Incorporation of Lipophilic Drugs in Sugar Glasses by Lyophilization using a Mixture of Water and Tertiary Butyl Alcohol as Solvent

Drooge, Dirk Jan van; Hinrichs, Wouter L. J.; Frijlink, Henderik W.

doi:10.1002/jps.10590

Cited by 65 publications

(30 citation statements)

References 45 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Some branches were connected during growth because of the anisotropic growth of ice, thereby forming the connections between pores. Previous experiments were conducted using TBA and revealed that TBA can alter the crystallization behavior of ice [21], [22]. The present study also indicated that the ice morphology exhibited an arbitrary shape at higher TBA concentrations.…”

Section: A Sponge Morphologysupporting

confidence: 74%

See 1 more Smart Citation

Preparation Chitosan Lactate-Hyaluronate Sponges with Unidirectional Porous Structure and Their Potential Use as Wound Dressings

Lai¹

2014

IJBBB

View full text Add to dashboard Cite

Abstract-Sponges were prepared from lactic acid-grafted chitosan (LCH) and hyaluronate (HA) to develop potential materials for wound dressing. Sponges with different microstructures can be obtained in a vertical temperature-controlled device and in an aluminum vessel. The morphology and permeability properties, including porosity, water permeability, gas permeability, water adsorption and in vitro biodegradation of two types of sponges were compared in detail. Sponges with microtubule-oriented structure can be obtained in a vertical temperature-controlled device with TBA (tertiary butyl alcohol). These sponges exhibited an applicable water permeation rate of 577 g•m -2 •day -1 and higher air permeability tensor of 3 × 10 -12 . The sponges with random micropores can be prepared in an aluminum vessel. These sponges exhibited a water permeation rate and an air permeability tensor of 452 g•m -2 •day -1 and 1.8 × 10 -14 g•m -2 •day -1 , respectively. These results also indicated that TBA greatly affected the microstructure of the resulting sponges. A parallel orientation of the pore structure resulted in higher porosity and higher water adsorption capacity than random pores. After lactic acid was grafted, the crystallinity of chitosan decreased and water solubility increased, causing rapid lysozymatic degradation of chitosan lactate-HA sponges. The resulting sponges exhibited high water content, gas permeability and appropriate water permeation; such sponges could easily be applied and removed. These properties indicated that these materials are highly applicable as wound dressing.Index Terms-Chitosan lactate, hyaluronate, sponge.

show abstract

Section: A Sponge Morphologysupporting

confidence: 74%

“…It is miscible with water in any proportion and could be removed rapidly and completely by freeze-drying because of its high vapor pressure and high melting point. Moreover, the toxicity of it is low [21]. The research of Kasraian revealed that TBA can have great effect on the crystal habit of ice [22].…”

Section: Chen Laimentioning

confidence: 99%

Preparation Chitosan Lactate-Hyaluronate Sponges with Unidirectional Porous Structure and Their Potential Use as Wound Dressings

Lai¹

2014

IJBBB

View full text Add to dashboard Cite

show abstract

“…These systems consist of amorphous carriers and the drug can be either molecularly dispersed or form an amorphous precipitate into its carrier, which can possibly crystallize upon time. Examples of carriers that favour the formation of glass solutions are sugars, such as dextrose, fructose, galactose, trehalose, sucrose, and different types of inulin, [53][54][55] or amorphous polymers such as PVP, Polyvinylpyrrolidone-co-vinylacetate (PVPVA) and HPMC. The earliest examples of such glassy dispersions were prepared with PVP [56] and currently this class represents the most intensively studied and applied solid dispersion system.…”

Section: Glass Solutionsmentioning

confidence: 99%

Review: physical chemistry of solid dispersions

2009

View full text Add to dashboard Cite

Objectives With poorly soluble drug candidates emerging in the drug discovery pipeline, the importance of the solid dispersion formulation approach is increasing. This strategy includes complete removal of drug crystallinity, and molecular dispersion of the poorly soluble compound in a hydrophilic polymeric carrier. The potential of this technique to increase oral absorption and hence bioavailability is enormous. Nevertheless, some issues have to be considered regarding thermodynamic instability, as well in supersaturated solutions that are formed upon dissolution as in the solid state. Key findings After a brief discussion on the historical background of solid dispersions and their current role in formulation, an overview will be given on the physical chemistry and stability of glass solutions as they form supersaturated solutions, and during their shelf life. Conclusions Thorough understanding of these aspects will elicit conscious evaluation of carrier properties and eventually facilitate rational excipient selection. Thus, full exploitation of the solid dispersion strategy may provide an appropriate answer to drug attrition due to low aqueous solubility in later stages of development.

show abstract

“…Tablets prepared by this technique have usually a light mass, with a very high specific surface area and a very porous open matrix network into which saliva rapidly moves to disintegrate lyophilized mass after it is placed in the mouth (29)(30).…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

An in vitro and in vivo comparative study of directly compressed solid dispersions and freeze dried sildenafil citrate sublingual tablets for management of pulmonary arterial hypertension

Zayed¹,

Kamel²,

Shukr³

et al. 2012

Acta Pharmaceutica

View full text Add to dashboard Cite

Pulmonary arterial hypertension (PAH) is a life-threatening disease. It is characterized by elevations in the pulmonary arterial pressure and pulmonary vascular resistance, leading to right ventricular failure and premature death (1). Treatments of PAH include medications, oxygen, and lung transplant. The main medications for pulmonary 411 Acta Pharm. 62 (2012) Original research paper DOI: 10.2478/v10007-012-0027-9 An in vitro and in vivo comparative study of directly compressed solid dispersions and freeze dried sildenafil citrate sublingual tablets for management of pulmonary arterial hypertension Sildenafilcitrate (SILD) orodispersable sublingual tablets (ODSTs) have been developed using two comparative techniques for improving their oral disintegration, dissolution and bioavailability in order to manage acute attacks of pulmonary arterial hypertension (PAH). The techniques employed were direct compression of SILD-poloxamer 188 solid dispersions (SDs) and freeze drying using various excipients. The physicochemical and solid--state properties, as well as the dissolution behavior of the tablets were evaluated. Moreover, SILD bioavailability in human volunteers from the prepared ODSTs was compared to that of the conventional oral tablet. Incorporation of SD of poloxamer188 in sublingual tablets together with Pharmaburst using the direct compression technique enhanced the extent and dissolution rate of SILD with 100 % of drug being dissolved after 7 minutes. However, the lyophilization process was superior in enhancing dissolution and 100 % of SILD was dissolved after only one minute. Moreover, the in vivo study showed that the AUC 0-12 of lyophilized tablets was significantly higher than that of directly compressed tablets, with bioavailability values of 159.81 and 140.85 %, respectively, compared to the commercial oral product.Keywords: sildinafil, orodispersable sublingual tablets, pulmonary arterial hypertension, poloxamer 188, solid dispersions, direct compression, freeze drying * Correspondence; e-mail: amany.kamel@yahoo.com Unauthenticated Download Date | 5/8/18 9:59 AM hypertension include: endothelin receptor antagonists, prostacyclin analogs and phosphodiesterase type 5 inhibitors (PDE5Is).Sildenafil citrate (SILD), a selective inhibitor of cGMP specific phosphodiesterase type 5 (PDE5), was approved by the FDA for the treatment of PAH in 2005. It improves cardiovascular diseases and is useful for patients with congestive heart failure as well as secondary pulmonary hypertension. It relaxes the arterial wall, and hence decreases the pulmonary arterial resistance and pressure. This improves symptoms of right-sided heart failure by reducing the workload of the right ventricle of the heart. Since PDE5 is primarily distributed within the arterial wall smooth muscle of the lungs and penis, SILD acts selectively in both of these areas without inducing vasodilation in other areas of the body,which is considered to be an advantage of SILD(2-3). SILD decreases myocardial apoptosis, fibrosis, and hypertrop...

show abstract

Incorporation of Lipophilic Drugs in Sugar Glasses by Lyophilization using a Mixture of Water and Tertiary Butyl Alcohol as Solvent

Cited by 65 publications

References 45 publications

Preparation Chitosan Lactate-Hyaluronate Sponges with Unidirectional Porous Structure and Their Potential Use as Wound Dressings

Preparation Chitosan Lactate-Hyaluronate Sponges with Unidirectional Porous Structure and Their Potential Use as Wound Dressings

Review: physical chemistry of solid dispersions

An in vitro and in vivo comparative study of directly compressed solid dispersions and freeze dried sildenafil citrate sublingual tablets for management of pulmonary arterial hypertension

Contact Info

Product

Resources

About