Abstract：
:The most effective and safe contraceptive method, intrauterine devices (IUDs), is still underutilized due to the pain barrier during IUD insertion. Lidocaine, a well-known local anesthetic, can be used to relieve IUD insertion pain. This study aimed at formulation, in vitro, in vivo and clinical evaluation of a novel lidocaine dual-responsive in situ gel. Pluronic and Gelrite® were used as thermosenstive and ion-activated polymers, respectively. In situ gels containing 2% lidocaine, pluronics and/or Gelrite® were prepared. The optimized dual-responsive formula (F5) was clear, with 95% drug content, free flowing at room temperature and gel at vaginal temperature (Tgel of 28 °C). This optimized dual-responsive in situ gel was found to be superior to single-responsive one due to presence of Gelrite®, imparting resistance to dilution effect of simulated vaginal fluids. DSC thermograms revealed no interaction between formulation components. Biocompatibility study showed no degeneration, necrosis or inflammation. Optimized dual-responsive in situ gel was further evaluated for pain reduction efficiency via a pilot randomized, double-blinded, placebo-controlled clinical trial showing ease of self-administeration by patients and significant pain reduction induced at all steps of IUD insertion. In conclusion, lidocaine dual-responsive in situ gel can be effectively used in prevention of pain during IUD insertion.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Abd Ellah NH,Abouelmagd SA,Abbas AM,Shaaban OM,Hassanein KMAdoi
10.1016/j.ijpharm.2018.01.033subject
Has Abstractpub_date
2018-03-01 00:00:00pages
279-286issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(18)30052-8journal_volume
538pub_type
杂志文章,随机对照试验abstract：:Alginate-chitosan (ALG-CS) blend gel beads were prepared based on Ca2+ or dual crosslinking with various proportions of alginate and chitosan. The homogeneous solution of alginate and chitosan was dripped into the solution of calcium chloride; the resultant Ca2+ single crosslinked beads were dipped in the solution of ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.12.019
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abstract：:Gels formed in situ following oral administration of dilute aqueous solutions of pectin (1.0 and 1.5%, w/v) to rats were evaluated as vehicles for the sustained release of the expectorant drug ambroxol hydrochloride. The solutions contained calcium ions in complexed form, which on release in the acidic environment of ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2003.11.027
更新日期：2004-03-01 00:00:00
abstract：:Clonazepam and lorazepam are two anxiolytics, antidepressant agents, having suitable features for transdermal delivery. The objectives of this study were to evaluate the in vitro percutaneous absorption of these drugs through excised human skin (stratum corneum and epidermis, SCE) and to determine their in vitro perme...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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abstract：:This study investigates drug-excipient interactions in amorphous solid dispersions (ASDs) of the model basic compound lumefantrine (LMN), with five acidic polymers. X-ray photoelectron spectroscopy (XPS) was used to measure the extent of the protonation of the tertiary amine in LMN by the five acidic polymers. The ext...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2016-12-05 00:00:00
abstract：:Self-emulsifying drug delivery systems (SEDDS) are lipid formulations that improve solubility and oral bioavailability of the incorporated drug with poor biopharmaceutical properties. As liquids they are traditionally filled into soft or hard capsules. Transformation of SEDDS into solid dosage form has been extensivel...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
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abstract：:In cutaneous drug delivery, it is widely accepted that the choice of excipients affects the delivery of a drug molecule to the skin. MALDI mass spectrometry imaging (MALDI-MSI) is an imaging technique which enables the simultaneous detection of multiple compounds. MALDI-MSI was applied to study the penetration of tofa...
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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abstract：:Porphyrin and their derivatives are being systematically studied as photosensitizers for photodynamic therapy. The ability to predict their membrane partition properties is of key importance to unveil their in vivo activity and applications. Several n-octanol/water partition coefficients (logP(OW)) of porphyrin deriva...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.08.008
更新日期：2007-02-01 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 临床试验,杂志文章
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更新日期：2007-04-20 00:00:00
abstract：:Recently, we synthesized novel amphiphilic gelatin-oleic acid (GO) conjugate to prepare self-assembled nanoparticles for drug delivery. The aim of this study was to investigate pharmaceutical potentialities of self-assembled GO nanoparticles for solubility enhancement and modified release of poorly water-soluble drugs...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.07.025
更新日期：2013-10-15 00:00:00
abstract：:The optimized formulation of N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug, was developed by utilizing the complexation between N-4472 and L-ascorbic acid (VC). It was found that the formulation with Gelucire((R)) 44/14, H...
journal_title：International journal of pharmaceutics
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doi：10.1016/s0378-5173(02)00346-0
更新日期：2002-10-10 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.05.055
更新日期：2009-08-13 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.01.020
更新日期：2015-03-01 00:00:00
abstract：:A wet-primed ready-to-use extracorporeal membrane oxygenation (ECMO) circuit is used in some centres for rapid deployment of ECMO during cardiopulmonary resuscitation. Yet, the potential release of plasticizer di(2-ethylhexyl)phthalate (DEHP) from the polyvinyl chloride tubing in the circuit during storage is a concer...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.01.030
更新日期：2005-04-27 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.01.054
更新日期：2008-06-05 00:00:00
abstract：:The aim of the present study was to investigate the relationship between formulation/process variables versus the critical quality attributes (CQAs) of cyclosporine ophthalmic ointments and to explore the feasibility of using an in vitro approach to assess product sameness. A definitive screening design (DSD) was used...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2018-06-10 00:00:00
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journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2011.02.051
更新日期：2011-05-16 00:00:00
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journal_title：International journal of pharmaceutics
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doi：10.1016/j.ijpharm.2009.02.006
更新日期：2009-05-21 00:00:00
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abstract：:The purpose of this study is to improve the solubility, in vitro dissolution, and oral bioavailability in rats of tadalafil (TDF) by using SD technique with a weak acid and a copolymer. TDF-SD was prepared via solvent evaporation, coupled with the incorporation of an acidifier and solubilizer. Tartaric acid enhanced t...
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2002-12-05 00:00:00
abstract：:Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
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更新日期：2017-06-30 00:00:00
abstract：:Hydrochlorothiazide (HCTZ) 60 mg strength tablets containing commonly used excipients and hydroxypropyl cellulose, marketed as either Klucel-EF (HPC, NF from Hercules, USA) or HPC-L (HPC, NF from Nippon Soda, Japan), as a binder were manufactured using identical aqueous wet granulation process. The tablets containing ...
journal_title：International journal of pharmaceutics
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更新日期：2006-02-03 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
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更新日期：2010-12-15 00:00:00
abstract：:Current treatment for pelvic organ prolapse (POP) and stress urinary incontinence (SUI) involves transvaginal implantation of surgical mesh, conventionally made of polypropylene (PP). However, it has recently become apparent that the mechanical properties of PP are unsuitable, resulting in serious complications such a...
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更新日期：2021-01-25 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
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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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更新日期：2012-11-01 00:00:00
abstract：:In this study, the preparation of N-pamitoyl chitosan (ChP) anchored oleic acid (OA) liposome was demonstrated. Two different types of water-soluble ChPs with different degrees of acylation (DA) were selected for this study. The presence of ChPs on the surface of OA liposome was confirmed with their micrographs and ph...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.11.013
更新日期：2013-01-30 00:00:00
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journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.08.095
更新日期：2017-10-30 00:00:00
