Fast Dissolving Tablet of Terbutaline Sulfate: Review
Green Royal Academy of Pharmaceutical Education & Sciences, Andhra Pradesh, India
- Corresponding Author:
- Shakeena G
Department of Pharmaceutical Analysis and Quality Assurance, Green Royal Academy of Pharmaceutical Education & Sciences, Ponguturu, Koyyalagudem, West Godavari–534312, Andhra Pradesh, India
Email: shakeena.[email protected]
Received date: 10-07-2016 Revised date: 12-08-2016 Accepted date: 18-08-2016
Visit for more related articles at Research & Reviews in Pharmacy and Pharmaceutical Sciences
Received:10-07-2016 Revised: 12-08-2016 Accepted:18-08-2016 *Corresponding author: Shakeena G, Department of Pharmaceutical Analysis and Quality Assurance, Green Royal Academy Of Pharmaceutical Education & Sciences, Ponguturu, Koyyalagudem, West Godavari–534312, Andhra Pradesh, India, Tel:9949581690. Email: [email protected] Keywords: Fast dissolving tablet, Microcrystalline cellulose, Oral route, Sodium starch glycolate, Terbutaline sulfate. ABSTRACT Terbutaline sulfate is employed to treat respiratory disease and respiratory disorders. Terbutaline belongs to a category of beta-adrenergic agonist bronchodilators. It is a β2 blocker used to treat cardiovascular diseases like high blood pressure, cardiopathy, and disturbances of regular recurrence, myocardial infarct and purposeful heart disorders. Fast dissolving tablets of terbutaline sulfate is ready by adding crystalline cellulose and sodium starch glycolate. Terbutaline sulfate half-life is 2-3 hours oral availability is 38 ± 14 % and it's eliminates quickly from plasma, microcrystalline cellulose and sodium starch glycolate was discharged 95.2% and 96.8% of drug at intervals 8-10 min. These tablets are used for patients who might have problem in swallowing of typical tablets; frequent administration is required to take care of therapeutic concentration. Fast dissolution and absorption of drug might turn out rapid onset of action. Fast dissolving drug delivery systems FDDDSs that disintegrate and release the active ingredient quickly which don't need water for swallowing. Oral administration of bitter medication with associate adequate degree of palatableness is achieved by taste masking. Fast dissolving tablet FDT is employed as super disintegrants which can give immediate disintegration and releases the drug in saliva. Fast dissolving tablets of terbutaline sulfate tablets are ready by the direct compression technique once incorporating with super disintegrants similar to crystalline cellulose and sodium starch glycolate in numerous concentrations. evaluation for prepared tablets were weight variation, thickness, hardness, friability, wetting time, drug content, water absorption quantitative relation, in vitro dispersion time, in vitro disintegration time and in vitro drug release..
Fast dissolving tablet, Microcrystalline cellulose, Oral route, Sodium starch glycolate, Terbutaline sulfate.
Now a days swallowing is tough for all age groups, specifically pediatric medicine, due to physiological changes related to these age groups. Oral route of administration is that the common technique for administering medicines. The parenteral route of administration is very important in treating medical emergencies during which patient cannot swallow [1-6]. However it's probable that a minimum of ninety two of all medication used to give general effects are administered by the oral route. Different classes that have issues using standard oral dose forms include are they mentally ill, uncooperative and sick patients, those with conditions of motion sickness, sudden episodes of allergic attack and coughing. Sometimes, it's going to be tough to swallow standard product due to unavailability of water. These issues led to the development of a novel kind of solid oral dose type called mouth-dissolving tablets, which disintegrate and dissolve rapidly in saliva without the need of the water [7-15]. They’re additionally referred to as fast dissolving tablets, melt-in-mouth tablets, rapid melts, porous tablets, oro-dispersible, fast dissolving or rapidly disintegrating tablets. The main proposal of the present review is to study the usefulness of fast dissolving drug delivery and concisely the ideal properties, limitations and advantages, conventional and patented technologies, assist marketed formulations in FDTs and evaluation [16-25].
Fundamentals of Designing FDT
For rapid dissolution of dose, water should quickly penetrate into the tablet matrix to cause quick disintegration and instant dissolution of tablet many techniques are used to attain these fundamentals to formulate FDT; like
• Tablet molding
• Freeze drying
• Spray drying
• Addition of disintegrating agent [26-38].
Key Ingredients Used In FDT
The main active ingredients used in FDT are Bronchodilators, Beta-blockers, Antitussive, anti-asthmatic agents, Antipyretic, Antiulcer agents, Coronary vasodilators, Peripheral vasodilators, Synthetic antibacterial agents, Antipasmodics, Muscle relaxants, Anticoagulants, Antihistaminic, Vitamins, Antihistamines (Figure 1).
Figure 1: Terbutaline Sulfate [±-α-[tert- butyl amino methyl]-3, 5-dihydroxybenzyl alcohol sulfate 2:1 salt]
• Polyethylene glycol is used as binders
• Alkyl sulfates, propylene glycol esters, lecithin, sucrose esters are used as emulsifying agents
• Mannitol, polydextrose, lactitol and starch hydrolysate, Lactitol are used as bulking agents
• Dextrose, fructose, sucralose are used as flavoring agents
Techniques used in the preparation of FDT are Lyophilization, Spray Drying, Sublimation, Tablet moulding, Taste masking, Addition of disintegrants etc [39-47].
Chemical formula: C12??H19NO32. H2SO4
Solubility of Terbutaline sulfate is taken orally. It is freely soluble in water and in 0.1N Hcl, slightly soluble in methanol, and insoluble in chloroform. Pharmacokinetics of Terbutaline sulphate is administered orally as well as subcutaneous route of administration. The pharmacokinetic parameters are as follows Bio availability as 60%, and its onset of action is 30 mins, t ½ is 3-4 hours, Tmax is 2-3 hours, C max is 9.6 3.6 ng/ml, AUC is 54.6 & 53.1 hr.ng/ml and its Duration of action is 8 hrs [48-68].
Clinical pharmacology of terbutaline sulfate it Stimulates β-adrenergic receptors and also stimulates the production of cyclic adenosine-3′, 5′-monophosphate, Decreases resistance of airways, relaxes uterine smooth muscle and inhibits uterine contractions [69-75]. (Table 1).
||Potentiation of vascular effects
||Extreme caution recommended with concomitant therapy or in patients receiving terbutaline ≤ 2 weeks after discontinuance of tricyclic antidepressants
|β-Adrenergic blocking agents
||Potential antagonism of pulmonary effects resulting in severe bronchospasm in asthmatic patients
||If concomitant therapy required, consider cautious use of cardio selective β-adrenergic blocking agents
|Diuretics, potassium depleting
||Potential for decreased serum potassium concentrations and/or ECG changes, especially when recommended β-adrenergic agonist dosage exceeded
||Use concomitantly with caution
||Potentiation of vascular effects
||Extreme caution recommended with concomitant therapy or in patients receiving terbutaline ≤ 2 weeks after discontinuance of MAO inhibitors
||Potential for additive adverse cardiovascular effects
||Concomitant use not recommended
Does not preclude use of an inhaled adrenergic agonist bronchodilator to relieve acute bronchospasm during long-term oral terbutaline therapy
Table 1: Interactions for Terbutaline Sulfate.
Fast dissolving tablets of Terbutaline sulfate may propose improved biopharmaceutical properties. The parameters like hardness, friability, diameter, thickness, weight variation and content uniformity was evaluated for all the batches of tablets these technologies have sufficient mechanical strength, quick dissolution/disintegration in the mouth. The characteristic and benefits of quick dissolving tablet administration without water wherever anytime cause their suitableness to geriatric and paediatric patients. The comparison of effect of natural and synthetic super disintegrant was discussed with in-vitro disintegration time and wetting time because these two are very important for quick and effective disintegration which leads to faster dissolution of dosage form.
- Soha S, et al. Fast-Dissolving Sublingual Films of Terbutaline Sulfate: Formulation and In Vitro/In Vivo Evaluation. Mol Pharmaceutics. 2013;10:2942-2947.
- Asija R, et al. A review on fast dissolving drug delivery system. Inter J Res Pharm Sci. 2014;4:7-12.
- Sanjay KB, et al. Design and Evaluation of Fast Dissolving Tablet of Terbutaline Sulphate, Research Journal of Pharmaceutical. Biological and Chemical Sciences. 2012;3:138-154.
- John PE and John CM Autism is not caused by Terbutaline. Autism-Open Access. 2015;5:1.
- Manoj G, et al. Does Anesthesia Induction during Electrophysiologic Studies Induce Tachycardia in Pediatric Patients. J Cardiovasc Dis Diagn. 2016;4:250.
- Sai KV, et al. Design and Development of Fast Dissolving Tablets of Ibuprofen, J Pharmacy and Pharmaceutical Sciences 2013.
- Rajnikant MS, et al. Development of Fast Dissolving Tablets Containing Ondansetron via Camphor Sublimation and its Characterization. J Pharmacy and Pharmaceutical Sciences. 2012.
- Kuljit Singh, et al. Fast Dissolving Tablet:A Novel Approach for Delivery of Glibenclamide. Pharmaceutics and Nanotechnolog. 2013.
- RenatiDamodar, et al. Formulation and Evaluation of Fast Dissolving Tablets of Diclofenac Sodium by Novel Hole Technology. J Mol Pharm Org Process Res 2014;2:116
- Damodar R and Vinay CV. Role of Novel Hole Technology in Fast Dissolving Tablets Review Article. J Mol Pharm Org Process Res. 2014;2:001.
- DW Newton and EY Fung DA. Williams Stability of five catecholamines and terbutaline sulfate in 5% dextrose injection in the absence and presence of aminophylline. American journal of health-system pharmacy 1981;38:1314-1319.
- Pendergast J, et al. Comparative efficacy of terbutaline administered by Nebuhaler and by nebulizer in young children with acute asthma. European Journal of Respiratory Diseases. 1989;151:406-408.
- S Drblik, et al. Comparative efficacy of terbutaline sulphate delivered by Turbuhaler dry powder inhaler or pressurised metered dose inhaler with Nebuhaler spacer in children during an acute asthmatic episode. Archives of Disease in childhood. 2003;88:319-323.
- Bye PT et al. Plasma cyclic AMP levels in response to exercise and terbutaline sulphate aerosol in normal and asthmatic subjects. European Journal of Respiratory Diseases. 1980;61:287-297.
- van den Berg W, et al. The effects of oral and subcutaneous administration of terbutaline in asthmatic patients. European Journal of Respiratory Diseases. Supplement 1984;134:181-193.
- Lalatendu Panigrahi, et al. The effect of pH and organic ester penetration enhancers on skin permeation kinetics of terbutaline sulfate from pseudolatex-type transdermal delivery systems through mouse and human cadaver skins. AAPS PharmSciTech. 2005;6:E167.
- Lam F, Elliott J, et al. Clinical Issues Surrounding the Use of Terbutaline Sulfate for Preterm Labor. 1998;53:85s-95s.
- Cotton DB, et al. Comparison of magnesium sulfate, terbutaline and a placebo for inhibition of preterm labor. A randomized study. The Journal of Reproductive Medicine. 1984;29:92-97.
- Miller JM Jr, et al. A comparison of magnesium sulfate and terbutaline for the arrest of premature labor. A preliminary report. The Journal of Reproductive Medicine. 1982;27:348-351.
- Rashid S and Sawh C. The Optimal Arterial Access for Coronary Angiography:Femoral Route versus the Radial Route. Journal of Vascular Medicine & Surgery. 2016;4:271.
- Burton M Altura, et al. Genotoxic Effects of Magnesium Deficiency in the Cardiovascular System and their Relationships to Cardiovascular Diseases and Atherogenesis, J Cardiovasc Dis Diagn. 2016;S1:1.
- Vladimir I Ermoshkin. Arteriovenous anastomoses and cardiovascular diseases. Arrhythmia and Cardiac Surgery. 2016;7:6.
- Shu-Tzu Huang, et al. The Importance of Continuity of Care in Children with Asthma. Gen Med Los Angeles. 2016;4:243.
- Inan MI, et al. Effort Dyspnea, if it is not Asthma? An Omega Epiglottis Case Report. J Clin Case Rep. 2016;6:813.
- Gadge PB and Rode SV. Automatic Wheeze Detection System as Symptoms of Asthma Using Spectral Power Analysis. J Bioengineer & Biomedical Sci. 2016;6:191.
- Naveed S, et al. Health-Related Quality of Life in Patients with Asthma, Survey based Study in Karachi, Pakistan. J BioequivAvailab. 2016;8:179-184.
- Xiaoyu M, et al. Magnesium Sulfate Combined Montelukast Sodium Clinical Observation on Treatment of Infantile Asthma. Neonat Pediatr Med. 2016;2:108.
- Finkel J, et al. Adequate Vitamin D3 Supplementation during Pregnancy:Decreasing the Prevalence of Asthma and Food Allergies. Matern Pediatr Nutr. 2015;1:105.
- Shah SA, et al. Impact of a Novel Plant-based Treatment Option in Improving Pulmonary Function Markers in Patients with Chronic Obstructive Pulmonary Disease and Asthma. Altern Integr Med. 2016;5:215.
- Ozolua RI, et al. Evaluation of the Anti-asthmatic and Antitussive Effects of Aqueous Leaf Extract of Ocimum gratissimum in Rodents. Med Aromat Plants. 2016;5:235.
- Assaf SJ, et al. Ventilation Heterogeneity and Airway Hyperreactivity in Children with Well Controlled Asthma. J Pulm Respir Med. 2016;6:321.
- de Souza A, et al. Asthma and Environmental Indicators:A Time-series Study. J Allergy Ther. 2016;7:232.
- Munesh T, et al. Acute Cardiorespiratory Decompensation in a Child with Nephrotic syndrome with Bronchial Asthma:Is it Exaggeration of Bronchial Asthma?. Clin Pediatr. 2016;1:104.
- Sonathi V, et al. Economic Evaluation of Omalizumab in the Treatment of Severe Allergic Asthma in Adult Patients in Greece:A Cost Effectiveness Analysis of Clinical Trial and Real-Life Data. Pharmacoeconomics. 2015;1:103.
- Sawaguchi H and Muraki M. Effect of Aging and Respiratory Infection to Duration of Hospitalization in Asthma Exacerbation. J Clin Respir Dis Care. 2015;1:105.
- Paris JM, et al. Asthma Diagnosis in Spain:Survey of Opinions, Attitudes and Knowledge among Primary Care Physicians. J Pulm Respir Med. 2015;5:308.
- Qutub MM et al. The Link between Uncontrolled Asthma and Sensitization to Inhalant Allergens:Evidence from Jeddah, Saudi Arabia. Fam Med Med Sci Res. 2015;5:191.
- Cortez M, et al. Lelp-1, Its Role in Atopic Dermatitis and Asthma:Poland and Portugal. J Allergy Ther. 2016;7:229.
- Volovitz B and Nussinovitch M. Presence and Treatment of Asthma Exacerbation in Infants and Children. PediatTherapeut 2016;6:276.
- Banerjee ER. Specific Spatio-Temporal Interplay of Cell Movement defines Asthma Pathogenesis. Biol Syst Open Access. 2015;4:140.
- Vodounon CA, et al. Nuclease Activity Associated with Secreting Granules by Lymphocytes in Patients with Bronchial Asthma. Biol Med Aligarh. 2015;8:264.
- Luljeta NA, et al. The Frequency of Influenza-Like Illness in Patients with Allergic Asthma on Immunotherapy. Immunome Res. 2015;11:103.
- Kulkarni H, et al. Cardiac Troponin I Levels in Children with Acute Severe Asthma Treated with IV Salbutamol. Lung Dis Treat. 2015;1:102.
- Abd Elfatah WA. The Effectiveness of Self-Control and Anxiety Management Training to Reduce Anxiety and Improve Health-Related Quality of Life in Children with Asthma. J Psychol Psychother. 2015;5:220.
- Zedan M and Osman A. Clinical Asthma Phenotypes;A Challenging but Promising Spectrum, Immunol Disord Immunother. 2015;1:e102.
- Reyes-Barron C, et al. Pharmacogenetics of Antidepressants. A Review of Significant Genetic Variants in Different Populations, Clin Depress. 2016;2:109.
- EL-Arabey AA and Abd-Allah AR. Antidepressants as a New Approach for Protective Interventions of Cisplatin-Induced Nephrotoxicity. J Kidney. 2015;1:102.
- Alekhya P, et al. Treatment and Disease Related Factors Affecting Non-adherence among Patients on Long Term Therapy of Antidepressants. J Depress Anxiety, 2015;4:175.
- Fonseca AP and Leala V. Use of Antidepressants to Treat Postpartum Depression, During Breast Feeding. J Depress Anxiety. 2014;3:148.
- Uguz F. The Current Status in Treatment of Depressive or Anxiety Disorders During Pregnancy with Antidepressants. J Clinic Case Reports. 2012;2:e114.
- Christopher IW. Herbal Diuretics. J Nutr Food Sci. 2016;6:469.
- Kuhn-Thiel AM, et al. MorbusDiureticus in the Elderly MDE–Inappropriate Application of Diuretics FourCase Reports. Aging Sci. 2014;2:124.
- Wu L, et al. QRAR Models for Diuretics using mixed Micellar Liquid Chromatography. J BioequivAvailab. 2011;3:169-173.
- Sultana N, et al. RP-HPLC Method for Simultaneous Determination of Captopril and Diuretics:Application in Pharmaceutical Dosage Forms and Human Serum. J Chromatograph SeparatTechniq. 2011;2:109.
- Zhouping W, et al. Sensitive flow-injection chemiluminescence determination of terbutaline sulfate based on enhancement of the luminol–permanganate reaction. Analy and Bioanaly Chem. 2004;3:834-840.
- Lam F, et al.Clinical Issues Surrounding the Use of Terbutaline Sulfate for Preterm Labor.Obstetrical & Gynecological Survey.1998;53:85s-95s.
- Borgström L, et al. The inhalation device influences lung deposition and bronchodilating effect of terbutaline. 1996;153:1636-1640.
- Robin KH, et al. Characterization of Polymorphs and Solvates of Terbutaline Sulfate. ACS Central Science. 2008;8:80-90.
- BorgstromL, et al. Lung deposition of budesonide inhaled via Turbuhaler:a comparison with terbutaline sulphate in normal subjects, Euro Resp J. 1994;7:69-73.
- Shah U and Augsburger L. Multiple sources of sodium starch glycolate, NF:evaluation of functional equivalence and development of standard performance tests.Pharm Dev Technol. 2002;7:345-59.
- Edge S, et al.Chemical characterisation of sodium starch glycolate particles.Int J Pharm. 2002;240:67-78.
- Harold Kim and Jorge Mazza. Asthma, Allergy, Asthma & Clinical Immunology. 2011;7:s1-s2.
- Peter JB. Severe asthma:Advances in current management and future therapy. The Journal of Allergy and Clinical Immunology.2012;129:48-59.
- Roberts JR, et al. Sustained-release terbutaline vs sustained-release theophylline in young patients with asthma. Am J Dis Child. 1986;140:650-654.
- Sandy W. FDA warns against certain uses of asthma drug terbutaline for preterm labor. FDA. 2011.
- Pierce RJ, et al.Comparison of intravenous and inhaled terbutaline in the treatment of asthma. Chest Jouranl. 1981;79506-511.
- Bateman JR, et al. Effects of terbutaline sulphate aerosol on bronchodilator response and lung mucociliary clearance in patients with mild stable asthma.Br J Clin Pharmacol. 1983;15:695-700.
- Ellul-Micallef R.Effect of terbutaline sulphate in chronic "allergic" cough.Br Med J. 1983;287:940-943.
- Smith PR, et al.A comparative study of subcutaneously administered terbutaline and epinephrine in the treatment of acute bronchial asthma. Chet Journal.1977;71:129-134.
- Robert P, et al. Terbutaline and Associated Risks for Neurodevelopmental Disorders. Child Development Research. 2014;2014:1-6.
- Federico FNI, et al. Severe Acute Asthma Exacerbation in Children: A Stepwise Approach for Escalating Therapy in a Pediatric Intensive Care Unit.J Pediatr Pharmacol Ther. 2013;18:88-104.
- Gary R, et al. Managing Asthma Exacerbations in the Emergency Department. ATS Journal.2009;6:357-366.
- Deepak JS, et al.Development and Evaluation Of Dry Powder Inhalation System Of Terbutaline Sulphate For Better Management Of Asthma. Inter J Adv in Pharm Sci. 2010.
- Sellers WFS.Inhaled and intravenous treatment in acute severe and life-threatening asthma. BJA.2013;117:1-14.
- Nilsson HT, et al.The fate of3H-terbutaline sulphate administered to man as an aerosol.European Journal of Clinical Pharmacology.1976;10:1-7.