Composition for injections, which contains hydroxychloroquine, for local application in treatment of haemorrhoid

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to an injection medical composition for local application in treatment of haemorrhoid, which contains hydroxychloroquine. In particular, the composition contains hydroxychloroquine in a physiological solution for injection with a local anaesthetic and an antioxidant.

EFFECT: injection composition by the invention ensures strengthening of haemorrhoid tissue for blocking metabolism in the haemorrhoid tissue, and as a result -necrosis of the haemorrhoid tissue.

5 cl, 8 dwg, 1 ex

 

The technical field

The present invention relates in General to injection drug formulations with a content of hydroxychloroquine for local application in the treatment of hemorrhoids, in particular for injecting a medicinal composition for the treatment of hemorrhoids introduced directly into the hemorrhoid region in order to strengthen the hemorrhoidal tissue to block metabolism in hemorrhoidal tissue, and as a result, for the deadening of hemorrhoidal tissue.

Background of invention

Hemorrhoids is the first cause of hospitalization in Korea, and 50% or more of the population 50 years and older suffer from this disease (according to the hospital Seoul national University). Also about 50% of the U.S. population suffers from this disease.

In General, hemorrhoidal disease, the so-called hemorrhoids, include the emergence of hemorrhoids, anal fissures, perianal tumors, anal fistula, and are the main symptoms, including bleeding, perforation of the rectum, pain, itching, rectal dysfunction and the failure of feces. Among them, the term "hemorrhoids" is the most commonly used.

Hemorrhoids occur due to the expansion and proliferation of vascular tissue below the skin and the mucous tissue of the anus and education is caused by stretching of the skin and SL is sistas shell, covering the blood vessels of the anus. Hemorrhoids are divided into internal hemorrhoids, external hemorrhoids and hemorrhoids mixed type. Hemorrhoids that occur over premonicion-anal line (approximately 1.5 cm above the inner edge of which extends muscles of the anus), refers to the internal hemorrhoids; hemorrhoids that occur below premonicion-anal line refers to external hemorrhoids; hemorrhoids that occur both above and below premonicion-anal line refers to the piles of mixed type. At the initial stage occurs either internal or external hemorrhoids, but in most cases, over time, internal or external hemorrhoids turn into piles of mixed type.

The degree of progression of internal hemorrhoids is divided in accordance with the degree of protrusion of hemorrhoids from the anal opening to: stage 1, in which hemorrhoids can be diagnosed by the presence of bleeding, but hemorrhoidal site does not protrude from the anus; stage 2 on which the hemorrhoidal site is when bowel movements, but when it returns to its original position after emptying; stage 3, which hemorrhoidal node performs during emptying of the bowel, with protruding hemorrhoidal node is returned in its original Polo which begins after a considerable time period after emptying the bowel or only as a result of pressure or fit; and stage 4 on which the hemorrhoidal site, acting during emptying of the bowel, is not returned to its original position with ease or is again immediately after it has been returned to its original position.

The degree of progression of external hemorrhoids objectively not separated or can be separated based on the time of occurrence of thrombosis in connection with the balance with the internal hemorrhoids. In particular, external hemorrhoids stage-1 is the occurrence of thrombosis and swelling within less than 10 days per year; to external hemorrhoids phase 2 refers to the occurrence of thrombosis and swelling for about 11-20 days per year; to external hemorrhoids stage 3 is the occurrence of thrombosis and swelling for more than 3 weeks per year; and to external hemorrhoids stage 4 refers to the frequent occurrence of thrombosis.

Common treatments for hemorrhoids include: a method to stop bleeding internal hemorrhoids; method of reducing thrombosis and associated swelling and pain when external hemorrhoids; internal use of drugs or suppositories; and sedentary baths.

Treatment of internal medicines for hemorrhoids-based drugs to stimulate circulation, and includes about 10 commercially available medicines. Suppositories for the treatment of hemorrhoids include loads the existing substances analgesic, anti-inflammatory, antibacterial and astringent properties, and cover about 20 commercially available medicines.

As ointments and suppositories for the treatment of hemorrhoids are mainly used formulations containing local anesthetics, steroids and antihistamines. Application of local anaesthetic or steroid funds temporarily relieves discomfort, but they slow down the healing process and have a high probability to cause a range of systemic and local side effects. Furthermore, the use of non-steroidal anti-inflammatory drugs around the wound is prohibited, as this slows down the process of treatment of the disease in General.

Also, surgical treatments are often not welcomed by patients and does not lead to the removal of roots hemorrhoids, as their application is deleted, only the protruding portion of hemorrhoids.

In Korean published patent application No. 10-2005-0102663 describes a means for external use for the treatment of hemorrhoids and anal fissures, which includes acetylsalicylic acid or its salt as an active ingredient.

Registered Korean patent No. 10-0863758 describes a pharmaceutical preparation for topical application for the treatment of acute or chronic anal the cracks, thrombotic internal or external hemorrhoidal diseases, medication contains antagonist of adenosine receptor selected from the group including theophylline and Tefillin.

In Korean published patent application No. 10-2008-0105857 describes a pharmaceutical composition for direct local external use, pharmaceutical composition contains caviar extract fish ball, egg yolk oil and the extract borozdoplodnik (Cnidium a rhizome) and is used for the treatment of diseases of the anus and rectum.

However, injectable pharmaceutical composition for the treatment of hemorrhoids with the contents of hydroxychloroquine as specified in the present invention, this was not known, and is injected directly into the affected area to strengthen the hemorrhoidal tissue to block metabolism in hemorrhoidal tissue and, as a result, for deadening.

Technical problem

The present invention provides an injectable pharmaceutical composition that contains hydroxychloroquine, for local application in the treatment of hemorrhoids. When the medicinal composition of the present invention is injected directly into the affected area so that it penetrates to the root of the hemorrhoid to necrosis of hemorrhoidal tissue, diseased tissue is reduced PR is approximately at 1/3 of its original size and as a result, split.

Regarding the mechanism of action of the present invention, when injecting a medicinal composition containing hydroxychloroquine, for topical application for the treatment of hemorrhoids in accordance with the present invention is injected directly into the affected area, it strengthens the affected tissue to block metabolism in it and, as a result, inactivates the affected tissue for its deadening.

Technical solution

The present invention relates to injectable pharmaceutical composition containing hydroxychloroquine, for local application in the treatment of hemorrhoids. In particular, the present invention relates to injectable pharmaceutical composition for topical application containing 5-10 g of hydroxychloroquine, dissolved in 10 ml of physiological saline for injection with a local anesthetic and an anti-oxidant.

In the medicinal composition of the present invention hydroxychloroquine preferably contained in an amount of 1-60% by weight/volume, and more preferably in the amount of 50% by weight/volume based on the volume of saline for injection.

In the present invention in addition of hydroxychloroquine to the physiological solution for injection 50% weight/volume will not dissolve easily, and thus, will be in view of the mist. In this case, it is preferable to use after dissolution in hot water.

If the content of hydroxychloroquine compared with the saline solution for injection is less than 1% weight/volume, the desired therapeutic effect is reached, and if the content exceeds 60% by weight/volume, hydroxychloroquine does not dissolve easily, which will lead to difficulties in the formulation and the rapid emergence of deadening fabric, which in turn will lead to undesirable consequences.

A local anesthetic used in the present invention is to eliminate pain during the introduction of the drug compound in the form of injections directly into the affected area. The preferred content of lidocaine as a local anesthetic is 1-2% weight/volume.

The antioxidant used in the present invention, serves to stabilize the drug compound. The preferred content of Riboflavin as an antioxidant is 0.1% weight/volume.

Injectable pharmaceutical composition for topical application may be prepared using the above-described technology of preparation in accordance with any conventional method known in this field.

For the treatment of hemorrhoids medicinal composition of the present invention is injected through injection directly into Parag is nnow region. Preferably, the medicinal composition of the present invention is applied 2-3 times with an interval of 3-4 days depending on the patient's condition.

With significant and very painful hemorrhoids patient pharmaceutical composition of the present invention can be used in small doses daily for one week or more.

Description of the drawings

Figure 1 shows a series of photographs which indicated the affected area hon 00 (women 82 years) after 5, 8 and 40 days after topical application of the pharmaceutical composition of the present invention.

Figure 2 shows a series of photographs which indicated the affected area Kim 00 (women 36 years) before and after 5 and 26 days after topical application of the pharmaceutical composition of the present invention.

Figure 3 presents a series of photographs which indicated the affected area By 00 (men 43 years) after 2, 5 and 19 days after topical application of the pharmaceutical composition of the present invention.

Figure 4 presents a series of photographs which indicated the affected area 00 Kim (male 56 years) after 3, 6 and 23 days after topical application of the pharmaceutical composition of the present invention.

Figure 5 shows a series of photographs which indicated the affected area Kim 00 (women 42 years) after 4 and 13 days after the local application of the drug is the composition of the present invention.

Figure 6 presents a series of photographs which indicated the affected area If 00 (women 35 years) after 5, 20, and 30 days after topical application of the pharmaceutical composition of the present invention.

Figure 7 presents the number of photos that include the affected area Cho 00 (men 36 years) before and after 3 and 23 days after topical application of the pharmaceutical composition of the present invention.

Figure 8 shows a series of photographs, which indicated the affected area If 00 (women 51 years) before and after 4 weeks of topical application of medicinal composition of the present invention.

The best option

Hereinafter, a detailed description of the present invention with reference to examples and test examples.

Example 1

Preparation of injectable pharmaceutical composition for local application in accordance with the present invention (hereinafter referred to as "Haemsol 50" (Chemsol 50)).

10 g of hydroxychloroquine was dissolved in 10 ml solution for injection was added 2% by weight/volume of lidocaine and 0.1% weight/volume of Riboflavin, therefore, was prepared injectable pharmaceutical composition for local application (Haemsol 50).

Introduction to hemorrhoidal node

0.2-0.3 ml of a solution Haemsol 50 was introduced 2-3 times with an interval of 3-4 days with a focus on the top of the hemorrhoids, Russ is atively as a triangular pyramid.

Test example 1

Hon 00 (woman, 82 years)

Suffered from hemorrhoids for over 60 years and has held various courses of treatment. To remove hemorrhoids was not possible, because he was too big, and the woman is too old for surgery.

Before the introduction of the solution Haemsol 50 the size of the hemorrhoids was 3.5×5.0 cm and cause severe pain.

1.2 ml of a solution Haemsol 50 were introduced quickly, and after 4 days the solution Haemsol 50 was introduced again.

8 days after entry of the solution Haemsol 50 the size of the hemorrhoids have grown to 4.5×6.5 cm, and the pain decreased.

Diseased tissue began to die within 14 days after entry of the solution Haemsol 50.

21 days after entry of the solution hemorrhoids completely peeled off and is dead, and the necrotic tissue was applied cream Silvadene.

Was treated for recovery of the tissue and prevent inflammation, tissue fully recovered on day 36 after the introduction of the solution (see figure 1).

Test example 2

Kim 00 (woman, 36 years)

Suffered from bleeding and hemorrhoids for a long period of time and experienced discomfort during bowel movements.

Before the introduction of the solution Haemsol 50 she was the top hemorrhoids 1.5×1.0 cm in diameter and lower hemorrhoids to 2.0×1.0 in diameter. After the first injection solution Haemsol 50 hemorrhoids increased slightly in size.

Chere is C 14 days after introduction of the solution hemorrhoids died, completely peeled off, and in its place was a large hole.

On the affected area was painted cream Silvagen avoid inflammation, were treated for tissue regeneration. After 26 days after the introduction of the fabric was fully restored (see FIG.2).

Test example 3

By 00 (male 43 years)

Before the introduction of the solution Haemsol 50 the size of the hemorrhoids was 1.0×2,0 see 5 days after the first injection solution Haemsol 50 appeared latent hemorrhoids 3,5×5,0 see 19 days after the second injection solution hemorrhoids completely died and peeled off. On dead tissue was applied cream Siladen, and completely regenerates 30 days after the introduction of the solution Haemsol 50 (FIG.3).

Test example 4

Kim 00 (male 56 years)

Suffered from hemorrhoids, although a long time had treated him.

Before the introduction of the solution Haemsol 50 the size of the hemorrhoids was to 2.0×2,5 see It gradually got bigger after the first injection solution Haemsol 50 and reached a size of 3.5×4.5 cm on day 6 after injection.

23 days after the introduction of the solution hemorrhoids completely peeled off.

On the affected area for about 2 weeks was applied cream Siladen, then the fabric was fully regenerated (see FIG.4).

Test example 5

Kim 00 (woman 42 years)

Suffered from hemorrhoids and bleeding for several years.

To webenertia Haemsol 50 the size of the hemorrhoids was 2.5×3,0 see 3 days after the introduction of the solution Haemsol 50 size hemorrhoids increased to 3.0×4,0 see

13 days after the introduction of the solution Haemsol 50 hemorrhoids completely died.

On the affected area was painted cream Siladen, fabric fully regenerates 2 weeks after the introduction of the solution Haemsol 50 (see FIG.5).

Test example 6

If 00 (woman, 35 years old)

After several years of disease hemorrhoids she underwent surgery. Hemorrhoids had anticipated after surgery in the form of the grapes (large hemorrhoids, separated by approximately 4 parts).

5 days after the introduction of the solution Haemsol 50 dimensions of the hemorrhoids have grown to 3.5×5,0 see

After 21 days after introduction of the solution Haemsol 50 hemorrhoids died and completely peeled off.

On the affected area was painted cream Siladen, fabric fully regenerates 31 days after introduction of the solution Haemsol 50 (see FIG.6).

Test example 7

Cho 00 (male 36 years)

Suffered from hemorrhoids for a long time.

Before the introduction of the solution Haemsol 50 the size of the hemorrhoids was 1.5×2,0, see

3 days after the introduction of the solution Haemsol 50 size hemorrhoids increased to 2.5×3,0 see

23 days after the introduction of the solution Haemsol 50 hemorrhoids died and completely peeled off.

Fabric fully regenerates 30 days after the introduction of the solution Haemsol 50 (see figure 7).

Test example 8

If 00 (woman, 51 years old)/p>

Suffered from extensive hemorrhoids, which created difficulties in bowel movements.

Before the introduction of the solution Haemsol 50 the size of the hemorrhoids was 3.5×5,0 see

10 days after the introduction of the solution Haemsol 50 hemorrhoids begin to die and flake off.

16 days after the introduction of the solution Haemsol 50 hemorrhoids completely died and peeled off. 6 weeks after introduction of the solution Haemsol 50 fabric fully regenerates (see FIG.8).

Industrial applicability

As described above, the present invention provides an injectable pharmaceutical composition for local application with the content of hydroxychloroquine for the treatment of hemorrhoids. With the introduction of the composition of the present invention directly into the affected area so that it penetrated to the root of the hemorrhoid and caused necrosis of cells of hemorrhoids, the affected tissue will shrink by about 1/3 of the original size, resulting in the application. Thus, the composition of the present invention makes it possible to treat hemorrhoid is a simple and fundamental way without surgical operations.

1. Injectable pharmaceutical composition for local application with the content of hydroxychloroquine for the treatment of hemorrhoids.

2. The composition according to claim 1, containing hydroxychloroquine in the amount of 1-10 g relative to 10 ml of physiological saline for injection.

3. The composition according to claim 2, containing hydroxychloroquine in the number is TBE 10 g relative to 10 ml of physiological saline for injection.

4. The composition according to any one of claims 1 to 3, also comprising a local anesthetic and an antioxidant.

5. The composition according to claim 4, in which a local anesthetic is lidocaine at 2% weight/volume, and antioxidant - Riboflavin in the amount of 1% weight/volume.



 

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EFFECT: water-soluble form of medication possesses high anti-burn activity, low cost and long storage term.

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are presented: a composition for treating cancer containing (a) a conjugate containing (i) a polypeptide vector containing an amino acid sequence min. 70% identical to AngioPep-2 (SEQ ID NO: 97); and (ii) paclitaxel or a paclitaxel analogue conjugated with the above polypeptide; (b) an optional tonicity agent; (c) a buffer agent; (d) an excipient; (e) a polyoxyethylene ester of fatty acid; and (f) 0.01-8% DMSO (versions), a method for preparing (versions), a method of treating cancer, a container comprising the above composition, and a kit comprising the container with the above composition.

EFFECT: invention differs by the fact that the declared conjugates (eg ANG 1005) may pass through the hematoencephalic barrier, be characterised by high absorption by the targeted cells, manifest higher stability or be removed from the cell in a lesser degree, while the based compositions may be dissolved in an aqueous solution; they differ by stability and the minimal decomposition at temperatures within the range of 40°C and 50°C.

53 cl, 3 dwg, 28 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: storage-stable pharmaceutical composition represents a liquid formulation containing bortezomib and a system of anhydrous solvents and applicable for injection. A primary ingredient of the system of anhydrous solvents is propylene glycol. Bortezomib is found in the concentration of at least 1 mg/ml. The pharmaceutical composition contains a total amount of aqueous buffer of 10 vol. % or more.

EFFECT: stable pharmaceutical composition according to invention maintains bortezomib degradation at the level of not less than 10 wt % when keeping the liquid formulation for at least three months in the ambient environment.

9 cl, 10 tbl

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