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Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).

Sci. Pharm., Volume 74, Issue 4 (December 2006) – 5 articles , Pages 159-223

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1441 KiB  
Article
Development of bioadhesive chitosan gels for topical delivery of lidocaine
by Jaleh Varshosaz, Fariba Jaffari and Sara Karimzadeh
Sci. Pharm. 2006, 74(4), 209-223; https://doi.org/10.3797/scipharm.2006.74.209 - 30 Dec 2006
Cited by 45 | Viewed by 1748
Abstract
Lidocaine (LC) is a local anesthetic agent. The aim of this study is prolonging the anesthetic effect of this drug for transdermal delivery. Gels of LC hydrochloride were prepared with three different molecular weights (MW) and concentrations of chitosan. lecithin was used as [...] Read more.
Lidocaine (LC) is a local anesthetic agent. The aim of this study is prolonging the anesthetic effect of this drug for transdermal delivery. Gels of LC hydrochloride were prepared with three different molecular weights (MW) and concentrations of chitosan. lecithin was used as permeation enhancer. Viscosity, bioadhesion, drug release from synthetic membranes, drug permeation through the biological barrier (rat skin) and antinocicetive effect of gels were studied. Increasing the concentration of chitosan caused to decrease the bioadhesion. Drug release studies in gels showed that increasing the concentration and MW of chitosan caused an increase in both the rate and extent and also in flux of drug probably because of the increase in repulsive forces between LC and chitosan cations. The flux of drug through the rat skin was higher for 3% high MW chitosan gel (H3) compared to the standard gel. LC was effective topically in hind paw formalin assay. It was most active immediately after its administration. The analgesic activity of LC in H3 gel could cover the duration of the formalin nociception. The maximal response of LC in comparable doses of H3 and standard gel was about 52% and 36% analgesia in the second phase, respectively compared to the control group. The higher response of the H3 gel may be attributed to the bioadhesive effect of chitosan base and the higher concentrations of LC compared to the standard gel. Full article
1369 KiB  
Article
Constituents from the leaves of Crataegus davisii Browicz
by Ulaş Sözer, Ali A. Dömnez and Ali H. Meriçli
Sci. Pharm. 2006, 74(4), 203-208; https://doi.org/10.3797/scipharm.2006.74.203 - 30 Dec 2006
Cited by 18 | Viewed by 1237
Abstract
From the leaves of Crataegus davisii five flavonoids ( hyperoside, vitexin 2’’- rhamnoside, vitexin 4’-rhamnoside, rutin, quercetin ) together with chlorogenic acid and crataequinone B were isolated. The flavonoid content of the leaves was determined according to DAB 10 and found as 1.09 [...] Read more.
From the leaves of Crataegus davisii five flavonoids ( hyperoside, vitexin 2’’- rhamnoside, vitexin 4’-rhamnoside, rutin, quercetin ) together with chlorogenic acid and crataequinone B were isolated. The flavonoid content of the leaves was determined according to DAB 10 and found as 1.09 %. The IC50 value was found as 1.57 mg/ml at antioxidant activity determination with DPPH method. Full article
1424 KiB  
Article
Constituents from the leaves of Crataegus davisii Browicz
by Ulas Sözer, Ali A. Dönmez and Ali H. Meriçli
Sci. Pharm. 2006, 74(4), 189-201; https://doi.org/10.3797/scipharm.2006.74.189 - 30 Dec 2006
Cited by 63 | Viewed by 1635
Abstract
From the leaves of Crataegus davisii five flavonoids ( hyperoside, vitexin 2’’- rhamnoside, vitexin 4’-rhamnoside, rutin, quercetin ) together with chlorogenic acid and crataequinone B were isolated. The flavonoid content of the leaves was determined according to DAB 10 and found as 1.09 [...] Read more.
From the leaves of Crataegus davisii five flavonoids ( hyperoside, vitexin 2’’- rhamnoside, vitexin 4’-rhamnoside, rutin, quercetin ) together with chlorogenic acid and crataequinone B were isolated. The flavonoid content of the leaves was determined according to DAB 10 and found as 1.09 %. The IC50 value was found as 1.57 mg/ml at antioxidant activity determination with DPPH method. Full article
1487 KiB  
Article
Chitosan Beads as a New Gastroretentive System of Verapamil
by Alaa Eldeen B. Yassin, Ibrahim A. Alsarra and Abdulah M. Al-Mohizea
Sci. Pharm. 2006, 74(4), 175-188; https://doi.org/10.3797/scipharm.2006.74.175 - 30 Dec 2006
Cited by 33 | Viewed by 1580
Abstract
The main objective of this project is to design a new extended release gastroretentive mutiparticulate delivery system for verapamil (VP) by incorporation into hydrogel beads made of chitosan. The beads were formed by dropping solutions of VP and chitosan in a solution of [...] Read more.
The main objective of this project is to design a new extended release gastroretentive mutiparticulate delivery system for verapamil (VP) by incorporation into hydrogel beads made of chitosan. The beads were formed by dropping solutions of VP and chitosan in a solution of tripolyphosphate using a syringe pump with adjustable constant rate. The formed beads were then further crosslinked using glutraldehyde and the excess glutraldehyde were then washed. The physical properties of the prepared beads such as beads sizes, shapes, friabilities and loading efficiencies were determined. The floating characteristics and the release profiles were also studied. The produced beads from all batches showed a very good spherical geometry with mean diameter in the range of 1.3 – 2.0 mm. The drug loading efficiency was around 42% for all batches. The % friabilities were less than 1% indicating that the beads surfaces are highly resistant to attrition. Batches B3 and B4 (prepared using medium molecular weight chitosan) showed both the slowest release rate among all the prepared batches and showed good floating characteristics comprising short onset (around 5 minutes) and the long duration of buoyancy (more than 6 hours). All the batches exhibited a kinetic model of combined mechanism of diffusion partially through a swollen matrix and partially through water-filled pores. The preparation of chitosan beads using this technique would provide a simple and commercially viable method of preparation of chitosan beads for controlling the release of some drugs. Full article
1484 KiB  
Article
Beneficial Interaction of Thymoquinone and Sodium Valproate in Experimental Models of Epilepsy: Reduction in Hepatotoxicity of Valproate
by Muhamma Raza, Abdullah A. Alghasham, Mohammad S. Alorainy and Tarig M. El-Hadiyah
Sci. Pharm. 2006, 74(4), 159-173; https://doi.org/10.3797/scipharm.2006.74.159 - 30 Dec 2006
Cited by 18 | Viewed by 1500
Abstract
The antiepileptic potential of thymoquinone (TQ) was studied in mice by using pentylenetetrazole (PTZ) and maximal electroshock seizure (MES)-induced convulsion models. In this investigation, the combined treatment of TQ and sodium valproate (SVP) was also studied. The aim of this part was to [...] Read more.
The antiepileptic potential of thymoquinone (TQ) was studied in mice by using pentylenetetrazole (PTZ) and maximal electroshock seizure (MES)-induced convulsion models. In this investigation, the combined treatment of TQ and sodium valproate (SVP) was also studied. The aim of this part was to minimize SVPinduced hepatotoxic implications, by reducing its antiepileptic dose. TQ in both PTZ- and MES- models increased SVP potency. The experiments dealing with the effects of TQ on the ED50 of SVP revealed that TQ reduced the ED50 of SVP in both the models. However, this potentiation of SVP antiepileptic response was relatively more significant in PTZ model at both 50 and 100 mg/kg doses of TQ. Although very well tolerated and effective, SVP is well known for its hapatotoxic implications. In the experiment dealing with subacute treatment, SVP (1300-1500mg/kg/day in drinking water) for 21 days, produced hepatotoxicity in mice, characterized by elevated serum ALT and AST, reduced levels of non protein sulfhydryls and increase in lipid peroxidation in hepatic cells. Hepato-protection was successfully achieved when TQ (5-5.5mg/kg/day) was combined with SVP in drinking water for the same duration. The protective activity of TQ was evident by averting any serum ALT rise seen in SVP treatment. Though there is no prevention to the rise in lipid peroxidation in hepatic tissue but the same time a significant recovery in glutathione was evident by TQ joint treatment. However, a combination of TQ and low dose of SVP may be useful strategy to minimize adverse reactions of SVP. From the results of the present study that disclosed a protective role of TQ against SVP toxic damage to the liver, it could be mentioned safely that TQ behaves as an antioxidant and protected liver against its harmful effects. It also protected against the liver enzyme induction seen in the case of SVP alone. Full article
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