Pluronic F-68 Montmorillonite As A Drug Delivery Vehicle For Extended Release Of Venlafaxine Hydrochloride.

IF 1.7 Q3 PHARMACOLOGY & PHARMACY Drug Research Pub Date : 2023-07-01 DOI:10.1055/a-2024-9964
Shilpa Jain, Monika Datta
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Abstract

Short half-life and low bioavailability of Venlafaxine hydrochloride (VF), an antidepressant drug, necessitates the frequent administration of VF tablets in a day in order to maintain adequate drug concentration in blood plasma. This generates the need for the development of formulations which could prolong the release of VF and reduce the multiple dosages. The present work explores the combination of Montmorillonite (Mt) with Pluronic F-68 (PF-68) (OrganoMT) for oral delivery of VF. The effect of various parameters including pH of aqueous drug solution, contact time and initial drug concentration on drug loading capacity of OrganoMT has been studied. The synthesized OrganoMT-VF complexes were characterized by various suitable techniques. XRD studies indicated that the VF molecules were intercalated within the OrganoMT layers. In vitro release behavior of VF from OrganoMT-VF complexes shows an extended-release pattern for a period of 30 h and reaches upto 70% and 60% compared to pure VF having complete release time of 5.5 h and 3.5 h in simulated gastric and intestinal fluid respectively. Various kinetic models were employed to elucidate the drug release mechanism where the best fitting was obtained with Korsmeyer Peppas model. The results suggest the possibility of designing an oral extended controlled release formulation for VF to minimize its administration frequency thereby increasing the effectiveness of drug. This improves patient compliance by reducing the dose from 4 times in 24 h to once in 24 h.

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Pluronic F-68蒙脱土缓释盐酸文拉法辛的药物载体
盐酸文拉法辛(Venlafaxine hydrochloride, VF)是一种抗抑郁药物,其半衰期短,生物利用度低,需要在一天内频繁服用VF片,以维持血浆中足够的药物浓度。这就产生了开发能够延长VF释放和减少多重剂量的制剂的需要。本研究探讨了蒙脱土(Mt)与Pluronic F-68 (PF-68) (OrganoMT)的组合用于口服给药VF。研究了药物水溶液pH、接触时间、初始药物浓度等参数对OrganoMT载药量的影响。用各种合适的技术对合成的OrganoMT-VF配合物进行了表征。XRD研究表明,VF分子嵌入到OrganoMT层中。与纯VF相比,OrganoMT-VF复合物的VF在模拟胃液和肠液中的完全释放时间分别为5.5 h和3.5 h,其体外释放行为显示出30 h的缓释模式,达到70%和60%。采用多种动力学模型来阐明药物释放机制,其中以Korsmeyer Peppas模型拟合效果最佳。研究结果表明,可以设计一种口服VF缓释制剂,以减少给药频率,从而提高药物的有效性。通过将剂量从24小时4次减少到24小时1次,提高了患者的依从性。
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来源期刊
Drug Research
Drug Research PHARMACOLOGY & PHARMACY-
CiteScore
3.50
自引率
0.00%
发文量
67
期刊介绍: Drug Research (formerly Arzneimittelforschung) is an international peer-reviewed journal with expedited processing times presenting the very latest research results related to novel and established drug molecules and the evaluation of new drug development. A key focus of the publication is translational medicine and the application of biological discoveries in the development of drugs for use in the clinical environment. Articles and experimental data from across the field of drug research address not only the issue of drug discovery, but also the mathematical and statistical methods for evaluating results from industrial investigations and clinical trials. Publishing twelve times a year, Drug Research includes original research articles as well as reviews, commentaries and short communications in the following areas: analytics applied to clinical trials chemistry and biochemistry clinical and experimental pharmacology drug interactions efficacy testing pharmacodynamics pharmacokinetics teratology toxicology.
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