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Mr. Sagar Kishor Savale
[Department of Pharmaceutics]
avengersagar16@gmail.com
2016-2017
Department of Pharmacy (Pharmaceu...
13-Aug-162
Drug delivery is the method or process of administering a pharmaceutical compound to achieve a
therapeutic effe...
13-Aug-163
 Oral drug delivery systems.
 Parenteral drug delivery systems.
 Mucosal drug delivery systems.
 Nasal drug...
13-Aug-164
ORAL DRUG DELIVERY SYSTEMS
Oral administration of drugs is the simplest, easiest and most common route of
admin...
13-Aug-165
DRUG SELECTION CRITERIA
 Drugs with molecular weight/size < 1000 Da.
 Drug solubility should be greater than ...
13-Aug-166
ORAL DISPERSIBLE SYSTEM
Drug Selection Criteria
 The drug should not have a bitter taste.
 The dose should be...
13-Aug-167
PULSATILE DRUG DELIVERY SYSTEMS
Drug Selection Criteria
 Chronopharmacotherapy of diseases which show circadia...
13-Aug-168
COLON TARGETED DRUG DELIVERY
Drug Selection Criteria
 Drugs which show poor absorption from stomach or intesti...
13-Aug-169
FLOATING DRUG DELIVERY SYSTEM
Drug Selection Criteria
 Drugs with narrow absorption window in stomach. E.g. Ri...
13-Aug-1610
TRANSDERMAL DRUG DELIVERY SYSTEMS
Drug Selection Criteria
 Dose should be low i.e. < 20mg/day.
 Half life sh...
13-Aug-1611
MUCOADHESIVE DRUG DELIVERY SYSTEMS
Drug Selection Criteria
 Drugs with less elimination half-life.
 Drugs wh...
13-Aug-1612
VESICULAR DRUG DELIVERY SYSTEMS
Drug Selection Criteria
 Drugs which have low bioavailability and varied phar...
13-Aug-1613
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Drug selection criteria for different drug delivery system (DDS)

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Drug selection criteria for different drug delivery system for selection of appropriate drug is targeted at particular drug delivery system.

Publié dans : Santé & Médecine
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Drug selection criteria for different drug delivery system (DDS)

  1. 1. Mr. Sagar Kishor Savale [Department of Pharmaceutics] avengersagar16@gmail.com 2016-2017 Department of Pharmacy (Pharmaceutics) | Sagar savale Drug Selection Criteria For Different Drug Delivery Systems
  2. 2. 13-Aug-162 Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. The method by which a drug is delivered can have a significant effect on its efficacy. Some drugs have an optimum concentration range within which maximum benefit is derived, and concentrations above or below this range can be toxic or produce no therapeutic benefit at all. On the other hand, the very slow progress in the efficacy of the treatment of severe diseases, has suggested a growing need for a multidisciplinary approach to the delivery of therapeutics to targets in tissues. From this, new ideas on controlling the pharmacokinetics, pharmacodynamics, non-specific toxicity, immunogenicity, bio recognition, and efficacy of drugs were generated. These new strategies are called drug delivery systems (DDS). To minimize drug degradation and loss, to prevent harmful side-effects and to increase drug bioavailability and the fraction of the drug accumulated in the required zone, various drug delivery and drug targeting systems are currently under development.
  3. 3. 13-Aug-163  Oral drug delivery systems.  Parenteral drug delivery systems.  Mucosal drug delivery systems.  Nasal drug delivery systems.  Pulmonary drug delivery systems.  Ocular drug delivery systems.  Transdermal drug delivery systems.  Vaginal & intrauterine drug delivery systems.  Rectal drug delivery systems.  Targeted drug delivery systems.
  4. 4. 13-Aug-164 ORAL DRUG DELIVERY SYSTEMS Oral administration of drugs is the simplest, easiest and most common route of administration. After absorption from the GIT, the drugs can be metabolically deactivated unless special measures are taken to protect them. Then the drug enters the systemic circulation and is distributed to the target and other tissues. The existence of first pass metabolism is the most significant challenge and disadvantage of oral drug delivery. This route is not suitable for the systemic delivery of drugs that are poorly absorbed or destroyed in the GIT. The most commonly used dosage forms for oral delivery of drugs are solids, liquids and disperse systems. Liquid systems include oral solutions. Disperse systems include suspensions and emulsions. Solid dosage forms include a wide variety of tablets, capsules, caplets and powders.
  5. 5. 13-Aug-165 DRUG SELECTION CRITERIA  Drugs with molecular weight/size < 1000 Da.  Drug solubility should be greater than 0.1μg/ml.  Drugs with high permeability should be selected, as matrix tablets are release rate limiting but not permeation rate limited.  A drug that is passively absorbed through the GIT is an ideal candidate for sustained release matrix tablets.  Drugs which exhibit absorption window due to site specific or active transport processes are poor candidates as they may have incomplete bioavailability. Ex: Riboflavin, folic acid, aminopenicillins and nucleoside analogues.  Drugs with low half-life.  Drugs with larger therapeutic window.  The drug should not be influenced by pH and enzymes.
  6. 6. 13-Aug-166 ORAL DISPERSIBLE SYSTEM Drug Selection Criteria  The drug should not have a bitter taste.  The dose should be lower than 20 mg.  The drug should have moderate to low molecular weight.  It should have good stability in water and saliva.  The drug must be partially non-ionized at the oral cavities pH.  It should have the ability to diffuse and partition into the epithelium of upper GIT.  It should have the ability to permeate oral mucosal tissue.  Drugs with shorter half-lives are unsuitable to be formulated as ODTs
  7. 7. 13-Aug-167 PULSATILE DRUG DELIVERY SYSTEMS Drug Selection Criteria  Chronopharmacotherapy of diseases which show circadian rhythms in their pathophysiology.  Drugs which show extensive first pass metabolism. Ex. β blockers and salicylamide.  Drugs which undergo extensive first pass metabolism require fast drug input to saturate metabolizing enzymes in order to minimize pre-systemic metabolism.  Drugs having short half-lives like β blockers.  Drugs which show biological tolerance like transdermal nitro-glycerine and Salbutamol sulfate.  Drugs needed to be targeted to the specific site in the intestine.  Drugs which cause gastric irritation (NSAIDS) and for the drugs which are not stable in GI fluids like proteins.
  8. 8. 13-Aug-168 COLON TARGETED DRUG DELIVERY Drug Selection Criteria  Drugs which show poor absorption from stomach or intestine are the best candidates.  Peptides, proteins, oligonucleotides and vaccines are potential candidates for colon targeted DDS.  Drugs used in the treatment of inflammatory bowel disease, ulcerative colitis, diarrhoea and colon cancer are ideal candidates.  Drug carrier is another factor which influences Colon targeted DDS. The selection of carrier for particular drugs depends on the physiochemical nature of the drug as well as the disease for which the system is to be used.  Factors such as chemical nature, stability and partition coefficient of the drug and type of absorption enhancer chosen influence the carrier selection. Moreover, the choice of drug carrier depends on the functional groups of the drug molecule.
  9. 9. 13-Aug-169 FLOATING DRUG DELIVERY SYSTEM Drug Selection Criteria  Drugs with narrow absorption window in stomach. E.g. Riboflavin and Levodopa.  Drugs which are basically absorbed from the stomach and upper part of GIT. E.g. Chlordiazepoxide and Cinnarazine.  Drugs that disturb normal colonic bacteria. E.g. Amoxicillin trihydrate.  Drugs which are locally active in stomach. E.g. Antacids and Misoprostol.  Drugs that degrade in the colon. E.g. Ranitidine HCl and Metronidazole.  Drugs that have poor bioavailability because of site-specific absorption from the upper part of GIT are potential candidates to be formulated as FDDS, thereby maximizing their absorption.
  10. 10. 13-Aug-1610 TRANSDERMAL DRUG DELIVERY SYSTEMS Drug Selection Criteria  Dose should be low i.e. < 20mg/day.  Half life should be 10h or less.  Molecular weight should be <400 Da.  Partition coefficient Log Po/w should be between 1.0 and 4.  Skin permeability coefficient should be 0.5x10-3 cm/h.  Drug should be non-irritating and non-sensitizing to the skin.  Oral bioavailability should be low.  Therapeutic index should be low.
  11. 11. 13-Aug-1611 MUCOADHESIVE DRUG DELIVERY SYSTEMS Drug Selection Criteria  Drugs with less elimination half-life.  Drugs which have poor bioavailability.  Drugs which require frequent dosing.  Drugs which show local action in the oral mucosa.
  12. 12. 13-Aug-1612 VESICULAR DRUG DELIVERY SYSTEMS Drug Selection Criteria  Drugs which have low bioavailability and varied pharmacokinetics.  Drugs which are poorly soluble.  Drugs with short half-life.  Drugs which require prolonged residence time in blood can be given as the vesicular preparations  prolong the residence time.  Drugs which require specific targeting. For example liver targeting can be done as their small size aids in RES uptake and they can be used to target the cancerous tissue.  As vesicles aid in dermal/transdermal delivery drugs which require dermal/transdermal delivery can be selected.  Only potent drugs can be selected.
  13. 13. 13-Aug-1613

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