Pharmaceutical Dosage Forms

Sue Burton ZP113

Learning Outcomes
On conclusion of this section you should:  Be able to explain the various routes of administration that are possible  Understand the purpose of multiple dosage forms  Be able to explain the dosage routes commonly used for the various routes of administration  Have some understanding of the factors which affect the selection of an appropriate dosage form

Why do we have different dosage forms?



Drugs are normally administered as part of formulations and not in their crude or raw state

 

Provide optimal drug action Mechanism to get active ingredients into

 

body tissues body orifices

    

Protect active ingredients Mask odours or tastes Prolong or extend action Protect against breakdown by gastric acid Optimise local drug action

Routes of administration
aural intra ocular intranasal oral sublingual intrarespiratory intracardiac intraspinal intravenous intrarterial

intramuscular rectal vaginal intra osseous intra synovial intrarticular

Enteral / Parenteral


Enteral anything involving the alimentary tract from mouth to rectum

  

Oral Sublingual Rectal

Parenteral


any other route

Means next to or besides the parenteral

Routes of administration


Route can vary absorption and distribution in the body minutes, days, weeks Local effect drug activity at the site of administration eg eye drops Systemic effect drug introduced into the circulatory system by the route of administration and carried to the site of activity

Oral Route of administration

  

Peroral Systemic or local effect Tablets, capsules, solutions, syrups, elixirs, suspensions, gels, powders

Advantages  Simplest  Self administration  Comfort and convenience  If used properly - safest  Drug taken orally is swallowed and there are various sites of absorption
  

stomach Small intestine Large intestine or colon

 

Systemic effect Local action

Disadvantages  Onset of action is slow  Absorption may be erratic  Some drugs destroyed by gastric enzymes and secretions  Hepatic metabolism before entering general circulation first pass effect  Solubility may be altered by other substances  Gastric emptying variable  Unsuitable for unconscious or vomiting patients and pre and post operatively

Buccal Route of administration

 

 

Not swallowed Administered orally and absorbed from the buccal mucosa or sublingually (under the tongue) Highly vascular mucosa and presence of saliva Tablets powders, troches or lozenges, spray

Advantages  Relatively quick onset of action  Drugs absorbed into systemic circulation avoid first pass effect  Drugs can be administered to unconscious patients  Anti-emetic drugs can be given this way Antinot swallowed  Dose can be controlled Patient counselling  Do not swallow tablet  Position correctly

Parenteral Route of administration

  

Drugs given by injection Systemic delivery of drugs Commonest Routes

   

intravenous (i.v) intramuscular (i.m) subcutaneous (s.c) intradermal (i.d)

Solutions and suspensions

id

sc

im

iv

Epicutaneous or transdermal route

 

Also called topical route Most common for local effects sometimes systemic Ointments, creams, pastes, plasters, powders, aerosols, lotions, solutions

Advantages  Skin is the largest organ in the body local effect  Limit side effects  Can be used for systemic effects avoid first pass metabolism Disadvantages  Erratic absorption  Effective only for small molecular weight drugs

Conjunctival/Intraocular Route
 

Local action The cornea of the eye has one of the highest nerve densities in the human body, as a result patients perceive pain and discomfort even at low thresholds of stimulation Ointments, solutions and suspensions in the form of drops

Aural Route
 

Local action Solutions and suspensions in the form of drops

Nasal route


Local action solutions, sprays and ointments, inhalations Systemic avoids first pass metabolism

Pulmonary / Intrarespiratory route

       

Inhalation Local or systemic effect Respiratory conditions eg asthma Drugs delivered to site of action lungs Rapid onset of action Avoid first pass effect Solutions, solids, aerosols Small particle size

Rectal Route
  

Local or systemic effect Solutions, ointments and suppositories Three veins

 

inferior (lower), middle drain into systemic circulation Upper rectal vein portal system liver first pass metabolism

 

Small fluid volume in the rectum slow rate of dissolution from the suppository Muscular movement spreads drug over a larger area increases absorption

Advantages  Can be used when oral route is unsuitable unconscious or uncooperative patient  Useful when drug causes GIT irritation  Can be used for local action Disadvantages  Absorption can be irregular and unpredictable  Less convenient than oral route  Low patient acceptability

Vaginal Route
 

Local effect Pessaries, tablets, capsules, solutions, sprays, creams, ointments and foams Occasionally used for systemic activity labour inducing drugs No first-pass effect first-

Urethral Route
  

Local effect Solutions, suppositories, pellets Inconvenient and low patient acceptability

Considerations in dosage form design and selection



Nature of the disease or illness being treated

 

Emergency or comatose patient parenteral Ambulatory patients easy form tablets or capsules Naueous / vomiting suppository or parenteral Skin, otic, opthalmic, nasal - topical

Age of the patient

  

Children oral liquid or chewable solid Adults solid oral most convenient Elderly small solid oral or liquid

Dosage form design and adherence



Adherence (compliance) depends on:

     

Understanding of rationale for therapy Perception of severity of disease or illness Trust or faith in doctor and/or pharmacist Side effects Ease and convenience of dosing Understanding of how to administer the medication

Therefore will depend on dosage form being used

Pharmacist dispensing must provide adequate counselling which empowers patient to use the medication correctly Instructions clear, non-confusing and nonuncomplicated Formulating pharmacists development of user-friendly userformulations that foster adherence

Summary
  

 

Reasons for various dosage forms Routes of administration Dosage forms used for each route of administration Considerations in selection of dosage form Dosage forms and adherence