Soluble dosage forms of n,n'-diaminodiphenylsulphone for effective application in treating various diseases

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to manufacturing pharmaceutical drugs. A drug represents a solution of N,N'-diaminodiphenylsulphone in a mixture of solvents: ethanol and water and at least one of the solvents specified in a group including propylene glycol, benzyl alcohol and glycofurol. Preferentially, the solution contains ethanol 25%, propylene glycol 58%, benzyl alcohol 1%, glycofurol 5% and water 11%.

EFFECT: what is prepared is the dosage form of N,N'-diaminodiphenylsulphone used for cerebral infarction, epilepsy, a traumatic marrow injury, a craniocerebral injury, leprosy, pneumocystis carinii infections, and any condition requiring fast and full absorption of the formulation.

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Field of the INVENTION

The present invention relates to the pharmaceutical industry, more precisely, to receive medicines to treat some of the symptoms of various diseases.

The ANTECEDENT

Chemotherapeutic treatment of leprosy and infections caused bypneurmocystis carinii,by taking pills N,N-diaminodiphenylsulfone. Use as soluble drug dosage forms sulfone is a technical problem due to the poor solubility of N,N-diaminodiphenylsulfone in the aquatic environment. Therefore, the present invention presents new dosage forms, allowing to increase the solubility sulfone up to 200 mg/3 ml, using co-solvents that are compatible with pharmaceutical activity, is safe for humans.

There is information that the solutions of N,N-diaminodiphenylsulfone using surface-active composition of Tween-80, in the proportion of 90% [Helton DR, Osborne DW, Pierson SK, Buonarati MH, Bethem RA., Pharmacokinetic profiles in rats after intravenous, oral, or dermal administration of dapsone, Drug Metabolism and Disposition, 28: 925-929 (2000)] have a great disadvantage in that Tween-80 is toxic in the concentrations necessary for dissolution of the sulfone, which consequently hinders its use for humans.

The present invention aims at habitsa the possibility of creating girorastvorimie compounds with N,N-diaminodiphenylsulfone for more rapid absorption of the active molecule and for possible use on persons unconscious, as well as compositions that would be safe for humans when used as a medicine in the form of a solution in any way of introduction, including all enteral and parenteral route.

N,N-diaminodiphenylsulfone is a drug currently used for the chemotherapy of leprosy treatment and as prophylaxis against pneumonia causedpneumocystis carinii.Recently, N,N-diaminodiphenylsulfone (Dapsone) showed others the possibility of its use, for example, as a neuroprotector and as an anti-epileptic funds. In these cases often require administration of a medicinal product to patients who are unconscious, which, consequently, makes impossible the application of solid dosage forms. These new uses of the drug, "Dapsone" were patented (patent # MX 246892, patent # MX 264912). Soluble forms are most appropriate for the above applications, because the treatment requires a more rapid absorption of the medicinal product, in comparison with the absorption rate of the solid forms.

BRIEF description of the INVENTION

The present invention aims at the description of the product for therapeutic use, based on the dissolution of N,N-diaminodiphenyl is ulpana in a mixture of compatible solvents for medical use for humans. N,N-diaminodiphenylsulfone has more applications, which often require administration of the drug to patients who are unconscious, so the use of solid forms of drugs used today, is inadequate.

Find ways to dissolve the N,N-diaminodiphenylsulfone found that a mixture of ethanol/propylene glycol/glucotrol/benzilovogo alcohol/water, with various additives (thickeners, stabilizers and/or flavorings) allow to obtain stable products, fully suitable for insertion through any enteral or parenteral route. To obtain solutions, through the synthesis of N,N-diaminodiphenylsulfone got the connection with the following formula:

.

In all cases, were used solvents and reagents USP class that does not contain pyrogens.

The test solution was happening in tanks made of glass or stainless steel, with volume from 10 ml to 5 l, by placing 200 mg/3 ml N,N-diaminodiphenylsulfone in a mixture of auxiliary solvents. After intensive stirring, a visual inspection of tanks, was established obtaining a solution of N,N-diaminodiphenylsulfone.

To determine the optimal mixing ratio of ethanol/propylene glycol/glucotrol/benzilovogo alcohol/water you need is to dissolve the N,N-diaminodiphenylsulfone, was used the simplex algorithm.

For stability studies of the solution of N,N-diaminodiphenylsulfone were used glass flask with a capacity of 10 ml, sealed gas burner.

Sterilization of glass flasks with soluble drug was carried out in an autoclave at 110°C.

BRIEF DESCRIPTION of FIGURES

Figure 1 is a graph in which the axis of abscissa shows the time, expressed in days, and on the y - axis the concentration of DDS.

Figure 2 shows the histological slice of rat brain, which was caused by cerebral infarction and put only indifferent excipients (base) of the medication.

Figure 3 shows histological slice of rat brain, which was caused by cerebral infarction and injected the solution.

Figure 4 shows histological slice of rat brain, which was caused by cerebral infarction and put oral solution.

Figure 5 shows the profile of plasma concentration with the use of oral composition.

Figure 6 shows the profile of plasma concentration during intravenous composition.

EXAMPLE

Synthesis of N,N-diaminodiphenylsulfone

N,N-Diaminodiphenylsulfone can be synthesized in various ways, but in this case, as the example suggests the following method of synthesis.

This is the synthesis took place in two stages:

1. 60 g of acetanilide was placed in an Erlenmeyer flask and slowly heated over a flame until dissolved solids. The resulting viscous liquid was cooled in a glass with ice, trying to keep the solids were at the bottom of the flask. One portion was added 165 ml of chlorosulfonic acid, not removing the flask from the ice bath. Then he removed the flask from the ice, gently shaking, and left the compound for the reaction for 10 minutes, after which it is again heated the reaction mixture to dissolve the remaining acetanilide, leaving the composition for another 10 minutes. Allowed to cool and carefully poured the product into the vessel with ice and water, filtering the precipitate and washing with cold water. Collected precipitate, dissolving it in chloroform and pressed three times with water, collecting the chloroform phase, the latter was placed in an ice bath, precipitating purified thionyl chloride (melting point of the intermediate reaction product: 149°C).

2. 123,6 ml of anhydrous nitrobenzene were placed in a reaction flask, added 89.2 g of aluminium chloride and slowly heated; hot mixture was added to 41.3 g of thionyl chloride, heating the reaction mixture at a temperature of 140-145°C and slowly added 13 g of acetanilide, maintaining the reaction temperature within two hours. At the end of this period he poured the mixture in 104 ml of water, acidified with hydrochloric acid, to precipitate some of the crystals of dark color, which then gave recrystallization with dissolved with acetic acid. These crystals was placed under reflux with 5N hydrochloric acid for 30 minutes, then neutralizing the reaction mixture, so that fell into the sediment a few white crystals (raw materials for DDS), which, in turn, will again recrystallized with ethanol.

CHEMICAL CHARACTERIZATION of the SYNTHESIZED COMPOSITION

To determine the identity of the synthesized compounds has reached the melting point of 151-153°C for the intermediate product of the reaction, thionyl chloride, and 172-175°C for VAT.

The stated melting point of these compounds 149°C and 175-176°C for the intermediate reaction product and DDS, respectively.

The PREFERRED METHOD of carrying out the INVENTION

A mixture of ethanol/propylene glycol/glucotrol/benzilovogo alcohol/water in different proportions for dissolving N,N-diaminodiphenylsulfone are used for medicines against various diseases such as cerebral infarction, epilepsy, traumatic injury, bone marrow, brain injury, brain hemorrhage, subarachnoid hemorrhage from aneurysm, leprosy, infections caused bypneumocystis carinii,and any state that requires rapid and complete absorption of the composition flowing through any route of administration of medicines.

The rst is the group of pharmaceutical agents in a dose of 0.2 mg/kg to 12 mg/kg can be repeated as many times as necessary during the period from 1 to 7 days.

Example 1. A solution of N,N-diaminodiphenylsulfone for administration in the form of solution through any enteral or parenteral route

Weigh from 50 mg to 500 g of N,N-diaminodiphenylsulfone and put it in a test tube. Add 5 parts of a mixture that contains a 2.9 parts of propylene glycol, of 1.25 parts of ethanol and 0.85 part of the water. The mixture is shaken until dissolved N,N-diaminodiphenylsulfone.

The resulting solution was poured into a glass flask which is then sealed and sterilized in an autoclave.

To determine whether dissolved N,N-diaminodiphenylsulfone and not did the sterilization process significant degradation of matter, solutions of N,N-diaminodiphenylsulfone were checked by chromatography fluids high precision with UV detection.

Evaluation of the NEUROPROTECTIVE EFFECT of SOLUBLE DOSAGE FORMS N,N-DIAMINODIPHENYLSULFONE

To assess the neuroprotective ability of soluble forms of Dapsone, an experiment was conducted on rats, for example, cerebral ischemia. In this example, in rats was induced by chronic cerebral ischemia by permanent blocking of middle cerebral artery as described in the continuation:

In animals was caused by selective chronic cerebral ischemia by intraluminal injection of surgical sutures che is ez carotid artery. All animals was carried out General anesthesia during surgery with halothane gas 1.5% after the facial mask. Animals were placed in a horizontal position on the back, fixed and shaved the front of the occipital region. Made an incision in the midline, reaching from the arm of the sternum to the Sterno-hyoid muscles, and to its side edges. In this place found the medial part of the Sterno sternocleidomastoid muscle and the cervical superficial aponeurosis on the deep sheet, the same that was affected to gain access to the common carotid artery under and inside the digastric muscle of the caudal abdomen.

Made dissection of the common carotid artery to loop hypoglossal nerve. It was found the bifurcation of the carotid artery, external carotid artery and the occipital and thyroid branches, the last two were connected by monofilament 8/0 and electrocoagulator for further incision. Was the incision of the internal carotid artery length of approximately 5 mm, and at this point was discovered pterygopalatine artery. It was installed a microchip or, in the absence of the latter, it was possible to connect it monofilaments 6/0. Stopping the flow through the arterial ducts introduced nylon monofilament 3/0 towards the internal carotid artery, through the deltoid branch is the current carotid artery, length 17 mm, starting from the branching. Then he closed the wound and left the animal to recover with unlimited access to feed and water. In all cases, the results of macroscopic and research on the status of the thread was confirmed by ischemia.

Evaluation of the NEUROPROTECTIVE ACTION of SOLUBLE DOSAGE FORMS N,N-DIAMINODIPHENYLSULFONE RATS

Were taken from serial histological sections of rat brain, was produced by staining with hematoxylin and eosin to determine the damage area. Revealing the neuroprotective actions on animals, which have introduced new pharmaceutical form of the drug, and the effect of indifferent auxiliary substances (bases) of the drug is depicted in figure 2.

Figure 2 shows that the damage zone is significantly smaller in animals treated with new soluble forms of drugs N,N-diaminodiphenylsulfone, in comparison with the control animals, which were injected indifferent excipients (basis) of the medication.

The PHARMACOKINETIC PROFILE of SOLUBLE DOSAGE FORMS N,N-DIAMINODIPHENYLSULFONE IN HEALTHY PATIENTS-VOLUNTEERS

18 healthy patients-volunteers took soluble dosage form of the preparation N,N-diaminodiphenylsulfone (DDS) orally in the form of the solution (figure 3), and intravenous (figure 4) and would and measured plasma concentrations of N,N-diaminodiphenylsulfone at different times. Figures 3 and 4 show the results of these tests.

After the calculation of the area under the curve pharmacokinetic profile for each rat, calculates the average bioavailability, which is more than 92% for the oral form, assuming 100% bioavailability of the area under the curve intravenous. This result indicates that the soluble form for oral administration is optimally absorbed in the digestive tract. The maximum concentration of oral achieved, on average, half an hour later, while literature data indicates the time to reach maximum plasma concentration is from 2 to 3 hours for solid forms (Breen GA, Brocavich JM, Etzel JV, Shah V, Schaefer P, Forlenza, S., Evaluation of effects of altered gastric pH on absorption of dapsone in healthy volunteers, Antimicrobial Agents and Chemotherapy Sep 1994; 38(9):2227-2229).

1. A solution of N,N'-diamino-diphenylsulfone in a mixture solvent of ethanol and water, and at least one solvent selected from the group comprising propylene glycol, benzyl alcohol and glucotrol.

2. The solution under item 1, in which N,N'-diamino-diphenylsulfone is contained in an amount of from 1 to 25% by volume mixture of ethanol and water.

3. The solution under item 1, in which the mixture of solvents is presented in the following proportions: from 1 to 25% of ethanol, from 0 to 70% propylene glycol, from 0 to 20% benzyl alcohol, from 0 to 25% of glycoluril and from 5 to 90% water.

4. The solution under item 1, in which the ω solvent mixture are presented in the following proportions: 25% ethanol, 58% of propylene glycol, 1% benzyl alcohol, 5% glycoluril and 11% water.

5. The method of treatment of a disease selected from the group consisting of cerebral infarction, epilepsy, traumatic spinal cord injury, traumatic brain injury, brain haemorrhage, leprosy, infections, Pneumocystis carinii, including the stage of introduction of the solution under item 1 to a patient in need of it.

6. The method according to p. 5, where the solution is injected in doses of from 5 to 300 mg per day.

7. The method according to p. 5, where the introduction is repeated every 24 hours.

8. The method of treatment of a disease selected from the group consisting of cerebral infarction, epilepsy, traumatic spinal cord injury, traumatic brain injury, brain haemorrhage, leprosy, infections, Pneumocystis carinii, including the stage of introduction of the solution on p. 3 to a patient in need of it.

9. The method of treatment of a disease selected from the group consisting of cerebral infarction, epilepsy, traumatic spinal cord injury, traumatic brain injury, brain haemorrhage, leprosy, infections, Pneumocystis carinii, including the stage of introduction of the solution on p. 4 to a patient in need of it.

10. The method according to p. 8, where the solution is injected in doses of from 5 to 300 mg per day.

11. The method according to p. 9, where the solution is injected in doses of from 5 to 300 mg per day.

12. The method according to p. 8, where the introduction is repeated every 24 hours.

13. The method according to p. 9, where the introduction is repeated every 24 hours.



 

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