OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for...

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OPHTHALMIC PREPARATIONS CIOBANU CRISTINA , PHD

Transcript of OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for...

Page 1: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

OPHTHALMIC PREPARATIONS CIOBANU CRISTINA , PHD

Page 2: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

Sourse of image. https://www.medicinenet.com/image-collection/eye_anatomy_detail_picture/picture.htm Dr. Cristina Ciobanu, SUMPh N. Testemitanu

Page 3: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

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

Page 4: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

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

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OPHTHALMIC FORMULATIONS

• OPHTHALMIC DROPS

• WASH

• IMPLANTS

• HELPFUL SOLUTIONS FOR USING CONTACT LENSES

• OPHTHALMIC OINTMENTS

• AEROSOLS

Dr. Cristina Ciobanu, SUMPh N. Testemitanu

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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

Page 7: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

FLOW DIAGRAM

Dr. Cristina Ciobanu, SUMPh N. Testemitanu

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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

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To obtain ophthalmic solutions we

need:

- active substances;

- solvents;

- auxiliaries;

Dr. Cristina Ciobanu, SUMPh N. Testemitanu

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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

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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

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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

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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

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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

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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

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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

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• 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.

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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

Page 19: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

Dr. Cristina Ciobanu, SUMPh N. Testemitanu

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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

Page 21: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

• 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

Page 22: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

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

Page 23: OPHTHALMIC PREPARATIONS · ophthalmic preparations are sterile pharmaceutical preparations used for the treatment and diagnosis of the diseased or injured eye. fr x provides for general

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