Iranian Journal of Pharmaceutical Sciences

Asthma, which is mainly distinguished by airway inflammation and bronchial hyper-responsiveness, is known as one of the most common chronic diseases
worldwide. It also is the most frequent chronic respiratory disorder amongst all age groups. On one side of the asthma story, there are massive investment of time, effort and money, a large number of pharmaceutical and academic research studies, health service modifications and revised guidelines. On the other side, there are unacceptably high, but mostly preventable, morbidity and mortality rates, socio-economic burdens and psychological problems due to asthma. A considerable proportion of doctor’s workload, hospital resources, health utilization costs, days off from school and work are caused by asthma. Our knowledge about this disorder and its complications is still on demand. There are significant questions regarding asthma and its pathophysiology which should be answered. National, regional and local initiatives are needed to be established to help health systems to overcome socio-economic burdens due
to this disease. These could only be done if a clear picture of this respiratory disorder and its management achievements are available. This review article is an
approach to present an image about asthma and its management based on the current understandings of the nature of this disorder.

Nitroglycerin has been reported to reduce activated partial thromboplastin time (aPTT) values in patients treated with concurrent heparin and nitroglycerin. However, studies have yielded conflicting results. To determine whether intravenous nitroglycerin alters the anticoagulant effect of heparin, we prospectively evaluated twenty patients admitted for coronary angioplasty by measuring their aPTT both before initiation and after addition of nitroglycerin to heparin therapy. The results showed that the mean of aPTT at the baseline when patients were on heparin alone was not significantly different from aPTT measured upon addition of nitroglycerin, and 30 min following the cessation of nitroglycerin infusion, when patients were still on the same dose of heparin. Therefore, no direct effect of nitroglycerin on the anticoagulant effect of heparin was observed in this study.

Tagetes minuta L. is considered as an annual plant growing in the temperate zones of South America. It has been used as carminative, anti-inflammatory, anti-abortion, vermifuge, bronchodilator and hypotensive. In the current study the locally cultured plant of Tagetes minuta L. was studied for phytochemical and larvicidal properties. The phytochemical analysis of aerial parts of the plant exhibited the presence of saponins, terpenoids, tannins, alkaloids and flavonoids. The efficacy of methanolic extract of the plant was tested against malaria vector, Anopheles stephensi. The probit analysis from the concentration and mortality exhibited the LC50 and LC90 values of 2.5 mg/l and 11.0 mg/l, respectively. Also the efficacies of the ethyl acetate, chloroform, methanolic and aqueous extracts of the plant were tested on Anopheles stephensi with the LC50 concentration of the methanolic extract. The results showed that the chloroform extract had the highest efficacy.

The protective effect of tomato extract and lycopene on acute doxorubicin-induced myocardial toxicity was evaluated in mice. Doxorubicin toxicity, induced by a
single intraperitoneal injection (15 mg/kg), was revealed by elevated serum CPKMB and histopathological observations. Tomato extract (1.2 and 2.4 g/kg, i.p.) and
lycopene (1.7 and 3.5 mg/kg, i.p.), prevented the rise in serum CPKMB and ameliorated cardiac cell injury. These results suggest that tomato extract and
lycopene inhibit doxorubicin-induced cardiotoxicity and might serve as a combination chemotherapeutic agent with doxorubicin to limit its cardiotoxic effects.

The abilities of Silybum marianum cell culture to biotransform benzaldehyde to benzyl alcohol in three culture systems were compared. Callus cultures of Silybum marianum were established from seedlings, and healthy suspensions and immobilized cultures grown on the Murashige and Skoog medium. S. marianum cells
were immobilized in both agar beads and fiber cotton matrixes. Benzaldehyde was fed to S. marianum cell suspension and immobilized cultures. Biotransformation reactions were detected over 24 hours of incubation. The cultures then were extracted with dichloromethane and the extracts were subjected to GC and GC-MS analysis. The S. marianum culture systems exhibit different conversion rates in the reduction of benzaldehyde. Immobilization seemed to have an effect on the secondary metabolism, the cells immobilized in fiber cotton matrix were more efficient at performing the reduction process than both the freely suspended and agar immobilized cells. The ability of cultured plant cells to biotransform substrate appears to be dependent on the type of the culture system.

Infant jaundice is observed during the first week of life in approximately 60% of term and 80% of preterm infants. Hyperbilirubinemia may lead to the development of kernicterus, hearing loss, and convulsion. The goal of therapy in hyperbilirubinemia is lowering blood bilirubin levels or at least preventing its increase. It is recommended that phototherapy and if unsuccessful, blood exchange transfusion be used to keep bilirubin in the normal levels. In the Iranian traditional medicine, Cotoneaster manna (purgative manna) is commonly used in the treatment of infant jaundice. However, no scientific data was available regarding its effectiveness. In this study, purgative manna which was obtained from Cotoneaster discolor Pojark from south eastern Iran was used as an oral drop preparation. After standardization of the manna and the drop, clinical study was performed on 200 hyperbilirubinemic newborns. The serum bilirubin was assayed twice a day, using spectrophotometric method. The results showed that 88% of the infants who were treated by purgative manna plus phototherapy were cured during the first 3 days of administration, but only 21% of the infants who were treatment by phototherapy alone were cured.

Mefloquine (MFQ), as a racemic mixture is used for the prophylaxis and treatment of malaria. Stereoselective pharmacodynamic and pharmacokinetic differences have been observed for MFQ. In the present study, the human blood was spiked with racemic MFQ. The concentration of MFQ enantiomers in various blood fractions including packed erythrocyte layer, platelet rich plasma and platelet poor plasma was determined. The results showed that the ratio of (+)-MFQ was about 1.5 time higher than (-)-MFQ in packed erythrocyte layer. Results obtained from the separated erythrocytes spiked with racemic MFQ showed no significant
difference between the enantiomer concentrations. It can be concluded that the stereoselective accumulation of MFQ enantiomers in erythrocytes might be in relation to protein binding or the presence of other blood cells.

Calcium acetate is used as an oral phosphate binder to control hyperphosphatemia in patients with chronic renal failure. Compared to calcium carbonate,
control of hyperphosphatemia can be achieved at lower calcium administration with calcium acetate which likely reduces the risk of hypercalcemia. In this study,
various formulations of calcium acetate tablets were prepared and their disintegration times, dissolution rates and phosphate binding capacities were determined. Dissolution test was carried out using the paddle method according to the United States Pharmacopoeia (USP XXIII). The binding efficiency of the tablets was compared by measuring the amount of insoluble phosphate after mixing with a sodium phosphate solution at pH 6. Calcium acetate tablets had a mean content of 809.6 mg of calcium acetate and a mean weight of 1087 mg. The average breaking load and disintegration times were 66.4±5.5 N and 24.5±2.1 min, respectively. Drug release after 30 and 60 min were 80.45% and 101.42%, respectively. The amount of nondissolved phosphorus following 60 min incubation of calcium acetate and/or calcium carbonate tablets were 372.8 mg (61.2%) and 463.2 mg (76.0%), respectively.
Weight variation, friability, disintegration time, and dissolution rate of calcium
acetate tablets were in the acceptable pharmacopoeial limits. Ahigh phosphate binding
capacity of calcium acetate tablets indicated that it can be a suitable alternative to
calcium carbonate in the management of hyperphosphatemia in patients with
chronic renal failure.