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Sci. Pharm.
Volume 71
Issue 4
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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 71, Issue 4 (December 2003) – 6 articles , Pages 263-364

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2319 KiB  
Article
In vitro Studies on Sustained Release Suppository Formulations of Tiaprofenic Acid with Sucrose Fattv Acid Ester
by Sevgi Gūngör, Mine Orlu, Yildiz Özsoy and Ahmet Araman
Sci. Pharm. 2003, 71(4), 357-364; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-29 - 15 Dec 2003
Cited by 1 | Viewed by 894
Abstract
The objective of this study was to evaluate the performance of Sucro Ester 7 (sucrose distearate) as additive for preparing sustained release suppositories of tiaprofenic acid. Suppocire AIM (semi-synthetic glycerides) was used as suppository base and formulations were prepared containing different ratios of [...] Read more.
The objective of this study was to evaluate the performance of Sucro Ester 7 (sucrose distearate) as additive for preparing sustained release suppositories of tiaprofenic acid. Suppocire AIM (semi-synthetic glycerides) was used as suppository base and formulations were prepared containing different ratios of sugar ester: Suppocire AIM. Content uniformity, disintegration time and in vitro release characteristics of suppositories were investigated. Significant decrease in the extent of drug release was observed with the increase in the content of sugar ester, which was due to the longer disintegration time of suppositories. Full article
8070 KiB  
Article
Synthesis and Pharmacological Evaluation of Fenamate Analogues: 1,3,4-Oxadiazol-2-ones and 1,3,4-Oxadiazole-2-thiones
by Aida A. El-Azzouny, Yousreya A Maklad, Herbert Bartsch, Wafaa A. Zaghary, Waleed M. Ibrahim and Mosaad S. Mohamed
Sci. Pharm. 2003, 71(4), 331-356; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-28 - 01 Dec 2003
Cited by 18 | Viewed by 1116
Abstract
A series of fenamate pyridyl or quinolinyl analogues of 1,3,4-oxadiazol-2-ones 5a-d and 6a-r, and 1,3,4-oxadiazole-2-thiones 5e-g and 6s-v, respectively, have been synthesized and evaluated for their analgesic (hot-plate) , antiinflammatory (carrageenin induced rat's [...] Read more.
A series of fenamate pyridyl or quinolinyl analogues of 1,3,4-oxadiazol-2-ones 5a-d and 6a-r, and 1,3,4-oxadiazole-2-thiones 5e-g and 6s-v, respectively, have been synthesized and evaluated for their analgesic (hot-plate) , antiinflammatory (carrageenin induced rat's paw edema) and ulcerogenic effects as well as plasma prostaglandin E2 (PGE2) level. The highest analgesic activity was achieved with compound 5a (0.5 ,0.6 ,0.7 mrnolkg b.wt.) in respect with mefenamic acid (0.4 mmollkg b.wt.). Compounds 6h, 6l and 5g showed 93, 88 and 84% inhibition, respectively on the carrageenan-induced rat's paw edema at dose level of 0.1rnrnol/kg b.wt, compared with 58% inhibition of mefenamic acid (0.2mmoll kg b.wt.). Moreover, the highest inhibitory activity on plasma PGE2 level was displayed also with 6h, 6l and 5g (71, 70,68.5% respectively, 0.lmmolkg b.wt.) compared with indomethacin (60%, 0.01 mmolkg b.wt.) as a reference drug. In addition 6i, 6k, 6p, 6r, 6t and 6v were devoid of any ulcerogenicity. Full article
2579 KiB  
Article
Effects Of 2-Methvl-3-propvnvlauinazolin-4-(3H)-one On Vascular Reactivitv In Isolated Porcine Tail Arteries
by Odafenkhoa Ojeikere, Cyril Usifoh and Anthony Ebeigbe
Sci. Pharm. 2003, 71(4), 321-329; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-27 - 10 Nov 2003
Cited by 1 | Viewed by 871
Abstract
The vascular effects of 2-methyl-3-propynylquinazolin-4-(3H)-one (QUIN) have been studied on isolated porcine tail arteries. QUlN had no effect on resting tension but relaxed, dose-dependently, arteries precontracted with noradrenaline or high-K+ in the order: NA > high-K+. Also, QUlN [...] Read more.
The vascular effects of 2-methyl-3-propynylquinazolin-4-(3H)-one (QUIN) have been studied on isolated porcine tail arteries. QUlN had no effect on resting tension but relaxed, dose-dependently, arteries precontracted with noradrenaline or high-K+ in the order: NA > high-K+. Also, QUlN inhibited both intracellular (ICD) and extracellular (ECD) Ca2+-dependent contractions in the order: ICD > ECD The results suggest that QUlN interferes with vascular Ca2+ mobilization. Full article
4878 KiB  
Article
Ratio Derivative S~ectrophotometricM ethod for the Determination of Some Oxicams in Presence of their Alkaline Dearadation Products
by Elham Anwer Taha, Eman Saad El- Zanfally and Nahla Nour Salama
Sci. Pharm. 2003, 71(4), 303-320; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-26 - 30 Oct 2003
Cited by 10 | Viewed by 979
Abstract
A new spectrophotometric method has been developed for the determination of some oxicams namely, lornoxicam (LX) , tenoxicam (TX) and meloxicam (MX), in the presence of their main alkaline degradation products, 2-aminopyridine ( I ) and 2-amino-5-methylthiazole (II) for (TX&MX), 2-aminopyridine and TX [...] Read more.
A new spectrophotometric method has been developed for the determination of some oxicams namely, lornoxicam (LX) , tenoxicam (TX) and meloxicam (MX), in the presence of their main alkaline degradation products, 2-aminopyridine ( I ) and 2-amino-5-methylthiazole (II) for (TX&MX), 2-aminopyridine and TX for lornoxicam. The method is based on the use of the first derivative of the ratio spectra (1DD) of the mentioned compounds and their corresponding degradates. The procedure does not require any separation steps. Linear calibration graphs of 1DD were obtained by measurement of the amplitudes at 316, 249 and 260nm for LX, 248.8 , 258.8 nm for TX and 287.2nm for MX. On carrying out measurements at the above mentioned wavelengths, the linearity range is found to be 2.5 - 35 μg ml-1 for LX and TX, 1.25 - 30 μg ml-1 for MX. The validity of the method was assessed by applying the standard addition technique. Statistical analysis of the results has been carried out revealing high accuracy and good precision. The suggested procedure could be used for the determination of the above mentioned drugs in pure and dosage forms as well as in presence of their degradation products. Full article
7090 KiB  
Article
Development of Buccoadhesive Systems of Pentarocine for Systemic Drug Delivery
by D. Sampathkumar, M. Thilek Kumar, J. Balasubrarnaniam and J. K. Pandit
Sci. Pharm. 2003, 71(4), 281-301; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-25 - 15 Oct 2003
Cited by 1 | Viewed by 868
Abstract
Bucoadhesive patches of Pentazocine (PZ) for unidirectional drug delivery were prepared by casting carboxy methyl cellulose (CMC) with glycerol or propylene glycol and CMC-hydroxy ethyl cellulose (HEC) with glycerol. In vitro mucoadhesivity of the prepared patches were determined using a modified mucoadhesive bond [...] Read more.
Bucoadhesive patches of Pentazocine (PZ) for unidirectional drug delivery were prepared by casting carboxy methyl cellulose (CMC) with glycerol or propylene glycol and CMC-hydroxy ethyl cellulose (HEC) with glycerol. In vitro mucoadhesivity of the prepared patches were determined using a modified mucoadhesive bond strength apparatus using rabbit small intestine mucosa (SIM). Drug release kinetics was evaluated from composite patches, prepared by covering all but one side of the PZ patches with 3M backing material. Biocompatability / buccoadhesion time and in vivo permeation of placebo and PZ loaded patches were determined using a double blind cross over study in healthy human volunteers. Drug release from CMC-glycerol patches and pure HEC patches showed zero order kinetics with diffusional exponent (n) ranging between 0.79 to 1.046, while that from CMC-HEC and CMC-propylene glycol patches showed an apparent zero order release kinetics. The prepared patches were well tolerated by the human volunteers as they did not produce any side effects at the contact surface. The in vitro mucoadhesivity of CMC-propylene glycol patches were significantly lower than CMC- glycerol based patches. The in vivo permeation of selected PZ patches delivered the drug well above the minimum buccal permeation rate, so as to attain effective blood concentration Full article
5225 KiB  
Article
Struktur und Eigenschaften des Benzidinblau-Chromophors N,N'-unsubstituierter Benzidine
by H.-J. Kallmayer and B. Trojan
Sci. Pharm. 2003, 71(4), 263-279; https://0-doi-org.brum.beds.ac.uk/10.3797/scipharm.aut-03-24 - 01 Oct 2003
Cited by 2 | Viewed by 831
Abstract
Die Benzidine A-E werden mit verschiedenen Oxidationsmitteln oxidiert und die entstehenden Benzidinblau-Chromophore isoliert. Spektrale Daten, Löseeigenschaften sowie die Farbigkeit und deren pH-Abhängigkeit charakterisieren die Benzidinblau-Chromophore als cr -Komplexe 7 und nicht als Radikalkationen 4. Full article
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