ophthalmic preparations · ophthalmic preparations are sterile pharmaceutical preparations used for...
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OPHTHALMIC PREPARATIONS CIOBANU CRISTINA , PHD
Sourse of image. https://www.medicinenet.com/image-collection/eye_anatomy_detail_picture/picture.htm Dr. Cristina Ciobanu, SUMPh N. Testemitanu
REQUIREMENTS OF OPHTHALMIC PREPARATION
CLARITY
ISOTONICITY
PH APPROXIMATELY EQUAL TO 7.4 (NEAR TO TEAR FLUID)
PURITY AND STABILITY
STERILITY
VISCOSITY
SURFACE ACTIVITY
PRESERVATION TO PREVENT THE GROWTH OF MICROORGANISMS
STERILE AND PARTICLE-FREE.
ISO-OSMOTIC WITH THE LACHRYMAL SECRETION.
OPTIMUM VISCOSITY
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
DEFINITION
• OPHTHALMIC PREPARATIONS ARE STERILE PHARMACEUTICAL PREPARATIONS USED FOR THE TREATMENT AND DIAGNOSIS OF THE DISEASED OR INJURED EYE.
• FR X PROVIDES FOR GENERAL MONOGRAPHS: - OCULOGUTTAE (EYE DROPS, EYE DROPS): STERILE, AQUEOUS OR OILY SOLUTIONS OR SUSPENSIONS CONTAINING ONE OR MORE ACTIVE DRUG SUBSTANCES FOR OCULAR APPLICATION. THEY ARE USED IN THE TREATMENT AND DIAGNOSIS OF DISEASES BY THE EYES.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
OPHTHALMIC FORMULATIONS
• OPHTHALMIC DROPS
• WASH
• IMPLANTS
• HELPFUL SOLUTIONS FOR USING CONTACT LENSES
• OPHTHALMIC OINTMENTS
• AEROSOLS
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
OPHTHALMIC PREPARATIONS HAVE THE FOLLOWING ADVANTAGES:
• - QUICK EFFECT;
• - DIRECT LOCAL EFFECT,
• - THE USE OF LOW CONCENTRATIONS OF ACTIVE SUBSTANCES;
• - EASY, NON-RASH APPLICATION;
• - AND ALSO THE POSSIBILITY OF OBTAINING DIFFERENT OPHTHALMIC FORMS,
NAMELY SOLUTIONS, SUSPENSIONS, EMULSIONS, ETC.
DISADVANTAGES
• - SOMETIMES LOCAL INTOLERANCE;
• - THE NEED FOR SPECIAL PARENTERAL PREPARATIONS FOR PREPARATION,
CONDITIONING AND ADMINISTRATION;
• - THE LENGTH OF EYE OPHTHALMIC SOLUTIONS IS LOW (4-5 MINUTES).
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
FLOW DIAGRAM
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
STERILISATION
THE USUAL METHODS OF STERILIZATION INCLUDE: • STEAM UNDER PRESSURE FOR 120 °C 8 MIN.;
• WITH FLUENT STEAM FOR 15-30 MIN.;
• BY FILTRATION THROUGH MICROPOROUS STERILE FILTERS.
ARE NOT SERILISED:
SOLUTIONS WITH ANTIBIOTICS (EXCEPTION LEVOMYCETINE)
PROTARGOL, COLARGOL SOLUTION;
PHETANOLUM SOLUTION;
AMINOACIDOS AND FERMENTS: CHYMOTRYPSIN, LIDASE, CYSTEINE ETC.
• MEDICINAL SUBSTANCES: RESORCIN AND ADRENALINE HYDROCHLORIDE ARE ADDED
INTO OPHTHALMIC DROPS AFTER THE SOLUTION’S STERILIZATION AND COOLING,
UNDER ASEPTIC CONDITIONS.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
To obtain ophthalmic solutions we
need:
- active substances;
- solvents;
- auxiliaries;
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
AUXILIARIES
• 1. ISOTONIC AGENTS – PH. PROVIDES FOR THE
ISOTONISATION OF HYPOTONIC SOLUTIONS.
• WHEN ACTIVE SUBSTANCES ARE PRESCRIBED IN AMOUNTS
BELOW 1%, THE SOLUTION IS PREPARED BY DISSOLVING THE
ACTIVE SUBSTANCE IN STERILE ISOTONIC SOLUTION.
• WHEN THE MASS OF THE ACTIVE SUBSTANCE IS GREATER
THAN 1%, THE MASS OF THE SUBSTANCE REQUIRED FOR
ISOTONICITY IS CALCULATED ACCORDING TO THE FORMULA
GIVEN IN THE "INJECTABILITY" MONOGRAPH.
• AS ISOTONICANTS, SODIUM CHLORIDE, SODIUM NITRATE,
BORIC ACID, GLUCOSE, SODIUM SULFATE; ETC. MAY BE USED.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
AUXILIARIES
• 2. PH ADJUSTMENT AGENTS
• THE LACRIMAL PH HAS THE FOLLOWING MEAN VALUE:
• PH = 7.4
• THE EYE TOLERATES SENSITIVE DEVIATIONS FROM THIS VALUE, THE
PH TOLERATED BY THE EYE BEING BETWEEN 7.5-9.5.
• NOT IN ALL CASES A CONVENIENT PH CAN BE ACHIEVED.
THEREFORE, WHEN CHOOSING THE PH, THE STABILITY OF THE DRUG
AND THEN THE LOCAL TOLERANCE ARE CONSIDERED.
• DUE TO THE LACRIMAL FLUID BUFFERING CAPACITY, OPHTHALMIC
SOLUTIONS WITH PH BETWEEN 4.5-9; ALKALINE SOLUTIONS ARE
BETTER TOLERATED THAN ACIDIC. Dr. Cristina Ciobanu, SUMPh N. Testemitanu
AUXILIARIES
3. VISCOSITY-INCREASING AGENTS: THESE AUXILIARIES ARE
USED TO OBTAIN A RETARDED EFFECT. VISCOSITY AGENTS MUST MEET THE
FOLLOWING CONDITIONS:
• - BE WATER-SOLUBLE;
• - BE CHEMICALLY AND PHARMACOLOGICALLY INERT;
AS VISCOSITY AGENTS FOR OPHTHALMIC SOLUTIONS, THE FOLLOWING
MAY BE USED:
• - METHYLCELLULOSE SOIL 0.25-1%;
• - HYDROXYETHYL CELLULOSE;
• - SODIUM CARBOXYMETHYL CELLULOSE;
• - POLYVINYL ALCOHOL 1.4-4%;
• - POLYVINYLPYRROLIDONE 2%. Dr. Cristina Ciobanu, SUMPh N. Testemitanu
AUXILIARIES
4. PRESERVATIVES IN OPHTHALMIC DROPS
THERE CAN BE USED:
BENZALKONIUM CHLORIDE;
CHLOROBUTANOL HYDRATE;
MIX OF NIPAGIN WITH NIPAZOL;
MIX OF LEVOMYCETIN 2% WITH BORIC ACID;
SORBIC ACID.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
ADDED FOR STABILIZATION OF OPHTHALMIC DROPS
STABILIZATION
OPTHTALMIC SOLUTIONS OF
MEDICINAL SUBSTANCES WHICH
REPRESENTS – A SALT OF A
STRONG ACID AND A WEEK BASE
– USE OF HYDROCHLORIC ACID
TO STABILIZE THIS DROPLETS
AND OPHTHALMIC WASHES IS
UNDESIRABLE BECAUSE THE ACID
CAN IRRITATE THE MEMBRANE
TO STABELISE THE EYE DROPS
HCL IT IS SUBSTITUTED BY AN
WEAK ACID, EX: BORIC ACID
1.9-2%).
• SOLUTIONS OBTAINED FROM
SALTS OF STRONG BASES AND
WEAK ACIDS ARE STABILIZED
WITH 0.1 N SODIUM
HYDROXIDE SOLUTION,
SODIUM HYDROCARBONATE
OR SODIUM TETRABORATE.
• THE ABOVE-MENTIONED MUST
BE ISOHIDRIC (THEIR PH IS TO
BE CLOSE OF THAT OF THE
TEAR LIQUID, BETWEEN 7.4
AND 7.7).
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Dicaine, Novocain, Mezatone, Zinc sulfates • Are stabilized with - Boric acid 1,9%
Atropine, Ephedrine, Pilocarpine, Scopolamine • Are stabilized with – a mix of Boric acid
+ teraborat sodium+Cloramfenicol
STABILIZATION – examples of using
tampon solutions
pH = 5
pH = 6,8
FORMULATION AND CHOSEN PREPARATION
TECHNIQUE, MUST INSURANCE THE FOLLOWING QUALITY
REQUIREMENTS:
OPHTHALMIC SOLUTIONS DO NOT CONTAIN DISSOLVED
INGREDIENTS OR FOREIGN PARTICLES.
PHYSICO-CHEMICAL STABILITY OF MEDICINAL SUBSTANCE
AND PHYSICAL STABILITY OF PHARMACEUTICAL FORM.
TOLERANCE (INNOCUOUS)
MICROBIOLOGICAL, CHEMICAL AND MECHANICAL PURITY
AND EFFICACY
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
• RP: SOLUTIO DICAINI 0,25%-10ML
D.S.. EXTERNALLY, EYE DROPS 2 TIMES A DAY, 3 DROPS IN THE
CONJUGATIVE SAC.
CALCULATIONS:
E NACL/DICAINI=0,18
1,0 G DICAIN-------------0,18G NACL
0,025G DICAIN----------XG NACL
X=0,0045
M NACL=0,09- 0,0045 =0,085 G
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
W.V.D
Aq. pro injectionibus 5 ml
Dicaini 0,025
Natrii chloridi 0,085 g
Aq. pro injectionibus ad 10 ml
T.Vol. – 10 ml
Sterlisetur 100°C - 30 min.
PREPARATION
• ASEPTICALLY DISSOLVE IN 5 ML OF WATER FOR INJECTIONS IN A
STERILE FLASK ADD 0.025 G OF DICANINE AND 0.08 G OF NACL.
• THE SOLUTION OBTAINED IS BROUGHT WITH WATER TO 10 ML. FILTER
THROUGH A GLASS FILTER NO.2.
• IT IS CLOSE WITH HERMETICALLY SEALED. IT IS STERILIZED.
THE OPHTHALMIC DROPS CONTAINING TOXIC SUBSTANCES AS
DICAINE ARE DISPENSED WITH THE FOLLOWING INDICATIONS:
• OPHTHALMIC DROPS;
• HANDLE WITH CARE;
• KEEP AWAY FROM CHILDREN;
• TO BE DISPENSED WITH THE SIGNATURA.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
OPHTHALMIC OINTMENTS
In Ophthalmic ointments are prescribed drug substances with • hormonal action anti-inflammatory (cortisone,
hydrocortisone, betamethasone, dexamethasone), • antibiotics (tetracycline, oxatetracycline, levomicetine,
erythromycin, amphotericin), • antiglaucoma (pilocarpine, fetanol), • antiviral (florenal), • antiallergic (methyluracil), • vitamin (A, B2, B6, B2, D, E etc.).
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
• 1. ARE PREPARED IN ASEPTIC CONDITION, AFTER PREPARATION ARE NOT
STERILIZED.
• 2. A MIX – VASELINE : ANHYDROUS LANOLINE 9:1 IS USED FOR
PREPARATION CALLED “OPHTHALMIC EXCIPIENT – PRO OCULIS”
• 3. FOR OPHTHALMIC OINTMENTS WITH ANTIBIOTICS A MIX – VASELINE :
ANHYDROUS LANOLINE 6:4 IS USED
• 4. EXCIPIENTS ARE STERILIZED WITH DRY HEAT AT 180 C FOR 30-45 MIN.
• 5. RESORCINE AND ZINC SULPHATE ARE DISSOLVED IN WATER, RESULTING
IN OINTMENT-EMULSIONS.
• EXCEPTION – WELL DISSOLVING IN WATER - SODIUM BENZYL
PENICILLIN IT IS INTRODUCED LIKE SUSPENSION
• 6. INSOLUBLE SUBSTANCES (BORIC ACID, STREPTOCIDE ETC.), ARE
GRINDED WITH STERILE VASELINE OIL ACCORDING TO DERYAHIN RULE.
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Rp.: Benzylpenicillini-natrii 50 000 UA Lanolini anhydrici 4,0 Vaselini pro oculi 6,0 Misce, ut fiat unguentum Signa. Appply twice a day on eye lid
The sodium salt of benzylpenicillin is introduced into the ointment only by
the type of suspension, since it is rapidly inactivated in aqueous solution.
Calculations:
Transform Units of Action into grams
Check in tables from the literature – 1 000 000 UA………….0,6 g
50 000 UA……………x
x= 0,03
Total mass of ointment 10,03
Dr. Cristina Ciobanu, SUMPh N. Testemitanu
Preparation of the ointment is carried out in aseptic conditions.
In a sterile mortar, slightly warmed, put 0,03 sodium salt of
benzylpenicillin and rub with a drop of sterile Vaseline oil, gradually
adding the entire base.
Mix until uniform and place in a sterile jar with a screw cap with a
gasket.
Make up for the release of labels: "Eye Ointment", "Aseptically Cooked",
"Store in a cool and dark place".
W.V.D
Nr. of prescription Date
Benzylpenicillini-natrii sterile 0,03 (100 000 UA=0,06)
Oleum vaselini 1 gtts
Basis (6:4) sterile 10,0
Total mass 10,003
Addita aseptice