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"solid dispersion"

Ling Lin, Guilan Quan, Tingting Peng, Zhengwei Huang, Vikramjeet Singh, Ming Lu, Chuanbin Wu
Dry powder for inhalation (DPI) is an attractive approach for the treatment of local lung diseases. However, the application of drugs with poor water solubility is often limited due to the dissolution obstacles in the fluid layer of the lung lining. In this study, fine solid-crystal suspension (FSCS) was proposed as a solvent-free method to improve the solubility of a drug with poor solubility (itraconazole) and achieve high deposition efficiency simultaneously. The FSCS, in which the crystalline drug particle was highly dispersed in the crystalline excipient, was initially prepared as drug-excipient extrudate by hot melt extrusion, followed by jet milling into fine particles...
September 10, 2017: International Journal of Pharmaceutics
Saeed Ghanbarzadeh, Hadi Valizadeh, Shadi Yaqoubi, Arash Asdagh, Hamed Hamishehkar
Background Tablets and capsules are the most accepted and widely used solid dosage forms in the medical therapy. Flow property of the powders is playing a key role in the various pharmaceutical fields especially in the fomulation of tablets and capsules. The high hygroscopic crystalline structure of anhydrous Divalproex sodium (DVX) makes it to be appear as waxy white flakes with almost no powder flowability which cause serious problems during the tabletting and capsule filling procedures. Purpose The main objective of this study was to improve the flowability of DVX powder...
September 12, 2017: Drug Research
Noriko Ogawa, Tomoki Hiramatsu, Ryohei Suzuki, Ryohei Okamoto, Kohei Shibagaki, Kosuke Fujita, Chisato Takahashi, Yoshiaki Kawashima, Hiromitsu Yamamoto
The aim of this study was to prepare and characterize solid dispersion particles with a novel amphiphilic polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer, as a water-soluble carrier. Solid dispersion particles were prepared by hot-melt extrusion and spray drying. Indomethacin (IMC) was used as a model comprising drugs with low solubility in water and d-mannitol (MAN) was used as an excipient. The physicochemical properties of prepared particles were characterized by scanning electron microscopy, thermal analysis, powder X-ray diffraction (PXRD) analysis, FTIR spectra analysis, and drug release studies...
September 8, 2017: European Journal of Pharmaceutical Sciences
Walter Ferreira da Silva Júnior, Jonas Gabriel de Oliveira Pinheiro, Danielle Lima Bezerra de Menezes, Natan Emanuell de Sobral E Silva, Patrícia Danielle Oliveira de Almeida, Emerson Silva Lima, Valdir Florêncio da Veiga Júnior, Eduardo Pereira de Azevedo, Ádley Antonini Neves de Lima
α,β Amyrin (ABAM) is a natural mixture of pentacyclic triterpenes that has shown a variety of pharmacological properties, including anti-inflammatory effect. ABAM is isolated from Burseraceae oilresins, especially from the Protium species, which is commonly found in the Brazilian Amazon. This work aimed to develop solid dispersions (SD) of ABAM with the following hydrophilic polymers: polyvinylpyrrolidone (PVP-K30), polyethylene glycol (PEG-6000) and hydroxypropylmethylcellulose (HPMC). The SDs were prepared by physical mixture (PM), kneading (KND) and rotary evaporation (RE) methods...
September 9, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Li Ming Lim, The-Thien Tran, Wean Sin Cheow, Kunn Hadinoto
The solubility enhancement afforded by amorphous drug nanoparticles was demonstrated in several studies to be superior to the traditional amorphization approach by microscale amorphous solid dispersion (or micro ASD in short). A closer look at these studies, however, revealed that they were performed using a very limited number of poorly-soluble drug models (i.e. itraconazole and cefuroxime). Herein we aimed to re-examine the solubility enhancement and physical stability of amorphous nanoparticles relative to that of the micro ASD using a different poorly-soluble drug model, i...
September 6, 2017: European Journal of Pharmaceutical Sciences
Magdalena Münster, Corinna Schoch, Carsten Schmidt, Jörg Breitkreutz
The taste of pharmaceuticals is of particular importance as it highly affects the compliance of patients, especially for patient groups like children. In view of oral solid dosage forms, various taste masking techniques can be applied encapsulating the active pharmaceutical ingredient (API) to prevent the interaction with the taste buds. Despite a delayed drug release in saliva, an immediate drug release in gastrointestinal media is desirable for efficient drug absorption. This combinatory approach is of particular interest for poorly soluble drugs still demonstrating an aversive, bitter taste, e...
September 5, 2017: European Journal of Pharmaceutical Sciences
Hanah Mesallati, Lidia Tajber
PURPOSE: To improve the pharmaceutical properties of amorphous ciprofloxacin (CIP) succinate salts via formulation as polymer/amorphous salt solid dispersions (ASSDs). METHODS: ASSDs consisting of an amorphous CIP/succinic acid 1:1 or 2:1 salt dispersed in PVP or Soluplus were produced by spray drying and ball milling. The solid state characteristics, miscibility, stability, solubility and passive transmembrane permeability of the ASSDs were then examined. RESULTS: The ASSDs had higher glass transition and crystallization temperatures than the corresponding amorphous succinate salts, and were also more stable during long-term stability studies...
September 5, 2017: Pharmaceutical Research
Hale Çigdem Arca, Laura I Mosquera-Giraldo, Durga Dahal, Lynne S Taylor, Kevin J Edgar
Drug therapy has been instrumental in prolonging the lives of patients infected by human immunodeficiency virus (HIV). In order to combat development of resistance, therapies involving three or more drugs in combination are recommended by the World Health Organization (WHO) to suppress HIV and prevent development of acquired immune deficiency syndrome (AIDS). It is desirable for multidrug combinations to be co-formulated into single dosage forms where possible, to promote patient convenience and adherence to dosage regimens, for which when amorphous solid dispersion (ASD) is particularly well-suited...
September 5, 2017: Molecular Pharmaceutics
Daisuke Tsunashima, Kazunari Yamashita, Ken-Ichi Ogawara, Kazuhiro Sako, Tadashi Hakomori, Kazutaka Higaki
OBJECTIVES: We aimed to prepare a once-daily modified-release oral formulation of tacrolimus by utilizing an extended-release granules (ERG). METHODS: Extended-release granules were prepared using ethylcellulose (EC), hydroxypropylmethylcellulose (HPMC) and lactose via a solvent evaporation method with ethanol. Physicochemical and biopharmaceutical studies were performed to determine the formulation with optimum release profile of tacrolimus from ERG. KEY FINDINGS: Tacrolimus existed in an amorphous state in ERG...
September 5, 2017: Journal of Pharmacy and Pharmacology
Taehoon Sim, Chaemin Lim, Jun Won Lee, Dong Wuk Kim, Youngsam Kim, Minsoo Kim, Seungmok Choi, Han-Gon Choi, Eun Seong Lee, Kil-Soo Kim, Wonku Kang, Kyung Taek Oh
OBJECTIVES: Solid dispersion formulations have attracted attention to improve solubility and bioavailability of water-insoluble drugs. In this study, the variation of solubility and bioavailability by different preparation methods were studied using itraconazole (ITZ) solid dispersions. METHODS: Itraconazole solid dispersions were prepared by a solvent-controlled precipitation method (SCPM) using HPMCAS-LF, HCl antisolvent or a spray-drying method (SDM) for comparison...
September 5, 2017: Journal of Pharmacy and Pharmacology
Riikka Laitinen, Korbinian Löbmann, Holger Grohganz, Petra Priemel, Clare J Strachan, Thomas Rades
Amorphous solid dispersions (ASDs) are probably the most common and important supersaturating drug delivery systems for the formulation of poorly water-soluble compounds. These delivery systems are able to achieve and maintain a sustained drug supersaturation which enables improvement of the bioavailability of poorly water-soluble drugs by increasing the driving force for drug absorption. However, ASDs often require a high weight percentage of carrier (usually a hydrophilic polymer) to ensure molecular mixing of the drug in the carrier and stabilization of the supersaturated state, often leading to high dosage volumes and thereby challenges in the formulation of the final dosage form...
September 1, 2017: International Journal of Pharmaceutics
Christian Luebbert, Gabriele Sadowski
Active Pharmaceutical Ingredients (APIs) are often dissolved in polymeric matrices to control the gastrointestinal dissolution and to stabilize the amorphous state of the API. During the pharmaceutical development of new formulations, stability studies via storage at certain temperature and relative humidity (RH) have to be carried out to verify the long-term thermodynamic stability of these formulations against unwanted recrystallization and moisture-induced amorphous-amorphous phase separation (MIAPS). This study focuses on predicting the MIAPS of API/polymer formulations at elevated RH...
August 31, 2017: International Journal of Pharmaceutics
Clara Correa-Soto, Niraj S Trasi, Paul D Schmitt, Yongchao Su, Zhen Liu, Elise Miller, Narayan Variankaval, Patrick J Marsac, Garth J Simpson, Lynne S Taylor
Various techniques have been used to detect crystallization in amorphous solid dispersions (ASD). However, most of these techniques do not enable the detection of very low levels of crystallinity (<1%). The aim of the current study was to compare the sensitivity of second harmonic generation (SHG) microscopy with powder X-ray diffraction (XRPD) in detecting the presence of crystals in low drug loading amorphous solid dispersions. Amorphous solid dispersions of the poorly water soluble compounds, flutamide (FTM, 15wt...
August 24, 2017: Journal of Pharmaceutical and Biomedical Analysis
Raman Dhivya, Jothi Ranjani, Patrick K Bowen, Jeyaprakash Rajendhran, Jeyanthinath Mayandi, Jamespandi Annaraj
Although curcumin is efficient in killing cancer cells, its poor water solubility and assocaited inadequate bioavailability remain major limitations to its therapeutic application. The formulation of curcumin micellar nanoparticles (NPs) encapsulated with a biodegradable polymer promises to significantly improve curcumin's solubility, stability, and bioavailability. The past decade has witnessed the development of nanoscale curcumin delivery systems: curcumin-loaded liposomes or nanoparticles, self-microemulsifying drug delivery systems (SMEDDS), cyclodextrin inclusions, solid dispersions, nanodisks, and nanotubes...
November 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
Ting Feng, Yumeng Wei, Robert J Lee, Ling Zhao
Curcumin (CUR) is a yellow polyphenolic compound derived from the plant turmeric. It is widely used to treat many types of diseases, including cancers such as those of lung, cervices, prostate, breast, bone and liver. However, its effectiveness has been limited due to poor aqueous solubility, low bioavailability and rapid metabolism and systemic elimination. To solve these problems, researchers have tried to explore novel drug delivery systems such as liposomes, solid dispersion, microemulsion, micelles, nanogels and dendrimers...
2017: International Journal of Nanomedicine
Ranjit Prasad Swain, Bharat Bhusan Subudhi
This study was undertaken to improve solubility and bioavailability of nateglinide by preparation of stable self-emulsifying solid dispersions (SESDs). The influence of semicrystalline polymers (poloxamer 407, gelucire 50/13) and method of preparation on dissolution behaviour, in vivo performance and stability of nateglinide SESDs were investigated. After optimization, SESDs were prepared at 1:5 weight ratio of nateglinide and polymer individually. All the SESDs were characterised by fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction and scanning electron microscopy...
August 28, 2017: Drug Development and Industrial Pharmacy
Tian Xie, Wei Gao, Lynne S Taylor
The purpose of this work was to evaluate the impact of polymer(s) on the dissolution rate, supersaturation and precipitation of indomethacin amorphous solid dispersions (ASD), and to understand the link between precipitate characteristics and redissolution kinetics. The crystalline and amorphous solubilities of indomethacin were determined in the absence and presence of hydroxypropylmethyl cellulose (HPMC) and/or Eudragit (®) EPO to establish relevant phase boundaries. At acidic pH, HPMC could maintain supersaturation of the drug by effectively inhibiting solution crystallization while EPO increased both the crystalline and amorphous solubility of the drug, but did not inhibit crystallization...
August 24, 2017: International Journal of Pharmaceutics
Benchawan Chamsai, Sontaya Limmatvapirat, Srisagul Sungthongjeen, Pornsak Sriamornsak
CONTEXT: Low bioavailability of orally manidipine (MDP) is due to its low water solubility. OBJECTIVE: The objective of this study was to increase the solubility and bioavailability of MDP by fabricating ternary solid dispersion (tSD) with D-α-tocopherol polyethyleneglycol-1000-succinate and copovidone. METHODS: In this study, solid ternary phase diagram was applied in order to check the homogeneity of tSD prepared by melting and solidifying with dry ice...
August 24, 2017: Drug Development and Industrial Pharmacy
Wenjun Huang, Taraknath Mandal, Ronald G Larson
We recently developed coarse-grained (CG) force fields for hydroxypropyl methylcellulose acetate succinate (HPMCAS) polymers and the model drug molecule phenytoin, and a continuum transport model to study the polymer-drug nanostructures presented during a dissolution test after solvation of solid dispersion particles. We model the polymer-drug interactions that contribute to suppression of drug aggregation, release, and crystal growth during the dissolution process, and we take these as indicators of polymer effectiveness...
September 5, 2017: Molecular Pharmaceutics
Johan Wendelboe, Matthias Manne Knopp, Fauzan Khan, Nabil Chourak, Thomas Rades, René Holm
The present study investigated the influence of in vitro dissolution conditions on the in vivo predictability of an amorphous solid dispersion of celecoxib (CCX) in the pH-sensitive polymer Eudragit(®) S 100. Different doses of a 25:75w/w% CCX:Eudragit(®) S 100 amorphous solid dispersion (CCX:EUD) were investigated. During in vitro dissolution a significant effect of the pH of the dissolution media on the release of CCX was observed. In fasted state simulated intestinal fluid (FaSSIF) pH 6.5, the release of CCX from the amorphous solid dispersion was comparable to that of crystalline CCX and lower than that of amorphous CCX whereas in FaSSIF pH 7...
August 18, 2017: International Journal of Pharmaceutics
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