Israel - English - Ministry of Health
The format of this leaflet was determined by the Ministry of
Health and its content was checked and approved
PATIENT LEAFLET IN ACCORDANCE WITH THE
PHARMACISTS’ REGULATIONS )PREPARATIONS( – 1986
The medicine is dispensed with a doctor’s
Ursolit 100, 300 Tablets
The active ingredient:
Ursodeoxycholic acid 100 mg.
Ursodeoxycholic acid 300 mg
For inactive ingredients see section 6. See also section
2 “Important information about some ingredients of the
Read the entire leaflet carefully before using the
medicine. This leaflet contains concise information about
the medicine. If you have any other questions, refer to the
doctor or the pharmacist.
This medicine has been prescribed for treatment of your
illness. Do not pass it on to others. It may harm them
even if it seems to you that their medical condition is
1. What is the medicine intended for?
The medicine is intended for the dissolution or reduction
in size of gallstones composed of cholesterol, and for
treatment of certain chronic liver diseases.
Therapeutic class: Bile acids.
2. Before using the medicine:
Do not use this medicine if:
You are sensitive )allergic( to the active ingredient
)bile acids( or any of the additional components the
preparation contains )for a list of inactive ingredients,
see section 6(.
You are suffering from an inflammatory exacerbation
of the gallbladder and/or biliary tract.
You are suffering from biliary obstruction.
You are suffering from a severe liver disease )other
than primary biliary cirrhosis(.
You are suffering from a stomach ulcer.
You are suffering from calcified gallstones.
Your gallbladder is not contracting properly.
You are suffering from an inflammation of the
You are suffering from biliary colic frequently )usually
characterized by pain in the upper right side of the
Special warnings regarding the use of the medicine:
The medicine should be used under medical
supervision )see also “tests and follow-up” in section 3(.
If you have previously suffered from any of the
conditions mentioned in the “Do not use this medicine
if” section - inform your doctor.
In case you are suffering from diarrhea during the
treatment, inform the doctor immediately, since he
may decide to reduce the dosage or discontinue the
In rare cases, some symptoms of biliary cirrhosis
)such as itching( may worsen in the beginning of the
treatment. In such a case, you should contact the
doctor, who may recommend to continue the treatment
with a lower daily dose )see also “Attention!” in
If you are sensitive to any type of food or medicine,
inform your doctor before starting treatment with this
If you are taking or have recently taken other
medicines, including non-prescription medicines and
food supplements, tell the doctor or the pharmacist.
Especially if you are taking:
Colestyramine and colestipol )for lowering lipid blood
levels(, active charcoal and aluminum-containing
antacids. If you must take these medicines, take them
at least two hours before or two hours after taking
Ciprofloxacin )antibiotics(, dapsone )antibiotics( and
nitrendipine )for lowering blood pressure( - Ursolit may
reduce the effect of these medicines. Their dosage may
need to be changed.
Ciclosporine )immunosuppressant( - Ursolit may affect
this medicine’s absorption. The doctor will test the
blood ciclosporine concentration and adjust the dosage
Rosuvastatin )for lowering cholesterol levels( - Ursolit
may affect the medicine’s action.
Contraceptive pills, estrogen and certain medicines for
lowering blood cholesterol and lipids such as clofibrate.
In certain cases these medicines may affect Ursolit’s
action. Consult with the doctor about this.
Use of the medicine and food
The medicine should be taken with or after a meal.
A low-cholesterol diet may contribute to the treatment’s
Pregnancy and breastfeeding
If you are planning pregnancy, are pregnant or
breastfeeding, consult a doctor before using the medicine.
Do not use the medicine during pregnancy unless the
doctor has decided that it is absolutely necessary.
Women who may become pregnant should use
contraceptives as will be recommended by the doctor.
A small amount of the medicine passes into breastmilk. If
you are breastfeeding, consult with your doctor.
Driving and operating machinery
Ursolit does not affect the ability to drive or operate
Use in children
This medicine is not intended for babies and children.
Safety of use in children has not been established.
Important information about some ingredients of
The preparation contains lactose and may cause an
allergic reaction in people who are sensitive to lactose.
Each tablet of Ursolit 100 contains 75 mg lactose
Each tablet of Ursolit 300 contains 100 mg lactose
3. How should you use the medicine?
Always use according to the doctor’s instructions.
Check with the doctor or pharmacist if you are uncertain.
The dosage and treatment regimen will be determined by
The doctor may recommend you to use Ursolit for up to
24 months, depending on the size of the gallstones. You
should continue treatment with Ursolit for 3 months after
the gallstones have been dissolved.
This medicine should be used at set intervals as
determined by the attending doctor.
The dosage will be determined by the doctor according to
your age and weight and disease severity.
The tablets may be halved or pulverized as necessary.
Do not exceed the recommended dose.
Attention! In rare cases, some symptoms of biliary
cirrhosis )such as itching( may worsen in the beginning
of the treatment. In such a case the treatment may
be continued at a lower daily dosage according to the
doctor’s orders. Afterwards, the doctor will increase the
dosage gradually )usually every week( up to the required
Tests and follow-up
During the first three months of treatment liver functions
tests should be performed every 4 weeks. Afterwards, it is
recommended to perform the test every 3 months.
If you accidentally take a higher dosage, diarrhea is
possible. If you are suffering from prolonged diarrhea,
contact the doctor immediately.
If you have diarrhea, be sure to drink enough fluids in
order to restore your salt-fluid balance.
If you took an overdose or a child accidentally swallowed
this medicine, go to the doctor or the emergency room
of the hospital immediately and take the package of the
medicine with you.
If you forgot to take this medicine at the required time,
do not take a double dose. Take the next dose at the
scheduled time and consult a doctor.
Follow the treatment as recommended by the doctor.
Even if there is an improvement in your health, do not
stop treatment with the medicine without consulting the
Do not take medicines in the dark! Check the label and
the dose every time you take the medicine. Wear glasses
if you need them.
If you have any other questions regarding use of the
medicine, consult the doctor or the pharmacist.
4. Side effects:
As with any medicine, using Ursolit may cause side
effects in some users. If the side effects do not go away,
if they are bothersome or if they worsen, consult your
doctor. Do not be alarmed when reading the list of side
effects. You may not experience any of them.
Common side effects )occurring in 1-10 out of 100
Soft stool and\or diarrhea )see also “Special warnings
regarding the use of the medicine” in section 2(.
Very rare side effects )occur in less than 1 out of
Severe pain in the upper right side of the abdomen,
worsening of cirrhosis which partially improves upon
discontinuation of treatment.
Side effects with unknown frequency )effects whose
frequency has not yet been determined(:
If a side effect occurs, if one of the side effects worsens,
or if you suffer from a side effect not mentioned in this
leaflet, consult your doctor.
Side effects may be reported to the Ministry of Health by
clicking on the link “report side effects due to medicinal
treatment” found on the Ministry of Health website
homepage )www.health.gov.il(, which will direct you to the
online form for reporting side effects, or by clicking on the
5. How to store the medicine?
Avoid poisoning! This medicine and any other medicine
must be kept in a closed place out of the reach of
children and/or infants to avoid poisoning. Do not
induce vomiting without an explicit instruction from the
Do not use the medicine after the expiry date )exp.
date( appearing on the package. The expiry date refers
to the last day of that month.
Store at a temperature lower than 25°C.
6. Additional information:
In addition to the active ingredient the medicine also
Lactose, Carboxymethyl-Cellulose Calcium, Maize
Starch, Povidone 25, Magnesium stearate
Maize Starch, Lactose, Povidone 25, Magnesium
stearate, Colloidal Silicone Dioxide
What does the medicine look like and what are the
contents of the package?
Ursolit 100: Round, biconvex, scored, white tablets.
Blister pack of 60, 100, 500 and 1000.
Not all package sizes may be marketed.
Ursolit 300: Round, biconvex, scored, white tablets.
Blister pack of 30 tablets.
License holder/manufacturer and the address: CTS
Chemical Industries Ltd., Kiryat Malachi.
This leaflet was checked and approved by the Ministry
of Health in: September 2017
Registration number of the medicine in the National
Drug Registry of the Ministry of Health: Ursolit 100:
192520542, Ursolit 300: 586326923
؟ءاودلا لمعتست فيك .3 .بيبطلا تاميلعت قفو ا
مود لامعتسلاا بجي
دكأتم نكت مل اذإ يلديصلا وأ بيبطلا ةراشتسا كيلع .بيبطلا لب
ق نم جلاعلا ة
يئاودلا ةعرجلا ديدحت
متيس مجحل ا
رهش 24 اهاصقأ ةرتفل تيلوسروأ لامعتساب بيبطلا كيصوي دق دعب رهشأ 3 ة
دمل تيلوسروأب جلاعلا ةلصاوم كيلع بجي .ة
يرارملا تاوصحلا نابوذ .جلاعملا بيبطلا لبق نم د
ح امك ةمظتنم تاقوأ يف ءاودلا اذه لامعتسا بجي ضرملا ةروطخ ةجرد ،كرمع بسحب بيبطلا لب
ق نم ة
يئاودلا ةعرجلا ديدحت
متيس .كنزوو .ةجاحلا بسحب صارقلأا سره وأ رطش نكمي .اهب ىصوملا ةعرجلا ز
مشتلا ضارعأ ضعب مقافتت دق ةردان تلااح يف !هبتنا رغصأ ة
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ةداع( جيردتلابو ،كلذ دعب .بيبطلا تاميلعت بسحب ،هيلع تناك ا
مم .ةبولطملا ة
يئاودلا ةعرجلا ىلإ لصي ى
يئاودلا ةعرجلا ةدايزب بيبطلا موقيس ةعباتملاو صوحفلا ةعبرأ لك دبكلا فئاظول صوحف ءارجإ بجي جلاعلا نم ىلولأا ةثلاثلا رهشلأا يف .رهشأ 3
لك صحفلا ءارجإب ىصوي كلذ دعب .عيباسأ لامتحا كلانهف ةبولطملا ة
يئاودلا ةعرجلا نم ربكأ ة
أطخ تلوانت اذإ .لصاوتم لاهسإ نم يناعت تنك اذإ ا
روف بيبطلا ىلإ ه
جوت .لاهسإ ثودحل لجأ نم لئاوسلا نم يفكي ام برش ىلع صرحاف ،لاهسلإاب ا
باصم تنك اذإ .كيدل لئاوسلاو حلاملأا نزاوت ةداعتسا بيبطلا ىلإ ا
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وبع كعم رضحأو ىفشتسملا يف ئراوطلا ةفرغ ىلإ وأ لوانت .ةفعاضم ةعرج لوانتت لاف ،بولطملا تقولا يف ءاودلا اذه لوانت تيسن اذإ .بيبطلا رشتساو د
دحملا تقولا يف ةيلاتلا ةعرجلا .بيبطلا ةيصوت بسح جلاعلا ىلع ةبظاوملا بجي نود ءاودلاب جلاعلا نع ف
قوتلا زوجي لاف ،ة
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سحت أرط ول ى
تح .بيبطلا ةراشتسا
لك يف ةعرجلا نم د
ملا عجار !ةمتعلا يف ةيودلأا لوانت زوجي لا .اهيلإ ةجاحب تنك اذإ ة
ظنلا عض .ءاودلا اهيف لوانتت .يلديصلا وأ بيبطلا رشتساف ،ءاودلا لامعتسا لوح ةيفاضإ ةلئسأ كيدل ترفوت اذإ :ةيبناجلا ضارعلأا .4 ضعب دنع ة
يبناج ضارعأ ثودح ىلإ تيلوسروأ لامعتسا ي
دؤي دق ،ءاود
لك لثم ،مقافتلاب ةذخآ وأ ةقلقم تناك وأ ةرباع ة
يبناجلا ضارعلأا نكت مل اذإ .نيلمعتسملا يناعت لا دق .ةيبناجلا ضارعلأا ةمئاق ةءارق دنع قلقت لا .بيبطلا ةراشتسا بجيف .اهنم دحاو يأ نم :)100 نيب نم نيلمعتسم 10-1 دنع رهظت( ةعئاش ة
"ءاودلا لامعتساب ق
صاخ تاريذحت" ا
ضيأ رظنا( لاهسإ وأ/و ن
يل زارب .)2 دنبلا يف :)10,000 نيب نم دحاو لمعتسم نم
لقأ دنع رهظت( ا
دج ةردان ة
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يولعلا نميلأا ءزجلا يف ديدش ملأ .جلاعلا فاقيإ دنع
يرارملا تاوصحلا س
.)ايراكيتروأ( ىرشلا :)دعب اهراشتنا ديدحت
متي مل ضارعأ( فورعم ريغ اهراشتنا ة
كح ضرع نم تيناع اذإ وأ ة
يبناجلا ضارعلأا دحأ مقافت اذإ ،
يبناج ضرع رهظ اذإ .كبيبط ةراشتسا كيلعف ،ةرشنلا هذه يف ركذ
يبناج طبارلا ىلع طغضلا ةطساوب ة
حصلا ةرازول ة
يبناج ضارعأ نع غيلبتلا ناكملإاب
يسيئرلا ةحفصلا يف دوجوملا "
يئاودلا جلاعلا بقع ة
يبناج ضارعأ نع غيلبتلا" ةرامتسلاا ىلإ ه
جوي يذلاو )www.health.gov.il( ة
حصلا ةرازو عقومل :طبارلا ىلإ لوخدلا قيرط نع وأ ،ة
يبناج ضارعأ نع غيلبتلل ةلص
؟ءاودلا نيزخت بجي فيك .5
ديعب قلغم ناكم يف رخآ ءاود يأو ءاودلا اذه ظفح بجي !ممستلا بنجت ؤيقتلا ببست لا .ممستلا ىدافتت كلذبو عضرلا لافطلأا وأ/و دلاولأا يديأ لوانتم .بيبطلا نم ةحيرص تاميلعت نودب
ودملا )Exp. Date( ةيحلاصلا ءاهتنا خيرات دعب ءاودلا لامعتسا زوجي لا .رهشلا سفن نم ريخلأا مويلا ىلإ ةيحلاصلا ءاهتنا خيرات ريشي .ة
يوئم ةجرد 25 نم
لقأ ةرارح ةجرد يف هن
زخ :ةيفاضإ تامولعم .6
:ىلع اضيأ ةلاعفلا ةداملل ةفاضلإاب ءاودلا يوتحي :100 تيلوسروأ
Lactose, Carboxymethyl-Cellulose Calcium, Maize
Starch, Povidone 25, Magnesium stearate
Maize Starch, Lactose, Povidone 25, Magnesium
stearate, Colloidal Silicone Dioxide
وبعلا ىوتحم وه امو ءاودلا ودبي فيك
طخ عم نيبناجلا لاك نم ةب
دحمو ةريدتسم ،ءاضيب صارقلأا :100 تيلوسروأ .رطشلل .1000 و 500 ،100 ،60 صارقلأا نم اهيف تاحيول ةبلع .تا
وبعلا ماجحأ عيمج ق
ت لا دق
طخ عم نيبناجلا لاك نم ةب
دحمو ةريدتسم ،ءاضيب صارقلأا :300 تيلوسروأ .رطشلل
صرق 30 اهيف تاحيول ةبلع
يئايميكلا تاعانصلل ط ص ك :هناونعو ع
نصملا /زايتملاا بحاص .يخلام تايرق
ربمتپس /لوليأ :خيرات يف ة
حصلا ةرازو لب
ق نم ت
ف ةرشنلا هذه
:ةحصلا ةرازو يف
لجس يف ءاودلا
586326923 :300 تيلوسروأ ,192520542 :100 تيلوسروأ
.ركذملا ةغيصب ةرشنلا هذه ةغايص تمت ،ةءارقلا ليهستلو طيسبتلا لجأ نم .نيسنجلا لاكل صصخم ءاودلا نإف ،كلذ نم مغرلا ىلع
LFL 622 09/17
רשואו קדבנ ונכותו תואירבה דרשמ ידי לע עבקנ הז ןולע טמרופ
1. TRADE NAME OF THE MEDICINAL PRODUCT
Ursolit 100 mg tablets
Ursolit 300 mg tablets
Each Ursolit 100 mg tablet contains: Ursodeoxycholic acid 100 mg
Each Ursolit 300 mg tablet contains: Ursodeoxycholic acid 300 mg
Ursolit 100mg also contains 75 mg Lactose monohydrate.
Ursolit 300mg also contains 100 mg Lactose monohydrate.
For full list of excipients, see section 6.1.
3. PHARMACEUTICAL FORM
Tablets for oral administration.
Ursolit 100: white round biconvex scored tablets.
Ursolit 300: white round biconvex scored tablets.
4. CLINICAL PARTICULARS.
4.1 Therapeutic Indications
Dissolution or reduction in size of radiolucent cholesterol in patient with a functioning
Treatment of chronic liver diseases including primary billiary cirrhosis, primary sclerosing
cholangitis, cystic fibrosis associated liver disease, billiary atresia, chronic hepatitis, and
4.2 Posology and method of administration
Gallstone dissolution: 8 to 12 mg/kg/day given in 2 divided doses.
If doses are unequal the larger dose should be taken in late evening to counteract the rise in
biliary cholesterol saturation which occurs in the early morning. The late evening dose may
usefully be taken with food to help maintain bile flow overnight.
The time required for dissolution of gallstones is likely to range from 6 to 24 months
depending on stone size and composition. Follow-up cholecystograms or ultrasound
investigation may be useful at 6 month intervals until the gallstones have disappeared.
Treatment should be continued until 2 successive cholecystograms and/or ultrasound
investigations 4-12 weeks apart have failed to demonstrate gallstones. This is because these
techniques do not permit reliable visualisation of stones less than 2mm in diameter.
The efficiency of Ursolit in treating radio-opaque or partially radio opaque gallstones has not
been tested but these are generally thought to be less soluble than radiolucent stones.
Non-cholesterol stones account for 10-15% radiolucent stones and may not be dissolved by
Chronic liver diseases: 10 to 15 mg/kg/day administered in 2 to 4 divided doses with food.
The dose may be adjusted according to the patient's age and severity of symptoms.
Ursolit tablets should not be used in patients:
With hypersensitivity to bile acids or any of the excipients listed in section 6.1
With radio-opaque calcified gallstones
With occlusion of the biliary tract (occlusion of the common bile duct or cystic duct).
With acute inflammation of the gall bladder or biliary tract.
With frequent episodes of biliary colic
With impaired contractility of the gall bladder.
With chronic liver disease, peptic ulcers or in those with inflammatory diseases of the
small intestine and colon.
4.4 Special warnings and precautions for use:
Ursolit should be taken under medical supervision.
During the first 3 months of treatment, the liver function parameters AST (SGOT),
ALT (SGPT) and γ-GT should be monitored by the physician every 4 weeks,
thereafter every 3 months. Apart from allowing for identification of responders and
non-responders in patients being treated for primary biliary cirrhosis, this monitoring
would also enable early detection of potential hepatic deterioration, particularly in
patients with advanced stage primary biliary cirrhosis.
When used for the dissolution of cholesterol gallstones:
In order to assess therapeutic progress and for timely detection of any calcification of
the gallstones, depending on stone size, the gall bladder should be visualised (oral
cholecystography) with overview and occlusion views in standing and supine
positions (ultrasound control) 6-10 months after the beginning of treatment.
If the gall bladder cannot be visualised on X-ray images, or in cases of calcified
gallstones, impaired contractility of the gall bladder or frequent episodes of biliary
colic, Ursolit should not be used.
When used for treatment of advanced stage of primary biliary cirrhosis:
In very rare cases decompensation of hepatic cirrhosis has been observed, which
partially regressed after the treatment was discontinued.
If diarrhea occurs, the dose must be reduced and in cases of persistent diarrhea, the
therapy should be discontinued.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactose
deficiency or glucose-galactose malabsorption should not take this medicine.
4.5 Interaction with other medicinal products and other forms of interaction:
Ursodeoxycholic acid should not be administered concomitantly with charcoal,
colestyramine, colestipol or antacids containing aluminium hydroxide and/or smectite
(aluminium oxide), because these preparations bind ursodeoxycholic acid in the
intestine and thereby inhibit its absorption and efficacy. Should the use of a
preparation containing one of these substances be necessary, it must be taken at
least 2 hours before or after ursodeoxycholic acid.
Ursodeoxycholic acid can increase the absorption of ciclosporin from the intestine. In
patients receiving ciclosporin treatment, blood concentrations of this substance
should therefore be checked by the physician and the ciclosporin dose adjusted if
In isolated cases ursodeoxycholic acid can reduce the absorption of ciprofloxacin.
Ursodeoxycholic acid has been shown to reduce the plasma peak concentrations
(Cmax) and the area under the curve (AUC) of the calcium antagonist nitrendipine.
An interaction with a reduction of the therapeutic effect of dapsone was also
These observations together with in vitro findings could indicate a potential for
ursodeoxycholic acid to induce cytochrome P450 3A enzymes. Controlled clinical
trials have shown, however, that ursodeoxycholic acid does not have a relevant
inductive effect on cytochrome P450 3A enzymes.
Oral contraceptives, oestrogenic hormones and blood cholesterol lowering agents
such as clofibrate may increase biliary lithiasis, which is a counter-effect to
ursodeoxycholic acid used for dissolution of gallstones.
4.6 Pregnancy and lactation
Animal studies did not show an influence of UDCA on fertility (see section 5.3). Human data
on fertility effects following treatment with UDCA are not available.
There are no or limited amounts of data from the use of UDCA in pregnant women. Studies in
animals have shown reproductive toxicity during the early phase of gestation (see section
5.3). URSOLIT must not be used during pregnancy unless clearly necessary.
Women of childbearing potential:
Women of childbearing potential should be treated only if they use reliable contraception:
non-hormonal or low-oestrogen oral contraceptive measures are recommended. However, in
patients taking URSOLIT tablets for dissolution of gallstones, effective non-hormonal
contraception should be used, since hormonal oral contraceptives may increase biliary
The possibility of a pregnancy must be excluded before beginning treatment.
According to few documented cases of breastfeeding women, milk levels of UDCA are very
low and probably no adverse reactions are to be expected in breastfed infants.
4.7 Effects on ability to drive and use machines
No effects on ability to drive and use machines have been observed.
4.8 Undesirable effects:
The evaluation of undesirable effects is based on the following frequency data:
Very common (≥ 1/10)
Common (≥ 1/100 to < 1/10)
Uncommon (≥ 1/1,000 to < 1/100)
Rare (≥ 1/10,000 to < 1/1,000)
Very rare / Not known (< 1/10,000 / cannot be estimated from available data)
In clinical trials, reports of pasty stools or diarrhea during ursodeoxycholic acid therapy were
Very rarely, severe right upper abdominal pain has occurred during the treatment of primary
Ursodeoxycholic acid may give rise to nausea and vomiting. The frequency of these effects
are not known.
During treatment with ursodeoxycholic acid, calcification of gallstones can occur in very rare
cases making them unable to be dissolved by bile acid therapy and resulting in surgery for
During therapy of the advanced stages of primary biliary cirrhosis, in very rare cases
decompensation of hepatic cirrhosis has been observed, which partially regressed after the
treatment was discontinued.
Skin and subcutaneaous disorders:
Very rarely, urticaria can occur.
Ursodeoxycholic acid may give rise to pruritus. The frequency of this effect is not known.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorization of the medicinal product is
important. It allows continued monitoring of the benefit/risk balance of the medicinal product.
Any suspected adverse events should be reported to the Ministry of Health according to the
National Regulation by using an online form
Diarrhea may occur in cases of overdose. In general, other symptoms of overdose are
unlikely because the absorption of ursodeoxycholic acid decreases with increasing dose and
therefore more is excreted with the faeces.
No specific counter-measures are necessary and the consequences of diarrhoea should be
treated symptomatically with restoration of fluid and electrolyte balance.
5. PHARMACOLOGICAL PROPERTIES
Pharmacotherapeutic group: Bile acid preparation
ATC code: A05AA02
5.1 Pharmacodynamics properties:
Ursolit is naturally occurring bile acid found in small quantities in normal human bile and in
larger quantities in the biles of certain species of bears. Ursolit suppresses hepatic synthesis
and cholesterol secretion and also inhibits intestinal absorption of cholesterol. It has little
inhibitory effect on synthesis and secretion into bile of endogenous bile acids and does not
appear to affect phospholipid secretion into bile.
Although insoluble in aqueous media, cholesterol may be solubilized in at least 2 ways in the
presence of dihydroxy bile acids. In addition to solubilizing cholesterol in micelles, Ursolit acts
by an apparently unique mechanism to cause dispersion of cholesterol as liquid crystals in
aqueous media. Thus even though administration of high doses (eg, 15 to 18 mg/kg/day)
does not result in concentration of ursodeoxycholic acid higher than 60% of the total bile acid
pool, ursodeoxycholic acid rich bile solubilizes cholesterol. The overall effect of Ursolit is to
increase the concentration level at which saturation of cholesterol occurs. The various actions
of Ursolit combine to change the bile of patients with gallstones from cholesterol –
precipitating to cholesterol – solubilizing.
5.2 Pharmacokinetic properties:
Absorption/Distribution - Ursodeoxycholic acid is absorbed in the small bowel after oral
administration. After absorption ursodeoxycholic acid enters the portal vein and undergoes
extraction from portal blood by the liver (ie, "first – pass" effect) where it is conjugated with
glycine or taurine and is then secreted into the hepatic bile ducts. In the bile it is concentrated
in the gallbladder and expelled into the duodenum in gallbladder via the cystic and common
ducts by gallbladder contractions provoked by physiologic responses to eating. With repeated
dosing, bile ursodeoxycholic acid concentrations reach steady state in about 3 weeks. After
ursodeoxycholic acid dosing is stopped, its concentration in bile falls exponentially, declining
to about 5% to 10% of its steady –state level in about 1 week.
Metabolism/Excretion – Small quantities of ursodeoxycholic acid appear in the systemic
circulation, and very small amounts are excreted into urine. A small portion of orally
administered drug undergoes bacterial degradation with each cycle of enterohepatic
circulation. Ursodeoxycholic acid can be oxidized and reduced, yielding 7-keto-lithocholic acid
or lithocholic acid respectively. Free ursodeoxycholic acid, 7-keto-lithocholic acid, and
lithocholic acid are relatively insoluble in aqueous media, and larger proportions of these
compounds are excreted via the feces. Reabsorbed free ursodeoxycholic acid is reconjugated
by the liver. Eighty present of lithocholic acid formed in the small bowel is excreted in the
feces, but the 20% that is adsorbed is sulfated in the liver to relatively insoluble lithocholyl
conjugates that are excreted into the bile and lost in feces. Absorbed 7-keto-lithocholic acid is
stereospecifically reduced in the liver to chenodiol.
6. PHARMACEUTICAL PARTICULARS
6.1 Ursolit 100 excipients: Lactose monohydrate, Carboxymethyl-Cellulose Calcium,
Maize Starch, Povidone , Magnesium Stearate
Ursolit 300 excipients: Lactose monohydrate, Maize Starch, Povidone,
Magnesium Stearate, Colloidal Silicone Dioxide
6.2 Special precautions for storage: Do not store above 25
7. MANUFACTURER/ MARKETING AUTHORIZATION HOLDER:
CTS Chemical Industries Ltd., 3 Hakidma St., Kiryat Malachi
8. MARKETING AUTHORIZATION NUMBER:
Ursolit 100: 0192520542
Ursolit 300: 0586326923
9. DATE OF REVISION OF THE TEXT:09.2017