析因设计在舒马曲坦直肠内原位凝胶制剂和评价中的应用。

IF 1.4 Q3 Pharmacology, Toxicology and Pharmaceutics
Hanan J Kassab, Hussein K Alkufi, Lina S Hussein
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引用次数: 1

摘要

该研究的目标是制备一种由舒马曲坦(SMT)组成的原位直肠内粘膜粘附凝胶,该凝胶结合了粘膜粘附聚合物(木葡聚糖)和热敏聚合物(泊洛沙姆407和泊洛沙姆188),以延长治疗偏头痛的直肠停留时间。通过将泊洛沙姆407(18%、19%或20%)与泊洛沙姆188(5%)、不同剂量(0.1、0.2和0.3)的粘膜粘合剂聚合物以及SMT(25mg/ml)混合,制备了九种SMT粘膜粘合剂直肠原位凝胶(RIG)配方。制备的栓剂经历了粘着力、凝胶化温度和凝胶化时间。当SMT和粘膜粘合剂聚合物加入泊洛沙姆混合物中时,凝胶化温度下降;然而,泊洛沙姆188具有相反的效果。这些聚合物支持制备的液体粘附在粘膜上并形成强凝胶的能力。泊洛沙姆溶液的转变凝胶化温度由于泊洛沙姆188的加入而升高。研究结果表明,由泊洛沙姆407(19%)、泊洛沙姆188(5%)和木葡聚糖(0.2%)组成的配方RIG5在8小时内具有36.33°C的理想转变温度、44.66°C的凝胶强度、6409°C的粘膜粘附力和93.98%的体外药物释放。有鉴于此,可以说SMT是在没有与其添加剂发生任何化学反应的情况下作为RIG成功制造的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Use of factorial design in formulation and evaluation of intrarectal <i>in situ</i> gel of sumatriptan.

Use of factorial design in formulation and evaluation of intrarectal <i>in situ</i> gel of sumatriptan.

Use of factorial design in formulation and evaluation of intrarectal <i>in situ</i> gel of sumatriptan.

Use of factorial design in formulation and evaluation of intrarectal in situ gel of sumatriptan.

The study's goal was to create an in situ intrarectal mucoadhesive gel of sumatriptan (SMT) combining mucoadhesive polymer (xyloglucan) and thermosensitive polymers (poloxamer 407 and poloxamer 188) to prolong rectal residence time for treatment of migraines. Nine SMT mucoadhesive rectal in situ gel (RIG) formulas were created by mixing poloxamer 407 (18%, 19%, or 20%) with poloxamer 188 (5%), a mucoadhesive polymer at various doses (0.1, 0.2, and 0.3) as well as SMT (25 mg/ml). The prepared suppositories underwent for mucoadhesive force, gelation temperature, and gelation time. When SMT and mucoadhesive polymer were added to the poloxamer mixture, the gelation temperature dropped; however, poloxamer 188 had the opposite effect. These polymers supported the prepared liquids' ability to adhere to mucous membranes and form a strong gel. The transition gelation temperature of the poloxamer solution rose as a result of the addition of poloxamer 188. The findings showed that the formula RIG5 which is composed of poloxamer 407 (19%), poloxamer 188 (5%), and xyloglucan (0.2%) had an ideal transition temperature of 36.33°C, gel strength of 44.66°C, mucoadhesive force of 6409°C, and in vitro drug release of 93.98% over an 8-hour period. In light of this, it can be said that SMT was successfully manufactured as RIG without causing any chemical reaction with its additives.

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来源期刊
CiteScore
2.00
自引率
7.10%
发文量
44
审稿时长
20 weeks
期刊介绍: Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is an Official Publication of Society of Pharmaceutical Education & Research™. It is an international journal published Quarterly. Journal of Advanced Pharmaceutical Technology & Research (JAPTR) is available in online and print version. It is a peer reviewed journal aiming to communicate high quality original research work, reviews, short communications, case report, Ethics Forum, Education Forum and Letter to editor that contribute significantly to further the scientific knowledge related to the field of Pharmacy i.e. Pharmaceutics, Pharmacology, Pharmacognosy, Pharmaceutical Chemistry. Articles with timely interest and newer research concepts will be given more preference.
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