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Biopharmaceutical evaluation of a tablet dosage form made from ethyl cellulose encapsulated aspirin particles.

Ethyl cellulose encapsulated aspirin particles, suitable for preparation of direct compression tablets were prepared by the solvent evaporation method. Ethyl acetate was used as a solvent for the polymer in combination with a saturated solution of aspirin as the dispersing medium to prevent partitioning and drug loss. This resulted in a high yield of free-flowing, non-aggregated particles. In vitro-in vivo evaluations of the experimental aspirin tablets (made by direct compression of ethyl cellulose encapsulated particles) and three different commercial aspirin products (a conventional tablet, a timed-release tablet, and a timed-release caplet) were undertaken. Comparison of the dissolution in acidic media at pH 1.2 showed different release profiles for these products. While the conventional tablet and the timed-release caplet showed the highest and the lowest rate of release, respectively; the timed-release tablet and the experimentally made tablet revealed an intermediate rate and very similar release profiles. The cumulative urinary excretion data collected in a complete crossover study, using five healthy subjects further indicated that the experimental tablet has an in vivo availability identical to that of the timed-release tablet.

Adult↗

Sustained-release dosage form of phenylpropanolamine hydrochloride (3). Application of factorial design.

In this study a 2(2) factorial design has been applied to the evaluation of dissolution characteristics of phenylpropranolamine hydrochloride (PPA.HCl) from tableted microcapsules. The kinetic model according to the Rosin-Rimmler-Sperling-Bennet-Weillbull (RRSBW) distribution was applied for the parametric representation of the dissolution curves. The effect of two factors; drug particle size and kind of disintegrating agent, on the dissolution rate of PPA.HCl were studied at two levels. The factorial design method proved to be useful for the examination of tableted microcapsules.

Capsules↗

Sustained-release dosage form of phenylpropanolamine hydrochloride. Part I: Microencapsulation and in vitro release kinetics.

Microcapsules of phenylpropanolamine hydrochloride with core:wall ratios of 1:1, 2:1 and 1:2 were prepared by the coacervation-phase separation method, using ethylcellulose as the coating material. Two batches of PPA.HCl powder with different particle sizes (> 58 microns and < 28 microns) were used as the core material. The different sizes of microcapsules were separated using a range of standard sieves (840-247 microns). The effects of drug particle size, the media pH and the core:wall ratio on the dissolution kinetics were studied, and evaluated kinetically.

Capsules↗

Sustained-release dosage form of phenylpropanolamine hydrochloride. Part II: Formulation and in vitro release kinetics from tableted microcapsules.

This work was planned to prepare sustained-action preparations of phenylpropanolamine hydrochloride by microencapsulation and by tableted microcapsules. Dissolution from both suspended microcapsules and the tablets was studied using the USP XXII basket method in simulated gastric and intestinal fluid without enzyme. The results were applied to zero-order, first-order, Hixson Crowell, RRSBW, Q/square root of t, (Bt)a and Higuchi kinetic models. Dissolution of PPA.HCl was found to be governed by the core:wall ratio, drug particle size, media pH and type of disintegrating agent. Dissolution kinetics were studied and evaluated.

Capsules↗

The objective and timing of drug disposition studies, appendix V. A comparison of the bioavailability of three dosage forms of terfenadine.

Antagonistic effect against histamine-induced wheals was used to evaluate the bioavailability of terfenadine in monkeys. A rapidly dissolving tablet formulation of terfenadine shows essentially identical bioavailability to a liquid suspesion. A less readily dissolving capsule formulation lags considerably in time with regard to availability, and some question remains as to whether the total quantity in the capsule is available.

Animals↗

Thermal analysis as a screening technique in preformulation studies of picotamide solid dosage forms.

The potential compatibilities of several commonly used pharmaceutical excipients with picotamide were evaluated using differential scanning calorimetry (DSC). The effects of aging and of mechanical treatment (blending, grinding, or kneading) of samples were also evaluated. Hot-stage microscopy (HSM) and scanning electron microscopy (SEM) were used as complementary techniques to implement and assist in interpretation of the DSC results. DSC analysis evidenced a noticeable modification of drug thermal features in the mixtures with palmitic acid, stearic acid, stearyl alcohol, polyethylene glycol (PEG) 20,000, and sorbitol, but HSM analysis showed that the DSC behavior was mainly because of the drug dissolution in the melted excipient, which allowed the presence of important solid-solid interactions to be excluded. Compatibility with Mg stearate was also found, even if sample manipulation induced the partial conversion of Mg stearate in a pseudo-polymorphic modification. Mechanical stress displayed an increased hygroscopicity of mixtures with glucose and lactose, as well as some solid-solid interactions with lactose and mannitol.

Calorimetry, Differential Scanning↗

Oral solid dosage forms that should not be crushed: 1994 revision.

This revision and update of an article published previously in Hospital Pharmacy (1992; 27:690-699) alerts healthcare practitioners about medications that should not be crushed. This list serves those who dispense and administer medications so that potential problems associated with disruption of special pharmaceutical formulations may be prevented. Products are identified that should not be crushed and for which a similar liquid form is available.

Administration, Oral↗

A topical dosage form of liposomal clofazimine: research and clinical implications.

A novel topical clofazimine (CLO) gel formulation containing liposomally encapsulated CLO, was prepared and investigated in vitro followed by a clinical evaluation. CLO liposomes were prepared by the lipid film hydration technique. Comparative in vitro diffusion studies were conducted with plain and liposomal CLO in HPMC K4M gel base (2% and 5%) using human cadaver skin (HCS). A double blind clinical study was conducted on eight leprosy patients. The results of these studies show that the new liposomal topical gel formulation not only prolongs the drug release but also promotes drug retention by the skin. Studies further support formation of a reservoir of drug on the skin modifying therapeutic efficacy of the formulation. The new liposomal gel formulation of CLO considerably reduces the healing time of external lesions due to a significantly prolonged skin residence time compared to plain CLO gel and hence is expected to reduce the time needed for leprosy treatment.

Administration, Topical↗

Application of infrared spectrophotometry to the identification of inorganic substances in dosage forms of Antacida group.

Powdered tablets from the Antacida group: Alusal, Milk of Magnesia, Alumag, Maalox, Magnosil, Alugastrin, Malugastrin, Rennie, and components deciding about their antiacidity like Al(OH)3, Mg(OH)2, Mg2Si3O8, NaAl(OH)2CO3, MgAl(OH)(SO4)2, CaCO3, MgCO3, were subjected to infrared spectrophotometric investigations. It was found that infrared spectra of each pharmaceutical compound are different and show a series of characteristic maxima, by which they can be identified with in the spectral range of 4000 cm-1-200 cm-1. Comparison of infrared spectra of finished products with spectra of their components it was showed that the application of infrared spectrophotometry methods enabled us to prove the presence of particular compounds used in formulations. Tablet mass and odorizing agents do not cause significant changes in spectra of the tablets studied, preparations from the Antacida group.

Antacids↗

Dissolution properties of different designed and formulated salbutamol tablet dosage forms.

Pharmaceutical availability or in vitro availability is one of the aspects of drug bioavailability. Dissolution can be described best as a tool that can provide valuable information about the availability of a drug product. Dissolution test was performed on three different designed and formulated of salbutamol tablet formulations marketed in Turkey. The test methods were the paddle method and the rotating basket method described in United States Pharmacopeia. All studied formulations showed a good agreement with pharmacopeial requirements. In particular all studied commercial tablet formulations showed a quite fast release of the antiasthmatic drug. Other type of table formulations showed slow release. In order to evaluate the dissolution rates five different kinetics have been examined and the best fitting kinetics was found to be RRSBW kinetic.

Albuterol↗