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  1. Artikel ; Online: Preparation and evaluation of a lipid-based drug delivery system to ımprove valsartan oral bioavailability: pharmacokinetic and pharmacodynamic analysis.

    Gülmezoğlu, Eda / Yıldız Türkyılmaz, Gülbeyaz / Karasulu, H Yeşim

    Drug development and industrial pharmacy

    2023  Band 48, Heft 12, Seite(n) 727–736

    Abstract: Antihypertensive treatment reduces the risk of cardiovascular complications in patients with high mortality with hypertension. Valsartan is highly selective antihypertensive that is rapidly absorbed after oral administration, but its oral bioavailability ...

    Abstract Antihypertensive treatment reduces the risk of cardiovascular complications in patients with high mortality with hypertension. Valsartan is highly selective antihypertensive that is rapidly absorbed after oral administration, but its oral bioavailability is only 25%. It is absorbed from the upper part of the gastrointestinal tract but is less soluble in this acidic environment. We aimed to develop a lipid-based formulation to produce a self-emulsifying drug delivery system (SEDDS) for valsartan. Solubility studies were performed to identify the components of the SEDDS that provided the best dissolution of valsartan. Ternary phase diagrams were drawn using the titration method with oil, surfactants and co-surfactants in which valsartan was highly soluble, and microemulsion formulations with the highest area were determined. Characterization and
    Mesh-Begriff(e) Rats ; Animals ; Valsartan/chemistry ; Antihypertensive Agents ; Emulsions/chemistry ; Chemistry, Pharmaceutical/methods ; Drug Delivery Systems/methods ; Surface-Active Agents/chemistry ; Solubility ; Biological Availability ; Lipids/chemistry ; Administration, Oral
    Chemische Substanzen Valsartan (80M03YXJ7I) ; Antihypertensive Agents ; Emulsions ; Surface-Active Agents ; Lipids
    Sprache Englisch
    Erscheinungsdatum 2023-01-12
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 751874-2
    ISSN 1520-5762 ; 0363-9045
    ISSN (online) 1520-5762
    ISSN 0363-9045
    DOI 10.1080/03639045.2022.2164588
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel ; Online: In vitro

    Diril, Mine / Özdokur, Kemal Volkan / Yıldırım, Yeliz / Karasulu, H Yeşim

    Pharmaceutical development and technology

    2023  Band 28, Heft 10, Seite(n) 915–927

    Abstract: Hepatocellular carcinoma (HCC), more than 800 000 cases reported annually, is the most common primary liver cancer globally. Doxorubicin hydrochloride (Dox-HCl) is a widely used chemotherapy drug for HCC, but efficacy and tolerability are limited, thus ... ...

    Abstract Hepatocellular carcinoma (HCC), more than 800 000 cases reported annually, is the most common primary liver cancer globally. Doxorubicin hydrochloride (Dox-HCl) is a widely used chemotherapy drug for HCC, but efficacy and tolerability are limited, thus critical to develop delivery systems that can target Dox-HCl to the tumour site. In this study, liver-targeting ligand glycyrrhetinic acid (Gly) was conjugated to polyethylene glycol (PEG)
    Mesh-Begriff(e) Animals ; Mice ; Carcinoma, Hepatocellular/drug therapy ; Carcinoma, Hepatocellular/pathology ; Liver Neoplasms/drug therapy ; Liver Neoplasms/pathology ; Doxorubicin/pharmacology ; Doxorubicin/therapeutic use ; Polyethylene Glycols ; Drug Delivery Systems ; Cell Line, Tumor
    Chemische Substanzen liposomal doxorubicin ; Doxorubicin (80168379AG) ; Polyethylene Glycols (3WJQ0SDW1A)
    Sprache Englisch
    Erscheinungsdatum 2023-12-18
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1331774-x
    ISSN 1097-9867 ; 1083-7450
    ISSN (online) 1097-9867
    ISSN 1083-7450
    DOI 10.1080/10837450.2023.2274394
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  3. Artikel: Microemulsions as novel drug carriers: the formation, stability, applications and toxicity.

    Karasulu, H Yesim

    Expert opinion on drug delivery

    2008  Band 5, Heft 1, Seite(n) 119–135

    Abstract: A microemulsion, made from water, oil, surfactants and cosurfactant is a thermodynamically stable system. The presence of the cosurfactant is often required in order to lower the interfacial tension of this interface, because a low interfacial tension is ...

    Abstract A microemulsion, made from water, oil, surfactants and cosurfactant is a thermodynamically stable system. The presence of the cosurfactant is often required in order to lower the interfacial tension of this interface, because a low interfacial tension is essential for the formation of microemulsions. The transparency of microemulsions arises from their small droplet diameter. The droplet diameter in stable microemulsions is usually within the range of 10 - 140 nm. Microemulsions are graphically represented as stability areas in triangular phase diagrams where each triangular corner designates a certain component. Microemulsions are actually quaternary (pseudoternary) systems. In pharmaceutical fields, the interest in microemulsions is increasing and, thus, they are applied to various administration routes.
    Mesh-Begriff(e) Animals ; Drug Carriers/chemistry ; Drug Carriers/toxicity ; Drug Compounding ; Drug Stability ; Emulsions/chemistry ; Emulsions/toxicity ; Humans ; Microchemistry ; Pharmaceutical Preparations/administration & dosage ; Thermodynamics
    Chemische Substanzen Drug Carriers ; Emulsions ; Pharmaceutical Preparations
    Sprache Englisch
    Erscheinungsdatum 2008-01
    Erscheinungsland England
    Dokumenttyp Journal Article ; Review
    ZDB-ID 2167286-6
    ISSN 1744-7593 ; 1742-5247
    ISSN (online) 1744-7593
    ISSN 1742-5247
    DOI 10.1517/17425247.5.1.119
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  4. Artikel ; Online: Formulation and In Vitro Evaluation of Self Microemulsifying Drug Delivery System Containing Atorvastatin Calcium.

    Diril, Mine / Türkyılmaz, Gülbeyaz Yıldız / Karasulu, H Yeşim

    Current drug delivery

    2019  Band 16, Heft 8, Seite(n) 768–779

    Abstract: Objective: The aim of this study was to develop a new dosage form as an alternative to the classical tablet forms of atorvastatin calcium (AtrCa). The formulation strategy was to prepare an optimum self micro emulsifying drug delivery system (SMEDDS) to ...

    Abstract Objective: The aim of this study was to develop a new dosage form as an alternative to the classical tablet forms of atorvastatin calcium (AtrCa). The formulation strategy was to prepare an optimum self micro emulsifying drug delivery system (SMEDDS) to overcome the problem of low solubility of the active substance.
    Methods: In this study, pseudo ternary phase diagrams were plotted determined by the solubility studies. According to the solubility studies; oleic acid was used as the oil phase, Tween 20 and Span 80 were used as the surfactants and ethanol was used as the co-surfactant. SMEDDS formulations were characterized according to pH, electrical conductivity, density, refractive index, viscosity, emulsification time, dispersibility, robustness of dilution stability, droplet size, polidispersity index, zeta potential, transmittance %, cloud point, content quantification %, chemical and physical stability. The lipolysis study was conducted under fed and fasted conditions. In vitro release studies and kinetic evaluation were carried out. Permeability studies were also examined with Caco-2 cell culture.
    Results: The droplet size of the optimized formulation did not change significantly in different medias over the test time period. Improved SMEDDS formulation will progress steadily without precipitating along the gastrointestinal tract. Lipolysis studies showed that the oil solution had been exposed to high amount of lipolysis compared to the SMEDDS formulation. The release rate of AtrCa from AtrCa- SMEDDS formulation (93.8%, at 15 minutes) was found as increased when the results were compared with commercial tablet formulation and pure drug. The permeability value of AtrCa from AtrCa- SMEDDS formulation was found higher than pure AtrCa and commercial tablet formulation, approximately 9.94 and 1.64 times, respectively.
    Conclusion: Thus, lipid-based SMEDDS formulation is a potential formulation candidate for lymphatic route in terms of the increased solubility of AtrCa.
    Mesh-Begriff(e) Atorvastatin/chemistry ; Caco-2 Cells ; Drug Compounding ; Drug Delivery Systems ; Emulsions/chemistry ; Ethanol/chemistry ; Hexoses/chemistry ; Humans ; Lipids/chemistry ; Oleic Acid/chemistry ; Particle Size ; Polysorbates/chemistry ; Solubility ; Surface Properties ; Surface-Active Agents/chemistry ; Tumor Cells, Cultured
    Chemische Substanzen Emulsions ; Hexoses ; Lipids ; Polysorbates ; Surface-Active Agents ; sorbitan monooleate (06XEA2VD56) ; Oleic Acid (2UMI9U37CP) ; Ethanol (3K9958V90M) ; Atorvastatin (A0JWA85V8F)
    Sprache Englisch
    Erscheinungsdatum 2019-08-20
    Erscheinungsland United Arab Emirates
    Dokumenttyp Journal Article
    ZDB-ID 2185284-4
    ISSN 1875-5704 ; 1567-2018
    ISSN (online) 1875-5704
    ISSN 1567-2018
    DOI 10.2174/1567201816666190820143957
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  5. Artikel ; Online: Synthesis, molecular modeling, in vivo study and anticancer activity against prostate cancer of (+) (S)-naproxen derivatives.

    Birgül, Kaan / Yıldırım, Yeliz / Karasulu, H Yeşim / Karasulu, Ercüment / Uba, Abdullah Ibrahim / Yelekçi, Kemal / Bekçi, Hatice / Cumaoğlu, Ahmet / Kabasakal, Levent / Yılmaz, Özgür / Küçükgüzel, Ş Güniz

    European journal of medicinal chemistry

    2020  Band 208, Seite(n) 112841

    Abstract: In this study, (S)-naproxen thiosemicarbazides (3a-d), 1,2,4-triazoles (4a-c), triazole-thioether hybride compounds (5a-p) were synthesized and their structures (3a, 3d, 4a and 5a-p) were confirmed by FT-IR, ...

    Abstract In this study, (S)-naproxen thiosemicarbazides (3a-d), 1,2,4-triazoles (4a-c), triazole-thioether hybride compounds (5a-p) were synthesized and their structures (3a, 3d, 4a and 5a-p) were confirmed by FT-IR,
    Mesh-Begriff(e) Animals ; Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/metabolism ; Antineoplastic Agents/therapeutic use ; Apoptosis/drug effects ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/therapeutic use ; Humans ; Male ; Methionyl Aminopeptidases/antagonists & inhibitors ; Methionyl Aminopeptidases/metabolism ; Mice, Nude ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Molecular Structure ; Naproxen/analogs & derivatives ; Naproxen/metabolism ; Naproxen/therapeutic use ; Prostatic Neoplasms/drug therapy ; Protein Binding ; Stereoisomerism ; Structure-Activity Relationship
    Chemische Substanzen Antineoplastic Agents ; Enzyme Inhibitors ; Naproxen (57Y76R9ATQ) ; METAP2 protein, human (EC 3.4.11.18) ; Metap2 protein, mouse (EC 3.4.11.18) ; Methionyl Aminopeptidases (EC 3.4.11.18)
    Sprache Englisch
    Erscheinungsdatum 2020-09-16
    Erscheinungsland France
    Dokumenttyp Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2020.112841
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  6. Artikel ; Online: Preparation and evaluation of novel microemulsion-based hydrogels for dermal delivery of benzocaine.

    Üstündağ Okur, Neslihan / Çağlar, Emre Şefik / Arpa, Muhammet Davut / Karasulu, H Yeşim

    Pharmaceutical development and technology

    2017  Band 22, Heft 4, Seite(n) 500–510

    Abstract: The purpose of the current research was to prepare and evaluate the potential use of microemulsion-based hydrogel (MBH) formulations for dermal delivery of benzocaine (BZN). The pseudoternary-phase diagrams were constructed for various microemulsions ... ...

    Abstract The purpose of the current research was to prepare and evaluate the potential use of microemulsion-based hydrogel (MBH) formulations for dermal delivery of benzocaine (BZN). The pseudoternary-phase diagrams were constructed for various microemulsions composed of isopropyl myristate (IPM) as oil phase, Span 20, Tween 20, Tween 80, cremophor EL and cremophor RH40 as surfactants, ethanol as cosurfactant and distilled water as aqueous phase. Finally, concentration of BZN in microemulsions was 2% (w/w). The physicochemical properties, such as conductivity, viscosity, pH, droplet size, polydispersity index and zeta potential of microemulsions, were measured. Carbopol 940 was used to convert BZN-loaded microemulsions into gel form without affecting their structure. Furthermore, excised rat abdominal skin was used to compare permeation and penetration properties of BZN loaded M3 and M3BHs with BZN solution. According to ex vivo study results, BZN-loaded M3BH1 showed highest flux values and high release rate values, and furthermore, this gel formulation had low surfactant content. Finally, in order to learn the localization of formulations within the dermal penetration, formulations and BZN solution were labeled with red oil O and subjected to fluorescence observation. In conclusion, BZN-loaded MBHs could be offered as a promising strategy for dermal drug delivery.
    Mesh-Begriff(e) Acrylic Resins/chemistry ; Administration, Cutaneous ; Anesthetics, Local/administration & dosage ; Anesthetics, Local/pharmacokinetics ; Animals ; Benzocaine/administration & dosage ; Benzocaine/pharmacokinetics ; Drug Carriers/chemistry ; Emulsions/chemistry ; Hydrogels/chemistry ; Male ; Myristates/chemistry ; Polyethylene Glycols/chemistry ; Polysorbates/chemistry ; Rats, Wistar ; Skin Absorption
    Chemische Substanzen Acrylic Resins ; Anesthetics, Local ; Drug Carriers ; Emulsions ; Hydrogels ; Myristates ; Polysorbates ; isopropyl myristate (0RE8K4LNJS) ; Polyethylene Glycols (30IQX730WE) ; cremophor (39279-69-1) ; carbopol 940 (4Q93RCW27E) ; Benzocaine (U3RSY48JW5)
    Sprache Englisch
    Erscheinungsdatum 2017-06
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1331774-x
    ISSN 1097-9867 ; 1083-7450
    ISSN (online) 1097-9867
    ISSN 1083-7450
    DOI 10.3109/10837450.2015.1131716
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  7. Artikel ; Online: Spirulina platensis (Cyanophyta) İle Hazırlanan Tablet ve Kapsüllerin in vitro Kalite Kontrol Çalışmaları.

    H. Yeşim Karasulu / Meltem Conk Dalay / Evren Şanal / Tamer Güneri

    Su Ürünleri Dergisi, Vol 18, Iss

    2015  Band 1

    Schlagwörter - ; Aquaculture. Fisheries. Angling ; SH1-691 ; Ecology ; QH540-549.5
    Sprache Englisch
    Erscheinungsdatum 2015-12-01T00:00:00Z
    Verlag Ege University
    Dokumenttyp Artikel ; Online
    Datenquelle BASE - Bielefeld Academic Search Engine (Lebenswissenschaftliche Auswahl)

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  8. Artikel ; Online: Permeation studies and histological examination of sheep nasal mucosa following administration of different nasal formulations with or without absorption enhancers.

    Karasulu, Ercüment / Yavasoğlu, Altug / Evrensanal, Z / Uyanikgil, Yigit / Karasulu, H Yesim

    Drug delivery

    2008  Band 15, Heft 4, Seite(n) 219–225

    Abstract: This study was designed to investigate the possible histological effects of different intranasal (IN) formulations of indomethacin (IND) on nasal mucosa in sheep. For this purpose, oil-in-water (O/W) emulsion (E) and solution (S) formulations including 3 ...

    Abstract This study was designed to investigate the possible histological effects of different intranasal (IN) formulations of indomethacin (IND) on nasal mucosa in sheep. For this purpose, oil-in-water (O/W) emulsion (E) and solution (S) formulations including 3 mg/mL of IND were prepared. Penetration enhancers such as polyvinylpyrolidone (PVP), citric acid (CA) and sodium taurocholate (NaT) were added to emulsion (1%) at the final step into the formulations. First, the effect of penetration enhancers on permeation of IND was evaluated by in vitro permeation studies in which sheep nasal mucosa was used. According to the permeation studies PVP showed the highest enhancing effect on the permeation rate of IND from sheep nasal mucosa. Furthermore, the IND permeation from E containing PVP (1.624 +/- 0.045 mg) was significantly higher than that obtained from E (0.234 +/- 0.012 mg) (p < 0.05). For the histological studies, white Karaman sheep of approximately 20 +/- 5 kg, aged 4 to 8 months were used. They were randomly divided into eight groups, each including three sheep. Five experimental groups received different formulations of IND emulsion without/ with penetration enhancers (E-PVP, E-CA, E-NaT, E) and IND solution (S), respectively. Parallel controls were composed of either untreated groups and were given blank emulsion or isotonic sodium chloride solution (0.31 mg/kg). 2 mL of each experimental formulation was applied to both nostrils of sheep, and 1/3 central and lower regions of the nose were dissected and prepared for light microscopy. Specimens stained with hematoxylin and eosin and Gomori's trichrome were examined by light microscopy. No signs of inflammation or erosion were noticed in the nasal mucosa of the control groups. Widened epithelial intercellular spaces were noticed in E-CA, E-NaT, and E-PVP groups as well with the E-PVP group showing the largest intraepithelial separations. E-CA and E-NaT groups showed significant decrease in the amount of goblet cells, while hypoplasia was considerably moderate in the E-PVP group. Finally, intranasal administration of IND emulsion with PVP may be considered as an alternative to intravenous and per oral administrations of IND to overcome their adverse effects.
    Mesh-Begriff(e) Administration, Intranasal ; Animals ; Anti-Inflammatory Agents, Non-Steroidal/administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal/adverse effects ; Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics ; Citric Acid/chemistry ; Emulsions/chemistry ; Emulsions/pharmacokinetics ; Excipients/chemistry ; Extracellular Space/metabolism ; Goblet Cells/metabolism ; Indomethacin/administration & dosage ; Indomethacin/adverse effects ; Indomethacin/pharmacokinetics ; Microscopy ; Nasal Mucosa/metabolism ; Oils/chemistry ; Permeability ; Pharmaceutical Solutions ; Povidone/chemistry ; Random Allocation ; Sheep ; Taurocholic Acid/chemistry ; Water/chemistry
    Chemische Substanzen Anti-Inflammatory Agents, Non-Steroidal ; Emulsions ; Excipients ; Oils ; Pharmaceutical Solutions ; Water (059QF0KO0R) ; Citric Acid (2968PHW8QP) ; Taurocholic Acid (5E090O0G3Z) ; Povidone (FZ989GH94E) ; Indomethacin (XXE1CET956)
    Sprache Englisch
    Erscheinungsdatum 2008-04-21
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1213261-5
    ISSN 1521-0464 ; 1071-7544
    ISSN (online) 1521-0464
    ISSN 1071-7544
    DOI 10.1080/10717540802006377
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  9. Artikel ; Online: Effect of microemulsion formulation on biodistribution of

    İlem-Özdemir, Derya / Üstündağ-Okur, Neslihan / Ay Şenyiğit, Zeynep / Oruç, Nevin / Aşıkoğlu, Makbule / Özütemiz, Ömer / Karasulu, H Yeşim

    Drug delivery

    2016  Band 23, Heft 8, Seite(n) 3055–3062

    Abstract: Background: Aprotinin is a monomeric globular polypeptide, which derived from bovine lung tissue and theoretically attractive molecule in ameliorating the effects of acute pancreatitis. Acute pancreatitis is an inflammatory condition of the pancreas ... ...

    Abstract Background: Aprotinin is a monomeric globular polypeptide, which derived from bovine lung tissue and theoretically attractive molecule in ameliorating the effects of acute pancreatitis. Acute pancreatitis is an inflammatory condition of the pancreas that is painful and at times deadly. Over the following two decades Aprotinin therapeutic potential on pancreatitis is proven experimentally, its clinical therapeutic success is limited due to low targeting to pancreas.
    Objective: The aim of this study was to evaluate the biodistribution of Technetium-99m (
    Method: Aprotinin was radiolabeled with
    Results: Aprotinin was radiolabeled by
    Conclusion: This might be concluding that microemulsions may be suggested as promising formulations for selectively targeting Aprotinin to pancreas inflammation.
    Mesh-Begriff(e) Animals ; Aprotinin/metabolism ; Chemistry, Pharmaceutical/methods ; Disease Models, Animal ; Emulsions/metabolism ; Male ; Pancreatitis/metabolism ; Particle Size ; Radionuclide Imaging/methods ; Radiopharmaceuticals/metabolism ; Rats ; Rats, Wistar ; Technetium/metabolism ; Tissue Distribution
    Chemische Substanzen Emulsions ; Radiopharmaceuticals ; Technetium (7440-26-8) ; Aprotinin (9087-70-1)
    Sprache Englisch
    Erscheinungsdatum 2016-10
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 1213261-5
    ISSN 1521-0464 ; 1071-7544
    ISSN (online) 1521-0464
    ISSN 1071-7544
    DOI 10.3109/10717544.2016.1145306
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  10. Artikel: Different geometric shaped hydrogel theophylline tablets: statistical approach for estimating drug release.

    Karasulu, H Yeşim / Ertan, Gökhan

    Farmaco (Societa chimica italiana : 1989)

    2002  Band 57, Heft 11, Seite(n) 939–945

    Abstract: The objective of this study was to develop a mathematical equation for the calculation of drug release from different shaped matrix tablets. By this way, release rate related to the geometric shape could be predicted with the help of the developed ... ...

    Abstract The objective of this study was to develop a mathematical equation for the calculation of drug release from different shaped matrix tablets. By this way, release rate related to the geometric shape could be predicted with the help of the developed mathematical equation. So, drug release could be estimated before the dissolution. Hydroxypropylmethylcellulose (HPMC) E50 as polymer and theophylline as active substance were used in the matrix tablets prepared for this purpose. Matrix tablets in three different geometrical shapes, namely in triangular, cylindrical and half-spherical forms were prepared by using two different drug-polymer ratio (1:0.5, 1:1) and diluent's in three different percentages (0, 20, 40%). Using rotating paddle and basket methods reported in USP XXIII carried out the release rate studies of these tablets. The Higuchi square-root time model best described the dissolution data. Differential scanning calorimetry (DSC) analysis was performed to identify any solid-state inactivation of the drug. The practical benefit of this work is to improve mathematical equation that can be used to predict accurately the required composition and in order to achieve the desired release profiles of different geometric shaped tablets. By using this equation new pharmaceutical products can be easily improved.
    Mesh-Begriff(e) Analysis of Variance ; Calorimetry, Differential Scanning ; Data Interpretation, Statistical ; Hydrogels ; Kinetics ; Reproducibility of Results ; Solubility ; Tablets ; Theophylline/analysis
    Chemische Substanzen Hydrogels ; Tablets ; Theophylline (C137DTR5RG)
    Sprache Englisch
    Erscheinungsdatum 2002-12-13
    Erscheinungsland France
    Dokumenttyp Journal Article
    ZDB-ID 130072-6
    ISSN 1879-0569 ; 0014-827X
    ISSN (online) 1879-0569
    ISSN 0014-827X
    DOI 10.1016/s0014-827x(02)01297-1
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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