{"title":"盐酸哌醋甲酯双峰时调给药的研制与表征。","authors":"Rajasekhar Reddy Poonuru, Ashwini Penala","doi":"10.1016/j.fhfh.2023.100127","DOIUrl":null,"url":null,"abstract":"<div><p>The study's goal was to develop chrono modulated pulsatile tablets of methylphenidate hydrochloride with an extended-release pattern in the morning and an immediate burst release in the afternoon for exaggerated symptoms of attention deficit hyperactivity disorder match the circadian rhythm of disease, where high levels of l-3, 4-dihydroxyphenylalanine (DOPA) are observed in the afternoon, necessitating higher drug concentrations. The core tablets were made with Kollidon CL-SF as a super disintegrant at 4% and 8% concentrations, with microcrystalline cellulose PH 102 (Pharma grade) and Ludipress as diluents.</p><p>The core tablets were then compress coated with a slow-release component blend containing different grades of hydroxypropyl methylcellulose (HPMC) at various concentrations of HPMC E50, HPMC E15M, or HPMC E4M, as well as 4% Ethocel. Among all formulations, the F10 formulation containing HPMC E50 at 70% showed the best drug release, with 60% of the dose released slowly over 4 h, followed by an immediate burst of the remaining 40% at the 5th hour. The effect of different diluents on <em>in vitro</em> drug release kinetics and <em>in vitro</em> dissolution studies were performed for all formulations, and A1 formulation containing Cellactose-80 as a diluent showed the best results, with results matching the circadian variations in the disease condition.</p></div>","PeriodicalId":12385,"journal":{"name":"Food Hydrocolloids for Health","volume":"3 ","pages":"Article 100127"},"PeriodicalIF":4.6000,"publicationDate":"2023-02-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development and characterization of bimodal chrono modulated drug delivery of methylphenidate hydrochloride\",\"authors\":\"Rajasekhar Reddy Poonuru, Ashwini Penala\",\"doi\":\"10.1016/j.fhfh.2023.100127\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The study's goal was to develop chrono modulated pulsatile tablets of methylphenidate hydrochloride with an extended-release pattern in the morning and an immediate burst release in the afternoon for exaggerated symptoms of attention deficit hyperactivity disorder match the circadian rhythm of disease, where high levels of l-3, 4-dihydroxyphenylalanine (DOPA) are observed in the afternoon, necessitating higher drug concentrations. The core tablets were made with Kollidon CL-SF as a super disintegrant at 4% and 8% concentrations, with microcrystalline cellulose PH 102 (Pharma grade) and Ludipress as diluents.</p><p>The core tablets were then compress coated with a slow-release component blend containing different grades of hydroxypropyl methylcellulose (HPMC) at various concentrations of HPMC E50, HPMC E15M, or HPMC E4M, as well as 4% Ethocel. Among all formulations, the F10 formulation containing HPMC E50 at 70% showed the best drug release, with 60% of the dose released slowly over 4 h, followed by an immediate burst of the remaining 40% at the 5th hour. The effect of different diluents on <em>in vitro</em> drug release kinetics and <em>in vitro</em> dissolution studies were performed for all formulations, and A1 formulation containing Cellactose-80 as a diluent showed the best results, with results matching the circadian variations in the disease condition.</p></div>\",\"PeriodicalId\":12385,\"journal\":{\"name\":\"Food Hydrocolloids for Health\",\"volume\":\"3 \",\"pages\":\"Article 100127\"},\"PeriodicalIF\":4.6000,\"publicationDate\":\"2023-02-22\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Food Hydrocolloids for Health\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S2667025923000122\",\"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/S2667025923000122","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
Development and characterization of bimodal chrono modulated drug delivery of methylphenidate hydrochloride
The study's goal was to develop chrono modulated pulsatile tablets of methylphenidate hydrochloride with an extended-release pattern in the morning and an immediate burst release in the afternoon for exaggerated symptoms of attention deficit hyperactivity disorder match the circadian rhythm of disease, where high levels of l-3, 4-dihydroxyphenylalanine (DOPA) are observed in the afternoon, necessitating higher drug concentrations. The core tablets were made with Kollidon CL-SF as a super disintegrant at 4% and 8% concentrations, with microcrystalline cellulose PH 102 (Pharma grade) and Ludipress as diluents.
The core tablets were then compress coated with a slow-release component blend containing different grades of hydroxypropyl methylcellulose (HPMC) at various concentrations of HPMC E50, HPMC E15M, or HPMC E4M, as well as 4% Ethocel. Among all formulations, the F10 formulation containing HPMC E50 at 70% showed the best drug release, with 60% of the dose released slowly over 4 h, followed by an immediate burst of the remaining 40% at the 5th hour. The effect of different diluents on in vitro drug release kinetics and in vitro dissolution studies were performed for all formulations, and A1 formulation containing Cellactose-80 as a diluent showed the best results, with results matching the circadian variations in the disease condition.