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Passage 1 (Questions 1 - 5)Oral drug delivery systems are limited by the short gastrointestinal transit time, leading to low bioavailability. Drug delivery systems that are able to retain the dosage form in the stomach are needed. Research into floating drug delivery systems (FDDS) may satisfy this need.FDDS can be approached by either effervescent or non-effervescent techniques. Ideal effervescent techniques achieve floating duration times greater than 16 hours in the stomach. Effervescent FDDS incorporate gas-generating agents, which provide buoyancy. Newer research focuses on non-effervescent systems, where the swelling of polymers joined to the drug entraps air within the polymeric matrix, providing buoyancy to the dosage form.A study was performed on the antidiabetic drug sulfonylurea glipizide. The drug and one of three polymers were mixed in a mortar according to the ratios described in Table 1. A drop of water was added, and the mixture was kneaded until a homogeneous paste was obtained. The mixture was then placed in an oven at 50°C for 30 min to remove water. The compound was then compressed into tablets which served as the basis for drug release and buoyancy measurements.Table 1 The density of glipizide, the three polymers, and the drug to polymer ratio used in each trialTo test in vitro drug release of solid dispersions, the tablets were placed into dissolution vessels containing 900 mL of 0.1 M HCl. Dissolution studies were carried out for one hour, with samples withdrawn at predetermined intervals. Drug concentrations were assayed using HPLC methods. The dissolution experiments were carried out in triplicate, and the results are shown in Figure 1. In vitro buoyancy was also tested. Tablets were placed in a vessel containing 500 mL of 0.1 M HCl. The time taken for the tablet to rise to the surface of the dissolution media (floating lag time) and total duration that the tablet remained on the surface (total floating time) were recorded. Figure 1 Drug release as a function of time and pill compositionThe Ksp for glipizide-cyclodextrin in a chyme solution at 37º C was determined to be 5.8 x 10-4. Increased solubility of drug dispersions may be achieved by wetting. This can be accomplished by using hydrophilic polymers, or by decreasing the polymer size.(Note: all pills for the above trials have the same volume.)

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Passage 1 (Questions 1 - 5)Oral drug delivery systems are limited by the short gastrointestinal transit time, leading to low bioavailability. Drug delivery systems that are able to retain the dosage form in the stomach are needed. Research into floating drug delivery systems (FDDS) may satisfy this need.FDDS can be approached by either effervescent or non-effervescent techniques. Ideal effervescent techniques achieve floating duration times greater than 16 hours in the stomach. Effervescent FDDS incorporate gas-generating agents, which provide buoyancy. Newer research focuses on non-effervescent systems, where the swelling of polymers joined to the drug entraps air within the polymeric matrix, providing buoyancy to the dosage form.A study was performed on the antidiabetic drug sulfonylurea glipizide. The drug and one of three polymers were mixed in a mortar according to the ratios described in Table 1. A drop of water was added, and the mixture was kneaded until a homogeneous paste was obtained. The mixture was then placed in an oven at 50°C for 30 min to remove water. The compound was then compressed into tablets which served as the basis for drug release and buoyancy measurements.Table 1 The density of glipizide, the three polymers, and the drug to polymer ratio used in each trialTo test in vitro drug release of solid dispersions, the tablets were placed into dissolution vessels containing 900 mL of 0.1 M HCl. Dissolution studies were carried out for one hour, with samples withdrawn at predetermined intervals. Drug concentrations were assayed using HPLC methods. The dissolution experiments were carried out in triplicate, and the results are shown in Figure 1. In vitro buoyancy was also tested. Tablets were placed in a vessel containing 500 mL of 0.1 M HCl. The time taken for the tablet to rise to the surface of the dissolution media (floating lag time) and total duration that the tablet remained on the surface (total floating time) were recorded. Figure 1 Drug release as a function of time and pill compositionThe Ksp for glipizide-cyclodextrin in a chyme solution at 37º C was determined to be 5.8 x 10-4. Increased solubility of drug dispersions may be achieved by wetting. This can be accomplished by using hydrophilic polymers, or by decreasing the polymer size.(Note: all pills for the above trials have the same volume.)

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