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Iraqi Journal of Pharmaceutical Sciences
Number of Followers: 0  

  This is an Open Access Journal Open Access journal
ISSN (Print) 1683-3597 - ISSN (Online) 2521-3512
Published by U of Baghdad Homepage  [2 journals]
  • Formulation and Evaluation of Acyclovir Microspheres

    • Authors: Pavani s, Mounika K, Naresh K
      Pages: 1 - 7
      Abstract: The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.
      PubDate: 2018-06-03
      Issue No: Vol. 27, No. 1 (2018)
       
  • Investigation of Solubility Enhancement Approaches of Ticagrelor

    • Authors: Ihsan A. Mohammed, Mowafaq M. Ghareeb
      Pages: 8 - 19
      Abstract: ABSTRACT                    Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.                   Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10'g/mL at room temperature. Ticagrelor exhibits no pKa value within the physiological range. Ticagrelor does not exhibit pH-dependent solubility and is defined as ‘low solubility low permeability’ under the Biopharmaceutics Classification System (Class IV). The mean absolute bioavailability of ticagrelor in healthy volunteers is 36 %                    Nanoparticles preparation and complexation is one of the recently used approaches to enhance the solubility of drugs. The aim of the present work was to improve the solubility and dissolution of ticagrelor by preparing nanoparticles and cyclodextrin inclusion complex of ticagrelor and then incorporated in to tablet dosage form. Fifteen formulas of nanoparticles were prepared by antisolvent precipitation method (solvent displacement method) utilizing one of the three polymers (PVP, Poloxamer, and HPMC) at three different drugs: polymer and solvent: anti-solvent ratios and nine formulas of cyclodextrin inclusion complex with HP'CD  by three preparation methods, physical trituration, kneading and solvent evaporation, which increase the solubility and dissolution rate of ticagrelor via formation of inclusion complex with HP'CD.               The prepared formulas were characterized regarding the saturated solubility, polydispersity index, particle size by nano laser particle size analyzer, % yield, entrapment efficiency, and flowability, FTIR, DSC, and SEM. The selected formulas were prepared as tablets.              The prepared tablets were evaluated for drug content, weight variation, hardness, and friability. In vitro dissolution data of the prepared tablets were analyzed using similarity factor (f2) and dissolution efficiency (DE).              Among all the prepared nanoparticles formulas, formula (F12) which contain HPMC as a polymer at polymer: drug ratio of (1:1) and solvent: antisolvent ratio of (1:1) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 9 times than that of the pure drug. The nanoparticle of the selected formula (F12) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 88 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the selected formula is a promising formula for the preparation of ticagrelor nanoparticles the incorporation in a tablet dosage form.           Regarding ticagrelor inclusion complex with HP'CD Solvent evaporation method was the most effective method regarding ticagrelor solubilization and optimum formula of inclusion complex (F23) show increment in saturated solubility about ten times that of pure drug.           The ticagrelor inclusion complex of the selected formula (F23) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 90 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).    
      PubDate: 2018-06-03
      Issue No: Vol. 27, No. 1 (2018)
       
  • Dissolution Enhancement of Raltegravir by Hot Melt Extrusion Technique

    • Authors: Ahmed S. Abdul Jabbar
      Pages: 20 - 29A
      Abstract: The objective of the study to develop an amorphous solid dispersion for poorly soluble raltegravir by hot melt extrusion (HME) technique. A novel solubility improving agent plasdone  s630 was utilized. The HME raltegravir was formulated into tablet by direct compression method. The prepared tablets were assessed for all pre and post-compression parameters. The drug- excipients interaction was examined by FTIR and DSC. All formulas displayed complying with pharmacopoeial measures. The study reveals that formula prepared by utilizing drug and plasdone S630 at 1:1.5 proportion and span 20 at concentration about 30mg (trail-6) has given highest dissolution rate than contrasted with various formulas of raltegravir. Keywords: Hot melt extrusion, Raltegravir, Plasdone S630.
      PubDate: 2018-06-04
      Issue No: Vol. 27, No. 1 (2018)
       
  • phytochemical investigations of Iraqi Abrus precatorius Linn. plant

    • Authors: Zahra'a S. Nassir, Enas J. Khadem
      Pages: 30 - 38
      Abstract:     The plant Abrus precatorius, which belong to Leguminosae (Fabaceae) family and known as Crab’s eyes, Rosary pea with characteristic red and black seeds. It was used in folk medicine in India, China and East Asian countries for treatment of various diseases.    The plant was extracted by '' general method of extraction'' (Harborne, 1973) using 80% aqueous ethanol as a solvent of extraction by soxhlet apparatus. Preliminary qualitative phytochemical screening were performed on the crude ethanolic extract  and revealed the presence of alkaloids, flavonoids ,terpenoids and phytosterols in Iraqi Abrus precatorius plant. Three different fractions were obtained from crude extract which are fraction one (chloroform fraction), fraction two (ethyl acetate fraction), and fraction three (petroleum ether fraction) which are represent alkaloids, flavonoids and steroids respectively. The alkaloid abrine was isolated from the chloroform fraction  in pure form by using preparative thin layer chromatography (PTLC) and then subjected to different physico-chemical and specteral analytical techniques to identify its chemical structure: melting point (M.P.), thin layer chromatography (TLC), high performance liquid chromatography (HPLC) , fourier transforms infrared spectra (FT-IR) and elemental microanalysis (CHNO).      
      PubDate: 2018-06-03
      Issue No: Vol. 27, No. 1 (2018)
       
  • Preparation and characterization of domperidone nanoparticles for
           dissolution improvement

    • Authors: Mohammed Sabar Al-lami, Malath H. Oudah, Firas A. Rahi
      Pages: 39 - 52
      Abstract: This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p' 0.05) effect on particle size. The best formula was obtained with lowest average particle size of 84.05. This formula was studied for compatibility by FTIR and DSC, surface morphology by FESEM and crystalline state by XRPD. Then domperidone nanoparticles were formulated into a simple capsule dosage form in order to study of the in vitro release of drug from nanoparticles in comparison raw drug and mixture of polymer:drug ratios of 2:1. The release of domperidone from best formula was highly improved with a significant (p' 0.05) increase.
      PubDate: 2018-06-03
      Issue No: Vol. 27, No. 1 (2018)
       
  • Darifenacin Hydrobromide loaded nanostructured lipid carrier for oral
           administration

    • Authors: Ali kathem Ala Allah, Ahmed Hussein
      Pages: 53 - 68
      Abstract: Darifenacin hydrobromide is a selective '3 receptor antimuscarinic drug and it is used in the management of urinary frequency, urgency, and incontinence in detrusor instability. It slightly soluble in water, undergoes extensive hepatic first-pass metabolism and has short elimination half-life (3–4 hours). Therefore, It has low bioavailability (15.4 % - 18.6 %). Darifenacin hydrobromide loaded NLCs were formulated by emulsification sonication using different ratios of solid lipid to liquid lipid, different types of surfactants, and different concentration of surfactants. Formula sixteen was considered as an optimized formula based on its particle size, PDI, zeta potential and entrapment efficiency. Formula sixteen subjected to further characterization such as DSC, FT – IR, XRD, AFM, and release study. FT-IR and DSC studies showed no interaction between drug and excipients. XRD study showed that drug in amorphous form. AFM study showed discrete lipid nanoparticles with no aggregation. Release study showed burst release in the first hour followed by sustained and controlled release up to 12 hours. The over all study showed the potential of NLC as a carrier for enhancing the bioavailability of darifenacin hydrobromide as compared to the conventional dosage form. Key words: Darifenacin hydrobromide, nanostructured lipid carrier, bioavailability.
      PubDate: 2018-06-04
      Issue No: Vol. 27, No. 1 (2018)
       
  • Synthesis and antimicrobial evaluation with DFT study for new thiazole
           derivatives

    • Authors: Sumayah Saadi Abbas, Ammar A.Razzak Mahmood Kubba
      Pages: 69 - 78
      Abstract: Two compounds,[2-amino-4-(4-nitro phenyl) 1,3-thiazole],(4) and [2-amino-4-(4-bromo phenyl) 1,3-thiazole],(5), were synthesized by refluxing thiourea (1) with each of  para-ntiro and para-bomophanacyl bromides(2) and (3) respectively, in absolute methanol. Then, by reaction of [5] with 3,5-dinitrobenzoyl chloride in dimethylformamide (DMF) yielded  (6) .On the other hand, reaction of (4) with chloroacetyl chloride in dry benzene afforded (7), which is  upon treatment with thiourea in absolute methanol, afforded (8) . The characterization of the titled compounds were done utilizing FTIR spectroscopy, 1HNMR, CHNS elemental analysis and by measurements of  their physical properties. The synthesized compounds had been screened for their, in vitro  preliminary antimicrobial activity against four Gram positive bacteria (Staph. aureus, Micrococcus luteus, Bacillus subtilis and Bacillus pumilus),  and four Gram negative bacteria (Pseud.aeroginosa, E.coli, Proteus mirabilis and Klebsiella pneumoniae)and three fungi species: (Saccharomyces cerevisiae, Candida Tropicalis and Candida albicans) using a minimum  inhibitory concentration (MIC) of 100 µg\ml of derivative  in dimethylsulfoxide, by  well diffusion method. Compound (6) showed moderate antibacterial activity against some tested Gram positive bacteria (Bacillus pumilus and Bacillus Subtilis) and a moderate antifungal activity towards Candida albicans. Computational study was performed   to calculate some of the thermodynamic parameters of synthesized derivatives by using density functional theory (DFT).
      PubDate: 2018-06-04
      Issue No: Vol. 27, No. 1 (2018)
       
  • Synthesis, Characterization and Antimicrobial Evaluation with DFT Study of
           New Two-Amino-4-(4-Chlorophenyl) Thiazole Derivatives

    • Authors: Ammar A Mahmood Kubba, Nedaa A. A. Rahim
      Pages: 79 - 88
      Abstract: 2-amino-4-(4-chloro phenyl)-1,3-thiazole (1) was synthesized by refluxing thiourea with para-chloro phenacyl bromide in absolute methanol. The condensation of amine compound (1)  with phenylisothiocyanate in the presence of pyridine will  produce 1-(4-(4-chlorophenyl)thiazol-2-yl)-3-phenylthiourea(2), which is  upon treatment with 2,4 dinitrophenyl hydrazine by conventional method, afforded 1- ( 4 - ( 4 – chlorophenyl ) thiazol – 2 – yl ) – 3 - phenylhydrazonamide,N' - ( 2 , 4 -dinitrophenyl) ,(3).The characterization of the titled compounds were performed utilizing FTIR spectroscopy, 1HNMR and CHNS elemental analysis, and by measurements of  their  physical properties.  The synthesized compounds had been screened for their, in vitro  preliminary antimicrobial activity against three Gram-positive bacteria: (Staph. aureus, Micrococcus luteus and  Bacillus subtilis) and three Gram-negative bacteria : (Pseud.aeruginosa, E.coli and  Proteus mirabilis) ,and two fungal strains(Candida albicans and Candida glabrata ), using a minimum  inhibitory concentration (MIC) of 100 µg\ml of  test compound, by  well diffusion method.  The derivatives showed moderate antibacterial activity against Gram-positive Staphylococcus aureus and Bacillus subtilis & high antifungal activity against Candida glabrata and Candida albicans. Computational study was performed to calculate some of thermodynamic parameters by using density functional theory (DFT)
      PubDate: 2018-06-20
      Issue No: Vol. 27, No. 1 (2018)
       
  • Preparation and characterization of timed drug delivery system of
           sumatriptan using natural polymers

    • Authors: Mina Shihab Al-anbagi, Nawal A. Rajab, Yehia I.Khalil
      Pages: 89 - 99
      Abstract: Pulsatile drug delivery systems are time-controlled dosage forms which are designed to release the active pharmaceutical ingredient after a predetermined lag time to synchronize the disease circadian rhythm. A migraine shows circadian rhythm with a marked increase in attacks between 6 a.m. and 8 a.m. Sumatriptan is a selective agonist at serotonin (5-Hydroxy tryptamine1  (5-HT1))receptors, is an effective treatment for acute migraine attacks. The aim of this work is to prepare time-controlled press-coated tablet with a lag time of 5.45 hrs. Six formulas of fast dissolving core tablets and three formulas of press-coated tablets were prepared by using direct compression method using different variables to prepare core tablets which include: different types and concentrations of superdisintegrants While different concentrations of natural and synthetic polymers were utilized in the preparation of press-coated tablets. The obtained results showed that formula  F4 of core tablet, which contained 25 mg of sumatriptan, 5% w/w sodium starch glycolate and avicel PH 102 as the diluent, was the selected formula that gave the fastest and complete release of sumatriptan. Also, formula C3 of the press-coated tablet, which contained pectin: EC100 mpa.s: HPMCK15M in concentration30mg: 10mg:160mg respectively, was selected as the best coating layer since it gave 5.45  hours lag time.
      PubDate: 2018-06-05
      Issue No: Vol. 27, No. 1 (2018)
       
  • Synthesis, Characterization and Alpha Glucosidase Inhibition activity of
           new Phthalimide Derivatives

    • Authors: Hassan ALi, Mohammed H. Mohammed, Sajida H. Ismeal
      Pages: 100 - 108
      Abstract:  Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as the end products (5a-j) while  the compounds (5k-o) required further reaction to deprotect aliphatic amine this achieved by treating the compounds with TFA to remove tert-Butoxycarbonyl group (6a-e). The alpha glucosidase inhibitory activity of some synthesized compounds (5a, 5f, 6a) were tested by using  -glucosidase from Saccharomyces cerevisiae, p-nitrophenol glucopyranoside (pNPG)  used as substrate and acarbose used as standard. All these test compounds shows   excellent inhibitory activity according to IC50 values which is ranging from (4.61-7.32).
      PubDate: 2018-06-05
      Issue No: Vol. 27, No. 1 (2018)
       
 
 
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