DRUG DOSAGE FORMS:
1. SOLID
PharmDr. Ondřej Zendulka, Ph.D.

Solid drug dosage forms
*  pulveres perorales (powders)
*  pulveres adspersorii (dust powders)
*  species (herbal teas)
*  tabulettae (tablets: uncoated, coated, film coated, gastro-resistant, sublingual…..)
*  capsulae (capsules: hard, soft, prolonged release…..)
*  implantata (implants)
*  suppositoria (suppositories)
*  globuli vaginales (pessaries- vaginal balls)
*  styli
*  tampona medicata
*

Pulveres
*  formed by powdered solid particles
*  one or more of active substances + excipients
*  internal/external use; undivided/divided, shape nonspecific/specific, single/multiple dose
Pulveres adspersorii:
*  shape nonspecific, for external use only
*  application in dry form directly onto skin
*  local effect, domain of dermatologists and pediatricians
*  antiseptic, antiitching, protective effects

IPP: Effective: Acidum boricum; Mentholum
                racemicum; Bismuthi subcarbonas;
                Ichthammolum, Tanninum
Adjuvants: Zinci oxidum; Talcum; Tritici    amylum; Oryzae amylum; Calcii    carbonas; Magnesii
oxidum leve;    Bentonitum
compositio – specification of components
subscriptio – M.f. pulv. adspers.
total amount usually 30-50g
Pulveres adspersorii
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IPP:
Remedii cardinalis (in gen.) amount in grams (10.0)
Remedii adjuvans amount in grams (5.0)
M.f.pulv. adspers.
DS:  …e.g. Dust powder.
Ex. Rp.
  Tannini    2,5
  Zinci oxidi
  Talci   aa ad 50,0
  M.f. pulv. adspers.
  D.S. Dust powder. Cover the afflicted place several times a day.
Task: Prescribe  antiprurigineous dust powder with methol (0,5%) and basis from  ZnO and talc.
Pulveres adspersorii

Pulveres
Perorales:
Undivided (non divisi):
• shape nonspecific
• administered in dry form – measuring cap, spoons
• for preparation of solutions (antacids, gargles)
• only for drugs with low efficacy (innacurate dosing)
• IPP: prescribed drug amount for the whole treatment, dosage is specified in the signatura.
•

Pulveres perorales
IPP:
Remedii cardinalis X,X
Remedii adjuvantis X,X
M.f.pulv.
DS:  …e.g. One table spoon into a glass of lukewarm water.
Ex.
Rp. Natrii sulfatis
    Magnesii sulfatis heptahydrici aa ad 200,0
    M. f. pulv.
    D.S. One table spool into a lukewarm water. Use on empty stomach.
Task. Prescribe antacid containing: Na2HPO4 and CaCO3 in the same amounts.
Natrium hydrogenphosphate, Calcium carbonate

Pulveres perorales
Divided (divisi)
• single dose
• for the prescription of highly effective
  drugs (Separanda, Venena)
• single dose of 0,1-0,5g weight
• vehicle: Lactosum monohydricum
• single dose usually in hard capsules

Pulveres perorales
IPP:
• subscriptio: Ad caps. gelat.
Prescription – dispensed x divided form
Dispensed form
• dose for single components are stated
• number of required doses is in subscription part (D.t.d. No. ...), instruction to prepare powder
is mentioned too (M.f.pulv.)

Pulveres perorales
Remedii cardinalis X.X
Remedii adjuvantis X.X
Lactosi monohydrici q.s.
M.f. pulv.
D.tal. Dos. No X (decem)
Ad caps. gelat.
DS:  …e.g. 1 cps twice a day
Ex.
Rp.
  Papaverini hydrochloridi 0,05
  Lactosi monohydrici   ad 0,4
  M.f.pulv.
  D.t.d. No. X (decem)
  Ad caps. gelat.
  S. for pain 1-2 capsules, maximum 6 pieces per day.
Task.: Prescribe peroral divided powder with caffeine (DTS 0,1g) and paracetamol (DTS 0,5g).
Coffeinum, Paracetamolum

Pulveres perorales
Divided form
*  total amount of each component necessary for IPP is stated
*  Number of requested doses is mentioned in subscription (Div.in dos.aeq. No. ...)
Ex. Rp.
   Remedii cardinalis amount in grams (0.5)
   Remedii adjuvans amount in grams (4.0)
   Lactosi monohydrici                   q.s.
   M.f.pulv.
   Div. in dos. aeq. No. X (decem)
   Ad caps. gelat.
   D.S. …e.g. 1 cps twice a day
Task.: Prescribe peroral divided powder with codein (DTS 0,015-0,03g) and diazepam (DTS
0,002-0,005g).
Codeinum monohydricum, Diazepamum

Species
*  herbal mixtures, herbal teas
*  the easiest form of herbal preparation
*  mixtures or single species herbal drugs
*  usually RMP
*  tea is prepared usually by pouring over one table spoon one cup of boiling water
IPP: in subscription M.f. spec.
Task. Prescribe herbal tea consisting of common balm,  valerian root and althea flower.Mixture
contain equal parts of all herbs (30g).
Melissae herba
Valerianae radix
Althae flos

Tabulettae
*  solid pressed shape specific preparations
*  usually flat rounded or disc like shapes
*  pressed from granulates
*  usually RMP
*  different types of tablets, can exert different influence especially on drug release
*
Non-coated tablets
*  classical pressed tablets
*  their disintegration is influenced only by the properties of granulates (grained powders)
t tablety

Tabulettae
Coated tablets = obducts (dragee)
• based on non-coated tablets, which are usually coated with sugar layer
• tablets are sprayed with sugar solutions
• function of layer – protective, marketing
• polymer film can be also used
Effervescent tablets
• contain weak acid salts: bicarbonates, citric or tartaric acid, sparkle in contact with water
and  CO2 is released
• sparkling solutions are prepared

Tabulettae
Tablets disperged in mouth
• quick disintegration
• fast onset of effect
Gastro-resistant tablets
• acid resistant coating
• prevets drug against breakdown in stomach
•
Controled release tablets
• prolonged or modified release
• matrix or membrane systems
• 2 phase release

>

Tabulettae
Sublingual or buccal tablets
• systemic/local effect
• slow/fast release of drug
Vaginal tablets
• local effect
• infectiuos diseases, birth induction
•

Capsulae
*  single dose preparations, different size, shape, color
*  contain drugs in edible coating
Hard capsules
*  usually dry content
*  coating is made of two parts
Soft capsules
*  filled with lipophillic solutions
*  single part coating
*
capsle

Capsulae
Gastro resistant capsules
• coating soluble in specific pH
Controlled release capsules
• membrane systems
•

Implantata
*  for parenteral use
*  must be aseptic
*  slow release of drug
*  contraceptives

Suppositoria
*  cylindric or conic shape, destined for the insertion into rectum
*  one or more drugs dispersed or dissolved in sup. basis
*  can contain excipients (solvents, antimicrobial agents)
*  local/systemic effect
*  solid at room temperature
*  melting at body temperature
RMP:
*  produced by pressing

Suppositoria
IPP:
• prepared by pouring
• hydrophobic bases: Cacao oleum, Adeps neutralis
• hydrophilic bases: gel forming mixtures:
                          Gelatinae glycerogelatum
         macrogols
• store at dry, cool, place
Prescription – similar to Pulveres divisi
       - dispensed or divided form
 - Massa pro suppositoriis. – base is not specified
     - q.s. – the amount of base is not specified
     - M.f.supp. or M.f.supp.
             pro inf.

Suppositoria
IPLP:
Ex.
Rp.
Paracetamoli       2,5
Massae pro supp. q.s. ut f. supp.No.V(quinque)
D.S. Insert one suppository in the rectum when necessary.
Rp.
Paracetamoli 0,5
Massae pro supp. q.s. ut f. supp.
D.t.d. No. V(quinque)
S. Insert one suppository if fever occurs.
Task. Prescribe 8 suppositories with diazepam DTS 0,00025-0,0005g for child.

Globuli vaginales
*  similar to suppositories
*  pressed or poured
*  same mass as suppossitories
*  with local effect

Drug dosage forms:
Semisolid
PharmDr. Ondřej Zendulka, Ph.D.

Semisolid drug dosage forms
• semisolid preparations are supposed to contain either drugs with  local or systemic effect
•
•can be used for skin protection or softening
•
• are homogenous
• dermatology – represented by single or composite base with dissolved or dispersed drug/drugs
•
• base composition can influence the final effect

Classification:
ointments
creams
gels
pastes
medicated patches
hydrophilic
hydrophobic
Semisolid drug dosage forms

Ointments (Unguenta)
- formed by one-phase base with dispersed solid or liquid drug
Classification:
ČL 2009
- hydrophobic ointments
- emulsifying ointments
- hydrophilic ointments
forms of drug dispersion
- solutions
- emulsions
- suspensions
- suspensions-emulsions

Ointments (Unguenta)
Bases for hydrophilic ointments

Macrogols
- polyethylene glycols, polyethylene oxides (PEG, PEO)
- m.w. 200-600 liquids, higher m.w. solid
- max. 10 % of water
- mixed liquid-solid polymers
- water soluble
- suitable in case of hypersensitivity to usuall bases
- hygroscopic
- bactericidal

Excipients of hydrophilic bases
Gel-forming macromolecular substances
- gelatine glycerogel
- metacrylates (Eudragit)
- celulose esters (Methocel, Tylosa)
- agar, gums
Rp. Gelatinae 12,5
Aquae cons. 25,0
Glyceroli 85% 62,5
M.f.glycerogelatum gelatinae.
ČL 2009 Macrogoli ung.

Ointments (Unguenta)
Bases for hydrophobic ointments
Hydrocarbon bases
- physically stable
- low capacity of water absorbtion (up to 10%)
- easy spreading, emoliens, skin penetration is limited
- can cause hypersensitive reactions
Silicone bases
- 10-50% of silicones which are emulsified by wool fat, cetylalcohol or by other emulsifier
Water number: maxim quantity of water in g , which can be dispersed in 100g of the ointment base ,
vaseline (9-15)

Excipients of hydrophobic bases
Hydrocarbons
- solid paraffin
- liquid paraffin
- vaseline – white + yellow
Aliphatic alcohols and acids
- cetylalcohol, stearylalcohol
- acids stearic, palmitic
Triacylglyceroles
- esters of fatty acids with glycerol
- fats (Cacao oleum, Adeps Suilus) + oils (Ricini ol., Helianthi ol…), natural/hydrogenated
- unstable, do not block perspiration

Excipients of hydrophilic bases
Semisynthetic and synthetic triglycerides
- often self-emulsifying properties
- known and stable composition
- Mygliol, Softisan
- ceramides – sphingolipids, form protection layer on skin
Waxes
- esters of fatty alcohols and  aliphatic acids
- white beeswax, cetaceum, wool fat
Silicones
-polysiloxanes, most often dimethylsiloxanes
-weak antioxidants

Ointments (Unguenta)
Excipients for hydrophobic bases

-vaselinum album
- vaselinum flavum
- adeps suilus
- cera alba
- paraffinum liquidum/solidum

Ointments (Unguenta)
Emulsifying bases
- consists usually from hydrocarbons and triacylglycerols
- contain emulsifier
- usually w/o
Emulsions - two-phases
- up to 15% water
- do not dry off, release the drug slowly

Masti (Unguenta)
Emulsifying bases

Hydrophillic - o/w
- Aquasorb/ Neoaquasorb
- u. emulsificans anionicum, nonionicum
- u. stearini
Hydrophobic - w/o
- Pontin®, Synderman®
- ung.cetylicum, u. lanalcoli
- u. monostearini, u. simplex

Emulsifying bases
v/o
v/o
o/v
Eye max. 10 g
Nose, ear      10 – 20 g
Face, hands   20 – 30 g
Legs 80 – 100 g
Larger surfaces   150 – 200 g

Unguenta ČL 2009
Pharmacopoeial ointments:
Alcoholis cetylici unguentum
Zinci oxidi unguentum
Un. constituens pro antibioticis
Un. emulsificans anionicum
Un. emulsificans nonionicum
Un. molle
Un. ophthalmicum simplex
Un. simplex
Un. Whitfield
Acidi borici unguentum 10%
Acidi salicilyci unguentum 10%
Alcoholum adipis lanae unguentum
Argenti nitratis unguentum compositum
Glyceroli unguentum
Ichtamoli unguentum
Jecoris aselli unguentum compositum
Macrogoli unguentum

Ointments (Unguenta)
Examples:
 Alcoholis cetylici ung.
Rp.
Alc. cetylici                     1,0
Adipis lanae                   7,5
Vaselini albi ad  50,0
Ung. simplex ČL 2009
Rp.
Propylis gallas 0,01
Ethanoli 96% 1,0
Alcoholis cetylici 5,0
Cerae albae 5,0
Adipis suillus 90,0
M.f.ung.
D. ad ollam.
Rp.
Remedium cardinale
Vehiculum
M.f.ung.
D. ad ollam.
S.
Př. Prescribe 50g 5% zinc ointments

Ocularia semisolida
•sterile (!)  eye oint., creams or gels
IPP: ointment base
•Unguentum ophthalmicum simplex
•M. f. oculentum.
•M. f. ung. ophthal.
•max 10g
•in sterile containers with applicator
•expiration 4 weeks

Creams (Cremores)
- 2-3 phases
- always contain water and oil phase
- drug is dissolved or dispersed in one phase or is suspended
Oleocreams
- emulsions w/o
- water phase 15-50% of weight (max. 74%)
- base = vaseline + woll fat
- Synderman, Pontin, Cutillan
- suitable for subchronic phases of disease
- good regenerative and emollient properties

Creams (Cremores)
Hydrocream
- emulsions o/w
- water phase 60-90% of weight
- easy evaporation of water = cooling effect
- can be washed away easily
- Neoaquasorb, cremor nonionicus, crem. anionicus

Krémy (Cremores)
Pharmaopoeial creams:
Alcoholis cetylici cremor
Alcoholum adipis lanae cremor
Aluminii acetotartratis cremor
Cremor anionicus
Cremor nonionicus
Cremor refrigerans

Pastes(Pastae)
- semisolid preparation which contain high portion of solid substance dsipersed in the base
- solid particles more than 25%
Classification:
Oleopastes – hydrophobic ointment base
Hydropastes – hydrophillic ointment base
Oleocream pastes – oleocream base
Hydrocream pastes – hydrocream base
Pharmacopheial pastes:
Zinci oxidi pasta
Zinci oxidi pasta mollis
Zinci oxidi pasta salicylata
Rp.
Remedium cardinale
Vehiculum
M.f.pasta
D. ad ollam.
S.

Medicated patches (Emplastra medicata)
- contain one or more of acive substances
- for skin applications
- patches guarantee the contact of active substance with skin, or can exert protective or
keratolytic effect
TTS – transdermal therapeutic systems – Emplastra transcutanea
Advantages: Disadvantages:
easy administration skin sensitization
controlled release of drug excipients allergy
(constant levels)
skip the first pass effect influence on skin microflora
easy drug discontinuation slow onset of effect ↑compliance price

Medicated patches (Emplastra medicata)
TTS
• excusively RMPs
• drug gets into the skin (penetration)
• drug passes through the skin (permeation)
• drug ghets to blood or lymphatic vessels (resorption)
•
• Angina pectoris (glyceroltrinitrate)
• Kinetosis (scopolamine)
• HRT (oestrogens) + contraceptives
• Pain and inflammation (fentanyl, flurbiprofen, diclophenac)
•Substance abuse discontinuation (nicotine)

Backing layer
Membrane
Adhesive layer
Protective layer
Reservoir (drug)
TTS with membrane controled release

TTS with matrix controlled release
Backing layer
Adhesive layer
Protective layer
Reservoir- matrix