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Sci. Pharm.
Volume 77
Issue 2
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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 77, Issue 2 (June 2009) – 13 articles , Pages 309-496

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240 KiB  
Article
NF-κB Inhibitory Activities of the Methanol Extracts and some Constituents therein of some Vietnamese Medicinal Plants
by Nguyen H. NAM and You Y. JAE
Sci. Pharm. 2009, 77(2), 389-400; https://doi.org/10.3797/scipharm.0903-15 - 14 May 2009
Cited by 12 | Viewed by 1606
Abstract
Eighty-seven methanol extracts of medicinal plants, most of them are currently used in Vietnamese oriental medicine, were screened for NF-κB inhibitory activity. Seven methanol extracts showed strong to moderate inhibitory activity. These include the extracts of Crinum latifolium (leaves), Evodia rutaecarpa (fruits), Polygonum [...] Read more.
Eighty-seven methanol extracts of medicinal plants, most of them are currently used in Vietnamese oriental medicine, were screened for NF-κB inhibitory activity. Seven methanol extracts showed strong to moderate inhibitory activity. These include the extracts of Crinum latifolium (leaves), Evodia rutaecarpa (fruits), Polygonum cuspidatum (rhizoma), Perilla ocymoides (leaves), Rubia cordifolia (leaves), Scutellaria barbata (leaves) and Sparganium stenophyllum (leaves). The NF-κB inhibitory activities of several metabolites isolated from some of these plants were also reported. Full article
221 KiB  
Editorial
Scientia Pharmaceutica, Autorenhinweise 2009
by Scientia Pharmaceutica Editorial Office
Sci. Pharm. 2009, 77(2), 483-496; https://doi.org/10.3797/scipharm.aut-09-02 - 05 May 2009
Viewed by 922
Abstract
n/a Full article
416 KiB  
Article
Formulation and Evaluation of Diltiazem Hydrochloride Gels for the Treatment of Anal Fissures
by Sanju DHAWAN, Bikash MEDHI and Sunny CHOPRA
Sci. Pharm. 2009, 77(2), 465-482; https://doi.org/10.3797/scipharm.0903-10 - 05 May 2009
Cited by 21 | Viewed by 2788
Abstract
The treatment for chronic anal fissure (CAF) has undergone a transformation in recent years from surgical to medical. Both the approaches share the common goal of reducing the spasm of anal sphincter. Though surgical treatment has a high success rate but it can [...] Read more.
The treatment for chronic anal fissure (CAF) has undergone a transformation in recent years from surgical to medical. Both the approaches share the common goal of reducing the spasm of anal sphincter. Though surgical treatment has a high success rate but it can permanently impair fecal continence in large number of patients. Smooth muscle relaxation seems to be a novel way by which more than 60% of the patients can be cured with the topical use of the agents. In the present investigation, diltiazem hydrochloride gels were prepared using FDA recommended polymers [hydroxypropylmethyl cellulose (HPMC), methylcellulose (MC) and polyethylene oxide (PEO grade 301 and 303)] for topical application in CAF. Increasing the concentration of the polymer significantly increased the consistency of the gels. All the formulations exhibited pseudoplastic flow with no thixotropy. The values of flow index (n) were found to be less than one for all the gels confirming the shear thinning behaviour of all the gels. HPMC and MC gels were found to be stable at accelerated stability conditions while the bioadhesion of PEO gels was highest. Even after exposure to heat and humidity, no significant change was observed in the content uniformity, pH, clarity, texture profile analysis and rheological properties of the HPMC and MC gels. The rheograms and various power law equation parameters of these gels were found comparable at various time points in the accelerated stability study. However, PEO gels failed in accelerated stability studies at one month sample. When four selected gel formulations (HPMCL4, MCL3, P1BL3 and P3BL3.5) were applied topically by six patients each, Gastrointestinal Quality of Life Index (GIQLI) score of each patient was improved at the end of 8 weeks. No adverse effects were reported by any of the patients. Hence 2% DTZ gel was found to be effective in the treatment of anal fissures. Full article
218 KiB  
Article
Simultaneous Aromatherapy Massage with Rosemary Oil on Humans
by Tapanee HONGRATANAWORAKIT
Sci. Pharm. 2009, 77(2), 375-388; https://doi.org/10.3797/scipharm.090312 - 30 Apr 2009
Cited by 6 | Viewed by 6878
Abstract
Massage of essential oils is increasing being used for the improvement of the quality of life and for the relief of various symptoms in patients, but scientific evaluation of the effects of fragrances in humans is rather scarce. The aim of this study [...] Read more.
Massage of essential oils is increasing being used for the improvement of the quality of life and for the relief of various symptoms in patients, but scientific evaluation of the effects of fragrances in humans is rather scarce. The aim of this study was to investigate the effect of rosemary oil (Rosmarinus officinalis L., Labiatae) on human autonomic parameters and emotional responses in healthy subjects after transdermal absorption. Thirty five healthy volunteers participated in the experiments. Four autonomic parameters, i.e. blood pressure, breathing rate, pulse rate, skin temperature were recorded. Emotional responses were assessed by means of rating scales. Compared to placebo, rosemary oil caused significant increases of breathing rate, systolic blood pressure, and diastolic blood pressure which indicate an increase of autonomic arousal. At the emotional level, subjects feel more attentive, more alert, more vigorous, and more cheerful than before the administration of the oil. This finding suggests an increase of arousal in terms of self-evaluation. In conclusion, our investigation demonstrates the stimulating effect of rosemary oil and provides evidence for its use in medicines for the relief of depression and stress in humans. Full article
215 KiB  
Article
Simultaneous Determination of Epinephrine and Norepinephrine by High Performance Liquid Chromatography
by Arun MISHRA, Adesh UPADHYAY, Arjun PATRA, Sachin CHAUDHURY and Pronobesh CHATTOPADHYAY
Sci. Pharm. 2009, 77(2), 367-374; https://doi.org/10.3797/scipharm.0902-07 - 04 Apr 2009
Cited by 26 | Viewed by 2444
Abstract
Epinephrine and non-epinephrine are major endogenous catecholamines which are known as neurotransmitter. The plasma levels of catecholamines are significant markers of several neuro-endocrine disorders and autonomic nervous system disorders. A method for the simultaneous quantitation of epinephrine and norepinephrine is described. The related [...] Read more.
Epinephrine and non-epinephrine are major endogenous catecholamines which are known as neurotransmitter. The plasma levels of catecholamines are significant markers of several neuro-endocrine disorders and autonomic nervous system disorders. A method for the simultaneous quantitation of epinephrine and norepinephrine is described. The related substances are resolved on a Phenomenex ODS analytical column C18 column (150 mm × 4.6 mm, 5 μm) using a mobile phase composed of a mixture of acetic acid and 50mM sodium acetate buffer pH 3.1 (1:99 v/v) at a flow rate of 1 ml/min with UV detector at 285 nm. The method is compatible with HPLC-MS and provides a tool for the control of substandard and counterfeit commercial preparations of epinephrine and norepinephrine. Full article
319 KiB  
Article
Preparation and In Vitro Evaluation of a Pegylated Nano-Liposomal Formulation Containing Docetaxel
by Afrouz YOUSEFI, Farnaz ESMAEILI, Sima RAHIMIAN, Fatemeh ATYABI and Rassoul DINARVAND
Sci. Pharm. 2009, 77(2), 453-464; https://doi.org/10.3797/scipharm.0806-08 - 19 Mar 2009
Cited by 70 | Viewed by 2685
Abstract
An improved pegylated liposomal formulation of docetaxel has been developed with the purpose of improving the docetaxel solubility without any need to use tween80 that is responsible for hypersensitivities following administration. Liposomes all had spherical shape with size of 130–160 nm. The most [...] Read more.
An improved pegylated liposomal formulation of docetaxel has been developed with the purpose of improving the docetaxel solubility without any need to use tween80 that is responsible for hypersensitivities following administration. Liposomes all had spherical shape with size of 130–160 nm. The most important finding of this study is that pegylated liposomes were prepared with significant increase in docetaxel encapsulation efficiency and stability of the formulation in comparison with last reports on docetaxel liposomes. In vitro release studies revealed that such a formulation could be stable in the blood circulation and meet the requirements for an effective drug delivery system. Full article
348 KiB  
Article
Development and Characterization of New Indomethacin Self-Nanoemulsifying Formulations
by Ehab I. TAHA
Sci. Pharm. 2009, 77(2), 443-452; https://doi.org/10.3797/scipharm.0811-24 - 14 Mar 2009
Cited by 3 | Viewed by 1219
Abstract
In the present work a new indomethacin (IND) self-nanoemulsifying drug delivery formulation (SNEDDF) have been prepared to enhance its dissolution which in turn could provide a better chance for IND oral absorption. IND SNEDDF have been prepared using different concentrations of castor oil [...] Read more.
In the present work a new indomethacin (IND) self-nanoemulsifying drug delivery formulation (SNEDDF) have been prepared to enhance its dissolution which in turn could provide a better chance for IND oral absorption. IND SNEDDF have been prepared using different concentrations of castor oil as a solvent for IND, Cremophor RH 40 (Cr-40) as surfactant and Capmul MCM-C8 (Ca-8) as co-surfactant. Droplets size and turbidity of IND SNEDDFs were measured. Dissolution profile of IND SNEDDFs filled in gelatin capsules was determined by using USP apparatus 2. Ternary phase diagram was constructed to identify the self-nanoemulsifying region after evaluation of IND SNEDDFs by the visual observation. The IND SNEDDFs were thermally characterized using differential scanning calorimetry (DSC) to ensure the compatibility among its ingredients. The present study revealed that the SNEDDFs increased IND dissolution rate and has the potential to enhance its bioavailability without interaction or incompatibility between the ingredients. Full article
499 KiB  
Article
Preparation and In Vitro Evaluation of Budesonide Spray Dried Microparticles for Pulmonary Delivery
by Sonali NAIKWADE and Amrita BAJAJ
Sci. Pharm. 2009, 77(2), 419-442; https://doi.org/10.3797/scipharm.0901-11 - 14 Mar 2009
Cited by 16 | Viewed by 1593
Abstract
The present study describes development and in vitro evaluation of budesonide microparticles prepared by spray drying for delivering drug directly to lungs via dry powder inhaler. This paper introduces new formulations for pharmaceutical applications which includes conventional formulations and novel spray dried microparticles [...] Read more.
The present study describes development and in vitro evaluation of budesonide microparticles prepared by spray drying for delivering drug directly to lungs via dry powder inhaler. This paper introduces new formulations for pharmaceutical applications which includes conventional formulations and novel spray dried microparticles viz., pulmosols, microspheres and porous particles. Optimized spray drying parameters for generation of microparticles were: inlet temperature, 130 °C; outlet temperature, 80 °C; aspirator rate, 240 mWc (60%); solution feed rate, 2 ml/min; spraying air flow pressure, 2 bar. Microparticles appeared to be spherical, low-density particles characterized by smooth surface. MMAD and GSD ranged from 2.5–4.6 μm and 1.5–2.7 respectively. Effective index of microspheres (54.48) and porous particle formulations (64.22) was higher than the conventional formulation (49.21) indicating more effective deposition of microparticles to the lungs. Carr’s Index (20–30%) and Hausner ratio (1.2–1.7) for all formulations indicated good powder flow properties. Formulations emitted a fine particle fraction of 25–47%. Microparticles showed extended in vitro drug release upto 4 hours with high respirable fractions, thus use of microparticles potentially offers sustained release profile along with improved delivery of drug to the pulmonary tract. Full article
219 KiB  
Article
The Reaction of Cyanoacetic Acid Hydrazide with 2-Acetylfuran: Synthesis of Coumarin, Pyridine, Thiophene and Thiazole Derivatives with Potential Antimicrobial Activities
by Rafat M. MOHAREB, Elham Ezz EL-ARAB and Karam A. EL-SHARKAWY
Sci. Pharm. 2009, 77(2), 355-366; https://doi.org/10.3797/scipharm.0901-20 - 14 Mar 2009
Cited by 34 | Viewed by 2429
Abstract
The hydrazide-hydrazone derivative 1 was formed through the reaction of cyanoacetic acid hydrazide with 2-acetylfuran. Compound 1 underwent a series of hetrocyclization reactions through its reaction with different chemical reagents to produce arylidene, coumarin, aryl hydrazone, pyridine, thiophene and thiazole derivatives 2–10. [...] Read more.
The hydrazide-hydrazone derivative 1 was formed through the reaction of cyanoacetic acid hydrazide with 2-acetylfuran. Compound 1 underwent a series of hetrocyclization reactions through its reaction with different chemical reagents to produce arylidene, coumarin, aryl hydrazone, pyridine, thiophene and thiazole derivatives 2–10. The MIC values for the newly synthesized products were tested against E. coli, B. cereus, B. subtilis and C. albicans compared with ampicilline and cycloheximide as reference drugs. Full article
254 KiB  
Article
Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose
by Gamal M. EL MAGHRABY and Abdullah H. ALOMRANI
Sci. Pharm. 2009, 77(2), 401-418; https://doi.org/10.3797/scipharm.0901-08 - 06 Mar 2009
Cited by 49 | Viewed by 1796
Abstract
Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on [...] Read more.
Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on the dissolution rate of itraconazole. Binary solid dispersions with HPMC, reduced the drug crystallinity, increased the equilibrium solubility but showed slow dissolution. Binary dispersions with Pluronic produced eutectic systems but the increase in solubility and dissolution was lower than that of HPMC systems. Ternary system comprising optimum proportions of drug with Pluronic and HPMC enhanced the dissolution rate showing dissolution efficiency comparable to that obtained with the marketed product of itraconazole. The study thus presented a system capable of increasing the dissolution rate of itraconazole with a potential for increased oral bioavailability by inhibiting its pre-systemic metabolism as well. Full article
389 KiB  
Article
Evaluation of a [67Ga]-Thiosemicarbazone Complex as Tumor Imaging Agent
by Amir R. JALILIAN, Pegah MEHDIPOUR, Mehdi AKHLAGHI, Hassan YOUSEFNIA and Kamaledin SHAFAII
Sci. Pharm. 2009, 77(2), 343-354; https://doi.org/10.3797/scipharm.0812-07 - 06 Mar 2009
Cited by 18 | Viewed by 1353
Abstract
[67Ga]labeled 2-acetylpyridine 4,4-dimethylthiosemicarbazone ([67Ga]- [APTSM2]2+) was prepared using freshly prepared [67Ga]GaCl3 and 2-acetylpyridine 4,4-dimethylthiosemicarbazone (APTSM2) for 30 min at 90°C (radiochemical purity: >97% ITLC, >98% HPLC, specific activity: 15–20 [...] Read more.
[67Ga]labeled 2-acetylpyridine 4,4-dimethylthiosemicarbazone ([67Ga]- [APTSM2]2+) was prepared using freshly prepared [67Ga]GaCl3 and 2-acetylpyridine 4,4-dimethylthiosemicarbazone (APTSM2) for 30 min at 90°C (radiochemical purity: >97% ITLC, >98% HPLC, specific activity: 15–20 Ci/mmol). Stability of the complex was checked in human serum for 37°C. The biodistribution of the labeled compound in vital organs of normal and fibrosarcoma bearing mice were compared with that of free Ga3+ cation up to 24h. Initial SPECT images and biodistribution results showed significant tumor uptake in fibrosarcoma-bearing mice after 2 hour post injection. Full article
410 KiB  
Review
Mouth Dissolving Tablets II: An Overview of Evaluation Techniques
by Dali SHUKLA, Subhashis CHAKRABORTY, Sanjay SINGH and Brahmeshwar MISHRA
Sci. Pharm. 2009, 77(2), 327-342; https://doi.org/10.3797/scipharm.0811-09-02 - 06 Mar 2009
Cited by 52 | Viewed by 2879
Abstract
Mouth dissolving tablets are well established dosage forms available in the market. The numerous advantages that they offer to the patients in terms of compliance as well as to the manufacturers in terms of huge revenues by line extension of products are well [...] Read more.
Mouth dissolving tablets are well established dosage forms available in the market. The numerous advantages that they offer to the patients in terms of compliance as well as to the manufacturers in terms of huge revenues by line extension of products are well known. In spite of such popularity, there seems to be lack of a standardized system to characterize these dosage forms. Enormous work has been done in this field, wherein some of the researchers have developed their own methods of evaluation. This article attempts to present a detailed review regarding technological advances made so far in the area of evaluation of mouth dissolving tablets with respect to special characteristics of these unique dosage forms. In the absence of any available standardized method, the author’s recommendation on critical issues in the field may be considered. Full article
202 KiB  
Review
Mouth Dissolving Tablets I: An Overview of Formulation Technology
by Dali SHUKLA, Subhashis CHAKRABORTY, Sanjay SINGH and Brahmeshwar MISHRA
Sci. Pharm. 2009, 77(2), 309-326; https://doi.org/10.3797/scipharm.0811-09-01 - 06 Mar 2009
Cited by 104 | Viewed by 10364
Abstract
Methods to improve patient’s compliance have always attracted scientists towards the development of fancy oral drug delivery systems. Among them, mouth dissolving drug delivery systems (MDDDS) have acquired an important position in the market by overcoming previously encountered administration problems and contributing to [...] Read more.
Methods to improve patient’s compliance have always attracted scientists towards the development of fancy oral drug delivery systems. Among them, mouth dissolving drug delivery systems (MDDDS) have acquired an important position in the market by overcoming previously encountered administration problems and contributing to extension of patent life. MDDDS have the unique property of rapidly disintegrating and/or dissolving and releasing the drug as soon as they come in contact with saliva, thus obviating the requirement of water during administration. Therefore, these dosage forms have lured the market for a certain section of the patient population which include dysphagic, bed ridden, psychic, geriatric and paediatric patients. Several techniques have been developed in the recent past, to improve the disintegration quality of these delicate dosage forms without affecting their integrity. This article focuses on the technologies available and the advances made so far in the field of fabrication of mouth dissolving tablets. Apart from the conventional methods of fabrication, this review also provides the detailed concept of some unique patented technologies like Zydis, Lyoc, Quicksolv, Orasolv, Durasolv, Flashtab, Oraquick, Wowtab and Ziplet alongwith their advantages and limitations. Full article
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