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Dosage forms, 1st Sem Pharmaceutics, Study notes of Pharmaceutical Chemistry

this will help to study in the pharmacy course in all the semester. It is a summary note but very important.

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DOSAGE FORMS
what is a drug ?
-> A drug is a natural or a synthetic compound or substance, which is used for treatment,
prevention and diagnosis of any disease or disorders.
It is also called as an API : active pharmaceutical ingredient i.e a raw form of the drug which
will have a biological effect in our body. It is available in any physical states :
- solid : paracetamol
- liquid : rivastigmine
- gaseous : Nitrous oxide
But, without a dose, drugs are nothing.
Dose : the amount or the quantity of drug required to give therapeutic effect in the
biological system.
We can’t give a drug in its raw form. They are administered in different dosage forms.
Dosage forms :
It is a physical form that helps to deliver a dose of drug into the body.
It is a carrier of the unit dose of drug
It consist : drug + excipient = Dosage forms
Excipients are inactive ingredients, also called ‘additives’, used to give a particular shape to
the formulation, increase stability and palatability.
Importance of dosage forms :
- Accurate dose
- Protection from gastric environment
Eg: Enteric coated tablets
- Protection against the micro-organism, external environment
Eg: Coated tablets, sealed ampoules
- Masking unpleasant taste and odor
Eg: Sugar coated tablets, using sweetening agents for liquid orals
- Provide drugs within body tissues
Eg: Parenterals
- Controlling releasing of drug
Eg: Sustain release and control release tablets
- Facilitating insertion of drug into body cavities
Eg: Implants, Suppositories
- Providing drug therapy through pulmonary route (inhalation therapy)
Eg: Nebulizers, aerosols
- Provide action of drug topically for local therapy
Eg: Ointments, lotions
The science of dosage form design or formulation is called pharmaceutics.
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DOSAGE FORMS

what is a drug?

-> A drug is a natural or a synthetic compound or substance, which is used for treatment, prevention and diagnosis of any disease or disorders. It is also called as an API : active pharmaceutical ingredient i.e a raw form of the drug which will have a biological effect in our body. It is available in any physical states :

  • solid : paracetamol
  • liquid : rivastigmine
  • gaseous : Nitrous oxide But, without a dose , drugs are nothing.

Dose : the amount or the quantity of drug required to give therapeutic effect in the

biological system. We can’t give a drug in its raw form. They are administered in different dosage forms.

Dosage forms :

It is a physical form that helps to deliver a dose of drug into the body. It is a carrier of the unit dose of drug It consist : drug + excipient = Dosage forms Excipients are inactive ingredients, also called ‘additives’, used to give a particular shape to the formulation, increase stability and palatability.

Importance of dosage forms :

  • Accurate dose
  • Protection from gastric environment Eg: Enteric coated tablets
  • Protection against the micro-organism, external environment Eg: Coated tablets, sealed ampoules
  • Masking unpleasant taste and odor Eg: Sugar coated tablets, using sweetening agents for liquid orals
  • Provide drugs within body tissues Eg: Parenterals
  • Controlling releasing of drug Eg: Sustain release and control release tablets
  • Facilitating insertion of drug into body cavities Eg: Implants, Suppositories
  • Providing drug therapy through pulmonary route (inhalation therapy) Eg: Nebulizers, aerosols
  • Provide action of drug topically for local therapy Eg: Ointments, lotions The science of dosage form design or formulation is called pharmaceutics.

Classification of dosage form :

Physical forms :

❖ Solid

● Powders :

  • internal use :
    • bulk powder
    • divided powders
      • simple and compound powders
      • powders enclosed in cachets
      • Tablet triturates / Moulded tablets
  • external use :
    • bulk powder
      • dusting powder (medical use & surgical)
      • insufflation
      • snuffs
      • dentifrices
  • special powder :
  • Eutectic powder
  • effervescent granules
  • hygroscopic ● Unit dosage forms :
  • Tablets
  • capsules
  • pills

❖ Liquid

● Monophasic

  • external use
  • internal use ● biphasic
  • emulsion
  • suspension

❖ Semisolid

● external

INTERNAL USE :

  • Bulk Powders : Bulk powders contain several doses of powder meant for internal use. They are supplied in wide mouthed containers for easy removal of content.
  • Divided Powder : Simple powder : Contains only one ingredient either in crystalline or amorphous form. The wrapping of powders may be single or double wrapped according to the type of drug :
  • If the drug is not resistant to atmosphere it can be single wrapped
  • If the drug is sensitive to atmosphere it should be double wrapped e.g : Aspirin powder : Rx Aspirin 300mg Make a powder Direction: One powder to be taken after every eight hours Compound powder : 2 or more than 2 substances are mixed together and divided in desired numbers of individual doses in a separate powder paper. e.g : Aspirin, paracetamol and caffeine powder Rx Aspirin 300mg Paracetamol 150mg Caffeine 50mg Make a powder Direction: One powder to be taken when need arises Powders enclosed in Cachets : Cachets are known as wafer capsules. These are solid unit dosage forms moulded from rice paper. These are used to enclose nauseous or disagreeable powder. e.g : Sodium aminosalicylate cachet Isoniazid cachet

Tablet triturates/ Moulded tablets : Powders are moulded in the form of tablets.

Molded tablets are flat, circular discs and contain a potent substance. Potent drug: Compounds having maximum dose of less than one grain or 60 mg.

EXTERNAL USE

  • Bulk Powder for external use Bulk powders meant for external use are non potent substance meant for external use They are supplied in cardboard, glass or plastic containers. There are different powders available for external use : Dusting Powders : Dusting powders are bulk powders for external use The powders are generally very fine in state to avoid irritation (antiseptic, astringent). To maintain the fine state, the powders must be passed through sieve number 80. Dusting powders are divided into 2 types based on their use a. Medical dusting powder Medical dusting powders are used for superficial skin conditions Commonly used ingredients are Talc (excellent lubricant) and starch (excellent absorbent) Medical dusting powders should not be applied on open wounds and hence should have the following label 1.FOR EXTERNAL USE ONLY 2.DO NOT APPLY ON OPEN WOUNDS AND BROKEN SKIN b. Surgical dusting powder Surgical dusting powders are used in body cavities, major wounds on burns, umbilical cords or infants. These preparations must be sterilized They also contain some antibacterial agent Dusting powders are dispensed generally in sifter top containers, they can also be applied with powder puff or sterilized gauze pad Rx Purified talc, sterilized 50g Starch 25g Zinc oxide 20g Salicylic acid 5g Make a powder Dispense 50g of dusting powder DIRECTION: Apply on affected part 2 or 3 times a day
  • Effervescent granules : Specially prepared solid dosage form of medicament meant for internal use. The basic requirement of effervescent granules are medicament along with tartaric acid, citric acid and sodium bi carbonate. Before administration, the desired quantity is dissolved in water. The acid and bicarbonate reacts together to produce effervescence The carbonate produced masks the bitter and saline taste of drugs There are 2 methods of preparation a. Heat method A porcelain dish/ stainless steel is placed over boiling water/ water bath. The dish must be sufficiently hot before transferring the weighed powders. because the water of crystallisation is liberated from citric acid if the dish is sufficiently hot. This liberated water acts as a source for forming a damp mass Heating of powders is done for 5min to get a coherent mass. The mass is passed through a sieve to obtain granules, these granules are dried in the oven at temp. 60 C and packed in airtight containers. b. Wet method The ingredients are weighed and transferred into a mortar. The mixture is moistened with non aqueous liquid (alcohol) to get a coherent mass. The coherent mass is passed through sieve 8 and dried at 60 C in an oven. The dried granules are passed through a sieve in order to break any lumps formed. The dried granules are packed in airtight containers
  • hygroscopic powder Powders which has the tendency to absorb moisture from the atmosphere are called as hygroscopic powders Eg: Ammonium citrate, pepsin, phenobarbitone These type of powders must be prepared in granular form, and should not be exposed to the atmosphere The granules must be double wrapped Some precautions must be taken during preparation using these powders : Equipments must be completely dried Inert diluents (lactose, starch) can be added which can act as adsorbents

Liquid dosage forms :

Liquid dosage forms are the liquid form of a drug dose for administration or consumption or application. For the preparation of liquid dosage form, a lot of additive ingredients are needed. Such as vehicles, stabilizers, preservatives, suspending agents, emulsifying agents, solubilizers, colors, flavors, etc. adv disadv

1) Monophasic dosage forms :

These refer to liquid preparation in which there is only one phase. It is also referred to as the true solution. True solution : A clear homogeneous mixture that is prepared by dissolving a solid, liquid or gas in a liquid.

  • FOR INTERNAL USE
    • Mixture : Liquid preparation in which medicaments are dissolved in a suitable vehicle.
  • Syrup : It is a concentrated aqueous solution of sugar, usually sucrose (66.7% w/w). Sweet viscous preparation Use as a preservative, sweetening agent, vehicule, viscosifying agent. 2 Types : 1. medicated (API) & 2. Flavoured syrup (aromatic or flavoured substances) container : white/amber colored bottle made up of glass/plastic store in a cool and dark place at T° not exceeding 25°C label : for internal use only Preparation : 1. tolu syrup IP : Rx tolu balsam (API treating bronchitis) Sucrose purified water (vehicule) -> add boiling purified water to tolu balsam, cool filter and add sucrose, heat on water-bath. QS of water added.
  1. simple syrup : Rx sucrose purified water -> add sucrose to purified water and heat to dissolve sucrose, cool it and QS water is added.

They are either dabbed on the skin or applied on a suitable dressing and covered with a waterproof dressing to reduce evaporation

  1. Liquids used in the mouth :
    • Gargle : An aqueous solution used to prevent or treat throat infections (pharyngitis)
    • Mouthwash :
    • Throat paint :
  2. Liquid to be instilled into body cavities :
    • ear drops :
    • nasal spray :
    • nasal drops :
    • Enamas :
    • Douches :