Search

The objective of the present study was to improve the dissolution rate and aphrodisiac activity of tadalafil by using hydrophilic polymers. Solid dispersions were prepared by solvent evaporation-Rota evaporator using Koliphore 188, KollidonR VA64, and KollidonR 30 polymers in a 1:1 ratio. Prepared tadalafil-solid dispersions (SDs) evaluated for yield, drug content, micromeritics properties, physicochemical characterizations, and aphrodisiac activity assessment. The optimized SDs TK188 showed size (2.175 ± 0.24 mm), percentage of content (98.89 ± 1.23%), yield (87.27 ± 3.13%), bulk density (0.496 ± 0.005 g/cm3), true density (0.646 ± 0.003 g/cm3), Carr's index (23.25 ± 0.81), Hausner ratio (1.303 ± 0.003) and angle of repose (<25°). FTIR spectrums revealed tadalafil doesn't chemically interact with used polymers. XRD and DSC analysis represents TK188 SDs were in the amorphous state. Drug release was 97.17 ± 2.43% for TK188, whereas it was 32.76 ± 2.65% for pure drug at the end of 2 h with 2.96-fold increase in dissolution and followed release kinetics of Korsmeyer Peppa's model. MDT and DE were noted to be 17.48 minutes and 84.53%, respectively. Furthermore, TK188 SDs showed relative improvement in the sexual behavior of the male rats. Thus the developed SDs TK188 could be potential tadalafil carriers for the treatment of erectile dysfunction. [ABSTRACT FROM AUTHOR]

Tadalafil (TDL) is a phosphodiesterase-5 inhibitor (PDE5I), indicated for erectile dysfunction (ED). However, TDL exhibits poor aqueous solubility and dissolution rate, which may limit its application. This study aims to prepare amorphous solid dispersion (ASD) by spray-drying, using glycyrrhizin-a natural drug carrier. Particle and physicochemical characterizations were performed by particle size, polydispersity index measurement, yield, drug content estimation, Fourier Transformed Infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and dissolution study. In order to evaluate the aphrodisiac activity of the prepared ASD, sexual behavior study was performed in male rats. It is further considered for the stability study. Our results revealed that TDL-GLZ spray-dried dispersion was a successful drug-carrier binary mixture. XRD and SEM showed that ASD of TDL with GLZ presented in the amorphous state and dented-spherical shape, unlike the drug indicating crystalline and spiked shaped. The optimized ASD3 formulation with particle size (1.92 µm), PDI (0.32), yield (97.78%) and drug content (85.00%) showed 4.07 folds’ increase in dissolution rate compared to pure TDL. The results obtained from the in vivo study exhibit significantly improved aphrodisiac activity with ASD3. The stability study revealed that the prepared ASD3 did not show any remarkable changes in the dissolution and drug content for 1 month storage at room temperature.

The objective of the present study was to improve the dissolution rate and aphrodisiac activity of tadalafil by using hydrophilic polymers. Solid dispersions were prepared by solvent evaporation-Rota evaporator using Koliphore 188, Kollidon® VA64, and Kollidon® 30 polymers in a 1:1 ratio. Prepared tadalafil-solid dispersions (SDs) evaluated for yield, drug content, micromeritics properties, physicochemical characterizations, and aphrodisiac activity assessment. The optimized SDs TK188 showed size (2.175 ± 0.24 µm), percentage of content (98.89 ± 1.23%), yield (87.27 ± 3.13%), bulk density (0.496 ± 0.005 g/cm3), true density (0.646 ± 0.003 g/cm3), Carr’s index (23.25 ± 0.81), Hausner ratio (1.303 ± 0.003) and angle of repose (

Khaya grandifoliola C. DC. (Meliaceae), is a large tree exploited for timber purpose, for treating various illnesses and to enhance libido in Nigerian indigenous traditional medicine. Therefore, this study evaluates the aphrodisiac potential of K. grandifoliola stem bark in male Wistar rats. Aphrodisiac potential was determined following the oral administration of graded doses: 250, 500 and 1000 mg/kg of crude MeOH extract of K. grandifoliola stem bark, and 100 and 200 mg/kg each of aqueous (AQ) and dichloromethane (DCM) fractions. Sildenafil citrate and distilled water served as positive and negative controls, respectively. Sexual behavioural parameters like mount, intromission and ejaculatory frequencies and latencies were recorded on day 7. Serum testosterone concentrations and haematological parameters were also monitored. The findings from the sexual behavioural study indicated that methanol extract of K. grandifoliola was active and significantly increased mount and intromission frequencies, and intromission and mount latencies in a dose- dependent manner, but had no effect on ejaculatory frequency and ejaculatory latency. Both AQ and DCM fractions were more active than the extract but comparable to Sildenafil citrate, with the DCM fraction being comparatively more active. Testosterone concentrations were also increased dose-dependently by all tested agents, but DCM fraction was the most active and comparable to Sildenafil citrate. Improvement in some haematological indices, HB and PCV was evident with DCM fraction From all indications, methanol extract of K. grandifoliola stem bark which increased serum testosterone and sexual behavioural indices has potential for improving sexual dysfunction in males, and the more active DCM fraction qualifies for further phytochemical investigation to isolate active compounds. These findings therefore justify the acclaimed local use of K. grandifoliola stem bark as an aphrodisiac in males. [ABSTRACT FROM AUTHOR]

Tadalafil (TDL) is a phosphodiesterase-5 inhibitor (PDE5I), indicated for erectile dysfunction (ED). However, TDL exhibits poor aqueous solubility and dissolution rate, which may limit its application. This study aims to prepare amorphous solid dispersion (ASD) by spray-drying, using glycyrrhizin-a natural drug carrier. Particle and physicochemical characterizations were performed by particle size, polydispersity index measurement, yield, drug content estimation, Fourier Transformed Infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and dissolution study. In order to evaluate the aphrodisiac activity of the prepared ASD, sexual behavior study was performed in male rats. It is further considered for the stability study. Our results revealed that TDL-GLZ spray-dried dispersion was a successful drug-carrier binary mixture. XRD and SEM showed that ASD of TDL with GLZ presented in the amorphous state and dented-spherical shape, unlike the drug indicating crystalline and spiked shaped. The optimized ASD3 formulation with particle size (1.92 µm), PDI (0.32), yield (97.78%) and drug content (85.00%) showed 4.07 folds' increase in dissolution rate compared to pure TDL. The results obtained from the in vivo study exhibit significantly improved aphrodisiac activity with ASD3. The stability study revealed that the prepared ASD3 did not show any remarkable changes in the dissolution and drug content for 1 month storage at room temperature. [ABSTRACT FROM AUTHOR]

This study aimed to investigate the effects of Kaempferia parviflora extract (KD) and exercise training on reproductive function in male rats. Sexually mature males were assigned to four groups: control, KD70 (received 70 mg kg−1 day−1 for 4 weeks), Ex (exercise training for 4 weeks), Ex + KD70 (exercise training with KD 70 mg kg−1 day−1). At the end of treatment regimes, sexual behaviours including mount latency (ML), mount frequency (MF), ejaculation latency (EL), post-ejaculation latency (PEL), number of mount within 30 min (MF30) and number of ejaculation (NEL) were assessed by a video camera, and fertility was tested by natural mating. Results showed that KD had no effect on the weights of reproductive organs, liver, kidneys and levator ani muscle. On the other hand, the weights of epididymis, seminal vesicles, prostate gland and levator ani muscle were significantly increased in the Ex and Ex+KD70 groups. ML and EL were shortened in all treatment groups, but PEL was decreased only in KP70 group. Only Ex and Ex + KD70 groups exhibited lower MF and higher NEL whilst MF30 were not changed in all groups. None of the treatments altered male fertility. It is concluded that KD enhanced sexual motivation whereas exercise training promoted both sexual motivation and performance. [ABSTRACT FROM AUTHOR]

Abstract: In this study, the aphrodisiac activities of Crocus sativus stigma aqueous extract and its constituents, safranal and crocin, were evaluated in male rats. The aqueous extract (80, 160 and 320mg/kg body wt.), crocin (100, 200 and 400mg/kg body wt.), safranal (0.1, 0.2 and 0.4ml/kg), sildenafil (60mg/kg body wt., as a positive control) and saline were administered intraperitoneally to male rats. Mounting frequency (MF), intromission frequency (IF), erection frequency (EF), mount latency (ML), intromission latency (IL) and ejaculation latency (EL) were the factors evaluated during the sexual behavior study. Crocin, at all doses, and the extract, especially at doses 160 and 320mg/kg body wt., increased MF, IF and EF behaviors and reduced EL, IL and ML parameters. Safranal did not show aphrodisiac effects. The present study reveals an aphrodisiac activity of saffron aqueous extract and its constituent crocin. [Copyright &y& Elsevier]