Formulating Poorly Water Soluble Drugs pptx

[...]... a wide range of drugs via oral delivery 1 Route-Specific Challenges in the Delivery of Poorly Water- Soluble Drugs 17 One of the main challenges in the delivery of poorly soluble drugs via the pulmonary and parenteral route is the limited number of approved excipients The development of novel excipients may offer new opportunities and enable more effective delivery of poorly soluble drugs However, the... vivo when poorly soluble drugs are administered via various routes of administration Poorly soluble drugs that are delivered orally commonly result in low bioavailability and high intersubject variability Additionally, poorly soluble compounds are known to have a higher predisposition for interaction with food resulting in high fast/fed variability (Gu et al 2007) In order to make low solubility drugs. .. Delivery of Poorly Water- Soluble Drugs Stephanie Bosselmann and Robert O Williams III Abstract Poor aqueous solubility of new chemical entities presents various challenges in the development of effective drug-delivery systems for various delivery routes Poorly soluble drugs that are delivered orally commonly result in low bioavailability and are subject to considerable food effects In addition, poorly soluble. .. (ultrasonic nebulizers) In the case of poorly water- soluble drugs, solutions may be obtained by employing different solubilizing agents such nonaqueous solvents or cyclodextrins Otherwise suspensions of micronized or even nanosized material which will show enhanced dissolution rates may be employed Solubilization and subsequent nebulization of poorly water- soluble drugs in the form of nonaqueous solutions... Production Jasmine M Rowe and Keith P Johnston 501 13 Emerging Technologies to Increase the Bioavailability of Poorly Water- Soluble Drugs Justin R Hughey and James W McGinity 569 Scientific and Regulatory Considerations for Development and Commercialization of Poorly Water- Soluble Drugs Zedong Dong and Hasmukh Patel 603 Index 631 14 Contributors Michael P Boquet Global Packaging... physiologically 1 Route-Specific Challenges in the Delivery of Poorly Water- Soluble Drugs 13 compatible with lung tissue in terms of pH, tonicity, and immunogenic potential, or of endogenous nature in order to avoid airway hyper-responsiveness, spasticity, or inflammation (Tolman and Williams 2009; Pilcer and Amighi 2010) Several formulations of poorly soluble drugs for pulmonary delivery have been developed and,... the solubilized formulation Finally, successful formulation design of poorly soluble drugs indented for pulmonary administration is mainly hindered by the limited number of excipients generally recognized as safe for this route of delivery This chapter reviews the specific challenges faced in the delivery of poorly water- soluble drugs for oral, parenteral, and pulmonary delivery 1.2 Oral Route of Administration... 2006) As cyclodextrins have shown to be valuable excipients in the delivery of poorly soluble drugs via the oral or parenteral route, great interest has been created to extent their use into pulmonary delivery as well Several studies have demonstrated that aqueous solutions containing inclusion complexes of poorly water- soluble drugs and cyclodextrins can be successfully nebulized with droplet sizes suitable... hypersensitivity reactions characterized by dyspnea, flushing, rash, chest pain, tachycardia, and hypotension (ten Tije et al 2003) Paclitaxel, a poorly water- soluble molecule with antineoplastic activity, was originally 1 Route-Specific Challenges in the Delivery of Poorly Water- Soluble Drugs 11 formulated in form of a nonaqueous solution for i.v infusion (Taxol®), in which the drug is solubilized in a mixture of Cremphor... excipients accepted for i.v administration is, however, rather limited which presents a common challenge for all formulation strategies mentioned 1.3.1 Challenges in Parenteral Delivery of Poorly Water- Soluble Drugs Poorly soluble weak acids or bases may be solubilized by pH modification of the solution to be administered Yet, if the drug is characterized by very low solubility, pH-adjustment to extreme values . Delivery of Poorly Water- Soluble Drugs 1 Stephanie Bosselmann and Robert O. Williams III 2 Optimizing the Formulation of Poorly Water- Soluble Drugs 27 Kevin. development with poorly water- soluble molecules. The volume begins with an analysis of the various challenges faced in the deliv- ery of poorly water- soluble