FORM 2
THE PATENTS ACT, 1970 (39 of 1970)
&
THE PATENTS RULES, 2003
PROVISIONAL SPECIFICATION
[See section 10, Rule 13]
HERBAL GASTROINTENSTINAL
CONTROLLED DRUG DELIVERY
DOSAGE FORMS INCLUDING PELLETS
AND PROCESS FOR THEIR
PREPARATION;
UNIJULES LIFE SCIENCES LTD., A CORPORATION ORGANIZED AND EXISTING UNDER THE LAWS OF INDIA, WHOSE ADDRESS IS NO. 1505/1, UNIVERSAL SQUARE SHANTINAGAR, NAGPUR, MAHARASHTRA, INDIA.
THE FOLLOWING SPECIFICATION DESCRIBES THE INVENTION.
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TECHNICAL FIELD
The present invention relates to a controlled release herbal gastrointestinal drug delivery dosage forms including pellets, tablets and capsules and process for their preparation.
DESCRIPTION
The enteric coated, colon targeted or sustained release pellets are known in the pharmaceutical art in the areas of the allopathy drugs. But such enteric coated, colon targeted or sustain release pellets and tablets are novel in administration and delivery of herbal drugs.
The invention describes a product comprising controlled release of active ingredients from drug coated pellets when the said drug comprises a crude extract of a herb or a phytochemical isolated from medicinal plants and the said pellets are formed by coating the said drug on inert aggregates of particulate matter commonly used in the art of pharmaceutical formulations, the said inert aggregates including, but not limited to, non-pareil seeds; and a process for making the said product. The said process of coating could be any of the process of applying a coat known in the art of pharmacy or a novel method. A process of imparting a property of controlled release or delayed release includes one or more of a method including but not limited to use of a polymer or a like material for facilitating a controlled release of the drug at the desired site of its release. The said controlled release pellets may be enteric coated, colon targeted or sustained release and the like. Such pellets may be filled into Gelatin or HPMC capsules or are pressed in to form a tablet. A controlled release dosage form of herbal pellets may also include treating a capsule or a tablet in a
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way that exposes the pellets for release of the drug and its absorption in a manner that is controlled.
Some results achieved in the exploratory work are given below, which are an account of interim results of the preferred embodiment, which shall be improved upon by further work and fine tuned until complete specification is submitted. The details of work done so far disclosed below serve as illustrations and do not limit the scope of actual techniques used or scope of or range of reaction conditions or process conditions claimed. The techniques and reaction conditions or process conditions disclosed below are subject matter of ongoing trials and fine tuning or trials in alternative or better conditions. Several other adaptations of the embodiments will be easily anticipated by those skilled in this art and they are also included within the scope of this work and be a part of this disclosure.
In one experiment, enteric-coated Garlic pellets are prepared which releases the medicaments in small intestine to avoid belching of Garlic odor by avoiding the release of medicaments in stomach. Garlic pellets are enteric coated with polymer Cellulose Acetate Pthalate, which releases the Garlic only in intestine not in stomach therefore belching of Garlic odor is avoided.
In another experiment on Colon delivery sennosides pellets the medicament is released in colon to avoid gripping action of sennoside in upper gastrointestinal region. Site of action of sennoside is in colon. The pellets are so designed to release sennoside in colon. Sennosides are presents in Cassia angustifolia Vahl., and is extracted from it. The action of Sennosides is mainly upon the large intestine and is, therefore, especially suitable in habitual constipation. The glycosides are absorbed from the intestinal tract and the active anthraquinones are excreted into the colon, where they stimulate and increase the peristaltic
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movements of the colon, decrease absorption of water from colon and produce a bulky softer fecal mass. This suggests their action is in lower bowel and have no effect in stomach and small intestine (Leng-Peschlow E. Dual effect of orally administered Sennosides on large intestine transit and fluid absorption in the rat. J Pharm parmacol, 38: 606-610, 1986). In the light of this information Sennosides colon targeting pellets is developed to provide effective safe therapy of laxation. In this experiment Sennosides is loaded over NP seeds and coated with Eudragit S100, which provides a coat which disintegrates only in colonic pH.
In yet another experiment Boswellic acid sustained release pellets releases Boswellic acid from the pellets for 12 hrs after oral administration. Boswellic acid is extracted from Boswellia serrata Roxb. ex Colebr. Boswellic acid has analgesic and anti-inflammatory action and therefore very useful in arthritis (Safayhi, H. et al. (1992) Boswellic acids: novel, specific, non-redox inhibitors of 5-lipoxygenase. J. Pharmaacol. Exp. Ther. 261:1143-6). In this experiment Boswellic acid pellets are prepared and coated with Eudragit RS RL 100 polymer or by any other polymer known in field of pharmacy, which releases the Boswellic acid from the pellets for 12 hrs. Therefore drug is available for more span of time and less dosage is required.
In yet another experiment on Turmeric {Curcuma longa Linn.) sustained release pellets which are designed to prolong the release of curcumin present in turmeric, so as to maintain the therapeutic effect for long time. Bioavailability of curcumin from Curcuma longa Linn, is poor when purified Saxena, R.C., World Congress on Biotechnological Developments in Medicinal Substances of Plant and Marine Origin, Lucknow. (India), Feb. 19-22(1995). To make more bioavailable curcumin pellets is coated with suitable polymer known to field of pharmaceutical art.
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The above pellets are prepared by one or more of a method available in the literature and art of pharmaceutics. By the time complete specification is filed, development of a novel method of coating and novel method of controlling release of a drug from pellet may also be developed as a part of this work. The pellets of this invention may or may not be coloured with any permitted colour. They may or may not be coated with finishing layer. Pellets may be coated with a combination of more herbs also. Pellets from more than one batch may also be mixed together in the dosage form or formulation of this invention.
Dated this 28th day of September, 2006.

(GIRISH VIJAYANAND SHETH) KRISHNA & SAURASTRI

FOR UNIJULES LIFE SCIENCES LTD.
By their Agent
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