Pharmaceutical Development and Technology最新文献

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Bile salt-enriched vs. non-enriched nanoparticles: comparison of their physicochemical characteristics and release pattern. 富含胆盐与不富含胆盐的纳米颗粒:它们的理化特性和释放模式的比较。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-09 DOI: 10.1080/10837450.2024.2320279
Marjan Emzhik, Amirsajad Qaribnejad, Azadeh Haeri, Simin Dadashzadeh
{"title":"Bile salt-enriched vs. non-enriched nanoparticles: comparison of their physicochemical characteristics and release pattern.","authors":"Marjan Emzhik, Amirsajad Qaribnejad, Azadeh Haeri, Simin Dadashzadeh","doi":"10.1080/10837450.2024.2320279","DOIUrl":"10.1080/10837450.2024.2320279","url":null,"abstract":"<p><p>Bile salts were first used in the preparation of nanoparticles due to their stabilizing effects. As time went by, they attracted much attention and were increasingly employed in fabricating nanoparticles. It is well accepted that the physicochemical properties of nanoparticles are influential factors in their permeation, distribution, elimination and degree of effectiveness as well as toxicity. The review of articles shows that the use of bile salts in the structure of nanocarriers may cause significant changes in their physicochemical properties. Hence, having information about the effect of bile salts on the properties of nanoparticles could be valuable in the design of optimal carriers. Herein, we review studies in which bile salts were used in preparing liposomes, niosomes and other nanocarriers. Furthermore, the effects of bile salts on entrapment efficiency, particle size, polydispersity index, zeta potential, release profile and stability of nanoparticles are pointed out. Finally, we debate how to take advantage of bile salts potential for preparing desirable nanocarriers.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"187-211"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139900306","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Engineering nanosystems for transdermal delivery of antihypertensive drugs. 用于透皮给药抗高血压药物的纳米系统工程。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-06 DOI: 10.1080/10837450.2024.2324981
Mingliang Fan, Wengang Liu, Liangfeng Zhao, Lirong Nie, Yu Wang
{"title":"Engineering nanosystems for transdermal delivery of antihypertensive drugs.","authors":"Mingliang Fan, Wengang Liu, Liangfeng Zhao, Lirong Nie, Yu Wang","doi":"10.1080/10837450.2024.2324981","DOIUrl":"10.1080/10837450.2024.2324981","url":null,"abstract":"<p><p>To control hypertension, long-term continuous antihypertensive therapeutics are required and five classes of antihypertensive drugs are frequently involved, including diuretics, β-blockers, calcium channel blockers, angiotensin II receptor blockers, and angiotensin-converting enzyme inhibitors. Although with demonstrated clinical utility, there is still room for the improvement of many antihypertensive drugs in oral tablet or capsule dosage form, in terms of reducing systemic side effects and first-pass hepatic drug uptake. Meanwhile, nanocarrier-mediated transdermal drug delivery systems have emerged as a powerful tool for various disease treatments. With benefits such as promoting patient compliance for long-time administration, enhancing skin permeability, and reducing systemic side effects, these systems are reasonably investigated and developed for the transdermal delivery of multiple antihypertensive drugs. This review aims to summarize the literature relating to nanosystem-based transdermal antihypertensive drug delivery and update recent advances in this field, as well as briefly discuss the challenges and prospects of engineering transdermal delivery nanosystems for hypertension treatment.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"265-279"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139983504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Atorvastatin-loaded cubosome: a repurposed targeted delivery systems for enhanced targeting against breast cancer. 阿托伐他汀载体立方体:增强乳腺癌靶向性的再利用靶向递送系统。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-09 DOI: 10.1080/10837450.2024.2323620
Eman M El-Marakby, Hend Fayez, M A Motaleb, Mai Mansour
{"title":"Atorvastatin-loaded cubosome: a repurposed targeted delivery systems for enhanced targeting against breast cancer.","authors":"Eman M El-Marakby, Hend Fayez, M A Motaleb, Mai Mansour","doi":"10.1080/10837450.2024.2323620","DOIUrl":"10.1080/10837450.2024.2323620","url":null,"abstract":"<p><p>Cancer ranks as one of the most challenging illnesses to deal with because progressive phenotypic and genotypic alterations in cancer cells result in resistance and recurrence. Thus, the creation of novel medications or alternative therapy approaches is mandatory. Repurposing of old drugs is an attractive approach over the traditional drug discovery process in terms of shorter drug development duration, low-cost, highly efficient and minimum risk of failure. In this study Atorvastatin, a statin drug used to treat abnormal cholesterol levels and prevent cardiovascular disease in people at high risk, was introduced and encapsulated in cubic liquid crystals as anticancer candidate aiming at sustaining its release and achieving better cellular uptake in cancer cells. The cubic liquid crystals were successfully prepared and optimized with an entrapment effieciency of 73.57% ±1.35 and particle size around 200 nm. The selected formulae were effectively doped with radioactive iodine <sup>131</sup>I to enable the noninvasive visualization and trafficking of the new formulae. The <i>in vivo</i> evaluation in solid tumor bearing mice was conducted for comparing<sup>131</sup>I-Atorvastatin solution,<sup>131</sup>I-Atorvastatin loaded cubosome and <sup>131</sup>I-Atorvastatin chitosan coated cubosome. The <i>in vivo</i> biodistribution study revealed that tumor radioactivity uptake of <sup>131</sup>I-Atorvastatin cubosome and chitosan coated cubosome exhibited high accumulation in tumor tissues (target organ) scoring ID%/g of 5.67 ± 0.2 and 5.03 ± 0.1, respectively 1h post injection compared to drug solution which recorded 3.09 ± 0.05% 1h post injection. Concerning the targeting efficiency, the target/non target ratio for <sup>131</sup>I-Atorvastatin chitosan coated cubosome was higher than that of <sup>131</sup>I-Atorvastatin solution and <sup>131</sup>I ATV-loaded cubosome at all time intervals and recorded T/NT ratio of 2.908 2h post injection.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"236-247"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140050117","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Paeoniflorin loaded liposomes modified with glycyrrhetinic acid for liver-targeting: preparation, characterization, and pharmacokinetic study. 用甘草酸修饰的芍药脂质体用于肝脏靶向治疗:制备、表征和药代动力学研究
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-02-29 DOI: 10.1080/10837450.2024.2319738
Menghuan Yang, Gang Jiang, Yumeng Li, Weidong Chen, Shantang Zhang, Rulin Wang
{"title":"Paeoniflorin loaded liposomes modified with glycyrrhetinic acid for liver-targeting: preparation, characterization, and pharmacokinetic study.","authors":"Menghuan Yang, Gang Jiang, Yumeng Li, Weidong Chen, Shantang Zhang, Rulin Wang","doi":"10.1080/10837450.2024.2319738","DOIUrl":"10.1080/10837450.2024.2319738","url":null,"abstract":"<p><strong>Objective: </strong>To enhance the retention times and therapeutic efficacy of paeoniflorin (PF), a liver-targeted drug delivery system has been developed using glycyrrhetinic acid (GA) as a ligand.</p><p><strong>Significance: </strong>The development and optimization of GA-modified PF liposomes (GPLs) have shown promising potential for targeted delivery to the liver, opening up new possibilities for liver disease treatment.</p><p><strong>Methods: </strong>This study aimed to identify the best prescriptions using single-factor experiments and response surface methodology. The formulation morphology was determined using transmission electron microscopy. Tissue distribution was observed through <i>in vivo</i> imaging, and pharmacokinetic studies were conducted.</p><p><strong>Results: </strong>The results indicated that GPLs, prepared using the thin film dispersion method and response surface optimization, exhibited well-dispersed and uniformly sized particles. The <i>in vitro</i> release rate of GPLs was slower compared to PF monomers, suggesting a sustained release effect. The liver-targeting ability of GA resulted in stronger fluorescence signals in the liver for targeted liposomes compared to non-targeted liposomes. Furthermore, pharmacokinetic studies demonstrated that GPLs significantly prolonged the residence time of PF in the bloodstream, thereby contributing to prolonged efficacy.</p><p><strong>Conclusion: </strong>These findings suggest that GPLs are more effective than PF monomers in terms of controlling drug release and delivering drugs to specific targets, highlighting the potential of PF as a liver-protective drug.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"176-186"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139906317","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Correction. 更正。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-22 DOI: 10.1080/10837450.2024.2329035
{"title":"Correction.","authors":"","doi":"10.1080/10837450.2024.2329035","DOIUrl":"10.1080/10837450.2024.2329035","url":null,"abstract":"","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"i"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140185169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quercetin nanocrystals prepared using a microfluidic chip with improved in vitro dissolution. 利用微流控芯片制备槲皮素纳米晶体,提高体外溶解度。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-02-22 DOI: 10.1080/10837450.2024.2315444
Guangyan Zheng, Wenli Wu, Zemei Liu, Yuanju Lv, Yongming Luo, Xin Che, Lihong Wang
{"title":"Quercetin nanocrystals prepared using a microfluidic chip with improved in vitro dissolution.","authors":"Guangyan Zheng, Wenli Wu, Zemei Liu, Yuanju Lv, Yongming Luo, Xin Che, Lihong Wang","doi":"10.1080/10837450.2024.2315444","DOIUrl":"10.1080/10837450.2024.2315444","url":null,"abstract":"<p><strong>Objective: </strong>In order to improve the dissolution property of quercetin (QCT), the quercetin nanocrystals (QNCs) were prepared in this study.</p><p><strong>Methods: </strong>QNCs were prepared by a 100 μm diameter Y-shape microfluidic channel. Some impact factors affecting the generation of QNCs such as concentration and flow rate were investigated. Furthermore, the fluid mixing in the microfluidic channel was simulated by fluid software.</p><p><strong>Results: </strong>XRPD and DSC analyses indicated that the prepared QNCs were amorphous. Stable QNCs with a particle size of 77.9 ± 3.63 nm and polydispersity index of 0.26 ± 0.02 were obtained. TEM showed that the as-prepared QNCs had a uniform spherical shape with an average particle size of about 100-300 nm. In the dissolution medium without cosolvent Tween -80, the dissolution of QCT was poor, its final accumulated dissolution was only 3.95%, while that of QNCs was 66%.</p><p><strong>Conclusion: </strong>When QCT was changed to QNCs by microfluidic technology, its dissolution property could be obviously improved. Therefore, microfluidic technology as a new method to prepare nanocrystals has a good applying prospect in improving dissolution property for poorly water-soluble drugs.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"143-152"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139730237","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation, in vitro anti-tumour activity and in vivo pharmacokinetics of RGD-decorated liposomes loaded with shikonin. 装载了 shikonin 的 RGD 装饰脂质体的制备、体外抗肿瘤活性和体内药代动力学。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-02-19 DOI: 10.1080/10837450.2024.2315457
Jiping Li, Hao Zhang, Xinliang Mao, Huilin Deng, Li Fan, Liling Yue, Chengchong Li, Siwen Pan, Xianchun Wen
{"title":"Preparation, <i>in vitro</i> anti-tumour activity and <i>in vivo</i> pharmacokinetics of RGD-decorated liposomes loaded with shikonin.","authors":"Jiping Li, Hao Zhang, Xinliang Mao, Huilin Deng, Li Fan, Liling Yue, Chengchong Li, Siwen Pan, Xianchun Wen","doi":"10.1080/10837450.2024.2315457","DOIUrl":"10.1080/10837450.2024.2315457","url":null,"abstract":"<p><p>Shikonin (SHK) has been evidenced to possess effects against various cancer cells. However, poor aqueous solubility and high toxicity restrict its application. In the study, RGD-decorated liposomes loaded with SHK (RGD-Lipo-SHK) were prepared <i>via</i> thin-film hydration method. Characterization and cellular uptake of liposomes was evaluated. Cytotoxicity of blank liposomes and different SHK formulations was measured against breast cancer cells (MDA-MB-231, MCF-7, and MCF-10A). Anti-tumour effects and pharmacokinetic parameters of different SHK formulations were appraised in tumour spheroids and in rat model, respectively. Liposomes displayed a particle size of less than 127 nm with a polydispersity index about 0.21. The encapsulation efficiency was about 91% for SHK, and drug leakage rate of liposomes was less than 6%. RGD-Lipo-SHK showed superior cellular internalization in the α<sub>v</sub>β<sub>3</sub>-positive MDA-MB-231 cells. Blank liposomes had no cytotoxicity to MDA-MB-231 and MCF-7 cells. Howbeit, different SHK formulations obviously inhibited proliferation of MCF-10A cells, especially free SHK. Meanwhile, RGD-Lipo-SHK significantly inhibited growth inhibition of tumour spheroids. The pharmacokinetics study indicated that the peak concentration, area under plasma concentration-time curves, half-life, and mean residence time of RGD-Lipo-SHK distinctly increased compared with those of free SHK. Altogether, these results demonstrated RGD-Lipo-SHK could reduce cytotoxicity, strengthen the antitumor-targeted effect, and prolong circulation time, which provides a foundation for further <i>in vivo</i> experimentations.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"153-163"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139707471","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon. 用于将布地奈德颗粒靶向送入降结肠的单层包衣的配制和优化。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-06 DOI: 10.1080/10837450.2024.2321250
Fatemeh Soltani, Hossein Kamali, Abbas Akhgari, Hadi Afrasiabi Garekani, Ali Nokhodchi, Fatemeh Sadeghi
{"title":"Formulation and optimization of a single-layer coat for targeting budesonide pellets to the descending Colon.","authors":"Fatemeh Soltani, Hossein Kamali, Abbas Akhgari, Hadi Afrasiabi Garekani, Ali Nokhodchi, Fatemeh Sadeghi","doi":"10.1080/10837450.2024.2321250","DOIUrl":"10.1080/10837450.2024.2321250","url":null,"abstract":"<p><p>The current budesonide formulations are inadequate for addressing left-sided colitis, and patients might hesitate to use an enema for a prolonged time. This study focuses on developing a single-layer coating for budesonide pellets targeting the descending colon. Pellets containing budesonide (1.5%w/w), PVP K30 (5%w/w), lactose monohydrate (25%w/w) and Avicel pH 102 (68.5%w/w) were prepared using extrusion spheronization technique. Coating formulations were designed using response surface methodology with pH and time-dependent Eudragits. Dissolution tests were conducted at different pH levels (1.2, 6.5, 6.8, and 7.2). Optimal coating formulation, considering coating level and the Eudragit (S + L) ratio to the total coating weight, was determined. Budesonide pellets were coated with the optimized composition and subjected to continuous dissolution testing simulating the gastrointestinal tract. The coating, with 48% S, 12% L, and 40% RS at a 10% coating level, demonstrated superior budesonide delivery to the descending colon. Coated pellets had a spherical shape with a uniform 30 µm thickness coating, exhibiting pH and time-dependent release. Notably, zero-order release kinetics was observed for the last 9 h in colonic conditions. The study suggests that an optimized single-layer coating, incorporating pH and time-dependent polymers, holds promise for consistently delivering budesonide to the descending colon.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"212-220"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139932386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Porous microneedle arrays as promising tools for the quantification of drugs in the skin: a proof of concept study. 多孔微针阵列是皮肤药物定量的理想工具:概念验证研究。
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-04 DOI: 10.1080/10837450.2024.2319734
Eyman M Eltayib, Achmad Himawan, Usanee Detamornrat, Wildan Khairi Muhtadi, Huanhuan Li, Luchi Li, Lalitkumar Vora, Ryan F Donnelly
{"title":"Porous microneedle arrays as promising tools for the quantification of drugs in the skin: a proof of concept study.","authors":"Eyman M Eltayib, Achmad Himawan, Usanee Detamornrat, Wildan Khairi Muhtadi, Huanhuan Li, Luchi Li, Lalitkumar Vora, Ryan F Donnelly","doi":"10.1080/10837450.2024.2319734","DOIUrl":"10.1080/10837450.2024.2319734","url":null,"abstract":"<p><p>This study aimed to demonstrate the potential of using porous microneedles (PMNs) as a promising tool for the noninvasive quantification of topically applied pharmaceutical products. We fabricated a porous microneedle (PMN) from a blend of cellulose acetate and dimethyl sulfoxide by casting and phase separation; it was characterized using scanning electron microscopy, Raman spectroscopy, differential scanning calorimetry, and a Texture Analyzer. An <i>ex vivo</i> study was conducted as a proof-of-concept study to assess whether this PMN could be used to quantify drug absorption through the skin after the topical administration of two nonequivalent products of sodium ibuprofen (gel and dissolving microneedles). Three cellulose acetate formulations (PMN1: 37.5%, PMN-2: 44.4%, and PMN-3: 50%) were used to prepare PMN patches; subsequently, these were evaluated for their morphological and insertion properties. Only PMN-2 microneedle patches were chosen to continue with the <i>ex vivo</i> study. The <i>ex vivo</i> study results demonstrated that PMNs could absorb and release sodium ibuprofen (SDIB) and differentiate between two different SDIB topical products. This can be attributed to the porous and interconnected architecture of these microneedles. This developmental study highlights the potential success of such a tool for the quantification of dermal drug concentration and supports moving to <i>in vivo</i> tests.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"164-175"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139747198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Preparation of tofacitinib sustained-release tablets using hot melt extrusion technology. 利用热熔挤压技术制备托法替尼缓释片
IF 3.4 4区 医学
Pharmaceutical Development and Technology Pub Date : 2024-03-01 Epub Date: 2024-03-04 DOI: 10.1080/10837450.2024.2323621
Sung-Yeop Kim, Ike de la Pena, Kwon Yeon Weon, Jun-Bom Park
{"title":"Preparation of tofacitinib sustained-release tablets using hot melt extrusion technology.","authors":"Sung-Yeop Kim, Ike de la Pena, Kwon Yeon Weon, Jun-Bom Park","doi":"10.1080/10837450.2024.2323621","DOIUrl":"10.1080/10837450.2024.2323621","url":null,"abstract":"<p><p>This study aimed to develop a tablet that shows a drug release profile similar to the tofacitinib sustained-release tablet (Xeljanz XR®; OROS™) using hot melt extrusion technology. Tofacitinib citrate was selected as the drug. HPMCAS, HPMCP, and Kollidon VA64 were used as thermoplastic polymers to prepare a hot-melt extrudate. The extrudate was obtained from a twin screw extruder and pelletizer. The granules were compressed using a single punch press machine and then coated. TGA, DSC, XRD, FT-IR, and SEM were performed on the hot melt extrudate to understand its physicochemical properties. Dissolution tests were performed using the paddle method (USP Apparatus II). The results showed that the crystallinity state of tofacitinib changed to amorphous after the hot melt extrusion process; however, no chemical change was observed. The drug release profile was similar to that of Xeljanz XR®, which has an initial lag time owing to its OROS™ formulation; a coating process was performed to obtain a similar drug release profile. The lag time was controlled by adjusting the thickness of the coating layer. Moreover, the extrudate size and compression force during tableting did not significantly affect drug release. In conclusion, the new tofacitinib sustained-release tablet prepared using hot melt extrusion showed a drug release behavior similar to that of Xeljanz XR<sup>®</sup>.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"248-257"},"PeriodicalIF":3.4,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139983505","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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