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| where can u apply androderm? |
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| where can u apply testoderm |
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| one of the matrix adhesive layer types |
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| one of the matrix adhesive layer types |
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| one of the matrix adhesive layer types |
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| non porous RATE CONTROLLING MEMBRANE copolymer |
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| Polyethylene/Polypropylene |
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| MICROPOROUS Rate CONTROLLING MEMBRANE colpolymer |
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Scopolamine
(Transderm Scop) |
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Nitroglycerin
(Transderm- Nitro) |
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Methyl Phenidate
(Daytrana) |
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| neulagia herpes pain and iontophoresis enhanced drug |
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| trimethicilone + stearic acid = |
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| levigating agent, preservative, emmolient |
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| cosolvent for better dissolution |
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| amino acid solubility enhancer |
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| amino acid solubility enhancer |
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| anti absorptionn / anti aggregation agent |
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| anti absorption/ anti aggregation agent |
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| sodium formaldehyde sulfoxylate |
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| methionine, cysteine molecular oxygen H2O2 aromatic aminoacids all undergo |
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| fridge or freeze proteins? |
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| dehydration. never completely dehydate 100% the biotech drugs |
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| p- hydroxy benzoic acids (parabens) |
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| monosaccharide or disacchride |
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| sucrose, or dextrose or lactose |
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osmotic bulking agents
and STABILIZER |
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| route ranking for protein peptides |
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| IV > NASAL > SQ. ORal is a fail cuz it breaks before its absorbed. |
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amount of AA for:
Ace inhibitors, TSH analogues |
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amount of AA for:
Calcitonin, cyclosporin (only peptide with oral bioavialbility) |
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amount of AA for:
Insulin,GH, interferon |
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| bioavailability of peptides, hi or low? |
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| metabolism of peptides, fast or slow? |
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| difference between protein and standardized synthetic drugs |
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| proteins have specialized uptake and binding mech |
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| Most peptide drugs Vd is Big or Small? |
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| Large. one of the exceptions. 7.6 Vd cuz it has lots of binding sites to distribute to outside the plasma |
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| Gasatrin releasing factor Vd is big or small? |
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| Volume of distribution. means more drug is in the plasma |
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| Small Vd + High Clearance = small or big t1/2 |
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| Erythropoiten t1/2 is small or larger? |
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| LONG. 8 to 9 hours. it is the exception |
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Vss and Vd area are 2x the Plasma Vd (which is Vc) for most peptide drugs.
what are the exceptions? |
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calcitonin
EPO
GH'
interferon
TNF |
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| Brain to blood Protein transport system |
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| Blood to brain Protein transport system |
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| Both blood to brain and brain to blood transport system |
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| four types of receptors: whats the ligand for alpha 2 Macroglobulin receptor? |
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| interleukin 1 beta and TGF Beta |
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four types of receptors: whats the ligand
for LDL receptor? |
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four types of receptors: whats the ligand
for Mannose Terminated Glycoprotein Receptor? |
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| four types of receptors: whats the ligand for (N acetyl galactosamine terminated asialo glycoprotein receptor ) AKA the GALACTOSE RECEPTOR? |
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| sources of nonlinearity in Peptide PK? |
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receptor mediated endocytosis (saturatable)
Endo + Exo peptidase (saturatable)
Binding proteins (saturatable like tPA)
this makes it dose dependent |
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hepatic and renal clearance
increasing the dose causes Vd to increase or decrease
increase dose increases t1/2 |
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if we increase the dose saturate the binding proteins in the PLASMA
what happens to Vd? |
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| Vd Goes UP as we increase the dose |
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| if its not being bound in the plasma by binding proteins it will go in the DEEP COMPARTMENT periphery and saturates binding sites there. what happens to vD? |
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| Vd goes down as we increase the dose |
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| suppositories are intended for |
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Insertion into rectum, vagina, urethra,
they melt or dissolve when inserted |
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| for suppositories, a decrease in particle size does what to absorption? |
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1. Oleaginous Fatty Base name:
2. Melt fast or slow?
3. miscible or immiscible with rectal fluid?
4. absorption fast or slow?
5. fatty suppository based are better for what type of drugs? |
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1. cocoa butter
2.fast melt
3. Immiscible with rectal fluid
4. slow absoprtion
5. Water soluble drugs |
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1. Water Soluble base name:
2. Melt fast or slow?
3. miscible or immiscible with rectal fluid?
4. absorption fast or slow?
5. fatty suppository based are better for what type of drugs? |
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1. PEG
2.dissolve fast
3. miscible with rectal fluid
4. slow absoprtion still
5. Lipid soluble drugs |
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| vaginal suppositories are what type of tablets? |
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Pessaries
Water soluble bases prefered |
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| Vaginal Suppositores 5grams |
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| Urethral suppositores (3-6mm) |
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| O/W surfactant for suppositories |
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Water soluble base of glycerin water and gelatin.
BASE IS HYDROSCOPIC
gives prolonged action and does NOT LEAK |
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| Fatty bases require fridge or not? |
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| water soluble bases require fridge or not |
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Fusion lubricants:
1.cocoa butter |
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| why should u not cool suppositories by fusion to rapidly? |
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| = temp too high or over filling or cool too rapidly |
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name the suppository manufacturer problem:
hollow nose suppository = |
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| excess lubricant like mineral oil forms a ball at the bottom and displaces the tip. |
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name the suppository manufacturer problem:
drug settled at nose tip |
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didnt stirr and base solidified, insoluble drug. drug not soluble in base and u heat it up and poured it too late cuz stopped stirring. like bismuth
keep stirring till just pourable to prevent this settling tip breaks off easily. |
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name the suppository manufacturer problem:
layered streaks of drug in suppository= |
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name the suppository manufacturer problem:
circular o shaped hole in suppository base top: |
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| put in ice bath and it contracts real hard. so you have that hole. |
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| split in half suppository: |
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| inssuficient mold lubrication. |
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| silicone dioxide in hydromorphone |
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| Suspending agent to prevent drug from going into tip of suppository |
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| Used as a stiffening agent but the promethazine probably is one of those drugs that lower the cocoa butter melting point and that means the cocoa butter would not be solid at room temperature ever. So the white wax gives you a solid suppository still. But if you do too much then the drug will now slowly release cuz its too stiff |
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| shape and dimensions of dosage for dinoprostone give what benefit? |
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| local effect or systemic absorption |
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how many years to develop biotech drugs?
5 or 7 or 12 or 15 years? |
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| advantage of biotech drugs |
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| disadavantage of biotech vs traditional |
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| What is the Cloning Process: |
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Gene of interest is cut out with restriction enzymes (RE)
Host plasmid (circular chromosome) is cut with same REs
Gene is inserted into plasmid and ligated with ligase
New engineered plasmid inserted into bacterium |
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• First, DNA is denatured to separate strands
• Next, primer is hybridized (specific location) on each DNA strand
• Finally, DNA polymerase enzyme is added for extension of the primer along the DNA strand to copy the target nucleic acid sequence
• Repeat as desired |
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| Nucleotide chain that contains the information for protein synthesis |
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Complimentary (to sense sequence) nucleotide chain
Antisense drugs recognize and bind to the nucleotide sense sequence of specific mRNA molecules preventing synthesis of unwanted proteins and actually destroying the sense molecules in the process. |
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| magic number of aminoacids that higher or lower tells if peptide or protein |
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| proteins at their isoelectric point in terms of stability and solubility? |
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for biodistribution of proteins
d |
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| vulnerable to hydrolysis and occur in acid ph hi temp |
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high temp
shearing
shaking
pressure |
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| o Non-Ionic Surfactants and Cylcodextrins: |
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Inhibit protein aggregation and precipitation
o |
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| Addition of Sugars (Dextran): |
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| Displace water and reduce microbial growth |
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| o Co-Solvents: (i.e. Glycerol, Polyethylene) |
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| Have a stabilizing effect |
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| Conversion of a solid to a gas (lyophilization or sublimation) |
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| atomize protein solution and particles and dry in air stream |
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| cost effective and prolongs shelf life |
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| better particle control and enhanced flow. good for non paraenteral |
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| CARBOXYMeTHLCELLULOSE gel for Diabetic foot ulcer |
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| inhalataion for cystic fibrosis |
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| Phophorthiate 2nd line treatment for cytalomeagovirus retinitis |
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Size dependant protein peptide elimination route:
<0.5 |
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Definition
| liver, blood (HYDROLYSIS) |
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Size dependant protein peptide elimination route:
0.5-1 |
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| Carrier mediated elimination LIVER more specific |
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Size dependant protein peptide elimination route:
1-50 |
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Definition
| Kidney GFR filtration FLUID endocytosis |
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Size dependant protein peptide elimination route:
50- 200 |
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| Opsonization Receptor mediated |
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Size dependant protein peptide elimination route:
>400 |
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Definition
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Definition
Must be less than 60kDa to filter through Glomerulus
• < 5kDa undergo hydrolysis (Bradykinin, Angiotensin)
• > 5kDa endocytosis (to be digested) |
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Definition
• Small Proteins and Peptides:
o Diffuse or Carrier transport to cytosol or Endoplasmic Reticulum
o Metabolized by proteases (calpains) and endo-/exopeptidases
• Large Proteins and Peptides:
o Passive Diffusion or adhere to hepatocytes membrane
Then fluid or receptor mediated endocytosis |
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| drug absorption limiting barrier |
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Definition
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Definition
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advantage of Matrix
and disadvantage |
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Definition
sleek thin, daily or multiple day application.
Dis: less control on release rate (rate limiting) |
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| Advantage and disadvantage of Reservoir |
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Definition
good for POTENT drugs
Release rate controlled
Bad: rupture of control membrane leads to dose dumping |
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Definition
| Used for patch formulations, ointments, solutions and suspensions |
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Term
| horizontal diffusion cell |
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Definition
| used for Liquid preparations (solution suspensions ONLY |
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Term
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Definition
A: Area of applicable system
Ko: Target Delivery Rate of the drug
Cp: Plasma Concentration
Vd: Volume of Distribution
Kel: Elimination Rate from Plasma |
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Term
o Flux (J) = (DKC)/h
Flux (J): The amount of drug transported through a unit of skin per unit of time
D: Diffusion coefficient of the drug
K: Partition Coefficient
C: Drug concentration in the vehicle or delivery system
h: Thickness of skin
SKIN enhancers |
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Definition
Increase drug permeability (DK) in the stratum Corneum
• Act as solvents to dissolve the skin lipids or denature skin proteins
Increasing the drug Solubility (C) in the Transdermal formulation (Patch) |
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Term
• Skin Penetration Enhancers:
o Work by
3 things |
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Definition
Disrupting the order of the stratum Corneum lipids
Interaction with cellular proteins
Increasing the solubility of the drug in the topical/Transdermal formulation |
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| • Unlike synthetic drugs, it is better to give protein and peptide drugs at _______ doses, over a ______ period of time to see a more dramatic result. |
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Definition
lower doses
longer periods |
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| Attachment of PEG to Protein/Peptide: |
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Definition
• Larger and more hydrophilic
• Discourages hepato-uptake
• Blocks receptor-mediated endocytosis (decreases clearance)
• Decreases distribution (V) |
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| Carbohydrate addition or change: |
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Definition
• May hide from receptor-mediated endocytosis (May decrease Clearance)
o Have to be careful not to affect target/receptor interactions
Cross-linking Carbohydrates may help |
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Term
o PK-PD model is used to understand the time course of concentrations and effects
o Standard Drugs: Desire constant drug plasma concentration to get constant effects
This may not be desired with peptide and protein drugs
BECAUSE |
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Definition
| They stimulate or mimic physiological effects and Protein PEPTIDE metabolism, elimination and binding all happen in one spot at one time |
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Term
TPA: Alteplase (rh-t-PA):
• Rapid metabolism, Deactivation by PAI-1
so whats great about Tenecteplase? |
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Definition
Tenecteplase: TPA variant
• Increased (3-10 Times) Potency
• Decreased (6-8 fold) in Clearance
• Higher fibrin specificity
• Resistant to PAI-1 |
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