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BIOPHARMACEUTICS
INTRODUCTION

 

 

Biopharmaceutics:

Study of the relationship between physiochemical and formulation properties of a drug in a dosage form and the therapeutic response observed after its administration.

OR

The study of factors that influence the rate and extent of absorption of a drug from a dosage form into the systemic circulation (ie. “bioavailability” of the drug from the dosage form).

 

Importance of Biopharmaceutics:

- Bioequivalence:

Different formulations with comparable bioavailabilities.

- Comparing bioavailability:

(i) Extent of absorption:

- AUC.

- Urinary excretion.

(ii) Rate of absorption:

- Time to peak level (tp).

- Absorption rate constant (ka).

- Practical problems in relation to bioequivalence.

- Reasons to aim for maximum bioavailability.

TABLE: Drugs With Potential Bioequivalency Problems

Acetazolamide

Hydrochlorothiazide

Promethazine

Acetyldigitoxin

Hydroflumethiazide

Propylthiouracil

Alseroxylon

Imipramine

Pyrimethamine

Aminophyllin

Isoproterenol

Quinethiazide

Aminosalicylic acid

Liothyronine

Quinidine

Bendroflumethiazide

Menadione

Rauwolfia serpentina

Benzthiazide

Mephenytoin

Rescinnamine

Betamethasone

Methazolamide

Reserpine

Bishydroxycoumarin

Methyclothiazide

Salicylazosulfapyridine

Chlorambucil

Methylprednisolone

Sodium sulfoxone

Chlorodiazepoxide

Methyltestosterone

Spironolactone

Chlorothiazide

Nitrofurantoin

Sulfadiazine

Chloropromazine

Oxtriphylline

Sulfadimethoxine

Cortisone-acetate

Para-aminosalicylic acid

Sulfamerazine

Deserpidine

para-methadione

Sulfaphenazole

Dexamethasone

Perphenazine

Sulfasomidine

Dichlorphenamide

Phenacemide

Sulfasoxazole

Dienestrol

Phensuximide

Theophylline

Diethylstilbestrol

Phenylaminosalicylate

Thioridazine

Dyphylline

Phenytoin

Tolbutamide

Ethinyl estradiol

Phytonadione

Triamcinolone

Ethosuxmide

Polythiazide

Trichlormethiazide

Ethotoin

Prednisolone

Triethyl melamine

Ethoxzolamide

Primidone

Trifluoperazine

Fludrocortisone

Probenecid

Triflupromazine

Fluphenazine

Procainamide

Trimeprazine

Fluprednisolone

Prochlorperazine

Trimethadione

Hydralazine

Promazine

Uracil mustand

   

Warfarin



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