Influence of Drug Concentration on In Vitro Release of Salicylic Acid from Ointment Bases

Bottari, F.; Colo, Giacomo Di; Nannipieri, E.; Saettone, M. F.; Serafini, M.F.

doi:10.1002/jps.2600631127

Cited by 54 publications

(11 citation statements)

References 18 publications

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“…The composition of STF was: sodium chloride 0.670 g, sodium bicarbonate 0.200 g, calcium chloride dihydrate 0.008 g, and purified water q.s. 100 ml (Bottari et al, 1974).…”

Section: Evaluation Of Formulationsmentioning

confidence: 99%

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

2010

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“…The composition of STF was: sodium chloride 0.670 g, sodium bicarbonate 0.200 g, calcium chloride dihydrate 0.008 g, and purified water q.s. 100 ml (Bottari et al, 1974).…”

Section: Evaluation Of Formulationsmentioning

confidence: 99%

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

2010

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“…13,14) When the amounts of DA and DP released from gel ointments were plotted against the square root of time, straight lines were obtained (Fig. 4).…”

Section: Discussionmentioning

confidence: 99%

Percutaneous absorption of dexamethasone acetate and palmitate, and the plasma concentration.

Ogiso

Ito

Iwaki

et al. 1987

CHEMICAL & PHARMACEUTICAL BULLETIN

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To investigate quantitatively the percutaneous absorption of dexamethasone acetate (DA) and palmitate (DP), gel and petrolatum ointments were prepared and applied to rat skin. DA in the presence of absorption enhancers (AzoneR and sorbitan monooleate) was rapidly absorbed, in the form of dexamethasone, through the skin, whereas the absorption after application of DA ointment without enhancers was relatively poor. DP was also efficiently absorbed in the presence and absence of enhancers, with bioavailability of 5.3 and 4.1%, respectively. The absorbed DP was slowly hydrolyzed in the systemic circulation. The percutaneous absorption of drugs from the petrolatum ointments with enhancers was slower than that from the gel ointments. The in vitro release rates of DA and DP from the gel ointments with enhancers were 7.3 and 6.1 mg/h1/2, respectively and were much higher than those from the petrolatum ointments. The partition coefficient of DP was much larger than that of DA. Thus, it is suggested that DA and DP gel ointments with enhancers are effective in terms of high absorption into the circulation.Systemic administration of cortisone and its synthetic analogs gives excellent results in clearing inflammatory skin lesions. Unfortunately, corticosteroids carry the risk of side effects such as peptic ulceration, hypokalemic alkalosis and edema.1) Corticosteroids have been frequently used in topical dosage forms for cutaneous diseases. It has been found that the esterification of the 17-and 21-hydroxy groups produces increased efficacy and improved penetration through skin, as shown in the case of betamethasone dipropionate and hydrocortisone butyrate propionate.2,3) The changes of molecular structure and technical advances in drug delivery systems have thus allowed increased utilization of transdermal formulations in corticosteroid therapy. Consequently, a kinetic study of esterified steroids in the systemic circulation would provide important information for practical application. Despite many studies on dermatologic preparations of corticosteroids, surprising little work has been carried out to define quantitatively the percutaneous absorption based on measuring plasma concentration. In this work, the in vivo percutaneous absorption of dexamethasone acetate and palmitate was investigated in rats, using gel and petrolatum ointments with or without absorption enhancers (AzoneR and sorbitan monooleate). In addition, various factors (the drug release rate, partition coefficient and hydrolysis in skin) which influence the penetration of drugs were investigated in relation to the percutaneous absorption. Experimental MaterialsDexamethasone acetate (DA, pharmaceutical grade) and dexamethasone palmitate (DP) and stearate were generous gifts of Nippon Merck-

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“…The composition of the ATF used was: sodium chloride 0.670 g, sodium bicarbonate 0.200 g, calcium chloride dihydrate 0.008 g, and purified water q.s. 100 ml (Bottari, Dicolo, Nannipieri, Saettone, & Serafini, 1974).…”

Section: Methods Of Preparationmentioning

confidence: 99%

“…A modified USP XXII dissolution testing apparatus (apparatus 1; Figure 5; Bottari et al, 1974;Dotegham, 1993) was used for evaluating the in vitro release profile using cellophane membrane (pore size: 0.45 μ), which does not hamper the diffusion of the drug. This phenomenon was confirmed by placing the plain drug on the membrane.…”

Section: Evaluation Of Formulationmentioning

confidence: 99%

In Situ Ophthalmic Gel of Ciprofloxacin Hydrochloride for Once a Day Sustained Delivery

Jain

Shah

Rajadhyaksha

et al. 2008

Drug Development and Industrial Pharmacy

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This article focuses on preparation and evaluation of a once a day ophthalmic delivery system for ciprofloxacin hydrochloride based on the concept of pH-triggered in situ gelation. The in situ gelling system involves the use of polyacrylic acid (Carbopol ® 980NF) as a phase transition polymer, hydroxypropyl methylcellulose (Methocel ® K100LV) as a release retardant, and ion exchange resin as a complexing agent. Ciprofloxacin hydrochloride was complexed with ion exchange resin to avoid incompatibility between drug and polyacrylic acid. The developed formulation was stable, and nonirritant to rabbit eyes and in vitro drug release was found to be around 98% over a period of 24 hours.Keywords pH-triggered in situ gel; ciprofloxacin hydrochloride; Carbopol ® ; hydroxypropyl methylcellulose; once a day ocular delivery system INTRODUCTIONToday, topical ophthalmic application is considered the preferred way to achieve therapeutic levels of active medicament used to treat ocular diseases. Solutions, suspensions, and semisolids like ointments and gels are conventionally available as ophthalmic delivery systems. From a biopharmaceutical standpoint, their use has met some criticism over their efficiency as drug delivery systems. Bioavailability, particularly for ocular solutions, ranges from 1% to 10% of the total administered dose. This could be due to the rapid precorneal kinetics resulting from reflex tearing and blinking. The basic disadvantage associated with the use of ocular formulation is rapid loss of both solutions and suspended solid. Ophthalmic ointments give blurred vision, leading to poor patient acceptance (Olejnic, 1993).

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Influence of Drug Concentration on In Vitro Release of Salicylic Acid from Ointment Bases

Cited by 54 publications

References 18 publications

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

New method for ophthalmic delivery of azithromycin by poloxamer/carbopol-based in situ gelling system

Percutaneous absorption of dexamethasone acetate and palmitate, and the plasma concentration.

In Situ Ophthalmic Gel of Ciprofloxacin Hydrochloride for Once a Day Sustained Delivery

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