Anthony J. Cutie

Compatibility of enteral products with commonly employed drug additives

Although drugs are routinely administered through gavage feedings set along with enteral products, there is little scientific data available to the physician, pharmacist, nurse, and dietician concerning the physical and chemical compatibility of drugs with enteral formulations. This study assesses the compatibility of Ensure (Ross Laboratories, Columbus, OH), Ensure Plus (Ross Laboratories, Columbus, OH), Osmolite (Ross Laboratories, Columbus, OH) with antibiotics, gastrointestinal agents, antipsychotic agents, urinary antiseptics cough and cold medications, and other commonly used additives. All enteral formulations were examined immediately after mixing for phase changes, creaming, and particle growth using a contrast light and a rotation viscometer. Results are presented in a tabular format. Guidelines and recommendations concerning how the addition of troublesome drug additives can be added are also presented.

Piroxicam Release from Dermatological Base: In-Vitro Studies using Cellulose Membrane and Hairless Mouse Skin

AbstractPiroxicam is one of the most potent non-steroidal, anti-inflammatory agents which also exhibits antipyretic activity. Piroxicam is well absorbed following the oral administration, however, its use has been associated with a number of gastro-intestinal disorders including bleeding and ulceration. To overcome these side effects, this study was undertaken to develop diadermatic dosage form using various polymeric gel and ointment bases containing 1% piroxicam were prepared to study the in-vitro release of the drug. Also, a series of additive ingredients, such as, alcohol USP, polyethylene glycol-400 and dimethyl sulfoxide (DMSO) were incorporated in these formulations at various concentration levels to evaluate their effects on drug release. The general rank order for the in-vitro drug release from all the bases evaluated was: gel base > hydrophillic base > emulsion base. In general, additives had little or no effect in enhancing the drug release from these bases. The in-vitro release data were treat...

The Effect of Selected Direct Compression Excipients on the Stability of Aspirin as a Model Hydrolyzable Drug

AbstractThe stability of a moisture sensitive drug is normally studied in relation to packaging which prevents water vapor ingress or minimizes its effect by using dessicants in a container. However, excipients contain intrinsic water which may degrade the drug. This paper deals with the stability of aspirin, as a model hydrolyzable drug, in combination with excipients having either hydrate water (dibasic calcium phosphate dihydrate and lactose) or variable adsorbed moisture depending upon environmental conditions (microcrystalline cellulose and pregelatinized starch). Tablets containing 10 and 50 per cent aspirin with these excipients were stored in open and closed bottles at various temperatures and humidities. Pregelatinized starch based tablets were stable in closed containers for 30 weeks while tablets containing microcrystalline cellulose or dibasic calcium phosphate dihydrate were unstable with respect to USP salicylic acid content. The stability of lactose based tablets was dependent on aspirin co...

Medicament Release from Ointment Bases: III. Ibuprofen: In Vitro Release and In-Vivo Absorption in Rabbits

AbstractThe in-vitro release of ibuprofen from various topical bases including: water-washable base, hydrophilic base, cream, Canadian formulary base, gel, emulsion, water-soluble base and University of California Hospital base were studied. Also, the effects of the additives (ethanol, polyethylene glycol—400, urea and dimethylsulfoxide) on the release rate of the drug from the water-washable base were evaluated.In general, the in-vitro release rate rank order of the drug was observed to be: water-washable base > hydrophilic base > Canadian formulary base > gel > PEG water washable > emulsion > cream > University of California base. The additive ingredients had a Little or no effect in enhancing the release of drug from the samples studied.The formulations with optimum in-vitro drug release were scaled up for in-vivo percutaneous absorption in rabbits. The blood samples were analyzed by a HPLC method. Among the candidates evaluated in-vivo, the bioavailability of the drug was significantly higher from the...

How to manage medications in the setting of liver disease with the application of six questions

Objective:  Reviewing the current literature to guide clinicians managing medications in the setting of liver disease.

QbD approach to investigate product and process variabilities for brain targeting liposomes

Abstract Efficacy of central nervous system-acting medications is limited by its localization and ability to cross the blood–brain barrier (BBB); therefore, the crux is in designing delivery systems targeted to cross the BBB. Toward this objective, this study proposed pegylated and glycosylated citalopram hydrobromide (Cit-HBr) liposomes as a delivery approach for brain targeting. The multicomponent liposomes were evaluated for drug encapsulation, vesicular size, size distribution, conductivity and drug release characteristics. Moreover, the interaction among the employed components was evaluated by Fourier transform infrared, differential scanning calorimetric and X-ray diffraction analysis. Through a systematic screening design of formulation and process variables in the optimization phase, an improvement of Cit-HBr loading, fine vesicular size with narrow size distribution, greater stability and sustained release features were achieved. The compatibility studies unveiled a significant interaction between Cit-HBr and dicetyl phosphate to control drug encapsulation and release properties. The optimization process showed a minimal range of design space to achieve the preset desirability; more precisely dicetyl phosphate, polyethylene glycol, N-acetyl glucosamine and freeze–thaw cycles of 3%, 5%, 4% and 2 cycles, respectively, were used. Using brain endothelial cell models, the optimized formulations showed an acceptable cell viability with preserved monolayer integrity and an enhanced flux and permeability. Thus, this study has proposed an optimized pegylated and glycosylated vector that is a promising step for brain targeting.

The Effect of Various Additives on the Stability of Isoproterenol Hydrochloride Solutions

AbstractThe effect of various additives on the rate of degradation of eight isoproterenol hydrochloride aqueous formulations was studied. In addition, the reaction was studied at various pH values and temperatures. From the latter data, activation parameters were determined. Rate constants increased from 10 to 100 times over a 25 degree increase in temperature. The activation energy for the reaction averaged approximately 25 kcal/mole. Ascorbic acid and sodium bisulfite appear to be the most efficient antioxidants in the system. Sequestering agents such as EDTA and citric acid do not appear to reduce the rate and, in one instance, EDTA seemed to enhance the degradation process. The reaction appears to be an oxidation of the catechol ring system of isoproterenol similar to that observed with epinephrine.Catecholamines such as isoproterenol and epinephrine are highly subject to degradative oxidation in solutions. A number of antioxidants and other substances are added to formulations containing these substa...

In-Vitro Release of Zinc Pyrithione from A Shampoo Base and the Effects of Various Additives on its Release Rate

AbstractZinc pyrithione has been established as one of the most effective anti-dandruff ingredients for use in shampoo formulations, through various clinical studies. However, the clinical efficacy is dependent upon its release rate from the vehicle and adsorption onto the scalp and hair. In light of these findings, the release of zinc pyrithione from a typical lotion shampoo base was investigated in-vitro. The shampoo formulation consisted of an anionic detergent, an amide and thickening agents commonly used in such products. The additives used included ethanol, dimethylsulfoxide (DMSO), polyethylene glyeol-400, propylene glycol and urea at 5%, 10% and 15% by weight of the formulations.Release experiments were carried out at 37°C, with diffusion cells immersed in beakers containing distilled water adjusted to pH 5.In general, the presence of the additive ingredient increased the release of zinc pyrithione. Among the samples evaluated, the formulations containing ethanol or propylene glycol gave the highe...

Diadermatic Dose Forms Of Testosterone: In-Vitro Release Studies and in-Vivo Absorption In A Human Male

AbstractThe study was undertaken to evaluate the in-vitro release of testosterone from various topical bases and to screen formulations with the optimum drug release for in-vivo evaluations in a human male. Several diadermatic bases containing 2% testosterone were prepared and studied for the in-vitro release of drug through the cellulose membrane using the diffusion methods. Also, additive ingredients such as, ethanol, polyethylene glycol-400, and dimethylsulfoxide (DMSO) at various concentration levels were included in these formulations to study their effects on the release rate of the drug. The general rank order of testosterone release from these bases was: water-washable base > hydrophilic base > University of California Hospital Base > gel base > cream base > water-soluble base > emulsion base. Except for the water-washable base containing 15% polyethylene glycol-400, all additives had little or no effect on the drug release. The formulations with the best in-vitro drug release were selected and ev...

Kinetic Aspects of the Decomposition of Clorazepate Potassium Salt

AbstractThe decompositation of clorazepate potassium salt (tranxene) In hydrocloric acid was examined at selected temperatures razging from 6 to 78°C. The energy of activation is evaluated and possible degradation pathways are elluded to. The energy of activation was found to be about 20 Kcal/mole.