Nanosizing--oral formulation development and biopharmaceutical evaluation.

Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: basic approaches and practical applications.

This literature review is a compilation of the composition and, in most cases, the preparation instructions for simulated biological fluids that may be used as dissolution media in the evaluation of dissolution profiles and amount of drug released from pharmaceutical dosage forms. The use of simulated biological fluids can give a better understanding of the release mechanisms and possible in vivo behavior of a product and enhance the predictive capability of the dissolution testing. A summary of the major characteristics of the most used routes of administration that may affect dissolution and absorption of drug substances is presented. The routes and simulated biological fluids covered by this review are: • Parenteral: simulated body fluid and simulated synovial fluid. • Oral: fasted-state simulated gastric fluid, fed-state simulated gastric fluid, fasted-state simulated intestinal fluid, fed-state simulated intestinal fluid, simulated colonic fluid, fasted-state simulated colonic fluid, and fed-state simulated colonic fluid. • Buccal and sublingual: simulated saliva. • Pulmonary: simulated lung fluid. • Vaginal: simulated vaginal fluid and simulated semen. • Ophthalmic: simulated tears. Simulated sweat is also included. Some examples of how these simulated biological fluids are used to evaluate dosage forms are included in each route of administration. INTRODUCTION Until some decades ago, most of the conventional pharmaceutical dosage forms were essentially injections, oral formulations (solutions, suspensions, tablets, and capsules), topical creams, and ointments. With the progress of drug delivery technology, novel dosage forms have been developed to overcome the problems associated with conventional drug delivery. Research has been directed toward the use of alternatives to the parenteral route for drugs that cannot be delivered orally. Potential alternative portals of drug entry to the systemic circulation include buccal, sublingual, nasal, pulmonary, and vaginal routes, among others. These routes of administration are also used for the local delivery of drugs directly to the site of action, with consequent reduction in the dose needed to produce a pharmacological effect, eliminating problems related to first-pass metabolism and possibly minimizing systemic side effects (1). An important application of dissolution testing is the prediction of in vivo performance of pharmaceutical dosage forms. The media typically used for quality control dissolution testing do not represent all aspects of the physiological conditions of the most used routes of administration and do not allow correlation with in vivo data. Prediction of dosage form performance in the site where most of the absorption occurs requires adequate simulation of the in vivo conditions. This paper describes some characteristics of the parenteral, oral, buccal and sublingual, pulmonary, ophthalmic, and vaginal routes that are important to consider when developing simulated media. A compilation of the composition and preparation of several simulated biological fluids, including simulated sweat, with potential use as dissolution media is presented. PARENTERAL ROUTE The most used routes of injection are intramuscular, intravenous, and subcutaneous and are normally associated with short-term effects. Novel implant devices that can adequately control drug release and provide a prolonged duration of effect have been developed (1). To evaluate the in vitro drug release from these dosage forms, the dissolution medium should have ion concentrations almost equal to those of the human plasma. Table 1 describes the ionic composition of simulated body fluid (SBF) and human blood plasma. Simulated body fluid was developed initially to evaluate the surface structural changes of glass-ceramics used to manufacture artificial vertebrae, ileum, tooth roots (2), and bioactive material used to repair hard tissues such as artificial middle-ear bone and maxillofacial implants (3). This simulated body fluid was prepared using the reagents listed in Table 2. These reagents were added to 700 mL of water in the order given in Table 2, one by one, after each reagent was completely dissolved. The pH was adjusted to 7.4 with 1 M *Corresponding author. diss-18-03-03.indd 15 8/31/2011 3:22:15 PM dx.doi.org/10.14227/DT180311P15

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Simulated Biological Fluids with Possible Application in Dissolution Testing

Supersaturating Drug Delivery Systems: The Answer to Solubility-Limited Oral Bioavailability?

https://cyberleninka.org/article/n/380530.pdf

Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability

Manufacture and characterization of mucoadhesive buccal films.

Hot-Melt Extrusion for Enhanced Delivery of Drug Particles

Development of a standardized dissolution test method for inhaled pharmaceutical formulations

High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers.

Solid dispersions containing various stabilizers and tacrolimus (TAC) prepared by an Ultra-rapid Freezing (URF) process were investigated to determine the effect on their ability to form supersaturated solutions in aqueous media and on enhancing transport across biological membranes. The stabilizers included poly(vinyl alcohol; PVA), poloxamer 407 (P407), and sodium dodecyl sulfate (SDS). In vivo absorption enhancement in rats was also investigated. Dissolution studies were conducted at supersaturated conditions in both acidic media for 24 h and at delayed release (enteric) conditions to simulate intestinal transit. The rank order of C/Ceqmax in the dissolution studies at acidic conditions was URF-P407 > URF-SDS > Prograf® (PRO) > URF-PVA:P407. For C/Ceqmax under enteric conditions, the order was URF-SDS > PRO > URF-PVA:P407 > URF-P407, and for the extent of supersaturation (AUC) in acidic and pH shift conditions it was URF-SDS>PRO>URF-PVA:P407>URF-P407. The pharmacokinetic data suggests URF-P407 had the greatest absorption having higher C
 max with a 1.5-fold increase in AUC compared to PRO. All URF compositions had a shorter T
 max compared to PRO. The nanostructured powders containing various stabilizing polymers formed by the URF process offer enhanced supersaturation characteristics leading to increased oral absorption of TAC.

Jason T. McConville

Papers

Manufacture and characterization of mucoadhesive buccal films.

Hot-Melt Extrusion for Enhanced Delivery of Drug Particles

Development of a standardized dissolution test method for inhaled pharmaceutical formulations

High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers.

Effect of Stabilizer on the Maximum Degree and Extent of Supersaturation and Oral Absorption of Tacrolimus Made By Ultra-Rapid Freezing