Diazepam Tablets Research Articles

Evaluation and Treatment of Vulvodynia: State of the Science.

Vulvodynia affects 7% of American women, yet clinicians often lack awareness of its presentation. It is underdiagnosed and often misdiagnosed as vaginitis. The etiology of vulvodynia remains unknown, making it difficult to identify or develop effective treatment methods. The purpose of this article is to (1) review the presentation and evaluation of vulvodynia, (2) review the research on vulvodynia treatments, and (3) aid the clinician in the selection of vulvodynia treatment methods. The level of evidence to support vulvodynia treatment varies from case series to randomized controlled trials (RCTs). Oral desipramine with 5% lidocaine cream, intravaginal diazepam tablets with intravaginal transcutaneous electric nerve stimulation (TENS), botulinum toxin type A 50 units, enoxaparin sodium subcutaneous injections, intravaginal TENS (as a single therapy), multimodal physical therapy, overnight 5% lidocaine ointment, and acupuncture had the highest level of evidence with at least one RCT or comparative effectiveness trial. Pre to posttest reduction in vulvar pain and/or dyspareunia in non-RCT studies included studies of gabapentin cream, amitriptyline cream, amitriptyline with baclofen cream, up to 6 weeks' oral itraconazole therapy, multimodal physical therapy, vaginal dilators, electromyography biofeedback, hypnotherapy, cognitive behavioral therapy, cold knife vestibulectomy, and laser therapy. There is a lack of rigorous RCTs with large sample sizes for the treatment of vulvodynia, rendering it difficult to determine efficacy of most treatment methods. Clinicians will be guided in the selection of best treatments for vulvodynia that have the highest level of evidence and are least invasive.

Intervention Effects of Okra Extract on Brain-Gut Peptides and Intestinal Microorganisms in Sleep Deprivation Rats.

Objective Okra, possessing various bioactive components, is used to treat different diseases. This study sought to estimate the intervention effects of okra extract (OE) on brain-gut peptides (BGPs) and intestinal microorganisms in sleep deprivation (SD) rats. Methods SD rat models were established using the modified multiple platform method and then treated with normal saline, diazepam tablets, or different doses of OE. Body weight and average daily water consumption of rats were recorded. Depressive behaviors of rats were assessed by the open field test and sucrose preference test. Serum levels of noradrenaline, melatonin, inflammatory factors (IL-1β/IL-6/TNF-α/IL-4/IL-10), and BGP indexes, including gastrin (GAS), motilin (MTL), 5-hydroxytryptamine (5-HT), cholecystokinin (CCK), and vasoactive intestinal peptide (VIP) were measured by ELISA. Additionally, the DNA relative contents of representative intestinal microorganisms in the collected rat feces were determined using RT-qPCR. Results SD decreased body weight and average daily water consumption and induced depressive behaviors as well as stress and inflammatory responses in rats. SD rats exhibited lowered GAS, MTL, 5-HT, and VIP but elevated CCK and showed diminished DNA relative contents of Bacteroidetes and probiotics (Bifidobacteria and Lactobacilli) but increased Clostridium perfringens. OE at different doses ameliorated the depressive behaviors and mitigated the stress and inflammatory responses in SD rats, raised the serum contents of GAS, MTL, 5-HT, and VIP, reduced CCK level, elevated the DNA relative contents of Bacteroidetes and probiotics, but diminished Clostridium perfringens. OE exhibited similar intervention effects to diazepam tablets (positive control). Conclusion OE exerts intervention effects on BGPs and intestinal microorganisms in SD rats.

Application of Microcrystalline Cellulose Powders Obtained from Gossypiumherbaceum As Dry Binder in the Formulation of Diazepam Tablets

Background: Microcrystalline cellulose (MCC) is a popular dry binder in tablet formulation. Differences in its processing methods can significantly affect its tableting properties. Aim: Assessment of the tableting and in-vitro release properties of diazepam tablets formulated with Gossypiumherbaceum (GH) derived MCC that was dried by two different methods. Methods: G.herbaceum bolls were de-lignified in sodium hydroxide solutions to obtain α-cellulose which was hydrolyzed with 2.0 N hydrochloric acid to obtain MCC. The neutralized damp MCC was separated into two portions. One portion was fluid bed dried (MCC-GossF) while the other portion was lyophilized (MCC-GossL). Diazepam tablets were prepared with 20, 30 and 40%w/w of MCC-GossF and MCC-GossL..Avicel PH 102 (AVH-102) served as comparing standard. The formulations were evaluated using standard methods. Results: The powders flowed well and the tablets met with British Pharmacopoiea specifications. Diazepam tablets containing MCC-GossL (DGL) were stronger than those of MCC-GossF (DCF) (p<0.05). The disintegration times were < 2 min and friability ≤ 1%. The strength of tablets containing AVH-102 (DAV) compared well with those of DGL tablets. More than 80% of diazepam was released from the tablets. Conclusion: The GH MCCs served as good dry binders in the formulation of diazepam tablets.

Development and characterization of bilayered tablets of diazepam for oral drug delivery: design, optimization and in vitro evaluation.

Aims: The oral bioavailability of drugs can be limited by their short residence time in the gastrointestinal tract. This study was performed to design bilayered floating tablets of diazepam comprising immediate-release and controlled-release layers. Methods: The tablets were prepared using sodium starch glycolate, polyvinyl pyrrolidone, hydroxypropyl methylcellulose and microcrystalline cellulose and evaluated for their characteristics. Results: The optimized formulation was found to be buoyant for 8h on simulated gastric fluid. Hydroxypropyl methylcellulose K4M and microcrystalline cellulose sustained the release of diazepam from the controlled-release layer. The optimized formulation exhibited an extended release period of 8h. Discussion/conclusion: It can be concluded that bilayered tablets of diazepam may extend the residence time of the drug at the site of absorption.

Panični napad u ambulanti hitne medicinske pomoći Beograd

Objective. Panic attack is defined as specific, frightening experience of intense fear and impending catastrophe that is accompanied by numerous somatic symptoms. The scope of study was to show the presentation of panic attack disorder in patients in EMS Belgrade Ambulatory Clinic, its frequency, temporal patterns and prescribed therapy. Methods. The research is a cross-sectional study of the work of a one general practitioner and a gerontology subspecialist from the City institute outpatient clinic in Belgrade EMS, in the period from 18.12. 2014. to 16.01. 2019. in each patient's medical record there was at least one or more complaints recorded. Results. Out of 8398 patients, 61 were found with a diagnosis of panic attack, which is 0.73% of the total number of examined patients. 50.82% were male and 49.18% female, with an average age of 39.92. The most common symptoms were respiratory, as well as numbness and tingling, dizziness, feelings of insecurity and fainting, in 80.3% of cases, patients had somewhat similar symptoms previously, whereas 31.1% presented with an actual panic attack. Of the total number of patients 21.3% of them have already been treated for anxiety and depressive disorder. Ten of them tried to help themselves by taking either bromazepam and diazepam tablets on their own, whereas 35.5% were actually prescribed diazepam by our staff physicians. Conclusion: Panic attack is most often presented as a respiratory manifestation. Patients call for medical assistance somewhat more frequently at nighttime when community healthcare centers are closed, however, this is of no statistical significance. The administered therapy was diazepam orally or intramuscularly.

Comparison of Epidural Dexmedetomidine Versus Ropivacaine Infusion Effectiveness in Preventing Erection Following Reconstructive Urethral Surgery: A Randomized Clinical Trial.

BackgroundOne of the most common devastating problems that occur after urethroplasty is erection, which causes surgical complications (fistula, wound dehiscence, and surgical graft failure) and the need for repairing the complications. We attempted to compare the effect of continuous epidural infusion of dexmedetomidine and ropivacaine as a post-surgical erection prevention strategy.ObjectivesIn this study, we aimed to compare the effect of dexmedetomidine and ropivacaine epidural infusion on the incidence of erection after reconstructive urethral surgery.MethodsAn RCT was conducted on 45 patients who were scheduled for reconstructive urethral surgery. They were randomly divided into three groups: (1) control (n = 15), (2) epidural dexmedetomidine (n = 15), (3) and epidural ropivacaine (n = 15). The control group received oral medication after surgery according to the conventional method (cyproterone compound tablets 50 mg BD and diazepam tablets 2 mg TDS for a week) to prevent erection. The DEX group received dexmedetomidine as continuous epidural infusion, and the ROP group received ropivacaine in addition to the conventional method. The occurrence of erection during day and night was recorded separately until the seventh day after surgery. Due to the long-time interval between case selection, participants from different groups were not matched with each other.ResultsThe incidence of erection in the dexmedetomidine group was lower than that in the ropivacaine group per person (0.87) and significantly lower than in the control group (2.8 per person). Also, there was significantly less erection in the ropivacaine group (1.2 per person) than in the control group. Our study showed that erection after surgery significantly decreased with the continuous epidural infusion of dexmedetomidine and ropivacaine.ConclusionsDexmedetomidine seems to have a significant preventive effect on erection after reconstructive urethral surgery.

Potential targets of Euodiae Fructus in treatment of insomnia based on network pharmacology

The acupoint application of Euodiae Fructus at Yongquan(KI1) can significantly improve the sleep quality of patients with insomnia with berberine as the main effective component for the efficacy. Nineteen active compounds and 203 drug targets were screened out from Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform(TCMSP). After comparison with GeneCards and Online Mendelian Inheritance in Man(OMIM), 24 common genes of diseases and drugs were obtained. STRING 11.0 was used to construct a protein-protein interaction(PPI) network of the overlapping genes, and Matthews correlation coefficient(MCC) was employed to screen the core genes, which were then subjected to enrichment analysis with gene ontology(GO) and Kyoto encyclopedia of genes and genomes(KEGG). The results revealed that the main compounds of Euodiae Fructus, such as berberine and rutaecarpine, participated in the biological processes(such as neurotransmitter receptor activity) by regulating C-reactive protein(CRP), estrogen receptor 1(ESR1), 5-hydroxytryptamine(5-HT) receptor, and interleukin-6(IL-6) to exert sedative, anxiolytic, and antidepressant effects. Sixty 4-week-old SPF mice were randomly divided into a control group, a model group, a positive drug(diazepam tablets) group, and low-, medium-, and high-dose berberine groups. Medication with corresponding drugs was performed for one week. The results demonstrated that berberine was potent in reducing the activities and standing times of mice, down-regulating the levels of CRP and IL-6 mRNA in the hypothalamus, and up-regulating the expression of 5-HT(P<0.01); however, no significant effect on ESR1 was observed. The network of Euodiae Fructus in treating insomnia was constructed by network pharmacology and verified by tests. The findings indicated that the therapeutic efficacy of Euodiae Fructus in treating insomnia was achieved by participating in multiple biological processes, such as neurotransmitter receptor activity, which provided a scientific basis for its clinical application.

Pharmacist's whistleblower claim for wrongful termination is rejected

Most pharmacists are “at will” employees, meaning that without an employment contract stating to the contrary, they can be discharged at the employer's will for any or no reason. Many state laws contain an exception to the “discharge at will” doctrine, providing that an employee may not be discharged from employment for refusing to participate in an illegal act or for reporting illegal acts by the employer. This provision encourages “whistleblowers” to report and put an end to illegal conduct they detect. A Mississippi pharmacist recently attempted to assert the whistleblower provision following her discharge from employment. The plaintiff, who had been designated as the pharmacy's Pharmacist-in-Charge (PIC), had what the court called a “rocky” relationship with the pharmacy owners. She thought that the owners “infringed on her authority as the PIC.” She wanted “full reign” over a pharmacy technician and the relief pharmacist, and she felt that she had not been given this needed authority. The event that led to termination of the plaintiff's employment occurred on the Saturday of a Labor Day weekend. At the end of that day, the relief pharmacist processed a verbal order for four diazepam tablets for a patient. On Tuesday morning, the plaintiff opened the pharmacy and discovered a new prescription for a larger quantity of the drug, with the notation to “take four tablets out” of the quantity dispensed. The prescription was dated with Tuesday's date. The plaintiff concluded that the relief pharmacist had unlawfully dispensed the four diazepam tablets on Saturday. She reported this allegedly illegal act to the pharmacy owners. The report apparently led to a series of “heated” discussions over a period of days, eventually resulting in the plaintiff being fired. The plaintiff's wrongful discharge lawsuit against her former employer was dismissed, and from the dismissal the pharmacist appealed. The court evaluated the evidence, which was somewhat contradictory. The court concluded that the relief pharmacist had received a verbal authorization to dispense a Schedule IV controlled substance, and that verbal prescriptions are allowed for these medications. The plaintiff contended that the prescription was not lawful because the prescription had not been “reduced promptly to writing,” as is required by law. In support of this argument, the plaintiff cited the delay between the Saturday when the order was received and the Tuesday date on the written prescription. The court noted that the word “promptly” is not defined in the relevant laws. The court examined the purpose of controlled substance regulations, concluding that they are “designed to ensure that the doctor examines the patient before delivering the prescription and to ensure that there is a legitimate medical reason for delivering the prescription.” The court ruled that the plaintiff had failed to provide any evidence “that a delay of such duration is a crime.” Dismissal of the plaintiff's wrongful discharge lawsuit was affirmed. All pharmacists, and particularly those designated as a pharmacy's PIC, have a significant responsibility to ensure that violations of pharmacy laws are avoided. When regulatory violations occur, they must be reported to appropriate pharmacy authorities. Whistleblower laws in many states protect a reporting pharmacist from retaliation based on the submission of such a report. Whistleblower laws apply when a clear violation of regulatory requirements has occurred or is reasonably suspected to have occurred. Unique interpretations of the law that support allegations of minor regulatory violations cannot be used as a smokescreen to avoid the consequences of major disagreements with management. The diversion of controlled substances is a very serious matter. Any activity related to controlled substance diversion must be reported to and taken seriously by management. Disagreements over the definition of a word like “promptly” may lead to interesting discussions, but it is unlikely that a clear violation of regulatory requirements will be identified by these discussions.

Predicting drug release from diazepam FDM printed tablets using deep learning approach: Influence of process parameters and tablet surface/volume ratio

The aim of this study was to apply artificial neural networks as deep learning tools in establishing a model for understanding and prediction of diazepam release from fused deposition modeling (FDM) printed tablets. Diazepam printed tablets of various shapes were created by a computer-aided design (CAD) program and prepared by fused deposition modeling using previously prepared polyvinyl alcohol/diazepam filaments via hot-melt extrusion. The surface to volume ratio (SA/V) for each shape was calculated. Printing parameters were varied including infill density (20%, 70% and 100%) and infill pattern (line and zigzag). Influence of tablet SA/V ratio and printing parameters (infill density and infill pattern) on the release of diazepam from printed tablets were modeled using self-organizing maps (SOM) and multi-layer perceptron (MLP). SOM as an unsupervised neural network was used for visualizing interrelation among the data, whereas MLP was used for the prediction of drug release properties. MLP had three layers (with structure 2-3-5) and was trained using back propagation algorithm. Input parameters for the modeling were: infill density and SA/V ratio; while output parameters were percent of drug release in five time points. The data set for network training was divided into training, validation and test sets. The dissolution rate increased with higher SA/V ratio, lower infill density (less than 50%) and zigzag infill pattern. The established ANN model was tested; calculated f 2 factors for two tested formulations (70.24 and 77.44) showed similarity between experimentally observed and predicted drug release profiles. Trained MLP network was able to predict drug release behavior as a function of infill density and SA/Vol ratio, as established design space for formulated 3D printed diazepam tablets.

The Mechanical and In vitro Release Properties of Diazepam from Tablets Containing Fluid Bed Dried and Lyophilized Cocos nucifera Microcrystalline Cellulose

Aim: This study aimed to evaluate the mechanical and in vitro release properties of diazepam from tablets containing fluid bed dried and lyophilized microcrystalline cellulose (MCC) obtained from the matured fruit husks of Cocos nucifera (CN).
 Study Design: Method of experiment.
 Place and Duration of Study: Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka from March 2015 to September, 2016
 Methods: Dried CN fruit husks were digested in sodium hydroxide to obtain alpha (α) cellulose which on hydrolysis with mineral acid (Hydrochloric acid) solution gave CN-MCC. The dry MCC obtained by either fluid bed or lyophilized drying of the wet CN-MCC were coded MCCF-Cocos and MCCL-Cocos respectively. Both MCCs were used in the formulation of diazepam tablets at 20, 30 and 40% w/w. Avicel PH 102 (AVC-102), was used as comparing standard. The tablets were evaluated for physical and dissolution properties using standard methods.
 Results: Results show the tablets passed the British Pharmacopoeia specifications for weight uniformity, crushing strength, disintegration time, friability and dissolution. Diazepam tablets containing MCCL-Cocos (coded DCL) were mechanically stronger than those containing MCCF-Cocos (coded DCF). Disintegration time was in the order of DCF > DCL tablets while friability was in the order of DCL < DCF tablets. Diazepam tablets containing AVC-102 (coded DAV) were mechanically stronger than DCL and DCF tablets. The dilution potential was in the order DAV > DCL > DCF. More than 80% of the diazepam content was released from DAV, DCL and DCF tablets.
 Conclusion: Generally, DAV, DCL and DCF tablets met the British Pharmacopoeia limits for mechanical properties and in vitro drug release with DCL tablets showing significantly (P = .05) superior mechanical properties while DCF showed faster drug release.

The analysis of the effect of psycho-intervention combined with diazepam on patients with sudden sensorineural hearing loss and anxiety

Objective: To investigate the therapeutic effect of psychological intervention combined with diazepam on sudden hearing loss patients with anxiety. Method: 108 cases of sudden hearing loss patients with anxiety were randomly divided into two groups(n=54 in each group): The control group received routine treatment of sudden hearing loss, the study group was given psychological intervention combined with diazepam tablets(2.5 mg once, twice a day) based on the routine treatment. The hearing and HAMA and SAS scores were reviewed after 10 days of treatment. Result: After 10 days of treatment, the average hearing threshold of patients in the control group and the study group were respectively increased by （19.65±7.89）dB and （26.93±9.04）dB (t=4.54, P=0.006), the HAMA score of two groups were respectively decreased by 4.68 and 10.75（t=9.949, P=0.000）and the SAS score of two groups were respectively decreased by 15.93 and 23.39 (t=6.773, P=0.000), and the total efficiency of hearing of two groups were 61.11% and 77.78% (χ²=4.441, P=0.035),respectively. the differences were statistically significant. Conclusion: Psychological intervention combined with diazepam can relieve anxiety in patients with sudden hearing loss effectively, and play a positive role in the development and prognosis of patients with sudden sensorineural hearing loss.

Characterisation of illicit ecstasy and diazepam tablets by colorant identification

Ecstasy and diazepam are two commonly abused drugs with a high potential for dependence.

Study on the effect of acupuncture at Sìshéncōng (四神聪 EX-HN 1) and Băihuì (百会 GV 20) on the serum amino acids neurotransmitters of insomnia patients

ObjectiveTo explore the efficacy of acupuncture at Sìshéncōng (四神聪 EX-HN 1) and Băihuì (百会 GV 20) as well as the possible mechanism. MethodsEighty cases of insomnia patients treated in our hospital were selected, and randomly divided into a control group and a treatment group according to the random number table method. Conventional treatment was carried out in the control group by giving diazepam tablets, and acupuncture at EX-HN 1 and GV 20 was conducted in the treatment group. The sleep time and quality, PSQI score, and the level changes of blood glutamic acid (GLU), γ-aminobutyric acid (GABA), norepinephrine (NE) and dopamine (DA) were compared in the patients in each group before and after treatment. ResultsCompared with the results before treatment, the time for falling asleep of the patients in the two groups shortened (both P<0.05), the levels of GLU and GABA increased (all P<0.05), the sleep time was longer (both P<0.05), and the levels of NE and DA, as well as the PSQI score reduced (all P<0.05). Compared with the control group, the levels of NE and DA, as well as the PSQI score of patients in the treatment group reduced after treatment (P<0.05), the time for falling asleep shortened (P<0.05), the levels of GLU and GABA increased (P<0.05), and the sleep time was longer (P<0.05). ConclusionAcupuncture at EX-HN 1 and GV 20 can prolong the sleep time, improve the sleep quality, and the clinical efficacy is superior to that of western medicine treatment. The mechanism may be related to the synthesis and release of amino acids neurotransmitters.

Diazepam Is No Better Than Placebo When Added to Naproxen for Acute Low Back Pain

Low back pain causes more than 2.5 million visits to US emergency departments (EDs) annually. Low back pain patients are often treated with nonsteroidal anti-inflammatory drugs and benzodiazepines. The former is an evidence-based intervention, whereas the efficacy of the latter has not been established. We compare pain and functional outcomes 1 week and 3 months after ED discharge among patients randomized to a 1-week course of naproxen+diazepam versus naproxen+placebo. This was a randomized, double-blind, comparative efficacy clinical trial conducted in an urban health care system. Patients presenting with acute, nontraumatic, nonradicular low back pain of no more than a duration of 2 weeks were eligible for enrollment immediately before discharge from an ED if they had a score greater than 5 on the Roland-Morris Disability Questionnaire, a validated 24-item inventory of functional impairment caused by low back pain. Higher scores on the questionnaire indicate greater functional disability. The primary outcome in the trial was improvement in the score between ED discharge and 1 week later. Secondary outcomes included pain intensity 1 week and 3 months after ED discharge, as measured on a 4-point descriptive scale (severe, moderate, mild, and none). All patients were given 20 tablets of naproxen 500 mg, to be taken twice a day as needed for low back pain. Additionally, patients were randomized to receive either 28 tablets of diazepam 5 mg or identical placebo, to be received as 1 or 2 tablets every 12 hours as needed for low back pain. All patients received a standardized 10-minute low back pain educational session before discharge. Using a between-group mean difference of 5 Roland-Morris Disability Questionnaire points, a previously validated threshold for clinical significance, we calculated the need for at least 100 patients with primary outcome data. Enrollment began in June 2015 and continued for 9 months. Five hundred forty-five patients were screened for eligibility. One hundred fourteen patients met selection criteria and were randomized. Baseline demographic characteristics were not substantially different between the 2 groups. One hundred twelve patients (98%) provided 1-week outcome data. The mean Roland-Morris Disability Questionnaire score of patients randomized to naproxen+diazepam improved by 11 (95% confidence interval [CI] 9 to 13), as did the mean score of patients randomized to naproxen+placebo (11; 95% CI 8 to 13). At 1-week follow-up, 18 of 57 diazepam patients (32%; 95% CI 21% to 45%) reported moderate or severe low back pain versus 12 of 55 placebo patients (22%; 95% CI 13% to 35%). At 3-month follow-up, 6 of 50 diazepam patients (12%; 95% CI 5% to 24%) reported moderate or severe low back pain versus 5 of 53 placebo patients (9%; 95% CI 4% to 21%). Adverse events were reported by 12 of 57 diazepam patients (21%; 95% CI 12% to 33%) and 8 of 55 placebo patients (15%; 95% CI 7% to 26%). Among ED patients with acute, nontraumatic, nonradicular low back pain, naproxen+diazepam did notimprove functional outcomes or pain compared with naproxen+placebo 1 week and 3 months after ED discharge.

A preliminary investigation to group disparate batches of licit and illicit diazepam tablets using differential scanning calorimetry

Application of Differential Scanning Calorimetry (DSC) coupled with principal component analysis for the qualitative analysis of licit and illicit diazepam tablets.

A didactic approach for quantification of diazepam tablets by UV spectrophotometry

The present paper describes a simple laboratory procedure for the quantification of diazepam, a central nervous system depressant benzodiazepine, by ultraviolet spectroscopy. Standard solutions of diazepam, prepared from a stock solution, were used to construct a calibration curve. Commercial tablets of diazepam were then analysed and the results obtained were in accordance with the expected percentage range of the manufacturer’s claim and with the specifications of the Portuguese Pharmacopeia.

The Solubility - Intrinsic Dissolution Rate of Diazepam and Inclusion Complexes Diazepam with 2-Hydroxypropyl-β-Cyclodextrin

When the fast absorption of diazepam is needed in order to suppress febrile convulsions and epileptic seizures, the most suitable is intravenous application diazepam. To avoid inappropriate self administration of such diazepam dosage form, orodispersible tablets of diazepam would be the dosage form of choice. Poor solubility of diazepam in water is directly related to its dissolution rate after release from a solid dosage form. Inadequate dissolution rate of diazepam can be the limiting factor for its absorption rate. Inclusion complexation of diazepam with 2-hydroxypropyl-β-cyclodextrin was carried out to increase the solubility of diazepam at pH 6.8. Determination of the intrinsic dissolution rate of diazepam as well as complexated diazepam was carried out to predict the absorption rate of diazepam at given pH value. The solubility of micronized diazepam (particle size 5.4 µm) at pH 6.8, was 0.043 mg mL-1, while the solubility of non-micronized diazepam (particle size 414.8 µm) at the same pH was 0.036 mg mL-1. Inclusion complexation of diazepam with 2-hydroxypropyl-β-cyclodextrin resulted in increased solubility of diazepam. One mole of 2-hydroxypropyl-β-cyclodextrin increased the solubility of micronized diazepam 6.82 fold, while two moles of 2-hydroxypropyl-β-cyclodextrin increased the solubility of diazepam 12.55 fold. Given that the values of intrinsic dissolution rates (IDR) of micronized diazepam, non-micronized diazepam and inclusion complex D: 2-HP-β-CD 1:1 were less than 0.1 mg min-1 cm-2, the absorption of diazepam dissolution would be the rate limiting step to absorption, while the inclusion complex D: 2-HP-β-CD 1:2 where an IDR value was greater than 0.1 mg min-1 cm-2 at pH 6.8, suggested that its dissolution might be the rate-limiting step to absorption. Hydroxypropyl-β-cyclodextrin increased the solubility of diazepam at pH 6.8, thus increasing the dissolution rate and causing faster absorption of diazepam at pH 6.8.

Formulation and Optimization of Orodispersible Tablets of Diazepam

Diazepam is one of the most prescribed benzodiazepines. The purpose of the present research was to optimize the formulation of orodispersible tablets of diazepam. Orodispersible tablets of diazepam were prepared using different types of superdisintegrants (Ac-Di-Sol, sodium starch glycolate, and crospovidone (CP)) and different types of subliming agents (camphor and ammonium bicarbonate (AB)) at different concentrations and two methods of tablets preparations (wet granulation and direct compression methods). The formulations were evaluated for flow properties, wetting time, hardness, friability, content uniformity, in vivo disintegration time (DT), release profiles, and buccal absorption tests. All formulations showed satisfactory mechanical strength except formula F5 which contains camphor and formula F9 which is prepared by direct compression method. The results revealed that the tablets containing CP as a superdisintegrant have good dissolution profile with shortest DT. The optimized formula F7 is prepared using 10% CP as a superdisintegrant and 20% AB as a subliming agent by wet granulation method which shows the shortest DT and good dissolution profile with acceptable stability. This study helps in revealing the effect of formulation processing variables on tablet properties. It can be concluded that the orodispersible tablets of diazepam with better biopharmaceutical properties than conventional tablets could be obtained using formula F7.

Impact of Particles Size Distribution on Diazepam 5mg Tablets Dissolution

Diazepam is one of most frequently prescribed benzodiazepines. It is classified as a class I substance according to the Biopharmaceutics Classification Scheme (BCS). Diazepam tablets were prepared using different API rawmaterials. Before the formulation, we measured particle size distribution on Malvern Instruments Ltd Mastersizer 2000. The tablets were prepared by employing conventional wet granulation. The formulations were evaluated for hardness, friability, content uniformity, in vitro disintegration time (DT), release profiles. The dissolution profile testing is performed on the two formulations with different particles size distribution. Test parameters were: medium 0.1 mol / l hydrochloric acid, 900 ml, temperature 37°C ± 0.5°C, Mixing Speed 100 rpm, Number of tested tablets 12, Testing Cycle 10, 15, 20, 25 and 30 min. Instrument: Varian Van Kel VK7025, Varian Cary 50. We used the spectrophotometric method with absorbance measuring on 242 nm for quantification. Results for particle size distribution for first Diazepam API particle distribution were d (0.10): 88.743 μm; d (0.50): 305.231 μm; d (0.90): 655.911 μm, and for the second raw-material of API was d (0.10):1.998 μm; d (0.50): 4.419 μm; d (0.90): 8.845 μm. The results of diazepam dissolution for two formulations and f2 value with reference drug are presented in Table 1:

Statistical Evaluation of Influence of Polymers Concentration on Disintegration Time and Diazepam Release from Quick Disintegrating Rapid Release Tablet

This study describes the formulation of rapidly disintegrating, fast dissolving diazepam tablets intended for use in the oral cavity. The tablets were prepared by the conventional wet granulation method using solid dispersion of the drug with PEG-4000 and/or PEG-6000. A 3(2) factorial design was used to reduce the number of experimental runs and to obtain several formulations by which tablets disintegrated within 3 min and released 85% of the drug in less than 30 min. Several tablet formulations prepared with different amounts of PEGs in solid dispersion met the above two criteria. However, tablets which were prepared with PEG-4000 alone at the lowest concentration disintegrated in the shortest time (32.12 sec) and released 85% of the drug most rapidly (11.03 min).