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Drug Development and Industrial Pharmacy

Eman Abd-Elrasheed, Sara Nageeb El-Helaly, Manal M El-Ashmoony, Salwa Salah
Intranasal Zaleplon solid dispersion was formulated to enhance the solubility, bioavailability and deliver an effective therapy. Zaleplon belongs to Class II drugs, and undergoes extensive first-pass metabolism after oral absorption exhibiting 30% bioavailability. A 23full factorial design was chosen for the investigation of solid dispersion formulations. The effects of different variables include drug to carrier ratio (1:1 and 1:2), carrier type (polyethylene glycol 4000 and poloxamer 407), and preparation method (solvent evaporation and freeze drying) on different dissolution parameters were studied...
December 13, 2017: Drug Development and Industrial Pharmacy
Jaber Emami, Mahboubeh Rezazadeh, Mahboubeh Mashayekhi, Mahboubeh Rostami, Ali Jahanian-Najafabadi
In the current study, retinoic acid (RA) was conjugated to Pluronic F127 (PF127) through an esterification process. Mixed micelles were formed with tocopheryl polyethylene glycol 1000 (TPGS) for co-delivery of paclitaxel (PTX) and RA to the cancer cells. Mixed micelles of RA-PF127 and TPGS in different weight ratios (10:0, 7:3, 5:5, 3:7, 0:10 w/w) were prepared and physicochemical properties including, particle size, zeta potential, critical micelle concentration (CMC), drug loading content, entrapment efficiency, drug release, cellular uptake and in vitro cytotoxicity, were investigated in details...
December 13, 2017: Drug Development and Industrial Pharmacy
Eskandar Moghimipour, Farid Abedin Dorkoosh, Mohsen Rezaei, Maryam Kouchak, Jafar Fatahiasl, Kambiz Ahmadi Angali, Zahra Ramezani, Mohsen Amini, Somayeh Handali
The aim of the present research was to evaluate the impact of coating layers on release profile from enteric coated dosage forms. Capsules were coated with Eudragit FS 30D using dipping method. The drug profile was evaluated in both phosphate buffer and Hank's solutions. Utilization X-ray imaging, gastrointestinal transmission of enteric coated capsules was traced in rats. According to the results, no release of the drug was found at pH 1.2 and the extent of release drug in pH 6.8 medium was decreased by adding the coating layers...
December 13, 2017: Drug Development and Industrial Pharmacy
Zora Ćetković, Sandra Cvijić, Dragana Vasiljević
OBJECTIVE: The aims of this study were to formulate simvastatin (SV)-loaded self-microemulsifying drug delivery systems (SMEDDS), and explore the potential of these drug delivery systems to improve SV solubility, and also to identify the optimal place in the gastrointestinal (GI) tract for the release of SV using coupled in vitro/in silico approach. SIGNIFICANCE: In comparison to other published results, this study considered the extensive presystemic clearance of SV, which could significantly decrease its systemic and hepatic bioavailability if SV is delivered into the small intestine...
December 12, 2017: Drug Development and Industrial Pharmacy
Rohan K Barse, Amol A Tagalpallewar, Chandrakant R Kokare, Jaya P Sharma, Pankaj K Sharma
CONTEXT: Short residence time, poor bioavailability and poor permeability are the major problems for conventional eye drops treatment. OBJECTIVE: The aim of this article is to develop, optimize and ex vivo-in vivo investigation of brimonidine tartrate in situ gel as compare to marketed eye drops for the treatment of glaucoma. MATERIALS AND METHODS: The effect of independent variables viz. concentrations of polymers, on various dependent variables like viscosity at physiological pH and in vitro drug release were studied by using 32 factorial design...
December 12, 2017: Drug Development and Industrial Pharmacy
Guozhong Yang, Meilin He, Suohui Zhang, Man Wu, Yunhua Gao
Swellable microneedles (SMNs) are made of hydrogels and can deliver drug with controlled delivery rate by the cross-link density of the hydrogel. In this study, an acryl resin-based SMNs was developed for poorly water-soluble drugs. The making process of the SMNs is very simple and only need 60 min. The SMNs has high mechanical strength and is not easily broken. In-vitro release of SMNs-loaded model drug, granisetron base (GRB), was investigated. The results showed that 7 days controlled release of GRB was obtained when SMNs contained pore-foaming agents (1...
December 8, 2017: Drug Development and Industrial Pharmacy
Pingfei Li, Shu Wang, Haoyuan Chen, Shiming Zhang, Shihui Yu, Yuenan Li, Mengsuo Cui, Weisan Pan, Xinggang Yang
The aim of this study was to prepare and evaluate ion-activated in-situ gel ophthalmic drug delivery system based on kappa-carrageenan (KC), using acyclovir as a model drug, hydroxypropyl methylcellulose (HPMC) as the viscosity agent and hydroxypropyl-β-cyclodextrin (HP-β-CD) as the penetration enhancer. The two ternary phase diagrams exhibited the effect of K+ and Ca2+ on the sol-to-gel transition, which turned out that KC was more sensitive to K+. The optimal ophthalmic matrix (prepared from KC and HPMC) was optimized with in-vitro drug release test...
December 6, 2017: Drug Development and Industrial Pharmacy
Mohamed S El Afify, Esmat A Zein El Dein, Bakheet E M Elsadek, Mostafa A Mohamed, Sanaa A El-Gizawy
Objective The goal of this study is to improve the transdermal delivery of phosphatidylcholine (PC) via constructing a novel nanolipid vesicular system (NLVS) with high level of permeability through the stratum corneum (SC). Significance In our study, a novel drug free NLVS was developed. The system depends on PC boundary cartilage lubrication to relieve osteoarthritic pain without developing gastrointestinal problems associated with anti-inflammatory drug. Materials and methods Full 23 factorial design is applied to optimize the quality of the prepared NLVS...
December 6, 2017: Drug Development and Industrial Pharmacy
K M Dos Santos, R M Barbosa, F G A Vargas, E P de Azevedo, A C S Lins, C A Câmara, C F S Aragão, T F Moura, F N Raffin
β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2 and 1:3)...
December 5, 2017: Drug Development and Industrial Pharmacy
Veronika Debevec, Stanko Srčič, Matej Horvat
The quality by design (QbD) paradigm guides the pharmaceutical industry towards improved understanding of products and processes, and at the same time facilitates a high degree of manufacturing and regulatory flexibility throughout the establishment of the design space. This review article presents scientific, statistical and regulatory considerations in design space development. All key development milestones, starting with planning, selection of factors, experimental execution, data analysis, model development and assessment, verification, and validation, and ending with design space submission, are presented and discussed...
December 4, 2017: Drug Development and Industrial Pharmacy
Ga-Hui Oh, Joo-Eun Kim, Young-Joon Park
The purpose of this study was to develop a hydrolysis-resistant optimized oral formulation of tenofovir disoproxil (TD) using a stabilizer. To develop a stabilized TD tablet bioequivalent to the commercial TD fumarate (TDF, Viread®) tablet, TD free base was prepared and its degradation profile and stability were investigated. The TD tablet showed antiviral activity, but its absorption was limited in the intestinal tract because of premature degradation. The drug subjected to severe conditions for the stress test was catalyzed under neutral, basic, oxidative, and thermolytic conditions, whereas it was comparatively stable under acidic, photolytic, and humid states...
December 4, 2017: Drug Development and Industrial Pharmacy
Vijay S Chudiwal, Sadhana Shahi, Swapnil Chudiwal
The objective of the present study was to develop sustained release gastro-retentive (SRGR) tablet formulation of Nicardipine Hydrochloride for once-a-day dosing using quality by design (QbD) approach. Quality target product profile (QTPP) of Nicardipine HCl SRGR tablet formulation was defined and critical quality attributes (CQAs) were identified. Potential risk factors were identified using a fish bone diagram and failure mode effect analysis (FMEA) tool and screened by Plackett-Burman design and finally Nicardipine HCl SRGR tablet formulation was optimized using Box-Behnken design...
December 2, 2017: Drug Development and Industrial Pharmacy
Futoshi Shikata, Susumu Kimura, Yusuke Hattori, Makoto Otsuka
We developed a method for the optimization of dissolution properties of solid oral dosage forms manufacturing using high shear wet granulation (HSWG) by using near-infrared spectroscopy (NIRS) with chemometrics in small-scale experiments. The changes in rheology and NIR spectra of the granules were monitored to verify the granulation mechanism and determine the suitable water amount for model formulation during the HSWG. Tablets were manufactured by altering the added water amount to investigate the impact of the granulation mechanism on drug product qualities...
December 1, 2017: Drug Development and Industrial Pharmacy
Nathalie R Wingert, Natália O Dos Santos, Sarah C Campanharo, Elisa S Simon, Nadia M Volpato, Martin Steppe
OBJECTIVE: This study aimed to develop and validate an in vitro dissolution method based on in silico-in vivo data to determine whether an in vitro-in vivo relationship could be established for rivaroxaban in immediate-release tablets. SIGNIFICANCE: Oral drugs with high permeability but poorly soluble in aqueous media, such as the anticoagulant rivaroxaban, have a major potential to reach a high level of in vitro-in vivo relationship. Currently, there is no study on scientific literature approaching the development of RIV dissolution profile based on its in vivo performance...
December 1, 2017: Drug Development and Industrial Pharmacy
Nika Jordan, Jure Zakrajšek, Simona Bohanec, Robert Roškar, Iztok Grabnar
The aim of the present research is to show that the methodology of Design of Experiments can be applied to stability data evaluation, as they can be seen as multi-factor and multi-level experimental designs. Linear regression analysis is usually an approach for analyzing stability data, but multivariate statistical methods could also be used to assess drug stability during the development phase. Data from a stability study for a pharmaceutical product with hydrochlorothiazide as an unstable drug substance was used as a case example in this paper...
December 1, 2017: Drug Development and Industrial Pharmacy
Suchiwa Pan-On, Soravoot Rujivipat, Anan Ounaroon, Waree Tiyaboonchai
OBJECTIVE: To develop clay facial mask containing turmeric extract solid dispersion (TESD) for enhancing curcumin water solubility and permeability and to determine suitable clay based facial mask. METHODS: The TESD were prepared by solvent and melting solvent method with various TE to PVP K30 mass ratios. The physicochemical properties, water solubility and permeability were examined. The effects of clay types on physical stability of TESD, water adsorption and curcumin adsorption capacity were evaluated...
November 30, 2017: Drug Development and Industrial Pharmacy
Fan Yu, Fuguang Jiang, Xinhui Tang, Bochu Wang
OBJECTIVE: The deeper research of N-Octyl-N-Arginine chitosan (OACS) as intravenous delivery was characterized, cell uptake study, pharmacokinetics and biodistribution of OACS micelles (GA-OACS) were investigated. SIGNIFICANCE: Gambogic acid (GA) can inhibit the growth of various cancer cells. However, the short elimination half-life time and treatment without targeting limits its application. OACS was synthesized as delivery carrier for GA by us, but the deeper characteration of OACS, such as molecular modeling, pharmacokinetics and biodistribution et al...
November 30, 2017: Drug Development and Industrial Pharmacy
Changhai Qu, Lingling Zhang, Xueying Du, Xiaoyan Zhang, Jiao Zheng, Yunfang Zhao, Pengfei Tu
OBJECTIVE: To prepare a new nanosystem of usnic acid with higher solid content and higher bioavailability. METHODS: Usnic acid nanocrystal suspensions were prepared by the wet milling method, and then the particle size distributions and zeta potential were determined with the Nano ZS90 laser diffraction particle size analyzer. The particles morphology of UA-NCS were observed by scanning electron microscopy method. In addition, solubility and dissolution of UA-NCS in water and phosphate buffer solution were determined in vitro, analyzed by the HPLC method, and then the cellular uptake and pharmacokinetic were carried out on the Caco-2 cells and rats, analyzed by the UPLC-MS/MS method...
November 29, 2017: Drug Development and Industrial Pharmacy
N C Loka, K K Saripella, C Pinto, S H Neau
Objective Fine particle ethylcellulose (FPEC) or poly(ethylene oxide) (PEO) addition to a Kollidon CL-SF was investigated to address low yield and poor sphericity in extruded-spheronized pellets. Significance The success of crospovidone as a diluent in extrusion-spheronization was dependent on a small particle size of the polymer. FPEC aided production of rugged and spherical pellets using a large particle size grade, Polyplasdone® XL. PEO acted as an extrusion-spheronization aid when ethylcellulose was the diluent...
November 28, 2017: Drug Development and Industrial Pharmacy
Linda Belhadji, Abdelkader HadjSadok, Nadji Moulai-Mostefa
The aim of this study was to prepare and evaluate calcium-free sustained release drug delivery systems, based on the in-situ gelation of oral suspensions containing chitosan, sodium alginate and Ranitidine as drug model. The combined effects of polymer concentrations and their interactions on the rheological characteristics of both gels and suspensions and, on the kinetics of drug release were evaluated by using a central composite face-centered (CCF) design. Rheological analysis showed that suspensions were potentially stable, with a viscosity increased by 1000 times compared to that of water...
November 24, 2017: Drug Development and Industrial Pharmacy
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