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A Review on Sublingual Dosage Form AEGAEUM JOURNAL ISSN NO: 0776-3808 A Review on Sublingual Dosage Form Yadav Dimple Shyamkumar*^, Ms.Jimmy Limbachiya^, Dr.Kinjal Solanki^, Dr.Vikram Pandhya^ ^Shankersinh Vaghela Bapu Institute of Pharmacy, Gandhinagar, Gujarat, India. E-mail- [email protected] Abstract Oral administration is one of the most convenient forms for the intake of drug due to ease of administration, painless, versatility, and paramount patient compliance. The demand of fast disintegrating tablets has been growing, during the last decades especially for geriatric and pediatric patients due to dysphasia. Despite of tremendous innovations in drug delivery, the oral route remains the preferred route for administration of therapeutic agents because of accurate dosage, low cost therapy, self-medication, non-invasive method and ease of administration which ultimately lead to high level of patient compliance. Peroral administration of drug has disadvantages such as Hepatic first pass metabolism and enzymatic degradation within the GI tract that limits oral administration of certain classes of drug like peptides and proteins. So, other absorptive mucosa is considered as potential sites for drug administration. Trans-mucosal routes of drug delivery (i.e. the mucosal linings of the nasal, rectal, vaginal, ocular, and oral cavity) offer several advantages over peroral administration for systemic delivery. Keywords: Sublingual Tablets, mechanisms, Properties of Sublingual Tablets, advantages and disadvantages, ingredients used in dosage, Sublingual drug delivery, Improved bioavailability, Techniques, Evaluation. recent trends on Sublingual Tablets and case study. INTRODUCTION Drug delivery through the sublingual route had emerged from the desire to provide immediate onset of pharmacological effect. Dysphasia (difficulty in swallowing) is a common problem of all age groups, especially geriatrics, pediatric, and patients who are mentally retarded, uncooperative, nauseated or on reduced liquid intake/diets have difficulties in swallowing these dosage forms. Drugs that are given sublingually reach directly in to the systemic circulation through the ventral surface of the tongue and floor of the mouth. The drug is rapidly absorbed into the reticulated vein that lies underneath the oral mucosa, and transported through the facial veins, internal jugular vein, and braciocephalic vein and then drained in to systemic circulation. Considering the oral cavity sublingual area is the most Volume 8, Issue 3, 2020 http://aegaeum.com/ Page No: 261 AEGAEUM JOURNAL ISSN NO: 0776-3808 permeable part of the buccal cavity. The decreasing order of permeability in the buccal cavity is the sublingual, the buccal area (cheek), then the palatal area. The order is generally based upon the relative thickness and the extent of blood supply to the specific part. Sublingual- Under the tongue. Sublingual dosage form can be define as dosage form that is to be placed beneath the tongue where it will dissolve and the drug will be absorbed directly through the sublingual mucosa. The dosage form not intended to be swallowed or chewed. Sublingual administration of the drug means placement of the drug under the tongue and drug reaches directly in to the blood stream through the ventral surface of the tongue and floor of the mouth. The drug solutes are rapidly absorbed into the reticulated vein which lies underneath the oral mucosa, and transported through the facial veins, internal jugular vein, and brachiocephalic vein and then drained in to systemic circulation.(1,2) Figure-1 Sublingual Introduction Sublingual Glands Another name of sublingual gland is salivary glands which are present in the floor of the mouth, underneath the tongue. Drugs having short delivery and infrequent dosing regimen could be delivered successfully through sublingual route because of high permeability and rich blood supply, the sublingual route produces a rapid onset of action. A good oral hygiene could be promoted with the help of sublingual glands. Sublingual glands are also known for their binding and lubricating functions, and sublingual gland secretion makes the food slippery and easily swallowable. High content of saliva in the masticated food helps the food to Volume 8, Issue 3, 2020 http://aegaeum.com/ Page No: 262 AEGAEUM JOURNAL ISSN NO: 0776-3808 move without any difficulty. Saliva secretion plays a major role in shaping the principle physiological environment of oral cavity in terms of pH, fluid volume and composition. Saliva secretion has been promoted by 3 major salivary glands which are parotid, submaxillary, sublingual glands. However minor salivary or buccal glands are also involved in saliva secretions which are situated in or immediately below the mucosa. Saliva regulates oral microbial flora by maintaining the oral pH and enzyme activity. Sublingual glands are known for their viscous saliva with limited enzymatic activity whereas parotid and submaxillary gland produces watery secretion. Saliva helps in lubricating the oral cavity; it facilitates swallowing and prevents demineralization of the teeth. Approximately 0.5-2.0L of saliva has been secreted by salivary gland. However the volume of saliva which is available constantly is around 1.1ml, thus providing a relatively low fluid volume available for drug release from delivery systems compared to GIT. If we compare the GI fluid and saliva, saliva is relatively less viscous. The flow rate of saliva which depends on 3 factors like the time of day, the type of stimulus and the degree of stimulation.(3,4) Fig. no 2 Sublingual gland. Why sublingual mucosa is more permeable than other region of oral mucosa: Sublingual mucosa is thinner than other oral region – sublingual epithelial has 8-12 cell region whereas epithelial about 40-50 cell layer thick. Sublingual region is very rich in blood supply. Volume 8, Issue 3, 2020 http://aegaeum.com/ Page No: 263 AEGAEUM JOURNAL ISSN NO: 0776-3808 Saliva tends to accumulate in sublingual region because two major salivary duct open into this region. Organised keratins and lipids are absent in sublingual mucosa. Polar lipids are found in the intercellular space of sublingual mucosa which increased permeation of hydrophilic compound. Note – Membrane coating granules are the permeability barrier in sublingual mucosa which are present in nonlamellar form.(5) 1.1.2 Disadvantages/ Limitation of Sublingual Tablet: • Although this site isn't well matched to sustained delivery systems. • Sublingual medication can't be used once a patient is uncooperative or unconscious. • Since articulator administration of medicine interferes with ingestion, drinking, and talking, this route is mostly thought-about unsuitable for prolonged administration. • High dose can not be administered. • Not appropriate for bitter and aggravating medication. • Less patient compliance. • Ingestion and drinking, smoking isn't allowed. • Extremely ionic drug can not be administered. (6-7) 1.1.3 Special Features of Sublingual Tablet: Easily administered. Available in various size and shapes. Should not be Obstructive. It should adhere to the oral cavity easily. Should processes fast dissolve without water. Rapid release. (8-9) 1.1.4 The Ideal Characteristics of a Drug To Be Selected: No bitter taste. Dose lowers than 20 mg. Small to moderate molecular weight. Good stability in water and saliva. Volume 8, Issue 3, 2020 4 http://aegaeum.com/ Page No: 264 AEGAEUM JOURNAL ISSN NO: 0776-3808 Partially no ionized at the oral cavities pH. Under going first pass effect. Many drug properties could potentially affect the performance of sublingual tablets like solubility, crystal morphology, particle size, hygroscopicity, compressibility and bulk density of drug. Some drugs undergoes extensive first pass metabolism which results in poor bioavailability of its oral dosage forms, that kind of drugs are suitable for sublingual dosage form. Drugs that are unstable in parenteral preparation are suitable for sublingual dosage form. Many pharmaceuticals are designed for sublingual administration, including cardiovascular drugs, steroids, barbiturates, enzymes, antiemetics, vitamins, minerals and vaccines. (10-11) 1.1.5 Advantage of Sublingual Tablet: Ease of administration to patients who refuse to swallow a tablet, such as paediatric , geriatric patients and psychiatric patients. A relatively rapid onset of action can be achieved compared to the oral route, and the formulation can be removed if therapy is required to be discontinued. The large contact surface of the oral cavity contributes to rapid and extensive drug absorption. Liver is bypassed and also drug is protected from degradation due to pH and digestive enzymes of the middle gastrointestinal tract. They also present the advantage of providing fast dissolution or disintegration in the oral cavity, without the need for water or chewing. Ease of administration to patients who refuse to swallow a tablet, such as paediatric, geriatric patients and psychiatric patients. Convenience in administration of drug and accurate dosing as compared to liquid formulations. Water is not required for swallowing the dosage form, which is convenient feature for patients who are traveling and do not have immediate access to water. Good mouth feels property helps to change the basic view of medication as "bitter pill", particularly for paediatric patients. Volume 8, Issue 3, 2020 5 http://aegaeum.com/ Page No: 265 AEGAEUM JOURNAL ISSN NO: 0776-3808 Fast dissolution of medicament and absorption
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