The aim of the current study was to design a porous osmotic pump–based drug delivery system for controlling the release of buspirone from the delivery system. The osmotic pump was successfully developed using symmetric membrane coating. The core of the tablets was prepared by direct compression technique and coated using dip-coating technique. Drug release from the osmotic system was studied using USP paddle type apparatus. The effect of various processing variables such as the amount of osmotic agent, the amount of swellable polymer, concentration of the core former, concentration of the plasticizer, membrane thickness, quantum of orifice on drug release from osmotic pump were evaluated. Different kinetic models (zero order, first order and Higuchi model) were applied to drug release data in order to establish the kinetics of drug release. It was found that the drug release was mostly affected by the amount of NaCl as osmotic agent, the swellable polymer, hydroxy propyl methyl cellulose (HPMC), the amount of PEG-400 and cellulose acetate in the coating solution and thickness of the semipermeable membrane. The optimized formulation released buspirone independent of pH and orifice quantum at the osmogen amount of 42%, hydrophilic polymer of 13% and pore size of 0.8 mm on the tablet surface. The drug release of osmotic formulation during 24 h showed zero order kinetics and could be suggested that this formulation as a once-daily regimen improves pharmacokinetic parameters of the drug and enhances patient compliance.

Objectives: Several studies indicate that central serotonergic neurons have important role in tolerance and dependency to morphine. The aim of this study was to investigate effect of buspirone (as a partial agonist of 5-HT1A receptors) in severity of morphine withdrawal syndrome in mice. Methods: Study was carried out on Swiss male albino mice weighing 25-30g. In order to induce dependency, we used daily subcutaneous injection of morphine at the schedule of: day 1=5 mg/kg; days 2-3=10 mg/kg; days 4-5=15 mg/kg; days 6-7=20 mg/kg and days 8-9=25mg/kg. Withdrawal syndrome was induced by intraperitoneal (i.p.) injection of naloxone (5 mg/kg) and then straub tail and jumps were recorded during 40 min period as indicators of morphine withdrawal syndrome. In treated groups, buspirone (5, 7.5 and 10 mg/kg, i.p.) was co-injected daily with morphine and severity of naloxone induced withdrawal behaviors were recorded at day 9. Results: Our results showed that naloxone induces sever (P<0.001) withdrawal behaviors (as indicated by straub tail and jumping behaviors) in morphine dependent mice. Daily coinjection of buspirone (5, 7.5 and 10 mg/kg) with morphine caused significant (P<0.001) reduction in straub tail and jumping behaviors. Buspirone (5, 7.5 and 10 mg/kg) did not produced any significant effect on morphine withdrawal syndrome. Conclusion: Results of this study show that buspirone attenuates morphine withdrawal behaviors.

Background and the purpose of the study: The available literatures show that 5-HT1A receptors are widely distributed throughout the basal ganglia, and their activation facilitate dopamine release. Neuroleptic drugs such as haloperidol induce Parkinson-like syndrome through blocking brain D2 receptors. This study aimed to investigate effect of buspirone, a partial agonist of 5HT1A receptor, on motor dysfunctions induced by haloperidol and involvement of 5HT1A receptors in this regard. Methods: Study was performed on the male mice weighing 25-30 g. Animals were divided randomly to groups of 10 animals. Motor dysfunction was induced by intraperitoneal (i.p.) injection of haloperidol (1 mg/kg). Catalepsy was assayed by bar-test method 5, 60, 120 and 180 minutes after drug administration and motor imbalance was studied by rotarod test. Results and major conclusion: Results showed that buspirone (20 mg/kg, i.p.) decreased significantly haloperidol-induced catalepsy and balance disorder in a dose dependent manner. Furthermore, 8-OH-DPAT (10 mg/kg, i.p.), as an agonist of 5-HT1A receptor, decreased haloperidol-induced catalepsy and balance disorder. The effect of buspirone (20 mg/kg, i.p.) on haloperidol-induced motor disorders was abolished by NAN-190 (10 mg/kg, i.p.), as a 5-HT1A receptor antagonist. From the results it may be concluded that buspirone improves haloperidol-induced catalepsy and balance disorder through activation of 5-HT1A receptors.

Objectives: To determine the safer and more effective between Buspirone and Alprazolam in the treatment of Anxiety. Method: A total of 100 patients, fifty female and fifty male aged between 35-50years were treated with Buspirone 5mg/b.d. and Alprazolam 1mg/o.d. for their anxiety who were reporting to Al-Shafa Hospital, Gujrat, Pakistan over a period of two months, during my administration of that hospital in the psychiatry outdoor department. The patients were followed up either on subsequent visits or by telephone. The medicines were provided by Tehran Darou/Chemie pharmaceutical company Tehran, Iran for this study. Results: Buspirone had lesser side effects and was more effective in releiving anxiety symptoms in 80 of these patients whereas 20 patients reported Alprazolam to be better. Still Alprazolam had more side effects in these 20 patients. Conclusion: Buspirone is superior to Alprazolam for the treatment of Anxiety.

Purpose: Several evidences show that serotonergic neurons play a role in the regulation of movements executed by the basal ganglia. Recently we have reported that single dose of buspirone improved 6-hydroxydopamine (6-OHDA) and haloperidol-induced catalepsy. This study is aimed to investigate effect of chronic intraperitoneal (i.p.) administration of buspirone on 6-OHDA-induced catalepsy in male Wistar rats.Methods: Catalepsy was induced by unilateral infusion of 6-OHDA (8 mg/2 ml/rat) into the central region of the SNc and was assayed by the bar-test method 5, 60, 120 and 180 min after drugs administration in 10th day. The effect of buspirone (0.5, 1 and 2 mg/kg, i.p. for 10 days) was assessed in 6-OHDA-lesioned rats.Results: The results showed that chronic injection of buspirone (0.5, 1 and 2 mg/kg, i.p. for 10 days) decreased catalepsy when compared with the control group. The best anticataleptic effect was observed at the dose of 1 mg/kg. The catalepsy-improving effect of buspirone was reversed by 1-(2-methoxyphenyl)- 4-[4-(2-phthalimido) butyl]piperazine hydrobromide (NAN-190), 0.5 mg/kg, i.p., as a 5-HT1A receptor antagonist.Conclusion: Our study indicates that chronic administration of buspirone improves catalepsy in a 6-OHDA-induced animal model of parkinson’s disease (PD). We also suggest that buspirone may be used as an adjuvant therapy to increase effectiveness of antiparkinsonian drugs. In order to prove this hypothesis, further clinical studies should be done.

Background and the Purpose of the study: Many drug substances and variety of naturally occurring dietary or herbal components are capable of interaction with the CYP enzyme system. The aim of the study was to investigate the effect of pomegranate juice pretreatment on the bioavailability of buspirone in rabbits.Methods: White New Zealand rabbits weighing 2.1±0.13 Kg were selected for study. The bioavailability of buspirone after pre-treatment with pomegranate juice (10 ml Kg-1 for seven days) was compared with an oral solution of 10 mg kg-1 of buspirone in distilled water. Animals were allowed free access to food and water, until night prior to dosing and were fasted for 10 hrs. In the first phase oral solution (10 mg kg-1) was administered through feeding tube followed by rinsing with 10 ml of water. In the second phase, the group was pretreated with pomegranate juice for 7 days and study was conducted after 15 days of washout period.Results and conclusion: The results showed that there was a significant (p<0.05) difference in the bioavailability of buspirone after pre-treatment with pomegranate juice. This increase in bioavailability might be due to inhibition of CYP3A4. Further studies are required to prove this mechanism in humans.

Objectives: To investigate the efficacy and side effects of buspirone in comparison with methylphenidate for controlling symptoms of children with attention deficit hyperactivity disorder (ADHD).Method: A total of thirty two 6-12 years old children with ADHD were examined. The teacher and parent ADHD Rating Scale (ADHD-RS) was used to gather data from both groups. Drug side effects were assessed based on side effect checklists for both drugs. Dosage of drug for patients was 0.5 mg/kg/day for the buspirone group and 0.3-1 mg/kg/day for the methylphenidate group. Data were analysed using paired t test, one way analysis of variance with repeated measures, independent t test and 2.Results: In the end of six weeks, both groups showed decreases in the total score of ADHD-RS in subscales of attention deficit, hyper-activity, and impulsivity (p<0.001). No significant differences were observed between the two groups on the parent (p=0.77) and teacher (p=0.23) rating scale scores. The groups were different regarding the inattention subscale, with methylphenidate being superior to buspirone. Side effects of buspirone were mild and rare in comparison with that of methylphenidate.Conclusion: Buspirone has a favorable side effect profile and it improves ADHD symptoms significantly. These preliminary findings of efficacy of buspirone in children with ADHD need further studies.