Routes of administration and dosage forms

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Routes of administration and dosage forms





Introduction


Following the administration of a medicine, the drug has to reach its site of action or receptor in order to produce an effect. How this is achieved is often a complex process affected by many factors. The first stage will be the release of the drug from the dosage form, to be followed by absorption into the body (unless it is for a surface effect at the site of administration). There is then a distribution process, usually in the blood, which will take the drug to the site of action. As soon as it is in the body, metabolic processes, especially in the liver, will start to change the drug and the elimination process will also commence. A detailed discussion of these processes is outside the scope of this book, although it does have a significant impact on the choice of both the route of administration and the actual dosage form. There is a growing awareness that the correct choices can have an important impact on therapeutic outcomes for the patient. This chapter will review the various routes of administration used for drug delivery and discuss some of their advantages and disadvantages. Brief details of a variety of dosage forms are also given. Figure 29.1 illustrates the principal routes of administration.




Routes of administration



The oral route


The oral route can produce either a systemic or a local effect. For a systemic effect, the drug, formulated in either a solid or a liquid form, is absorbed from the gastrointestinal tract (GIT). This is the most commonly used route for drug administration. There are several reasons for this:



However, there are disadvantages which should be borne in mind:



image The onset of action is relatively slow


image Absorption from the GIT may be irregular


image Some drugs are destroyed by enzymes and other secretions found in the GIT


image Because the blood supply from the GIT passes through the liver via the hepatic portal system, it is subject to hepatic metabolism before it enters the systemic circulation. This is called first pass or presystemic metabolism


image Drug solubility may be altered by the presence of other substances in the GIT, e.g. calcium


image Gastric emptying is very variable and can be influenced by factors such as food, drugs, disease state and posture. Not only does it affect the onset of action, but if it is extended it may cause a drug to be inactivated by gastric juices owing to prolonged contact


image It is an unsuitable route of administration in unconscious or vomiting patients and for immediate pre- or postoperative use.



The buccal routes


A drug is administered by these routes by being formulated as a tablet or spray and is absorbed from the buccal cavity. The highly vascular nature of the tongue and buccal cavity, and the presence of saliva, which can facilitate the dissolution of the drug, make this a highly effective and useful route for drug administration. It can also be used for a local action.


Two sites are used for absorption from the buccal cavity:



It is important that patients are made aware of the difference between the two sites and they should be given full instructions on how to administer their tablets, to ensure maximum benefit. (For details of suitable patient instructions, see Ch. 39.)


The advantages of the buccal route:




The rectal route


For administration by this route, drugs are formulated as liquids, solid dosage forms and semi-solids (see Ch. 37). The chosen preparation is inserted into the rectum from where the drug is released to give a local effect or it may be absorbed to give a systemic effect.


The rectum is supplied by three veins, namely the middle and inferior (lower) rectal veins, which drain directly into the systemic circulation and the upper rectal vein, which drains into the portal system, which flows into the liver. This means that, depending on the position within the rectum, only some of the drug absorbed from the rectum will be subject to the first pass effect. Bioavailability, therefore, may be less than 100% but may be better than that obtained from other parts of the GIT.


The amount of fluid present in the rectum is small, estimated at approximately 3 mL of mucus. This affects the rate of dissolution of the drug released from the suppository. However, there is also muscular movement which spreads the drug over a large area and promotes absorption.


The advantages and disadvantages of this route of administration are as follows.






The inhalation route


Drugs are administered usually by inhalation through the nose or mouth to produce either local or systemic effects. This route is used predominantly for local administration to treat respiratory conditions such as asthma. For this, drugs are delivered directly to the site of action, i.e. the lungs. A variety of dosage forms are used, from simple inhalations consisting of volatile ingredients such as menthol to sophisticated inhaler devices (see Ch. 43). A major benefit of the inhaled route is that the drug dose required to produce the desired effect is much smaller than for the oral route, with a consequent reduction in side-effects. Because of the high blood flow to the lungs and their large surface area, drug absorption by this route is extremely rapid and can be used to give systemic action.

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Jun 24, 2016 | Posted by in PHARMACY | Comments Off on Routes of administration and dosage forms

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