Pharmacokinetics of 16-dehydropregnenolone hydroxypropyl-β-cyclodextrin inclusion complex following peroral administration.

Abstract:

:16-Dehydropregnenolone (16-DHP) is an active compound with an unsatisfied in vivo behavior and poor water-solubility, which limits its clinical application. To improve its in vivo behavior and water-solubility, a Hydroxypropyl-beta-Cyclodextrin (HP-β-CD) inclusion complex of 16-DHP was prepared in this paper. Pharmacokinetic studies after oral administration of 16-DHP-HP-β-CD at doses of 37.5, 75, 150 mg/kg were carried out to investigate its dose proportionality in rats. The relative bioavailability was researched by comparing the area under the plasma concentration-time curve of 16-DHP-HP-β-CD and free 16-DHP after oral administration in rats at the dose of 75 mg/kg. At the same time, tissue distribution of 16-DHP-HP-β-CD after oral administration at the dose of 240 mg/kg in mice was also investigated. Consequently, 16-DHP-HP-β-CD appeared to be a linear pharmacokinetic character after peroral administration to the rat at the doses tested. Compared to free 16-DHP, inclusion complex could significantly improve the relative bioavailability (467%). Tissue distribution studies indicated that 16-DHP-HP-β-CD tended to distribute into stomach, intestine, lung, brain and liver.

journal_name

Pharm Dev Technol

authors

Sun Y,Jia L,Zhou H,Mao M,Wang X,Wei L,Sun L

doi

10.1080/10837450.2016.1193192

subject

Has Abstract

pub_date

2017-03-01 00:00:00

pages

218-228

issue

2

eissn

1083-7450

issn

1097-9867

journal_volume

22

pub_type

杂志文章
  • Effects of light intensity, n-alcohols, water-soluble colorants, and solution viscosity on photoisomerization of sorivudine.

    abstract::Effects of various factors, such as light intensity, polarizability of n-alcohol solvents, addition of colorants, and viscosity of solutions on the kinetics of the photoisomerization of therapeutically effective E-isomer of sorivudine to its less effective Z-isomer were studied. Solutions of known concentrations of E-...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100000047

    authors: Desai D,Li D,Janjikhel R,Lang B,Jain N

    更新日期:2001-01-01 00:00:00

  • Fabrication and evaluation of Phytomenadione as a nanostructure lipid carrier for enhancement of bioavailability.

    abstract::Owing to its limited aqueous solubility, Phytomenadione (vitamin K) undergoes a low bioavailability (50%) with a large inter-individual variability after oral administration. Therefore, the aim of this work was to incorporate vitamin K into nanostructure lipid carrier systems to improve its aqueous solubility and bioa...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2017.1312440

    authors: Aljaeid BM,Hosny KM

    更新日期:2018-04-01 00:00:00

  • Decreasing acute toxicity and suppressing colorectal carcinoma using Sorafenib-loaded nanoparticles.

    abstract::Objective: A polymer-based nanoparticle was constructed to target sorafenib delivery to colorectal carcinoma cells and decrease the side effects of the drug.Methods: Sorafenib-loaded nanoparticles (S-NPs) based on PEG-PLGA were prepared using a double emulsion solvent evaporation method. The properties of S-NPs were e...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2020.1718704

    authors: Li N,Chen Y,Sun H,Huang T,Chen T,Jiang Y,Yang Q,Yan X,Wu M

    更新日期:2020-06-01 00:00:00

  • Novel potential drug against T. cruzi and its interaction with surfactant micelles.

    abstract::The interaction of 5-nitro-2-furfurilylidene benzhydrazide (5NFB), potential anti-trypanosomal compound, with micellar solutions was studied. The results indicated that 50 mug of 5NFB completely kills 20 million T. cruzi epimastigote cells within 3 days, whereas the same amount of benznidazole kills 30% of the cells a...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450701212727

    authors: Rangel-Yagui CO,Hsu HW,Barbosa LR,Caetano W,Pessoa A Jr,Tavares LC,Itri R

    更新日期:2007-01-01 00:00:00

  • Taste masking of naproxen sodium granules by fluid-bed coating.

    abstract::The taste of oral dosage forms is an important argument regarding patient's compliance and acceptability. For this reason, it is often necessary to mask an undesirable and unpleasant taste of an active pharmaceutical ingredient. The purpose of this study was to mask the taste of naproxen sodium by a new fluid-bed coat...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.757784

    authors: Stange U,Führling C,Gieseler H

    更新日期:2014-03-01 00:00:00

  • Formulation strategy of nitrofurantoin: co-crystal or solid dispersion?

    abstract::Poor solubility and bioavailability of drugs are often affected by its microscopic structural properties. Nitrofurantoin (NF), a Biopharmaceutics Classification System class II item, has a low water solubility with low plasma concentrations. To improve its therapeutic efficacy, formulation strategy of solid dispersion...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1689401

    authors: Teoh XY,Bt Mahyuddin FN,Ahmad W,Chan SY

    更新日期:2020-02-01 00:00:00

  • Glucose-sensitive gel rheology of dextran-concanavalin A mixtures suitable for self-regulating insulin delivery.

    abstract::Aqueous concentrated plain mixtures of dextran and concanavalin A (con A) were examined for their rheological response to glucose for comparison with previously studied partially photopolymerized acrylic derivatives. Non-destructive oscillatory tests were undertaken within the linear viscoelastic range to examine the ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903002181

    authors: Taylor MJ,Tanna S,Sahota TS

    更新日期:2010-01-01 00:00:00

  • Estimation of initial dissolution rate of drug substance by thermal analysis: application for carbamazepine hydrate.

    abstract::We have proposed a theory indicating the correlation between the dissolution rate and the heat of solution of drug substances. The initial dissolution rates of the drug substances containing amorphous were predicted accurately from their heats of solution. In this report, the possibility for the theory to estimate the...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120002234

    authors: Yoshihashi Y,Yonemochi E,Terada K

    更新日期:2002-01-01 00:00:00

  • Preparation and characterization of a powder containing an oily liquid drug with Eudragit EPO or L100 copolymer.

    abstract::Oily liquid drugs are not convenient for oral administration. We developed a powder containing clofibrate (CF), a model of an oily drug, using aminoalkyl methacrylate copolymer (EPO) or methacrylic acid copolymer (L100). CF or a mixture of CF and soybean oil was emulsified with EPO or L100 aqueous solution. Using a hi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1086370

    authors: Fujii M,Kawakami A,Saito A,Tuchiya H,Koizumi N,Watanabe Y

    更新日期:2016-12-01 00:00:00

  • A measurement of the unstirred aqueous boundary layer in a Franz diffusion cell.

    abstract::The unstirred aqueous boundary layer (ABL) thickness was determined for modified Franz diffusion cells using three test compounds--parathion, 4-hexylresorcinol, and 2,4-dinitrochlorobenzene (DNCB). Steady-state fluxes through one, two, and three dialysis membranes in series were achieved in donor-saturated, infinite-d...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2011.572895

    authors: Miller MA,Kasting G

    更新日期:2012-11-01 00:00:00

  • Solid-state characterization of fluconazole.

    abstract::Two polymorphs and three solvates of fluconazole were isolated and characterized by x-ray powder diffractometry, IR spectroscopy, differential scanning calorimetry (DSC), thermogravimetry, and their dissolution rates. The different forms were prepared by crystallization of the original powder in different solvents at ...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-120015052

    authors: Alkhamis KA,Obaidat AA,Nuseirat AF

    更新日期:2002-11-01 00:00:00

  • Novel organogels for topical delivery of naproxen: design, physicochemical characteristics and in vitro drug permeation.

    abstract::Taking into account possible irritation of the skin upon contact with naproxen (NPX) crystals and lower bioavailability after administration of the suspended or ionized drug, the aim of the work was to design and characterize novel and easy-to-formulate gels with the entirely dissolved drug in the acidic form. The for...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1135342

    authors: Osmałek T,Milanowski B,Froelich A,Górska S,Białas W,Szybowicz M,Kapela M

    更新日期:2017-06-01 00:00:00

  • Influence of dissolution media pH and USP1 basket speed on erosion and disintegration characteristics of immediate release metformin hydrochloride tablets.

    abstract:PURPOSE:To investigate the influence of the pH of the dissolution medium on immediate release 850 mg metformin hydrochloride tablets. METHODS:A traditional wet granulation method was used to manufacture metformin hydrochloride tablets with or without a disintegrant. Tablet dissolution was conducted using the USP appar...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.892132

    authors: Desai D,Wong B,Huang Y,Tang D,Hemenway J,Paruchuri S,Guo H,Hsieh D,Timmins P

    更新日期:2015-01-01 00:00:00

  • Evaluation of the gum from Hakea gibbosa as a sustained-release and mucoadhesive component in buccal tablets.

    abstract::The objective of this paper was to evaluate the mucoadhesive and sustained-release properties of the water-soluble gum obtained from Hakea gibbosa (hakea), for the formulation of buccal tablets. Flatfaced tablets containing hakea were formulated using chlorpheniramine maleate (CPM) as a model drug. Two types of tablet...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100101370

    authors: Alur HH,Pather SI,Mitra AK,Johnston TP

    更新日期:1999-08-01 00:00:00

  • Effect of drug-carrier interaction on the dissolution behavior of solid dispersion tablets.

    abstract::The objective of this study was to compare the dissolution behavior of tablets prepared from solid dispersions with and without drug-carrier interactions. Diazepam and nifedipine were used as model drugs. Two types of carriers were used; polyvinylpyrrolidone (PVP K12, K30 and K60) and saccharides (inulin 1.8 kDa, 4 kD...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450903286529

    authors: Srinarong P,Kouwen S,Visser MR,Hinrichs WL,Frijlink HW

    更新日期:2010-09-01 00:00:00

  • About the equivalence between different batches of a glycopeptide drug.

    abstract:CONTEXT:Teicoplanin is a glycopeptide antibiotic consisting of a combination of different active components. Clinical equivalence between different batches of this drug is not guaranteed by the present pharmacopeial specification of chemical composition based on an HPLC chromatogram. OBJECTIVE:To test a modification o...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1035726

    authors: Boix-Montañes A,Garcia-Arieta A

    更新日期:2016-08-01 00:00:00

  • Iontophoretic enhancement of leuprolide acetate by fatty acids, limonene, and depilatory lotions through porcine epidermis.

    abstract::The effect of chemical enhancers (e.g., fatty acids, limonene, depilatory lotions) and iontophoresis was investigated on the in vitro permeability of leuprolide acetate through porcine epidermis. Franz diffusion cells and Scepter iontophoretic power source were used for the percutaneous absorption studies. Anodal iont...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-200032986

    authors: Rastogi SK,Singh J

    更新日期:2004-11-01 00:00:00

  • Formulation and in vitro characterization of poly(dl-lactide-co-glycolide)/Eudragit RLPO or RS30D nanoparticles as an oral carrier of levofloxacin hemihydrate.

    abstract::The main objective of this study was to design positively charged Levofloxacin Hemihydrate (Levo-h)-loaded nanoparticles with improved entrapment efficiency and antibacterial activity. PLGA alone or in combinations with Eudragit® RLPO or RS30D with or without positively charged inducing agent; 1,2-dioleoyl-3-trimethyl...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1041044

    authors: Hasan AA,Sabry SA,Abdallah MH,El-Damasy DA

    更新日期:2016-09-01 00:00:00

  • In vitro release of colchicine using poly(phosphazenes): the development of delivery systems for musculoskeletal use.

    abstract::A colchicine release system utilizing biodegradable poly(phosphazenes) was investigated in vitro for intra-articular administration. Polymer degradation and drug release studies were performed on colchicine-loaded poly(phosphazenes) containing either imidazolyl (I-PPHOS) or ethyl glycinato (EG-PPHOS) side chain substi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837459809028479

    authors: Ibim SM,el-Amin SF,Goad ME,Ambrosio AM,Allcock HR,Laurencin CT

    更新日期:1998-02-01 00:00:00

  • Formulation and evaluation of curcumin gel for topical application.

    abstract::The aim of the present investigation was to develop and study topical gel delivery of curcumin for its anti-inflammatory effects. Carbopol 934P (CRB) and hydroxypropylcellulose (HPC) were used for the preparation of gels. The penetration enhancing effect of menthol (0-12.5% w/w) on the percutaneous flux of curcumin th...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450802409438

    authors: Patel NA,Patel NJ,Patel RP

    更新日期:2009-01-01 00:00:00

  • Development of thermodynamically stable nanostructured lipid carrier system using central composite design for zero order permeation of econazole nitrate through epidermis.

    abstract::The investigation was aimed at developing thermodynamically stable topical delivery system of nanostructured lipid carrier of econazole nitrate (EN) for the treatment of deep seated fungal infection by improving its permeability. Fifteen formulations (F1-F15) of nanostructured lipid carriers (NLCs) were prepared by so...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2012.659256

    authors: Keshri L,Pathak K

    更新日期:2013-05-01 00:00:00

  • Effect of degree of methoxylation and particle size on compression properties and compactibility of pectin powders.

    abstract::This study examines the effect of the degree of methoxylation (DM) and particle size on compression properties and compactibility of pectin powders. A powder classification system based on sequential handling of compression parameters was applied. A single size fraction (90-125 μm) of pectin powders with DM values ran...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2010.535831

    authors: Salbu L,Bauer-Brandl A,Alderborn G,Tho I

    更新日期:2012-05-01 00:00:00

  • Formulation development and systematic optimization of stabilized ziprasidone hydrochloride capsules devoid of any food effect.

    abstract:CONTEXT AND OBJECTIVE:The objective of the study was to develop a stable capsule formulation of ziprasidone hydrochloride which can be administered without regards to food intake. MATERIALS AND METHODS:The unstable anhydrous form of ziprasidone hydrochloride was stabilized employing hot-melt extrusion and further opti...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2015.1055764

    authors: Banerjee S,Shankar KR,Prasad Y R

    更新日期:2016-11-01 00:00:00

  • Waxy corn starch: a potent cofiller in pellets produced by extrusion-spheronization.

    abstract::The purpose of this study was to assess the usefulness of waxy corn (maize) starch as a cofiller and diluent in pellets produced by aqueous extrusion-spheronization. Waxy corn starch was combined with microcrystalline cellulose (MCC) in the range of 20-50% of the entire composition. Pellets containing ordinary corn st...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1081/pdt-100100521

    authors: Junnila R,Palviainen P,Heinämäki J,Myllärinen P,Forssell P,Yliruusi J

    更新日期:2000-01-01 00:00:00

  • Synthesis, characterization, and kinetic release study of methotrexate loaded mPEG-PCL polymersomes for inhibition of MCF-7 breast cancer cell line.

    abstract::In this study, we designed a polymersome system for the controlled release of methotrexate (MTX) as an anticancer drug with the objective of improving the loading efficiency of the drug in polymersomes as well as achievement of an efficient control on the release rate of drug from nanocarriers. We synthesized mono met...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2018.1425433

    authors: Nosrati H,Adinehvand R,Manjili HK,Rostamizadeh K,Danafar H

    更新日期:2019-01-01 00:00:00

  • Dual drug nanocrystals loaded microparticles for fixed dose combination of simvastatin and ezetimibe.

    abstract::Dual drug nanocrystals loaded nano embedded microparticles (DNEMs) were prepared for fixed dose combination of simvastatin (SIM) and ezetimibe (EZE) using NanoCrySP technology. The purpose was to generate nanonized SIM and EZE dispersed in matrix of single crystallization inducing excipient and investigate their in vi...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1669181

    authors: Nandi S,Kaur A,Bansal AK

    更新日期:2020-01-01 00:00:00

  • Preliminary study of an offline simultaneous determination of metoprolol tartrate and hydrochlorothiazide in powders and tablets by reflectance near-infrared spectroscopy.

    abstract::A preliminary study of the feasibility of using near-infrared spectroscopy (NIRS) for the offline simultaneous determination of metoprolol tartrate (MTP) and hydrochlorothiazide (HTZ) in powders and tablets has been carried out. An industrial tableting process was simulated using an instrumented tablet press replicato...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2014.949268

    authors: Vranic BZ,Vandamme TF

    更新日期:2015-01-01 00:00:00

  • Polymorphism and solvates of flecainide base.

    abstract::Flecainide base is pharmaceutically active substance used for production of flecainide acetate which is known in market as Tambacor, Almarytm, Apocard, Ecrinal or Flecaine. It is determined that flecainide base forms four polymorphic forms abbreviated as Ib, IIb, IIIb and IVb. Flecainide base form Ib is thermodynamica...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.763259

    authors: Veldre K,Eglīte Z,Actiņš A,Zvirgzdiņš A,Rozenberga L,Tamanis E

    更新日期:2014-02-01 00:00:00

  • Preparation, preliminary pharmacokinetics and brain tissue distribution of Tanshinone IIA and Tetramethylpyrazine composite nanoemulsions.

    abstract::Objective: Tanshinone IIA (TSN) and Tetramethylpyrazine (TMP) were combined in a composite, oil-in-water nanoemulsions (TSN/TMP O/W NEs) was prepared to prolong in vitro and vivo circulation time, and enhance the bioavailability of TSN. Material and methods: Physicochemical characterization of TSN/TMP O/W NEs was char...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.1080/10837450.2019.1656237

    authors: Wang B,Hong L,Liu Y,Bedingfield SK,Zhang C,Peng C,Qian J,Zha L

    更新日期:2019-12-01 00:00:00

  • Influence of the type of vegetable oil on the drug release profile from lipid-core nanocapsules and in vivo genotoxicity study.

    abstract::The use of rice bran (RB), soybean (SB) or sunflower seed (SF) oils to prepare lipid-core nanocapsules (LNCs) as controlled drug delivery systems was investigated. LNCs were prepared by interfacial deposition using the preformed polymer method. All formulations showed negative zeta potential and adequate nanotechnolog...

    journal_title:Pharmaceutical development and technology

    pub_type: 杂志文章

    doi:10.3109/10837450.2013.829097

    authors: Rigo LA,Frescura V,Fiel L,Coradini K,Ourique AF,Emanuelli T,Quatrin A,Tedesco S,Silva CB,Guterres SS,Pohlmann AR,Beck RC

    更新日期:2014-11-01 00:00:00