液體制劑(英文)課件

1、Liquid pharmaceutical PreparationsDr. Murat Kizaibek (木拉提克扎衣別克 博士） Traditional Kazakh Medicine Research Institute of Ili Kazakh Autonomous Prefecture Xinjiang Medical University Apr 22, 2012A solution is a homogenous one-phase system consisting of two or more components. solvent + soluteThe solvent

2、is that phase in which the dispersion occurs and the solute is that component which is dispersed as small molecules or ions in the solvent.Liquid preparations: the formulation prepared by dispersing drug substance in the appropriate solvents and used internally or externally.Attention: injections an

3、d extractions are not included in this chapterIntroductionClassification of liquid preparations (I) According to dispersion system Homogeneous system: thermodynamic stable Low molecular solutions: solute 100 nm Suspensions: 500 nmemulsionsuspensioncolloidsolutionClassification of liquid preparations

4、 ()According to administration route oral: drops, syrups, emulsions, suspensions, mixture External: Dermal: lotion, liniment For ENT (ears,nose,throat): nasal drops, auristillae For ophthalmic administration: eye drops, collyria For rectal, vaginal and urethral administration: enema, irrigationsDisa

5、dvantages of liquid dosage form Chemical stability: hydrolysis, oxidation Physical stability: emulsion, suspension Liquids are bulky and therefore inconvenient to transport and store.Solutions often provide suitable media for the growth of micro-organism and may therefore require the addition of a p

6、reservative.Quality control of liquid dosage formsHomogeneous formulations: should be clear solution.Non-homogeneous formulations: particles should be small with a narrow particle size distribution.Liquid formulations for oral should be palatable.For all liquid formulations: with accurate content st

7、able conservative convenient packagewaterWaterWater is the most widely used solvent for use as a vehicle for pharmaceutical products because of lack of toxicity , physiological compatibility and its ability to dissolve a wide range of materialsDistilled waterFree of salt Free of pyrogen Free from ca

8、rbon dioxide or free from airEthanol (ethyl alcohol) Glycerin (USP: glycerol) Glycerin (USP: glycerol) Glycerin is a clear syrupy liquid with a sweet taste. miscible with both water and alcohol. widely used particularly as a auxiliary solvent in conjugation with water or alcohol. used in many intern

9、al preparations. 10% water-containing glycerin no irritation 30% glycerin has preservative qualities.Propylene glycolFor pharmaceutical use: 1,2-propylene glycol.useful solvent with a wide range of applications and is miscible with water and alcohol.frequently substituted for glycerin in modern phar

10、maceutical formulations.Mixture of propylene glycol and water can decrease the hydrolysis of drug substance and increase stability.Polyethylene glycol (PEG)TypeAppearance(25)MolecularWeightpHPEG 200Colorless liquid1802205.07.0PEG 300Colorless liquid2703305.07.0PEG 400Colorless liquid3604405.07.0PEG

11、600Colorless liquid5406605.07.0PEG 800White paste7208805.07.0PEG 1000White paste90011005.07.0PEG 1500White solid135016505.07.0PEG 2000White solid180022005.07.0PEG 3000White solid270033005.07.0PEG 4000White solid360044005.07.0PEG 6000White solid540070005.07.0PEG 8000White solid720088005.07.0Polyethyl

12、ene glycol (PEG)General formula: MW10 have an affinity for water (hydrophilic) and number 30%)spearmint oil (0.05%)cinnamyl aldehyde (0.01%)eucalyptus oil (0.01%0.05%) SweetenersSucrose Dextrose Liquid glucosehoney GlycerinSorbitolMannitolStevioside: 300 times of sucrose, 0.0250.05% ,used together w

13、ith sucrose and saccharin.Saccharin/ Saccharin sodium : 200700 times of sucrose, 0.03%. Aspartame：150200 times of sucrose, no bitternessFlavoringsNatural products fruit juices aromatic oils such as peppermint and lemon oils herbs and spices and distilled fractions of these They are available as conc

14、entrated extracts, alcoholic or aqueous solutions, syrups or spirits. Artificial products: they tend to be cheaper, more readily available, less variable in chemical composition and more stable than natural products. They are usually available as alcoholic or aqueous solutions or as powders.Selectio

15、n of suitable flavoringsTaste of product Suitable masking flavor SaltyApricot, butterscotch, cinnamon, orange, liquorice, peach, raspberry, vanilla ()BitterAnise() , chocolate, mint, passion fruit, wild cherry SweetVanilla, fruits, berries SourFruit or citrus flavors: Citrus fruits, liquorice, raspb

16、erry Mucilage Used for the masking of sour. Commonly used : CMC-Na MC Starch Sodium alginate Acacia GelatinEffervescent ()Composition: sodium bicarbonate + organic acid ( citric acid, tartaric acid).Produce CO2 when it comes in contact with water.Application: for the mask of bitter, salty, and astringent taste.Colorants () Natural colorants Vegetative: Red: beet red, carmine red. Yellow: turmeric yellow, carotene Blue: pine leaf Green: