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ceutics review 1
| question | Definition |
|---|---|
| Liberation | Particle size, surface area, solubility, dissolution rate |
| absorption | aq solubility, ionization state, pH lipophilicity directly affects permeability |
| Distribution | lipophilicity, plasma protein binding, membrane permeability increased lipophilicity->greater tissue distribution |
| Metabolism | the higher the lipophilicity->extensive metabolism ionization state |
| Excretion | bile, sweat,milk,urine,lungs urine->hydrophilic + ionized drugs |
| Portition coefficient | non polar environment compared to polar |
| ANDA | abbreviated new animal drug application |
| BLA | biologics lisence application bio->vaccine/protein |
| IND | investigational new drug application submit to FDA before a new drug can be tested in clinical trials |
| USP | united states pharmacobeia identity,strength,quality,purily of meds, food ingredients & dietary supplements |
| FDA | food and drug administration saftey, efficacy, security |
| SNDA | supplemental new drug application FDA submitted before a new formulation |
| In vitro | in lab/petri dish |
| Ex vivo | helacells, in tissues/cells |
| In vivo | in animals/ rats |
| NDA | new drug application must be submitted to FDA before new drug is marketed for human use |
| NAPA | New animal drug application FDA submitted before a new drug is marketed in animals |
| Drug approval process | Discovery->pre-clinical development-> INDA-> clinical-> NDA/BLA->market->p4 clinical |
| phase 1 | saftey + tolerability 20-100 |
| phase 2 | efficacy + optimal dose 100s |
| phase 3 | confirm safely + efficacy establish risk/benefit 100s-thousands |
| PK | pharmacokinetics |
| PD | pharmacodynamics |
| After market | adverse reactions, produce defect, sNDA ex: tab->solution |
| Solutions | ADME |
| Liquids/sometimes solids | higher IMF, lower vp, higher bp, mp, osp, viscosity, s.ten |
| amorphous | weaker |
| crystalline | stronger |
| solids | different polymorphs->different mp stronger IMF-> higher mp |
| solution aq: strong electrolytes | ionize completley in h20 ex: NaCl, HCl, NaOH, KCl |
| solutions aq: weak electrolytes | partially ionize in h20 most drugs/bases ex: HOAc, NH4OH, vinegar |
| Acid solute to solvent? | lower vp, higher bp, lower fp, higher os.p more solute=more osp |
| osmolarity | permeable + nonpermeable |
| Tonicity | nonpermeable |
| hypertonic solution | cell shrinks |
| hypotonic solution | cell swells |
| Boric acid | eye drops not IV injection |
| ionic | NaCl.....Na^s+....Cl^s- Strongest IMF dipole forces |
| ionic dipole | NaCl + h20 forces of attraction between an ionic molecule and a polar molecule with permanent dipoles |
| dipole-dipole | H^s+-Cl^s-... H^s+-Cl^s- polar +permanent dipoles |
| ion induced dipole forces | forces of attraction between an ionic molecule and a non polar molecule |
| dipole-induced dipole | forces of attraction between a polar molecule and a non polar molecule that is polarizable |
| recall 1 | severe adverse health issues, high |
| recall 1 | severe adverse health issues, high |
| recall 2 | temporary/reversible adverse health isssues, moderate |
| recall 2 | temporary/reversible adverse health isssues, moderate |
| recall 3 | no harm of health issues, low |
| induced dipole-induced dipole | weakest IMF |
| hydrogen bond | second strongest ex Fluorine, oxygen, nitrogen |
| solutions of nonelectrolytes | no ions present sugars,alcohols |
| polymorph: metastable | unstable polymorph |
| polymorph: stable | stable polymorph |
| induced dipole-induced dipole | weakest IMF |
| polymorph: enantiotropic | reversible |
| polymorph: monotropic | irreversible |
| what happens to the bioavailability of a drug that undergoes an irreversible polymorphic change? | lower bioavailability freely soluble->poorly soluble |
| chemical stability | hydrolysis, oxidation, maillard reaction more in liquid state than solid |
| hydrogen bond | second strongest ex Fluorine, oxygen, nitrogen |
| solutions of nonelectrolytes | no ions present sugars,alcohols |
| polymorph: metastable | unstable polymorph |
| polymorph: stable | stable polymorph |
| polymorph: enantiotropic | reversible |
| polymorph: monotropic | irreversible |
| what happens to the bioavailability of a drug that undergoes an irreversible polymorphic change? | lower bioavailability freely soluble->poorly soluble |
| chemical stability | hydrolysis, oxidation, maillard reaction more in liquid state than solid |
| recall 1 | severe adverse health issues, high |
| recall 2 | temporary/reversible adverse health isssues, moderate |
| recall 3 | no harm of health issues, low |
| induced dipole-induced dipole | weakest IMF |
| hydrogen bond | second strongest ex Fluorine, oxygen, nitrogen |
| solutions of nonelectrolytes | no ions present sugars,alcohols |
| polymorph: metastable | unstable polymorph |
| polymorph: stable | stable polymorph |
| polymorph: enantiotropic | reversible |
| polymorph: monotropic | irreversible |
| what happens to the bioavailability of a drug that undergoes an irreversible polymorphic change? | lower bioavailability freely soluble->poorly soluble |
| chemical stability | hydrolysis, oxidation, maillard reaction more in liquid state than solid |