Aim: The present study aims to improve the poor water solubility of zaltoprofen which is a non-steroidal anti-inflammatory drug (NSAIDs) with a potent analgesic effect using solid dispersion then formulate it as a hollow type suppository to be more convenient for geriatric patients. Materials and Method: Zaltoprofen solid dispersions were prepared by solvent evaporation technique in different zaltoprofen: Soluplus® ratios. Results: Among the formulations tested, zaltoprofen solid dispersion preparation using 1:5 (zaltoprofen: Soluplus®) ratio showed the highest solubility and selected for further investigation. Solid dispersion characterization was evaluated by differential scanning calorimetry (DSC), X-ray diffraction study (XRD) and Fourier transformation infrared spectroscopy (FTIR). DSC and XRD analysis showed a complete transformation of zaltoprofen in the solid dispersion from a crystalline state to amorphous state. The selected zaltoprofen solid dispersion was further incorporated into hollow type suppositories using witepsol H 35 as a suppositories base. The hollow type suppositories were evaluated for hardness test (breaking strength), melting time, softening time and in vitro drug dissolution rate. Formula F8 containing zaltoprofen solid dispersion in the whole of hollow type suppository showed the shortest and significantly the highest dissolution rate profile (100% within 15 min) compared to other hollow type suppository formulas prepared that contain zaltoprofen powder in its whole. Conclusion: It is concluded that the development of zaltoprofen solid dispersions using Soluplus® as hollow-type suppositories could be used as a promising approach for improving the solubility of poorly water-soluble drugs
Schiff bases (Sh1-Sh3) have been synthesized (p-aminophenol) was condensed with different aromatic aldehyde in ethanol inthe presence of glacial acetic acid as catalyst. These Schiff bases on treatment with monochloroacetyl choride gave 3-chloro-1-(4-hydroxyphenyl)-4-(substituted)azetidin-2-one(Az4-Az6), with αmercaptoacetic acid gave 3-(4-hydroxyphenyl)-2-( substituted)thiazolidin-4-one (Th7-Th9) and with anthranilic acid gave 3-(4-hydroxyphenyl)-2(substituted)-2,3-dihydroquinazolin-4(1H)-one (Qu10-Qu12). The purity of the derivatives was confirmed by TLC. The some compoundsidentify by (FT-IR and1H, 13C-NMR) data. Some of derivatives were evaluated activity against several microbesto determine ability to inhibit bacterial in some h
... Show MoreTo assess the biochemical, mechanical and structural characteristics of retained dentin after applying three novel bromelain‑contained chemomechanical caries removal (CMCR) formulations in comparison to the conventional excavation methods (hand and rotary) and a commercial papain‑contained gel (Brix 3000). Seventy‑two extracted permanent molars with natural occlusal carious lesions (score > 4 following the International Caries Detection and Assessment System (ICDAS‑II)) were randomly allocated into six groups (n = 12) according to the excavation methods: hand excavation, rotary excavation, Brix 3000, bromelain‑contained gel (F1), bromelain‑chloramine‑T (F2), and bromelain chlorhexidine gel (F3). The superficial and deepe
... Show MoreAbstract
Lack of safe available non-resistant treatment for visceral leishmaniasis (Kala-azar) keeps limiting the complete cure of this disease ,drugs that have toxic side effects or lack of effectiveness have led to disease relapse ,all these factors have lightened the way to the search for imperative drugs from natural resources that have been shown to have antileishmanial activity through literature survey
. In the present study, the comparative in vitro anti-leishmania activity of various fractions of Osteospermum ecklonis aerial parts fractions have been evaluated. Extracts were prepared through maceration and Soxhlet apparatus using 85% meth
... Show MoreTill now, isatin derivatives have received a lot of interest in organic and medicinal chemistry due to their significant biological and pharmacological activities. Schiff’s and Mannich bases of isatins are an effective group of heterocyclic derivatives that play a significant role in medicinal chemistry as antimicrobial agents. In light of these facts, new Schiff bases and Mannich bases of isatin were synthesized. The monomer Mannich bases; 3(a-e) have been synthesized by reacting isatin with different secondary amines, piperidine, morpholine, and pyrrolidine, dimethylamine, diphenylamine, separately, and formaldehyde, while the dimer (5) formed by using piperazine and formaldehyde which then react separately with Phenylhydrazine
... Show MoreAmoxicillin 1 was treated with thiosemicarbazide and Phosphoryl chloride to obtain a new derivatives that contains 1,3,4-thiadiazole moiety 2. Schiff bases compounds were synthesized by the reaction of compound 2 with different aldehydes such as benzaldehyde and some substituted Benzaldehyde; p-hydroy, p-Chloro, p-Nitro, p-Dimethylamino, p-Methyl, p-Methoxy, p-Ethoxy to give compounds 3a-h. The obtained compounds have tested towards gram -ve and gram +ve bacteria. The compound shows good to moderate result towards the bacteria.
Background: This in vitro study compares a self-etch primer (SEP) to an etch-and-rinse (EaR) for bonding sapphire brackets by evaluation of the enamel etch-pattern, shear bond strength, amount of remnant adhesive and enamel surface damage following thermal and fatigue cyclic loading. Material and Methods: Ceramic (sapphire) brackets were bonded to 80 extracted human premolars using two enamel etching protocols: conventional EaR using 37% phosphoric acid (PA) gel (control), and a SEP (Transbond Plus). Each group was subdivided into two subgroups (n=20 teeth) according to the time of bracket debonding: after 24 h water storage or following 5000 thermo-cycles plus 5000 cycles fatigue loading, to determine the shear bond strength (SBS), adhesiv
... Show MoreThis study was performd on 50 serum specimens of patients with type 2 diabetes, in addition, 50 normal specimens were investigated as control group. The activity rate of LAP in patients (560.46 10.504) I.U/L and activity rate of LAP in healthy(10.58 4.39)I.U/L.The results of the study reveal that Leucine aminopeptidase (LAP) activity of type 2 diabetes patient s serum shows a high signifiacant increase (p < 0.001) compare to healthy subjects. Addition preparation leucine amide as substrate of LAP, identification melting point and spectra by FTIR. K