Title of Invention	A PROESS FOR THE PREPARATION OF A PHARMACEUTICAL FOR THE TREATMENT OF LEUCODERMA
Abstract	A process for the preparation of a pharmaceutical composition for the treatment of leucoderma comprising mixing tyroslne with a diluent and optionally conventional additives such as herein described to obtain a first mixture, preparing a second mixture of methionine and the diluent and adding the second mixture to the first mixture, before adding the zinc salt thereto.

Full Text

FIELD OF THE INVENTION The present invention relates to a herbal pharmaceutical preparation for the treatment of ieucoderma. BACKGROUND OF THE INVENTION Leucoderma or vitiligo is a disease commonly associated with failure of pigmentation of the skin. Para-ami nobenzoic acid, panthothenic acid and biotin are alleged to function in the process deal ing with pigmentation of the skin. It is true that gray-haired condition has been produced in rats, dogs, guinea-pigs and silver foxes on certain types of deficient diets: but it seems a far cry from this experi mental procedure to the process of aging as it occurs in human being. An enzyme tyrosinase converts Tyrosine into melanin, a brownish black pigment present in 'skin and hair. The mechanism by which this transformation is hydroxylation' accompl ished i s not known. Accordi ng to Raper, a of benzene nucleus possibly takes place, followed by ring closure whereby indole derivatives are formed. para- ami nobenzoic acid modifies the for mation of melanin. In the Tyrosi ne-tyrosi nase reaction, a typical red stage 1 is reached before the black preclpitate of melani n is obtained. In the presence of the acid, the red stage is not seen and in the place of the black mel ani n precipi tate, a browni sh product i s obtai ned. It has also been claimed that mel anophore hormone of the pi tui tary accelerates the tyrosine-tyrosi nase reaction. There are di fferent degrees and forms of the di sease and the cure mai nly i 1 depends on the extent of manifestation. This is due to the shortage or complete absence of tyrosinase In the system. Several ayurvedic preparations are known to be prescribed for vitiiigo such as a composi tion comprisl ng Psora! ia Coryf ol i a, common! y known as buchki dana and Pavoni a Odorata, common! y known as udi cha. Another commonly prescribed compost ti on i s a mi xture of Pl umbago Rosea Linn. ( Raktachita) and Mussaenda frondosa Lin (Nagbal11). However, presentl y no cure is known for the disease, particul arl y in its advanced stages. OBJECTS OF THE INVENTION It is therefore an object of this invention to propose a pharmaceutical preparation for the treatment of 1 eucoderma. It is a further object of this invention to propose a pharmaceutical preparation for the treatment of leucoderma which is cheap and can be made easily avail able. Another object of this Invention is to propose a pharmaceutical preparation for the treatment of 1 eucoderma which is efficient even for advanced stages of the di sease. DESCRIPTION OF THE INVENTION Accordi ng to this invention, there is provided a pharmaceuti ca! preparation for the treatment of leucoderma comprising tyrosine, a dil uent and optional ly methionine and an inorganic salt of zi nc. According to this invention, there is further provided a process for the preparati on of a pharmaceuti cal composition for the 2 treatment of & process for the preparation of a pharmaceutical composition for the treatment of leucoderma comprising mixing tyrostne with a diluent and optionally conventional additives such as herein described to obtain a first mixture, preparing a second mixture of methionine and the diluent and adding the second mixture to the first mixture, before adding the zinc salt thereto. The pharmaceutical preparation is in the form of an oral formulation or a topical formulation. The topical formulation comprises tyrostne and a diluent in a carrier such as water. About 1 to 3 gms of the mixture of tyrostne and the diluent is dissolved in about 45 to 135 ml distilled water and 5 to 15 ml of a preservative such as 90% rectified spirit Is added to It to obtain the topical formulation. The oral formulation comprises tyrosine, methlonlne, diluent and an Inorganic salt of zinc In accordance with this invention, the oral formulation is prepared by thoroughly mixing tyrosine with a diluent and slowly Increasing the proportion of the diluent to obtain a mixture of tyrosine and the dfluent. Thereafter, methlonlne Is mixed with the diluent and the dilution is slowly increased by increasing the proportion of sugar to obtain a mixture of methionine and the diluent. The two mixtures are then mixed thoroughly and zinc sulphate Is added to It, followed by a further mixing. Thereafter, optional additives are added to the mixture obtained to obtain the oral formulation. 3 About 5 to 9 gms of the mixture of tyrosine and the diluent Is mixed with 1 to 5 gms of methfonfne mixture and about 1 gm of (he Inorganic salt of zinc Is mixed together to obtain the oral formulation. Ths inorganic saft of zinc Is any salt of zinc, preferably a sulphate. The diluent used Is a sugar such as lactose, fructose, sucrose, glucose, etc., preferably lactose. The binder Is a compound such as carboxymethyl cellulose; the disintegrate used is starch; the glidant used is such as aerosil; magnesium stearate. The lubricant used Is a compound such as talcum powder and the preservative Is a p-hydroxybenzoate compound such as methyl paraben (methyl p-hydroxybenzoate), propyl paraben (propyl p-hydroxybenzoate) etc. The carrier used for the topical formulation Is a solvent such as water. The Invention win now be explained In greater detail with the help of the following norvllmftlng examples. EXAMPLE 1 About 1 gm of tyroslne Is thoroughly mixed with about 9 gms of lactose (80-100 mesh) placed in a mortar and the mixture is macerated for 60 mins. Every 6 mins. of maceration is followed by mixing for 1 min. This process is repeated 10 times. The mixture Is transferred in a bigger mortar and fresh lactose of 90 gms is mixed with it for about 10 mins. It is again macerated 4 for 5 mi ns. and mixed for a minute. This process is repeated 1Ø times. Fresh lactose, 9ØØ gms is taken In a big mortar and the mi xture obtained earlier is poured over it, foil owed by thorough mixing for about 10 mins. . This is again followed by maceration for 5 mins. and mixing for a min. , 10 ti mes to obtain the tyrosine mixture of 1000 dilution. In a similar way, about 300 mg of methionine is mixed with 2.7 gms of 1actose for about 5 mins. . This is fol 1 owed by maceration for 5 mi ns. and mi xi ng for a mi n. , 10 times to obtai'n a mi xture. In another mortar, about 27 gms lactose Is taken and the mixture i s poured over i t and mi xed thoroughly. It i s macerated for 5 mins. and mi xed for a mi n. , 10 tl mes to obtain a mi xture, which is agal n mi xed wi th about 270 gms of 1 actose. This is agai n followed by maceration for 5 mins. and mixing for 1 mi n. , 10 ti mes to obtai n the methionine mi xture of 1000 di 1 ution. TOPICAL FORMULATION About 2 gms of the tyrosi ne mixture is dissolved in about 90 ml distil 1 ed water and to this sol uti on, about 10 ml 90% recti f i ed spirit is added and the mixture is shaken to obtain the topical formul ation. ORAL FORMULATION About 7 gms of tyrosi ne mi xture and 3 gms of methi on!ne are mixed thoroughly for about 20 mins. and 100 mgs or 0.1 gms zinc sut phate, pul verised to a very fine mesh size added to the mixture with thorough mixing. 5 EXAMPLE 2 For the preparation of cap lets? tyrosine and methionine are diluted separately with lactose (80-100mesh) as per homoeopathic method of dilution to 1000 times. Both the diluted forms of tyrosine and methionine are we 31 mixed. Zinc sulphate is pulverised to very fine mesh. Powder obtained, le. mixture of tyrosine + methionine are mixed geometrically with zinc sulphate powder. So all the three active ingredients are well mixed with lactose. This mixed powder is the starting for tablet (cap let) manufacture. FOR THE PRODUCTION OF 5 Ø , Ø Ø Ø CAPLET 1. Tyrosine 0.7 mg x 1 Ø Ø Ø = 0.7 g x 50,000 35 kgs. 2. Methionine 0.3 mg x 1000 = 0.3 g x 50,000 15 fcgs. 3. Zinc sulphate 1.9 mg « 0.001 g K 50,000 = 50 kgs. 5 Ø kgs 5 Ø gms Carboxymethyl cellulose = 10 kgs. Starch powder, dried = 2.5 kgs. Talcum powder = 0-6 kgs. Aerasil = 0-5 fcgs. Magnesium Stearate = 0.6 kgs. Propyl paraben = 10 gms. Methyl paraben =50 gms. 64.31 kgs. These ingredients except talcum powder are mixed together thoroughly in tablet mixing drum for 45 mins.. The powder is then slugged, le. they are preliminary compression of fine powder into 6 rough tablets or slugs followed by their grinding into granular particl es. The granul es are separated, mixed with 1 ubricants, i e. talcum powder and compressed in suitable tablet punching machine. Average wt. of each caplet/tablet = 1.2862 g approx. Hardness =5-7 kgs. Moisture = Less than 1% Disintegration = Less than 10 mins. CAPSULE MAKING Powder of the three active ingredients for 5 Ø, Ø Ø Ø capsules = 50.05 kgs. are mixed with 1-5 fcgs. light Mag. Carb. and 0.5 kgs. Aerosil and mixed thoroughly. Total weight terms to 52.05 fcgs. Average weight of content of each capsule = 1.041 gms. apprax.. The powder is now fIled in number ' Ø Ø Ø ' capsules. The preparation according to the invention has been administered to a number of patients and the results have been quite encouraging. The treatment is based on administering the preparation in daily doses with very low concentration of the constituents, alongwith application of the topical formulation - App1ication of the topical formulation on the affected area is followed by exposure to sunlight. The preparation works on the principle of Arndt., le. weal stimuli excite-physiologic activity, moderately strong ones favour it, strong ones retard it and very strong ones arrest it- The results of the chemical trials is as follows s 7 Total No- of Stopped treatment Not cured Under- Cured Pat 3ents treatment 32 2 2 9 19 The preparation has been successfully used for treating vitiligo and has been particularly successful when the disease is detected in the early stages- Cure is possible within 15 days to lm, If detected in the late stages, le. from a year to about 6 years old t cure is possible within i to 3 years. Extreme cases have so far not been cured, 8 WE CLAIM 1. A process for the preparation of a pharmaceutical composition for the treatment of leucoderma comprising mixing tyrosinewith a diluent and optionally conventional additives such as herein described to obtain a first mixture, preparing a second mixture of methionfne and the diluent and adding the second mixture to the first mixture, before adding the zinc salt thereto. 2. The process as claimed in claim 1 wherein said pharmaceutical composition is in the form of an oral or topical formulation. 3. The process as claimed In claim 1 wherein said conventional additives are carriers, binders, dlsintegrants, glidants, anti-adhesives, lubricants and preservatives. 4. The process as claimed in claim 1 wherein about 5-9 gms of the first mixture, about 1-5 gms of the second mixture and about 1 gm of zinc salt Is used for the oral formulation. 5. The process as claimed in claim 1 wherein during the step of mixing tyroslne or methtonine with the diluent, the proportion of diluent is slowly Increased In the mixture. 6. The process as claimed In claim 1 wherein said first mixture Is mixed with a carrier such as water, and preservative such as rectified spirit for the topical formulation. 7. The process as claimed in claim 1 wherein the diluent Is pulverised to 80- 100 mesh size. 8. The process as claimed in claim 1 Where in the zine salt is zinc sulphate. 9 9. The process as claimed In claims 2, 3 wherein the diluent for the oral formulation is a sugar such as glucose, lactose, sucrose, fructose and the like, preferably lactose. 10. The process as claimed In claims 2, 3 wherein the carrier for the topical formulation is water. 11. The process as claimed In claim 3 wherein the binder ts a compound such as carboxy-methyl cellulose. 12. The process as claimed In claim 3 wherein the dlslntegrant used Is such starch. 13. The process as claimed in claim 3 wherein the glidant used is such as aerosll, magnesium stearate. 14. The process as claimed in claim 3 wherein the lubricant used is such as talcum powder. 15. The process as claimed in claim 3 wherein the preservative used is a paraben compound such a methyl paraben (methyl p-hydroxybanzoate), paraben (propyl p-hydroxybenzoate). 16. The process as claimed in claim 3 wherein the oral formulation is in the form of tablets and capsules. Dated this 11th day of July. 2003. 10 A process for the preparation of a pharmaceutical composition for the treatment of leucoderma comprising mixing tyroslne with a diluent and optionally conventional additives such as herein described to obtain a first mixture, preparing a second mixture of methionine and the diluent and adding the second mixture to the first mixture, before adding the zinc salt thereto.

Documents:

00387-kol-2003-abstract.pdf

00387-kol-2003-claims.pdf

00387-kol-2003-correspondence.pdf

00387-kol-2003-description(complete).pdf

00387-kol-2003-form-1.pdf

00387-kol-2003-form-18.pdf

00387-kol-2003-form-2.pdf

00387-kol-2003-form-26.pdf

00387-kol-2003-form-3.pdf

387-kol-2003-granted-abstract.pdf

387-kol-2003-granted-claims.pdf

387-kol-2003-granted-correspondence.pdf

387-kol-2003-granted-description (complete).pdf

387-kol-2003-granted-examination report.pdf

387-kol-2003-granted-form 1.pdf

387-kol-2003-granted-form 18.pdf

387-kol-2003-granted-form 2.pdf

387-kol-2003-granted-form 26.pdf

387-kol-2003-granted-form 3.pdf

387-kol-2003-granted-letter patent.pdf

387-kol-2003-granted-reply to examination report.pdf

387-kol-2003-granted-specification.pdf