Release and absorption rates of intramuscularly and subcutaneously injected pharmaceuticals (II)
Identifieur interne : 002C17 ( Main/Exploration ); précédent : 002C16; suivant : 002C18Release and absorption rates of intramuscularly and subcutaneously injected pharmaceuticals (II)
Auteurs : J. Zuidema [Pays-Bas] ; F. Kadir [Pays-Bas] ; H. A. C. Titulaer [Pays-Bas] ; C. Oussoren [Pays-Bas]Source :
- International Journal of Pharmaceutics [ 0378-5173 ] ; 1994.
English descriptors
- Teeft :
- Absorption, Absorption phase, Absorption process, Absorption rate, Aggregation, Ahsorption, Ahsorption drugs, Aqueous solutions, Aqueous systems, Aqueous vehicle, Artelinic acid, Artemisinin, Arterial concentrations, Blood flow, Blood supply, Burst effect, Cell turnover, Chloroquine, Complete absorption, Cosolvents, Cosolvents complexing agents, Cultured muscle cells, Destabilising factors, Dissolution, Dissolution rate, Dissolution surface, Drug, Drug absorption, Drug administration, Drug concentration, Drug concentrations, Drug lipophilicity, Drug release, Drug saturation, Eling, Experimental data, First case, Former study, Further absorption, Glycol, Granulocyte, Greater absorption rate, High concentrations, Higher aggregation state, Higher doses, Hirano, Hydrophilic, Hydrophilic compound, Hydrophilic compounds, Hydrophilic drugs, Important role, Initial absorption rate, Initial phase, Injection, Injection components, Injection depth, Injection site, Injection sites, Injection trauma, Injection volume, Interstitial fluid, Intramuscular, Intramuscular administration, Intramuscular injection, Intraperitoneal injection, Intravenous, Intravenous injection, Kadir, Large vessels, Larger volumes, Limited value, Lipophilic, Lipophilic compounds, Lipophilic drugs, Lipophilicity, Lipoprotein, Liposomal, Liposomal chloroquine, Liposomal depots, Liposomal material, Liposomal preparations, Liposomcs, Liposome, Local clearance, Lower concentrations, Lymph nodes, Lymphatic, Lymphatic system, Lymphatic transport, Macrophage, Mathematical model, Mobile phase, Model compound, Model drugs, More lipophilic, Muscle components, Muscle homogenates, Next example, Oily systems, Oily vehicle, Oily vehicles, Other cosolvents, Other words, Particle size, Partition coefficients, Phagocytosis, Pharmaceutical, Phospholipid, Polyethylene glycol, Positive correlation, Possible explanation, Possible role, Propylene glycol, Rapid absorption, Rapid action, Release characteristics, Release formulations, Release preparations, Release systems, Serum filtrate, Serum opsonins, Specific cases, Specific rheological features, Stationary phase, Subcutaneous, Subcutaneous injection, Subcutaneous injection sites, Testosterone propionate, Tissue components, Tissue fluids, Turnover, Vehicle flow, Vehicle volume, Vivo absorption rate, Yamada, Zuidcma, Zuidema.
Abstract
Abstract: The rate and extent of intramuscular (i.m.) and subcutaneous (s.c.) drug absorption are very erratic and variable. The lipophilicity of the compound plays an important role. Aqueous drug solutions and suspensions of the more lipophilic compounds are often absorbed incompletely within the therapeutically relevant time. More hydrophilic compounds are absorbed completely. Injection depth, drug concentration and vehicle volume, pH-pKa relation, vehicle, cosolvents and surfactants have strong influences on the absorption profile of lipophilic drugs. Aqueous solutions of hydrophilic drugs are less sensitive to these factors. Drug solutions in oil and even suspensions in oil are often thought to be sustained release preparations. In fact, rapid absorption has often been observed. Slow release is not a property of the oily vehicle but is achieved by a high lipophilicity of the dissolved or suspended compound. Liposomal preparations are currently under investigation as i.m. and s.c. injectable sustained release preparations. Factors that induce drug release at the injection sites are the proteins and especially lipoproteins in the interstitial fluids, originating from serum filtrate and from turnover of inflammatory cells. Phagocytosis by macrophages and fat cells may play an important role in the local clearance of liposomal material from the injection site. Sustained release of some pharmaceuticals with normal or long half-lives appeared in specific cases preferable to rapid release. In addition, high arterial drug concentrations during the absorption phase may result in undesired effects even when venous drug concentrations are within the safe range.
Url:
DOI: 10.1016/0378-5173(94)90103-1
Affiliations:
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Oussoren</name><affiliation wicri:level="4"><country xml:lang="fr">Pays-Bas</country><wicri:regionArea>Department of Biopharmaceutics, Faculty of Pharmacy, Department of Biopharmaceutics PO Box 80082, Utrecht University, 3508 TB Utrecht</wicri:regionArea><orgName type="university">Université d'Utrecht</orgName><placeName><settlement type="city">Utrecht</settlement><region nuts="2">Utrecht (province)</region></placeName></affiliation></author></analytic><monogr></monogr><series><title level="j">International Journal of Pharmaceutics</title><title level="j" type="abbrev">IJP</title><idno type="ISSN">0378-5173</idno><imprint><publisher>ELSEVIER</publisher><date type="published" when="1994">1994</date><biblScope unit="volume">105</biblScope><biblScope unit="issue">3</biblScope><biblScope unit="page" from="189">189</biblScope><biblScope unit="page" to="207">207</biblScope></imprint><idno type="ISSN">0378-5173</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0378-5173</idno></seriesStmt></fileDesc><profileDesc><textClass><keywords scheme="Teeft" xml:lang="en"><term>Absorption</term><term>Absorption phase</term><term>Absorption process</term><term>Absorption rate</term><term>Aggregation</term><term>Ahsorption</term><term>Ahsorption drugs</term><term>Aqueous solutions</term><term>Aqueous systems</term><term>Aqueous vehicle</term><term>Artelinic acid</term><term>Artemisinin</term><term>Arterial concentrations</term><term>Blood flow</term><term>Blood supply</term><term>Burst effect</term><term>Cell turnover</term><term>Chloroquine</term><term>Complete absorption</term><term>Cosolvents</term><term>Cosolvents complexing agents</term><term>Cultured muscle cells</term><term>Destabilising factors</term><term>Dissolution</term><term>Dissolution rate</term><term>Dissolution surface</term><term>Drug</term><term>Drug absorption</term><term>Drug administration</term><term>Drug concentration</term><term>Drug concentrations</term><term>Drug lipophilicity</term><term>Drug release</term><term>Drug saturation</term><term>Eling</term><term>Experimental data</term><term>First case</term><term>Former study</term><term>Further absorption</term><term>Glycol</term><term>Granulocyte</term><term>Greater absorption rate</term><term>High concentrations</term><term>Higher aggregation state</term><term>Higher doses</term><term>Hirano</term><term>Hydrophilic</term><term>Hydrophilic compound</term><term>Hydrophilic compounds</term><term>Hydrophilic drugs</term><term>Important role</term><term>Initial absorption rate</term><term>Initial phase</term><term>Injection</term><term>Injection components</term><term>Injection depth</term><term>Injection site</term><term>Injection sites</term><term>Injection trauma</term><term>Injection volume</term><term>Interstitial fluid</term><term>Intramuscular</term><term>Intramuscular administration</term><term>Intramuscular injection</term><term>Intraperitoneal injection</term><term>Intravenous</term><term>Intravenous injection</term><term>Kadir</term><term>Large vessels</term><term>Larger volumes</term><term>Limited value</term><term>Lipophilic</term><term>Lipophilic compounds</term><term>Lipophilic drugs</term><term>Lipophilicity</term><term>Lipoprotein</term><term>Liposomal</term><term>Liposomal chloroquine</term><term>Liposomal depots</term><term>Liposomal material</term><term>Liposomal preparations</term><term>Liposomcs</term><term>Liposome</term><term>Local clearance</term><term>Lower concentrations</term><term>Lymph nodes</term><term>Lymphatic</term><term>Lymphatic system</term><term>Lymphatic transport</term><term>Macrophage</term><term>Mathematical model</term><term>Mobile phase</term><term>Model compound</term><term>Model drugs</term><term>More lipophilic</term><term>Muscle components</term><term>Muscle homogenates</term><term>Next example</term><term>Oily systems</term><term>Oily vehicle</term><term>Oily vehicles</term><term>Other cosolvents</term><term>Other words</term><term>Particle size</term><term>Partition coefficients</term><term>Phagocytosis</term><term>Pharmaceutical</term><term>Phospholipid</term><term>Polyethylene glycol</term><term>Positive correlation</term><term>Possible explanation</term><term>Possible role</term><term>Propylene glycol</term><term>Rapid absorption</term><term>Rapid action</term><term>Release characteristics</term><term>Release formulations</term><term>Release preparations</term><term>Release systems</term><term>Serum filtrate</term><term>Serum opsonins</term><term>Specific cases</term><term>Specific rheological features</term><term>Stationary phase</term><term>Subcutaneous</term><term>Subcutaneous injection</term><term>Subcutaneous injection sites</term><term>Testosterone propionate</term><term>Tissue components</term><term>Tissue fluids</term><term>Turnover</term><term>Vehicle flow</term><term>Vehicle volume</term><term>Vivo absorption rate</term><term>Yamada</term><term>Zuidcma</term><term>Zuidema</term></keywords></textClass><langUsage><language ident="en">en</language></langUsage></profileDesc></teiHeader><front><div type="abstract" xml:lang="en">Abstract: The rate and extent of intramuscular (i.m.) and subcutaneous (s.c.) drug absorption are very erratic and variable. The lipophilicity of the compound plays an important role. Aqueous drug solutions and suspensions of the more lipophilic compounds are often absorbed incompletely within the therapeutically relevant time. More hydrophilic compounds are absorbed completely. Injection depth, drug concentration and vehicle volume, pH-pKa relation, vehicle, cosolvents and surfactants have strong influences on the absorption profile of lipophilic drugs. Aqueous solutions of hydrophilic drugs are less sensitive to these factors. Drug solutions in oil and even suspensions in oil are often thought to be sustained release preparations. In fact, rapid absorption has often been observed. Slow release is not a property of the oily vehicle but is achieved by a high lipophilicity of the dissolved or suspended compound. Liposomal preparations are currently under investigation as i.m. and s.c. injectable sustained release preparations. Factors that induce drug release at the injection sites are the proteins and especially lipoproteins in the interstitial fluids, originating from serum filtrate and from turnover of inflammatory cells. Phagocytosis by macrophages and fat cells may play an important role in the local clearance of liposomal material from the injection site. Sustained release of some pharmaceuticals with normal or long half-lives appeared in specific cases preferable to rapid release. In addition, high arterial drug concentrations during the absorption phase may result in undesired effects even when venous drug concentrations are within the safe range.</div></front></TEI><affiliations><list><country><li>Pays-Bas</li></country><region><li>Utrecht (province)</li></region><settlement><li>Utrecht</li></settlement><orgName><li>Université d'Utrecht</li></orgName></list><tree><country name="Pays-Bas"><region name="Utrecht (province)"><name sortKey="Zuidema, J" sort="Zuidema, J" uniqKey="Zuidema J" first="J." last="Zuidema">J. Zuidema</name></region><name sortKey="Kadir, F" sort="Kadir, F" uniqKey="Kadir F" first="F." last="Kadir">F. Kadir</name><name sortKey="Oussoren, C" sort="Oussoren, C" uniqKey="Oussoren C" first="C." last="Oussoren">C. Oussoren</name><name sortKey="Titulaer, H A C" sort="Titulaer, H A C" uniqKey="Titulaer H" first="H. A. C." last="Titulaer">H. A. C. Titulaer</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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