Film dosage form for administration of active substances from hemp, sticking to mucouse

FIELD: medicine.

SUBSTANCE: film dosage form sticking to mucous, containing at least on active substance from hemp. The form contains the polymeric matrix, which is used as a reservoir for the active substance and sticking to mucous. The form can have the multilayer structure. It can also contain the non-active ingredients, odorants or aromatisors. The film form is used in treatment of pain in such diseases as carcinomatosis, AIDS, trauma and other disorders.

EFFECT: invention provides better tolerance to administered substances and rapid onset of administered drug, simplifies administration procedures.

19 cl

 

The present invention relates to adhering to the mucosa of the film forms containing isolated from hemp active substances suitable for the introduction extracted from hemp active substances for therapeutic purposes. The invention also relates to the use of such forms for the treatment of painful conditions in humans or animals.

Substances included in the composition of Indian hemp (Cannabis saliva L.), have many pharmacological actions, the most famous of which is a psychotropic effect. In addition, the components of hemp also have antiemetic effect, anticonvulsant effect, muscle relaxant effect, analgesic effect, sedative effect and increases the appetite for action.

With regard to psychotropic or causing euphoria actions hemp, as well as associated with such action probability based application contained in the hemp active substances for therapeutic purposes is strictly limited.

It has long been known that the components of hemp can be used to treat insomnia, various types of neuralgia, rheumatic pain, and gastrointestinal disorders. Favourable therapeutic effect components hemp is also marked with the following statement.

Pain when carcinomatosis and as a result is their chemotherapy; pain syndrome and "devastation" when AIDS; nausea and vomiting as side effects of chemotherapy, as well as AIDS or hepatitis; neuropathic pain; loss of appetite or extreme exhaustion, especially in AIDS or carcinomatosis in the later stages.

The symptoms of paralysis due to multiple sclerosis or transverse traumatic injuries; dystonic motor disorders; asthma; seizures or generalized epilepsy; withdrawal symptoms associated with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; senile dementia, in particular Alzheimer's disease; nausea; arthritis; glaucoma; migraine; dysmenorrhea.

Currently, the requirements of the market responds only selected synthetically from hemp R-(6A,10A)-Δ-9-tetrahydrocannabinol (dronabinol). This isomer tetrahydrocannabinol (THC) is marketed under the name Marinol and is intended for oral administration as capsules. Marinol used to deal with significant weight loss in patients with AIDS and cancer patients after chemotherapy suffer from severe vomiting.

In addition to the above isomer of THC, for therapeutic purposes also apply extracts of hemp and hemp oil. They are usually applied Perera is Ino, i.e. in the form of capsules.

In extracts of hemp contains possessing pharmacological action of tetrahydrocannabinol (preferably Δ-9-tetrahydrocannabinol in small quantities Δ-9-tetrahydrocannabinol), cannabidiol, cannabinol and cannabichromene. These various substances are also referred to as cannabinoids (see Merck Index, 12th edition, 1996, str, No. 1794, and str, No. 9349).

Oral application is contained in the cannabis substances, in particular, R-(6A,10A)-Δ-9-tetrahydrocannabinol in the form of capsules, tablets, pills or other forms for oral administration or in the form of liquid preparations for oral administration has the following disadvantages:

because after taking the above forms of the drug is absorbed in the gastrointestinal tract, the active ingredient starts to work late. This is a disadvantage, particularly with regard to the above indications, which typically requires rapid onset of action (e.g., anesthesia);

- when passing through the gastrointestinal tract of the substances contained in the cannabis at least partially decompose and lose activity under action of acid and enzymes, resulting in only a portion of the administered dose is absorbed and exerts a systemic effect;

in this regard, there may be undesirable bursts, Ural branch of the high concentration of active substance in the plasma, often causing side effects;

in addition, after oral application of a substantial part of the active substance in the process of passing through the liver has time to be metabolized (effect presystemic metabolism).

These disadvantages are particularly important with regard to portability issues such medicines in terms of the above indications. An additional disadvantage of the mentioned oral forms is the fact that in certain situations for patients particularly unpleasant for a long time to hold in the mouth tablet or capsule (covered in oily solution).

Thus, the present invention is the creation of molds for injection contained in the cannabis substances, which is free from the above described disadvantages and is characterized, in particular, improved portability, and simplified rules of admission, as well as useful pharmacological properties, in particular, rapid onset of action.

This problem is solved in adhering to the mucosa of the film form according to claim 1, containing at least one active substance from the group comprising substances contained in the cannabis, additional embodiments of which are described in the dependent clauses. The objective of the invention is also solved by PR the changes adherent to the mucosa of the film form according to the invention for treating a variety of diseases and symptoms.

Form according to the invention is preferably in the form of a thin, small flat items or records (pastilles) applied on the mucous membrane of the oral cavity, to which they stick due to its ability to adhere to the mucosa. Use on the mucous membrane of the oral cavity is preferably in the sublingual region or buccal mucosa. In addition, as applications can also be considered other mucosal surfaces of the oral cavity, for example, the mucous membrane of the nose.

In the process of applying the substance(s)contained in hemp, released from the mold and get into saliva, and then are absorbed into the mucous membrane of the oral cavity (i.e. crosslist). The release of the active substance in the contact area on the surface of the application can be done directly from the form in the mucous membrane of the oral cavity. In the process of application form absorbs saliva, and it contains the active substance is released under the action of diffusion.

In this regard, it is advisable that the active substance is released in the saliva after only a short time, and the mix of saliva and the active substance immediately reached all areas of the mucous membrane of the oral cavity, where its absorption. The amount of saliva in which the Rast is areeda and scatters released active substance per unit of time, is relatively small and is not excessive salivation, which mainly excludes the possibility of swallowing the active substance (which are referred to unwanted absorption in the gastrointestinal tract).

Since the absorption of the active substance occurs, bypassing the gastrointestinal tract, it is possible to avoid the above mentioned drawbacks of the delay in the commencement of the action, the effect of presystemic metabolism), characteristic of other oral forms (e.g. tablets).

Also simplified the rules of admission forms according to the invention, since their application does not require special training. Due to the small thickness of the film forms, receiving their patients generally do not experience discomfort.

In a preferred embodiment form according to the invention are polymeric matrix, which serves as a reservoir for the active substance and having the ability to stick to the mucosa. At least one layer or at least one surface of the mold has the ability to stick to the mucosa. The form may consist of one layer or multiple layers. In the case of a multilayer structure of at least one of the layers contains the active substance(s).

In the simplest case, the form is made in the form of preferably a single layer of polymeric mA the matrix, able to adhere to the mucous membrane and containing one or more active substances selected from hemp. Active ingredient(s) may be in the form of a solution, dispersion or emulsion.

The polymer matrix preferably contains one or more polymers, which can dissolve in water and/or swell in an aqueous environment. Due to the choice of such polymers can affect the ability of the matrix to adhere to the mucous membrane and release of the active substance.

As soluble or swellable in water of the polymers is particularly applicable to polymers selected from the group including: starch and starch derivatives, dextran; cellulose derivatives such as carboxymethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, hypromellose, hydroxypropylmethylcellulose, sodium carboxymethyl cellulose, ethylcellulose or propylethylene; polyacrylic acid, polyacrylates, polyvinylpyrrolidone, polyethylene oxides, polyacrylamides, polyethylene glycol, gelatin, collagen, alginates, pectins, pullulan, tragakant, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, carrageenan and natural resins.

The proportion of the polymer is preferably 5 to 95 wt.%, particularly preferably 15-75 wt.% in terms of dry weight of the form.

In site Cetelem the embodiment form according to the invention contain the extract of cannabis or hemp oil, preferably, in quantities of 0.5-50 wt.%, particularly preferably, in the amount of 1-30 wt.%. Specialists in the art known methods for producing pharmaceutically acceptable extracts of hemp or hemp oil.

The invention also relates to forms of the above-mentioned type containing as active ingredient at least one of cannabinoids selected from the group comprising tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromene. Particularly preferred as the active substance is tetrahydrocannabinol, in particular, R-(6A,10A)-Δ-9-tetrahydrocannabinol. Active substances on the basis of cannabinoids can be natural, semi synthetic or synthetic origin. The content of active substance is preferably 0.1 to 20 wt.%, particularly preferably, 0.5 to 10 wt.% in very rare on dry weight of the form.

A separate form preferably contains 0.5-20 mg, particularly preferably 1-10 mg of active ingredient, for example, tetrahydrocannabinol.

Form according to the invention may optionally contain one or more additives selected from the group comprising: fillers, pigments, flavorings, fragrances, perfumes, emulsifiers, plasticizers, sweeteners, preservatives, substances that increase penetration, regulatory and antioxidants. Specialists in the art within the principle of a known substance, applicable for such purposes.

Particularly suitable is the addition of flavoring agents, fragrances and aromatic substances, individually or in combination. For example, to improve the taste add a refreshing taste substance (for example, menthol, eucalyptol). It simultaneously promotes inconspicuous consumption of drugs, because its smell is not different from the smell of regular candy with a refreshing taste. In addition, simplified admission rules.

Particularly applicable are, for example, flavouring and aromatic substances, selected from the group comprising menthol, eucalyptol, lemon, phenylethanol, camphene, pinene, spicy aromatic substances, such as n-butylphthalide or cineole, as well as eucalyptus oil or thyme oil, methyl salicylate, turpentine oil, chamomile oil, ethylvanillin, 6-methylcoumarin, citronellol and n-butyl ester of acetic acid.

Form according to the invention, containing isolated from hemp active substances, are plates, i.e. they are thin and flat, for example, are thin, flat items or small lozenges. Such a flat plate can have various geometric shapes, such as circular, ellipsoidal or elongated.

The thickness preferably the composition is yet 0.01 to 2 mm, particularly preferably, 0.05 to 0.5 mm To neutralize the feeling of a foreign body layer must have a minimum possible thickness (preferably, less than 0.2 mm).

To achieve special effects form according to the invention may have a two-layer or multilayer structure. Individual layers may differ from each other by one or more of the following parameters: the composition of the polymers, the content of active substances, the concentration of active substances, the content of additives.

Considering the already mentioned properties of forms according to the invention, containing isolated from hemp active substances, they can be effectively used in the treatment of the following diseases or symptoms, especially:

pain when carcinomatosis and due to chemotherapy; pain syndrome "devastation" when AIDS; nausea and vomiting as side effects of chemotherapy, as well as AIDS or hepatitis; neuropathic pain; lack of appetite or extreme exhaustion, especially in AIDS or carcinomatosis in the later stages;

symptoms of paralysis due to multiple sclerosis or transverse traumatic injuries; dystonic motor disorders; asthma; seizures or generalized epilepsy; withdrawal symptoms associated with alcohol dependence, benzodiazepine dependent is thew and opiate dependence; Parkinson's disease; senile dementia, in particular Alzheimer's disease; nausea; arthritis; glaucoma; migraine; dysmenorrhea.

1. Adhering to the mucosa of the film form, containing the extract of cannabis or hemp oil for administration of an extract of cannabis or hemp oil for therapeutic purposes, characterized in that the form contains a polymer matrix, which serves as a reservoir for the active substance and having the ability to adhere to the mucosa, the polymeric matrix comprises one or more water-soluble and/or swellable in water polymers are preferably chosen from the group comprising starch and starch derivatives, dextran; cellulose derivatives such as carboxymethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, hypromellose, hydroxypropylmethylcellulose, sodium carboxymethyl cellulose, ethylcellulose or propylethylene; polyacrylic acid, polyacrylates, polyethylene oxides, polyacrylamides, polyethylene glycol, gelatin, collagen, alginates, pectins, pullulan, tragakant, chitosan, alginic acid, arabinogalactan, galactomannan, agar-agar, carrageenan and natural resins, and the proportion of polymer in the polymeric matrix is preferably 5-95 wt.%, particularly preferably 15-75 wt.%.

2. Form according to claim 1, characterized in that it contains the extract of cannabis or hemp oil, preferably in quantities of 0.5-50 wt.%, particularly preferably 1-30 wt.%.

3. Form according to claim 1 or 2, characterized in that it contains one or more substances selected from the group comprising menthol, eucalyptol, lemon, phenylethanol, camphene, pinene, spicy aromatic substances, such as p-butylphthalide or cineole, as well as eucalyptus oil or thyme oil, methyl salicylate, turpentine oil, chamomile oil, ethylvanillin, 6-methylcoumarin, citronellol, p-butyl ester of acetic acid.

4. Form according to claim 1 or 2, characterized in that its thickness is 0.01-2 mm, preferably 0.05 to 0.5 mm

5. Form according to claim 1 or 2, characterized in that it contains one or more non-active ingredients selected from the group comprising fillers, pigments, flavorings, fragrances, perfumes, emulsifiers, plasticizers, sweeteners, preservatives, substances that increase penetration, pH regulators and antioxidants.

6. Form according to claim 1 or 2, characterized in that it contains one or more substances selected from the group including odorants, odorous substances and aromatic substances, in particular from the group comprising menthol, eucalyptol, lemon, phenylethanol, camphene, pinene, spicy aroma is practical matter, such as p-butylphthalide or cineole, as well as eucalyptus oil or thyme oil, methyl salicylate, turpentine oil, chamomile oil, ethylvanillin, 6-methylcoumarin, citronellol, p-butyl ester of acetic acid.

7. Form according to claim 1 or 2, characterized in that it has a multilayer structure in which at least one layer contains the active substance.

8. The use of the extract of hemp or hemp oil adhering to the mucosa of the film form according to claim 1 for the treatment of pain associated with carcinomatosis and due to chemotherapy; pain syndrome "devastation" when AIDS; nausea and vomiting as side effects of chemotherapy, as well as AIDS or hepatitis; neuropathic pain; lack of appetite or extreme exhaustion, especially in AIDS or carcinomatosis in the later stages, symptoms of paralysis, caused by multiple sclerosis or transverse traumatic injuries; dystonic motor disorders; asthma; seizures or generalized epilepsy; withdrawal symptoms associated with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; senile dementia, in particular Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhea.

9. Application isolated from cannabis act is his substance, selected from the group including tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromene, in adhering to the mucosa of the film form according to claim 1 for the treatment of pain associated with carcinomatosis and due to chemotherapy; pain syndrome "devastation" when AIDS; nausea and vomiting as side effects of chemotherapy, as well as AIDS or hepatitis; neuropathic pain; lack of appetite or extreme exhaustion, especially in AIDS or carcinomatosis in the later stages, symptoms of paralysis, caused by multiple sclerosis or transverse traumatic injuries; dystonic motor disorders; asthma; seizures or generalized epilepsy; withdrawal symptoms associated with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; senile dementia, in particular Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhea.

10. The use of claim 8 or 9, characterized in that the form is a form according to claim 2.

11. The use of claim 8 or 9, characterized in that the form is a form according to claim 3.

12. The use of claim 8 or 9, characterized in that the form is a form according to claim 4.

13. The use of claim 8 or 9, characterized in that the form is a form according to claim 5.

14. Application on P8 or 9, characterized in that the form is a form according to claim 7.

15. Use PP and 9, characterized in that the treatment is carried out by application form on the mucous membrane of the oral cavity, particularly in the sublingual region or buccal mucosa.

16. Use PP and 9, characterized in that the form is a form according to claim 6.

17. Applying adherent to the mucosa of the film form according to claim 1, containing as active substance one of cannabinoids, preferably selected from the group including tetrahydrocannabinol, cannabinol, cannabidiol and cannabichromene, in particular for the treatment of pain associated with carcinomatosis and due to chemotherapy; pain syndrome "devastation" when AIDS; nausea and vomiting as side effects of chemotherapy, as well as AIDS or hepatitis; neuropathic pain; lack of appetite or extreme exhaustion, especially in AIDS or carcinomatosis in the later stages, symptoms of paralysis, caused by multiple sclerosis or transverse traumatic injuries; dystonic motor disorders; asthma; seizures or generalized epilepsy; withdrawal symptoms associated with alcohol dependence, benzodiazepine dependence and opiate dependence; Parkinson's disease; a hundred is as dementia, in particular Alzheimer's disease; arthritis; glaucoma; migraine; dysmenorrhea.

18. The application 17, wherein the form is a form according to any one of claim 2 or 3.

19. The application 17, characterized in that it is carried out on the mucous membrane of the oral cavity, particularly in the sublingual region or buccal mucosa.



 

Same patents:

FIELD: medicine.

SUBSTANCE: composition contains: a. core composition including therapeutically active agent, swelling agent and capillary agent; b. coating composition including water-insoluble polymer and water-soluble polymer.

EFFECT: composition releases therapeutically active agent in pulse mode at preset time.

21 cl, 15 tbl, 7 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes medicinal formulations and methods for providing the increasing rate of release of paliperidone. The medicinal formulations of sustained release provide the therapeutically effective mean and stable state of the paliperidone concentrations in plasma in a single administration per a day. This dosing regimen as a single dose per a day results to a single plasma paliperidone concentration peak for each 24 h period. Except for, the paliperidone plasma concentration occurs at later period after administration of dose and shows less value as compared the paliperidone plasma concentration that is achieved after administration of paliperidone in medicinal formulation with immediate release.

EFFECT: improved and valuable properties of formulations.

20 cl, 9 dwg, 2 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to tablet containing cetirizine and pseudoephedrine used in treatment of allergic disorders. Invention relates to a tablet comprising two separate layers. Invention relates to combinations of two pharmaceutical substances representing cetirizine and pseudoephedrine prepared in the weight ratio pseudoephedrine to cetirizine = 12-30. Pseudoephedrine-containing segment comprises inert pharmaceutical excipients and an alkalinizing agent. Pharmacokinetics patterns of cetirizine and pseudoephedrine are similar practically with pharmacokinetic pattern of medicinal preparations containing each of these components taken separately in the same doses. Invention provides the development of combination of pharmaceutical substances useful in treatment being without adverse effects.

EFFECT: improved and valuable medicinal properties of tablet.

44 cl, 5 tbl, 3 ex

FIELD: pharmaceutical agents.

SUBSTANCE: invention relates to solid pharmaceutical formulations for peroral administration useful in treatment of mild and moderately severe dementia such as Alzheimer's disease. Claimed formulation contains Rivastigmin or pharmaceutically acceptable salts thereof. Formulation represent gelatin capsule filled with pellet mixture or mixture of magnesium stearate with nonpareils, or matrix tablet.

EFFECT: preparation with controlled prolonged Rivastigmin release and improved tolerance.

3 cl, 5 ex, 15 tbl

FIELD: pharmaceutical industry.

SUBSTANCE: invention discloses solid oral dozed pharmaceutical form of hydrocodon with controlled release. Pharmaceutical form comprises analgetically effective amount of hydrocodon or pharmaceutically acceptable salt thereof and controlled-release material. Pharmaceutical forms of hydrocodon are suitable to be administered once a day and provides early commencement of therapeutical effect, which lasts at least about 24 h.

EFFECT: enhanced analgetic action.

44 cl, 3 tbl, 3 ex

New drug // 2240110
The invention relates to pharmaceutical industry

The invention relates to a pharmacy, preformed composition, which is able to immediately deliver the first active agent contained in the outer shell, and further continuously and in a controlled amount to deliver the second active agent from the osmotic inner part until the dosage form floats in the surrounding liquid

FIELD: medicine.

SUBSTANCE: therapeutic-cosmetic agent for the external use contains pantohematogen, water, polymeric gel-forming component, as well as dimethyl sulfoxide and water. The components are taken in particular quantitative ratio.

EFFECT: agent shows stable efficiency in treatment of osteoarthrosis and spinal osteochondrosis.

7 cl, 2 dwg

FIELD: medicine.

SUBSTANCE: therapeutic-cosmetic agent for the external use contains pantohematogen, water, polymeric gel-forming component, as well as dimethyl sulfoxide and water. The components are taken in particular quantitative ratio.

EFFECT: agent shows stable efficiency in treatment of osteoarthrosis and spinal osteochondrosis.

7 cl, 2 dwg

FIELD: medicine.

SUBSTANCE: invention relates to the compositions for care of the oral cavity, which contain the components of the Indian Mulberry, known as Morinda citrifolia L., for treatment of single or multiple abnormalities of the oral cavity and dental abnormalities, including the periodontal diseases, such as gingivitis and periodontitis, tooth destruction, bad smell and other disorders and irritations of the oral cavity.

EFFECT: composition provides efficient care of the oral cavity.

36 cl, 20 tbl, 11 ex

FIELD: medicine; cosmetology.

SUBSTANCE: invention relates to the agents for elimination of grey hair. The agent contains the chromogenic agent, which contains the beer yeast, hop and water in the following correlation, in mass%: 5-10 of the beer yeast, 2.5-5 of hop, water - the rest.

EFFECT: these components are harmless and provide efficient restoration of dark color in grey hair.

1 tbl, 3 ex

FIELD: medicine; cosmetology.

SUBSTANCE: invention relates to the agents for elimination of grey hair. The agent contains the chromogenic agent, which contains the beer yeast, hop and water in the following correlation, in mass%: 5-10 of the beer yeast, 2.5-5 of hop, water - the rest.

EFFECT: these components are harmless and provide efficient restoration of dark color in grey hair.

1 tbl, 3 ex

FIELD: medicine; cosmetology.

SUBSTANCE: invention relates to the cosmetic agents, namely cosmetic agent for care and maintenance of the natural hair function; contains the routine cosmetic raw materials, differs in containing the 2-furanon derivative , at least one polymeric compound and at least one compound of protein hydrolysates and their derivatives.

EFFECT: invention efficiently maintains natural hair function.

6 cl, 32 ex, 1 dwg

FIELD: medicine; cosmetology.

SUBSTANCE: invention relates to the cosmetic agents, namely cosmetic agent for care and maintenance of the natural hair function; contains the routine cosmetic raw materials, differs in containing the 2-furanon derivative , at least one polymeric compound and at least one compound of protein hydrolysates and their derivatives.

EFFECT: invention efficiently maintains natural hair function.

6 cl, 32 ex, 1 dwg

FIELD: medicine; cosmetology.

SUBSTANCE: invention relates to the cosmetic agents, namely cosmetic agent for care and maintenance of the natural hair function; contains the routine cosmetic raw materials, differs in containing the 2-furanon derivative , at least one polymeric compound and at least one compound of protein hydrolysates and their derivatives.

EFFECT: invention efficiently maintains natural hair function.

6 cl, 32 ex, 1 dwg

FIELD: medicine; cosmetology.

SUBSTANCE: composition for local application contains: i) anti-dandruff agent; ii) conjugated linoleic acid and iii) cosmetic acceptable dissolvent or carrier.

EFFECT: invention provides increased efficiency in treatment and prevention of dandruff and itching of scalp skin.

14 cl, 1 dwg, 2 ex

FIELD: medicine; cosmetology.

SUBSTANCE: composition for local application contains: i) anti-dandruff agent; ii) conjugated linoleic acid and iii) cosmetic acceptable dissolvent or carrier.

EFFECT: invention provides increased efficiency in treatment and prevention of dandruff and itching of scalp skin.

14 cl, 1 dwg, 2 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying hesperidin compound or one of its derivatives chosen out of the group that consists of hesperidins, α-glycosyl-hesperidin, methyl-hesperidin, hesperetin conjugate and sulfate or glucoronide, as active compound that stimulates osteogenesis and inhibits osseous resorption for obtaining a composition indicated for osteogenesis stimulation and/or inhibiting human or animal osseous resorption. The innovation illustrates the decrease of osseous demineralization and improves biomechanical properties of femur due to hesperidin action.

EFFECT: higher efficiency.

18 cl, 14 dwg, 4 tbl

Up!