Design and Development of Terbutaline Sulphate Fast Mouth Dissolving Tablet

G. Singh, G. Singh, J. Malik
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Abstract

Asthma is a chronic inflammatory disease that causes an associated increase in airway hyperreactivity leading to recurrent episodes of wheezing, shortness of breath, chest tightness, and coughing, especially at night and early in the morning. Terbutaline sulfate is a selective beta2 adrenergic agonist. It is highly selective for β2 adrenergic receptors and has a long-lasting effect. It is given for symptomatic relief of bronchospasm and obstructive airway disease. Terbutaline sulfate is effective when taken orally, subcutaneously, or by inhalation. Although effects are rapidly observed after inhalation, the use of inhaled sympathomimetic drugs is initially associated with possible tachyphylaxis of resistance to beta-agonists, cardiac arrhythmias due to β1-adrenergic receptor stimulation, and Freon propellants. Raised concerns about hypoxemia and arrhythmia due to fluorinated hydrocarbons in many patient groups, including the elderly, children, the mentally ill, and uncooperative or nauseous patients, have difficulty swallowing conventional dosage forms such as tablets. Swallowing conventional tablets is further hampered by conditions such as water unavailability, allergic reactions, and coughing fits. These problems can be overcome by developing rapidly disintegrating and dissolving tablet dosage forms for oral administration, as they dissolve in saliva and do not require water to be swallowed. When ingested, saliva serves to quickly dissolve the dosage form. A fast mouth dissolving tablet (FMDT) is an oral solid dosage form that dissolves rapidly when placed on the tongue, releasing a drug that dissolves or disperses in saliva and can be swallowed without the need for drinking water. Additionally, some of the saliva-soluble drugs from the mouth, throat, and esophagus are absorbed once saliva enters the stomach, increasing bioavailability by avoiding first-pass metabolism.
硫酸特布他林快速口腔溶片的研制
哮喘是一种慢性炎症性疾病,可引起气道高反应性增加,导致反复发作的喘息、呼吸短促、胸闷和咳嗽,尤其是在夜间和清晨。硫酸特布他林是一种选择性β 2肾上腺素能激动剂。它对β2肾上腺素能受体具有高度选择性,并具有持久的作用。用于支气管痉挛和气道梗阻性疾病的症状缓解。硫酸特布他林口服、皮下或吸入均有效。虽然吸入后可迅速观察到效果,但吸入拟交感神经药物的使用最初可能与β -激动剂耐药的快速反应、β1-肾上腺素能受体刺激引起的心律失常和氟利昂推进剂有关。对许多患者群体(包括老年人、儿童、精神病患者和不合作或恶心的患者)由于氟化碳氢化合物导致的低氧血症和心律失常的担忧日益增加,这些患者难以吞咽片剂等常规剂型。由于缺水、过敏反应和咳嗽发作等情况,进一步阻碍了常规药片的吞咽。这些问题可以通过开发快速分解和溶解的口服片剂剂型来克服,因为它们可以溶解在唾液中,不需要吞咽水。当摄入时,唾液可以迅速溶解剂型。快速口腔溶解片剂(FMDT)是一种口服固体剂型,当放在舌头上时迅速溶解,释放出溶解或分散在唾液中的药物,无需饮用水即可吞咽。此外,一些来自口腔、咽喉和食道的唾液溶性药物一旦进入胃就被吸收,通过避免首过代谢提高生物利用度。
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