Abstract：
:Lansoprazole (LPZ) is a representative drug that shows a high inter-subject variation of bioavailability (BA). Solid preparation composed of surfactant, adsorbent and LPZ were prepared to improve the dissolution and absorption of LPZ, and the BA of LPZ was measured in rats and dogs. As surfactant, Tween 80, polyoxy 60 hydrogenated caster oil derivative (HCO-60) and PEG-8 caprylic/capric glycerides (Labrasol) were used. As adsorbant, porous silicon dioxide (Sylysia 550, 320), magnesium aluminometa silicate (Neusilin S2, NS2N, US2) and porous calcium silicate (Florite RE) were used. After small intestinal administration of LPZ, 5.0 mg/kg, solution with HCO-60 showed the highest plasma LPZ concentration versus time curve of which C(max) and AUC was 0.46+/-0.01 microg/mL and 0.73+/-0.03 microgh/mL. By comparing to that after i.v. injection of LPZ solution, 2.0 mg/kg, the BA of LPZ from HCO-60 solution was 39.0%, which was about seven times higher than that of LPZ powder. To solidify the LPZ solution with HCO-60, adsorbents were used and the obtained solid preparations were used for in vitro release experiment. Sylysia 320, Neusilin S2 and Neusilin NS2 showed the T50% of about 1h. To evaluate the BA of these solid preparations, absorption study was performed in rats. Sylysia 550 system showed the higher AUC than other systems, showing the BA of 28.1%. Sylysia 550 system was filled in an enteric capsule and was orally administered to dogs and BA was compared with enteric tablet. The AUC of Sylysia 550 system was 2.16+/-0.26 microgh/mL and was greater than enteric tablet and the BA of 71.7% was obtained. Solid system composed of LPZ, surfactant and adsorbent has suggested the possibility as a good tool to improve the BA of LPZ.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Ito Y,Arai H,Uchino K,Iwasaki K,Shibata N,Takada Kdoi
10.1016/j.ijpharm.2004.10.010keywords:
subject
Has Abstractpub_date
2005-01-31 00:00:00pages
69-77issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(04)00622-2journal_volume
289pub_type
杂志文章abstract：:D-borneolum is commonly used as a permeation enhancer in Traditional Chinese Medicine (TCM) formulas for transdermal application. Additionally, two other sources of borneolums were recorded in the 2015 edition of the Chinese Pharmacopoeia (ChP), including L-borneolum and borneolum syntheticum. To guide the selection a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119225
更新日期：2020-04-30 00:00:00
abstract：:Sodium salts are often used in drug formulation but their partial solubility parameters are not available. Sodium alters the physical properties of the drug and the knowledge of these parameters would help to predict adhesion properties that cannot be estimated using the solubility parameters of the parent acid. This ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00374-9
更新日期：2000-01-20 00:00:00
abstract：:A reproducible double emulsion/solvent evaporation procedure is developed to formulate magnetic solid lipid nanoparticles (average size≈180 nm) made of iron oxide cores embedded within a glyceryl trimyristate solid matrix. The physicochemical characterization of the nanocomposites ascertained the efficacy of the prepa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.03.005
更新日期：2016-05-17 00:00:00
abstract：:Drug development is a long process which requires careful evaluation of the drug substance (active pharmaceutical ingredient, API), drug product (tablet, capsule etc.) and the bioperformance (both pre-clinical and clinical) before testing the efficacy of the final dosage form. The earliest assessment of a new drug sub...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.08.055
更新日期：2018-10-25 00:00:00
abstract：:The purpose of this study was to construct isotretinoin-loaded SLN (IT-SLN) formulation with skin targeting for topical delivery of isotretinoin. PRECIROL ATO 5 was selected as the lipid of SLN. Tween 80 and soybean lecithin were used as the surfactants to stabilize SLN. The hot homogenization method was performed to ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.08.007
更新日期：2007-01-10 00:00:00
abstract：:Polysaccharide-coated liposomes have been studied for their potential use for peptide drug delivery by the oral route because they are able to minimize the disruptive influences on peptide drugs of gastrointestinal fluids. The aim of this work was to synthesize and characterize a modified polysaccharide, O-palmitoylsc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.06.040
更新日期：2006-11-15 00:00:00
abstract：:The dehydration of nedocromil magnesium (NM) pentahydrate proceeds in two steps, corresponding to the loss of four water molecules in the first step and one water molecule in the second step. The effects of temperature, particle size, sample weight, water vapor pressure and dehydration-rehydration cycle on both the ki...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00700-6
更新日期：2001-03-14 00:00:00
abstract：:Water-soluble calixarenes are promising macrocyclic compounds which have found numerous applications in chemistry and biology. However, these compounds have been less studied in regard to their behavior in aqueous solutions and mechanisms of drug solubilization. The present work is devoted to the evaluation of the sol...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.09.011
更新日期：2010-12-15 00:00:00
abstract：:The purpose of this study was to investigate the use of 6-carboxycellulose (OC), a biocompatible and bioresorbable polymer, as a prodrug carrier for amine drugs. Phenylpropanolamine hydrochloride (PPA.HCl) was used as a model drug. OC and PPA were reacted in dimethylformamide (DMF) in the presence of 1,3-dicyclohexylc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00725-6
更新日期：2001-07-31 00:00:00
abstract：:The unique properties of single-walled carbon nanotubes (SWNTs) enable them to play important roles in many fields. One of their functional roles is to transport cargo into cell. SWNTs are able to traverse amphipathic cell membranes due to their large surface area, flexible interactions with cargo, customizable dimens...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.03.017
更新日期：2017-05-30 00:00:00
abstract：:Cyclodextrin-containing polymers have proved themselves to be useful for controlled release. Herein we describe the preparation of membranes of poly(methylmethacrylate) (PMMA) containing hydroxypropyl-beta-cyclodextrins (HP-beta-CDs) using a supercritical CO(2)-assisted phase inversion method, for potential applicatio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.04.029
更新日期：2009-07-06 00:00:00
abstract：:Peptides and polypeptides have important pharmacological properties but only a limited number have been exploited as therapeutics because of problems related to their delivery. Most of these drugs require a parenteral delivery system which introduces the problems of pain, possible infection, and expertise required to ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.11.046
更新日期：2012-02-28 00:00:00
abstract：:Drugs in the gastrointestinal tract are exposed to a medium of partially digested food, comprising mixtures of fat, protein and carbohydrate. The dissolution behaviour of itraconazole was evaluated in bio-relevant media which were developed to take this into account. Media containing milk with different fat contents, ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.09.003
更新日期：2009-01-21 00:00:00
abstract：:Artemether (AM) plus azithromycin (AZ) rectal co-formulations were studied to provide pre-referral treatment for children with severe febrile illnesses in malaria-endemic areas. The target profile required that such product should be cheap, easy to administer by non-medically qualified persons, rapidly effective again...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.04.023
更新日期：2014-07-01 00:00:00
abstract：:Blend uniformity analysis (BUA) is a routine and highly regulated aspect of pharmaceutical production. In most instances, it involves quantitative determination of individual components of a blend in order to ascertain the mixture ratio. This approach often entails the use of costly and sophisticated instrumentation a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.07.073
更新日期：2012-11-15 00:00:00
abstract：:The main objectives of the present study were (i) to evaluate the effect of the mucus layer on saquinavir-loaded nanostructured lipid carriers (SQV-NLCs) uptake and (ii) to evaluate the mucopenetrating properties of dextran-protamine (Dex-Prot) coating on NLCs as per SQV permeability enhancement. Three different NLC f...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.04.027
更新日期：2014-07-01 00:00:00
abstract：:Cyclosporin A (CyA) is an immunosuppressive drug used topically to treat ocular inflammatory disorder such as dry eye disease (DES). It is a lipophilic cyclic peptide with molecular weight of 1202.6Da. The aim of this study was to develop surfactant free aqueous 0.2% (w/v) CyA eye drops where the drug is present in an...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.07.044
更新日期：2017-08-30 00:00:00
abstract：:A series of mesocellular foams (MCFs)-based mesoporous silica nanospheres (DH-MCF-P123-n, (n=12, 2, 0.5)) were synthesized as controlled-release deliveries for a typical antidepressant drug, venlafaxine. The foams were 3-(2,3-dihydroxypropoxyl)propyl-grafted and the P123 template partially preserved. We studied the re...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.12.048
更新日期：2012-03-15 00:00:00
abstract：:The relationships between data of passage through Caco-2 cultured cell lines (log Papp), taken from the literature, for 38 structurally unrelated compounds and both n-octanol lipophilicity parameters (log P(N) and log D(7.4)) and phospholipid affinity indexes were investigated. Phospholipid affinity(log k W(IAM)) was ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.01.019
更新日期：2016-03-16 00:00:00
abstract：:Optical surface roughness of starch acetate compacts was investigated by specular reflection of a laser beam as a function of angle of incidence. The intensity data was fitted using the model of Gaussian and Lorentzian curves to solve numerical values for optical surface roughness which was observed to be order of 1 m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00077-0
更新日期：1999-05-25 00:00:00
abstract：:Streamlining the manufacturing process has been recognized as a key issue to reduce production costs and improve safety in pharmaceutical manufacturing. Although data available from earlier developmental stages are often sparse and unstructured, they can be very useful to improve the understanding about the process un...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.01.018
更新日期：2013-02-28 00:00:00
abstract：:In the present study, a novel synthesis technique based on the flow focusing (FF) technology is investigated for the preparation of green fluorescent protein (GFP)-loaded poly(D,L-lactide-co-glycolide) (PLGA) microparticles. To our knowledge, this novel technique has never been applied to the formulation of proteins i...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.07.017
更新日期：2009-10-01 00:00:00
abstract：:The main objective of the study was to evaluate if the liquid crystalline cubic phase gel of glyceryl monooleate (GMO) protects insulin from agitation induced aggregation. The aggregation of Humulin(R), Regular Iletin I(R) and Regular Iletin II(R), in cubic phase GMO gels at 30 U/g of gel was compared with that in PBS...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00288-4
更新日期：1999-11-25 00:00:00
abstract：:The objective of this study was to determine, using a Caco-2 cell monolayer model, the extent to which the paracellular and transcellular routes are altered by citicholine (CDP-Ch) and DMSO in the presence of human serum albumin (HSA). The apparent permeability (Papp) of mannitol in the presence of 4% (w/v) HSA was in...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(02)00588-4
更新日期：2003-01-30 00:00:00
abstract：:The objective of this work is to use phage display libraries as a screening tool to identify peptides that facilitate transport across the mucus barrier. Mucus is a complex selective barrier to particles and molecules, limiting penetration to the epithelial surface of mucosal tissues. In mucus-associated diseases such...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.09.055
更新日期：2018-12-20 00:00:00
abstract：:The effect of different preparation parameters were analyzed with respect to the rheological and pharmaceutical characteristics of hydrogel blend patches, as transdermal delivery formulation. Mixtures of pectin and gelatin were employed for the production of patches, with adjustable properties, following a two-step ge...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.06.081
更新日期：2013-09-15 00:00:00
abstract：:The purpose of this study was to develop the correlation of cycle parameters between a laboratory and a production freeze-dryer. With the established correlation, key cycle parameters obtained using a laboratory dryer may be converted to those for a production dryer with minimal experimental efforts. In order to devel...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2005.06.022
更新日期：2005-09-30 00:00:00
abstract：:Naltrexone hydrochloride (NTX) is a promising treatment for corneal disorders linked to diabetes mellitus (diabetic keratopathy). However, NTX has a major stability problem due to autoxidation, which is likely to hinder its formulation as eye drops for treatment of diabetic keratopathy. In this study, in-house develop...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.011
更新日期：2012-08-20 00:00:00
abstract：:Cyclodextrin-based nanosponges (CD-NSs) are insoluble, highly cross-linked 3D network polymers used in several scientific and technological fields, the main area of investigation concerns the pharmaceutical applications, in which CD-NSs have been mostly employed as drug delivery systems. CD-NSs can be generally groupe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.06.072
更新日期：2017-10-15 00:00:00
abstract：:This study was aimed at developing a liposome delivery system for a new and potential antitumor lipophilic prodrug of 5-fluorouracil (5-Fu)-N(3)-O-toluyl-fluorouracil (TFu), intended to improve the bioavailability and therapeutic efficacy of 5-Fu by oral and intravenous administration. TFu-loaded liposomes were prepar...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.11.017
更新日期：2008-04-02 00:00:00
