydrocolloids) and Super disintegration were investigated. The in-vitro drug release and disintegration time of the optimized batch were found to be 91.83 percent and 29 sec, respectively. These positive conclusions demonstrated that mouth dissolving film of Telmisartan can be formulated using HPMC E15 as a film-forming polymer and Sodium Starch Glycolate as a super disintegrant for improving bioavailability and therapeutic outcome.</p></div>\",\"PeriodicalId\":12385,\"journal\":{\"name\":\"Food Hydrocolloids for Health\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":4.6000,\"publicationDate\":\"2022-12-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.sciencedirect.com/science/article/pii/S2667025922000115/pdfft?md5=2e529dbd69625ceef89b1d4dd7d1b275&pid=1-s2.0-S2667025922000115-main.pdf\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Food Hydrocolloids for Health\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2667025922000115\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, APPLIED\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Food Hydrocolloids for Health","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S2667025922000115","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
Development, optimization and characterization of hydrocolloid based mouth dissolving film of Telmisartan for the treatment of hypertension
Telmisartan, a BCS class II antihypertensive, has low oral bioavailability due to first-pass metabolism and a poor solubility profile, causing dissolving problems. Telmisartan is a suitable choice for the Rapid Release Drug Delivery System since it needs rapid absorption for a quick beginning of the activity. The goal of this research was to create and describe a solid dispersion employing hydrocolloid incorporated mouth dissolving film of Telmisartan. To make a Mouth Dissolving Film, first, prepare a solid dispersion using the Kneading Method, then use the Solvent Casting Metrpose of screening Carrier for the further formulation, solid dispersion is assessed for solubility, drug content, and drug release rate. The in-vitro drug release investigation revealed that solid dispersion had better solubility and rapid drug release than pure drug. Physical appearance, surface PH, thickness uniformity, disintegration duration, drug content uniformity, folding durability, and in-vitro drug release were among the physicochemical and mechanical parameters assessed on the produced films. A 32-level factorial design was used to improve the approach. The effects of film appearance, disintegrating time, and in-vitro drug release behavior on the composition of Film-forming polymer(hydrocolloids) and Super disintegration were investigated. The in-vitro drug release and disintegration time of the optimized batch were found to be 91.83 percent and 29 sec, respectively. These positive conclusions demonstrated that mouth dissolving film of Telmisartan can be formulated using HPMC E15 as a film-forming polymer and Sodium Starch Glycolate as a super disintegrant for improving bioavailability and therapeutic outcome.