Hongfei Liu, Ying Bao, Xiangping Lai, Yingshu Feng, Dan Yang, Rui Sun, Caleb Kesse Firempong, Haibing He
{"title":"盐酸马南亭口服液缓释给药系统的构建与体内外评价","authors":"Hongfei Liu, Ying Bao, Xiangping Lai, Yingshu Feng, Dan Yang, Rui Sun, Caleb Kesse Firempong, Haibing He","doi":"10.1080/03639045.2024.2329746","DOIUrl":null,"url":null,"abstract":"<p><strong>Objective: </strong>The purpose of the present study was to formulate a menantine hydrochloride (MH) sustained-release suspension.</p><p><strong>Methods: </strong>Menantine hydrochloride drug resin complex (MH-DRC) was prepared with strong acid cation exchange resin as carrier using water bath method. The MH-DRC was characterized using scanning electron microscopy, X-ray diffraction and infrared spectroscopy. The MH-coated microcapsule (MH-CM) with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. The rats were given both the MH sustained-release suspension and the commercial MH sustained-release capsule by intragastric administration. The plasma concentration-time curves and related pharmacokinetic parameters were also investigated using a non-atrioventricular model.</p><p><strong>Results: </strong>MH and ion-exchange resin were ionically bonded. AmberliteIRP®69 had a higher affinity for MH at the initial concentration of 5 mg·mL<sup>-1</sup> and a reaction temperature of 25.0 ± 0.5 °C. <i>In vitro</i> drug release profile showed that both the drug resin complex and the coated microcapsules had a certain level of sustained-release effect. The <i>t<sub>1/2</sub></i> of MH sustained-release suspension was extended from 68.44 h to 72.79 h with the peak blood concentration being decreased to 3.56 μg·mL<sup>-1</sup> and the <i>T<sub>max</sub></i> extended to 12 h compared with the commercial MH sustained-release capsule. The concentration-time curve of the self-made MH sustained-release suspension was flattened and the average relative bioavailability (<i>F<sub>r</sub></i>) was 116.65% compared with the commercial MH sustained-release capsules.</p><p><strong>Conclusions: </strong>The findings showed that the MH sustained-release suspension was successfully formulated with acceptable pharmacokinetic indices for effective treatment of Alzheimer's disease.</p>","PeriodicalId":2,"journal":{"name":"ACS Applied Bio Materials","volume":null,"pages":null},"PeriodicalIF":4.6000,"publicationDate":"2024-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Construction and <i>in vitro</i>/<i>in vivo</i> evaluation of menantine hydrochloride oral liquid sustained-release drug delivery system.\",\"authors\":\"Hongfei Liu, Ying Bao, Xiangping Lai, Yingshu Feng, Dan Yang, Rui Sun, Caleb Kesse Firempong, Haibing He\",\"doi\":\"10.1080/03639045.2024.2329746\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Objective: </strong>The purpose of the present study was to formulate a menantine hydrochloride (MH) sustained-release suspension.</p><p><strong>Methods: </strong>Menantine hydrochloride drug resin complex (MH-DRC) was prepared with strong acid cation exchange resin as carrier using water bath method. The MH-DRC was characterized using scanning electron microscopy, X-ray diffraction and infrared spectroscopy. The MH-coated microcapsule (MH-CM) with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. The rats were given both the MH sustained-release suspension and the commercial MH sustained-release capsule by intragastric administration. The plasma concentration-time curves and related pharmacokinetic parameters were also investigated using a non-atrioventricular model.</p><p><strong>Results: </strong>MH and ion-exchange resin were ionically bonded. AmberliteIRP®69 had a higher affinity for MH at the initial concentration of 5 mg·mL<sup>-1</sup> and a reaction temperature of 25.0 ± 0.5 °C. <i>In vitro</i> drug release profile showed that both the drug resin complex and the coated microcapsules had a certain level of sustained-release effect. The <i>t<sub>1/2</sub></i> of MH sustained-release suspension was extended from 68.44 h to 72.79 h with the peak blood concentration being decreased to 3.56 μg·mL<sup>-1</sup> and the <i>T<sub>max</sub></i> extended to 12 h compared with the commercial MH sustained-release capsule. The concentration-time curve of the self-made MH sustained-release suspension was flattened and the average relative bioavailability (<i>F<sub>r</sub></i>) was 116.65% compared with the commercial MH sustained-release capsules.</p><p><strong>Conclusions: </strong>The findings showed that the MH sustained-release suspension was successfully formulated with acceptable pharmacokinetic indices for effective treatment of Alzheimer's disease.</p>\",\"PeriodicalId\":2,\"journal\":{\"name\":\"ACS Applied Bio Materials\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":4.6000,\"publicationDate\":\"2024-04-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Applied Bio Materials\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/03639045.2024.2329746\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/3/23 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"MATERIALS SCIENCE, BIOMATERIALS\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Applied Bio Materials","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/03639045.2024.2329746","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/3/23 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"MATERIALS SCIENCE, BIOMATERIALS","Score":null,"Total":0}
Construction and in vitro/in vivo evaluation of menantine hydrochloride oral liquid sustained-release drug delivery system.
Objective: The purpose of the present study was to formulate a menantine hydrochloride (MH) sustained-release suspension.
Methods: Menantine hydrochloride drug resin complex (MH-DRC) was prepared with strong acid cation exchange resin as carrier using water bath method. The MH-DRC was characterized using scanning electron microscopy, X-ray diffraction and infrared spectroscopy. The MH-coated microcapsule (MH-CM) with optimized formulation was further dispersed in a suitable medium to obtain a sustained-release suspension. The rats were given both the MH sustained-release suspension and the commercial MH sustained-release capsule by intragastric administration. The plasma concentration-time curves and related pharmacokinetic parameters were also investigated using a non-atrioventricular model.
Results: MH and ion-exchange resin were ionically bonded. AmberliteIRP®69 had a higher affinity for MH at the initial concentration of 5 mg·mL-1 and a reaction temperature of 25.0 ± 0.5 °C. In vitro drug release profile showed that both the drug resin complex and the coated microcapsules had a certain level of sustained-release effect. The t1/2 of MH sustained-release suspension was extended from 68.44 h to 72.79 h with the peak blood concentration being decreased to 3.56 μg·mL-1 and the Tmax extended to 12 h compared with the commercial MH sustained-release capsule. The concentration-time curve of the self-made MH sustained-release suspension was flattened and the average relative bioavailability (Fr) was 116.65% compared with the commercial MH sustained-release capsules.
Conclusions: The findings showed that the MH sustained-release suspension was successfully formulated with acceptable pharmacokinetic indices for effective treatment of Alzheimer's disease.
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