Abstract：
:Metformin has several problems such as low bioavailability, short half-life, and narrow absorption window, sustained and site-specific drug delivery system is required. Floating drug delivery systems are very useful to achieve these purposes. However, conventional floating systems have several limitations; lag time, a high proportion of excipient in the tablet, using non-biocompatible excipient, and requirement of a complicated procedure. To overcome these obstacles, we developed a hollow-core floating tablet (HCFT). The HCFT immediately floated in pH 1.2, 4.0, 6.8 medium, and even distilled water. The floating duration time of HCFT was>24 h. From the in vitro release study, it was confirmed that HCFT showed the sustain release profile of metformin for 12 h. Water uptake and matrix erosion were evaluated for predicting the buoyancy and drug release kinetics of HCFT in the body. Factor analysis was applied to optimize the formulation. There were significant (p < 0.05) differences in metformin plasma concentration of 4 h and 6 h between two groups. Compared with Glucophage® XR, the relative bioavailability of metformin HCFT was 123.81 ± 3.52%. The X-ray imaging of optimized formulation revealed that HCFT was constantly floating in the stomach region of the rabbit, thereby indicating improved gastric retention for>6 h. Consequently, all the findings indicate that HCFT could be an effective gastric retention system and applied extensively to other drugs with narrow absorption windows.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Wook Huh H,Na YG,Kang H,Kim M,Han M,Mai Anh Pham T,Lee H,Baek JS,Lee HK,Cho CWdoi
10.1016/j.ijpharm.2020.120113subject
Has Abstractpub_date
2021-01-05 00:00:00pages
120113eissn
0378-5173issn
1873-3476pii
S0378-5173(20)31098-Xjournal_volume
592pub_type
杂志文章abstract：:Phenoporlamine hydrochloride is a novel compound that is used for the treatment of hypertension. The purpose of this study was to develop a sustained release tablet for phenoporlamine hydrochloride because of its short biological half-life. Three floating matrix formulations of phenoporlamine hydrochloride based on ga...
journal_title：International journal of pharmaceutics
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abstract：:Isooctyl p-methoxycinnamate(OMC) is a commonly used chemical ultraviolet B sunscreen that suffers rapid degradation with current delivery systems following sun exposure. In this study, deoxycholate-mediated liposome (DOC-LS) endocytosis was employed to improve the antioxidation effects of OMC following topical adminis...
journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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pub_type： 杂志文章,随机对照试验
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更新日期：2020-08-30 00:00:00
